Ligand source activities (1 row/activity)





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CHEMBL3980643 214974 None 0 Human Functional pIC50 = 10 10.0 6 2
Agonist activity at human recombinant ETB receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization by fluorimetric methodAgonist activity at human recombinant ETB receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization by fluorimetric method
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)[C@@H](C)CC 10.1016/j.ejmech.2016.06.006
5311032 60266 None 31 Human Functional pIC50 = 9.4 9.4 - 1
Antagonist activity at ETB receptor in human BSMC assessed as inhibition of endothelin-1 or 3-mediated Ca2+ mobilization preincubated for 5 mins followed by endothelin-1 or 3 addition by fura-2/AM dye-based spectrofluorimetric methodAntagonist activity at ETB receptor in human BSMC assessed as inhibition of endothelin-1 or 3-mediated Ca2+ mobilization preincubated for 5 mins followed by endothelin-1 or 3 addition by fura-2/AM dye-based spectrofluorimetric method
ChEMBL 641 12 4 7 4.8 CCCC[C@@H](NC(=O)[C@@H](Cc1cn(C(=O)OC)c2ccccc12)NC(=O)[C@H](CC(C)(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1016/j.ejmech.2016.06.006
CHEMBL1515091 60266 None 31 Human Functional pIC50 = 9.4 9.4 - 1
Antagonist activity at ETB receptor in human BSMC assessed as inhibition of endothelin-1 or 3-mediated Ca2+ mobilization preincubated for 5 mins followed by endothelin-1 or 3 addition by fura-2/AM dye-based spectrofluorimetric methodAntagonist activity at ETB receptor in human BSMC assessed as inhibition of endothelin-1 or 3-mediated Ca2+ mobilization preincubated for 5 mins followed by endothelin-1 or 3 addition by fura-2/AM dye-based spectrofluorimetric method
ChEMBL 641 12 4 7 4.8 CCCC[C@@H](NC(=O)[C@@H](Cc1cn(C(=O)OC)c2ccccc12)NC(=O)[C@H](CC(C)(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1016/j.ejmech.2016.06.006
CHEMBL1741040 60266 None 31 Human Functional pIC50 = 9.4 9.4 - 1
Antagonist activity at ETB receptor in human BSMC assessed as inhibition of endothelin-1 or 3-mediated Ca2+ mobilization preincubated for 5 mins followed by endothelin-1 or 3 addition by fura-2/AM dye-based spectrofluorimetric methodAntagonist activity at ETB receptor in human BSMC assessed as inhibition of endothelin-1 or 3-mediated Ca2+ mobilization preincubated for 5 mins followed by endothelin-1 or 3 addition by fura-2/AM dye-based spectrofluorimetric method
ChEMBL 641 12 4 7 4.8 CCCC[C@@H](NC(=O)[C@@H](Cc1cn(C(=O)OC)c2ccccc12)NC(=O)[C@H](CC(C)(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1016/j.ejmech.2016.06.006
10187997 110028 None 0 Human Functional pIC50 = 9.2 9.2 -4 4
Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin B receptor of chinese hamster ovary(CHO) cells.Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin B receptor of chinese hamster ovary(CHO) cells.
ChEMBL 564 13 1 7 4.2 CCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm970101g
CHEMBL323464 110028 None 0 Human Functional pIC50 = 9.2 9.2 -4 4
Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin B receptor of chinese hamster ovary(CHO) cells.Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin B receptor of chinese hamster ovary(CHO) cells.
ChEMBL 564 13 1 7 4.2 CCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm970101g
1009 194 None 25 Human Functional pIC50 = 9.1 9.1 1479 2
EDNRB- dependent phosphatidylinositol hydrolysis assayEDNRB- dependent phosphatidylinositol hydrolysis assay
ChEMBL 558 11 2 6 5.8 CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2 10.6019/CHEMBL4507261
5310991 194 None 25 Human Functional pIC50 = 9.1 9.1 1479 2
EDNRB- dependent phosphatidylinositol hydrolysis assayEDNRB- dependent phosphatidylinositol hydrolysis assay
ChEMBL 558 11 2 6 5.8 CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2 10.6019/CHEMBL4507261
CHEMBL332794 194 None 25 Human Functional pIC50 = 9.1 9.1 1479 2
EDNRB- dependent phosphatidylinositol hydrolysis assayEDNRB- dependent phosphatidylinositol hydrolysis assay
ChEMBL 558 11 2 6 5.8 CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2 10.6019/CHEMBL4507261
CHEMBL284250 213319 None 0 Human Functional pIC50 = 9.1 9.1 1 4
Functional inhibition of ET-1 induced [Ca2+] increase in human Girardi heart (hGH) cells, which express Endothelin B receptorFunctional inhibition of ET-1 induced [Ca2+] increase in human Girardi heart (hGH) cells, which express Endothelin B receptor
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)[C@@H](NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)O 10.1016/0960-894X(95)00237-N
10603409 110667 None 0 Human Functional pIC50 = 9.1 9.1 -1 4
Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin B receptor of chinese hamster ovary(CHO) cells.Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin B receptor of chinese hamster ovary(CHO) cells.
ChEMBL 584 13 1 7 4.1 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCCl 10.1021/jm970101g
CHEMBL325581 110667 None 0 Human Functional pIC50 = 9.1 9.1 -1 4
Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin B receptor of chinese hamster ovary(CHO) cells.Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin B receptor of chinese hamster ovary(CHO) cells.
ChEMBL 584 13 1 7 4.1 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCCl 10.1021/jm970101g
10210629 8766 None 0 Human Functional pIC50 = 9.0 9.0 -7 4
Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin B receptor of chinese hamster ovary(CHO) cells.Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin B receptor of chinese hamster ovary(CHO) cells.
ChEMBL 592 15 1 7 5.0 CCCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm970101g
CHEMBL109644 8766 None 0 Human Functional pIC50 = 9.0 9.0 -7 4
Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin B receptor of chinese hamster ovary(CHO) cells.Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin B receptor of chinese hamster ovary(CHO) cells.
ChEMBL 592 15 1 7 5.0 CCCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm970101g
CHEMBL3143473 213793 None 0 Human Functional pIC50 = 8.9 8.9 1071 2
Antagonistic activity against endothelin B (ETB) receptor using human girardi heart cells.Antagonistic activity against endothelin B (ETB) receptor using human girardi heart cells.
ChEMBL None None None CCCC[C@@H](NC(=O)[C@@H](Cc1cn(COC)c2ccccc12)NC(=O)[C@H](CC(C)(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1016/0960-894X(95)00084-7
CHEMBL3305972 213793 None 0 Human Functional pIC50 = 8.9 8.9 1071 2
Antagonistic activity against endothelin B (ETB) receptor using human girardi heart cells.Antagonistic activity against endothelin B (ETB) receptor using human girardi heart cells.
ChEMBL None None None CCCC[C@@H](NC(=O)[C@@H](Cc1cn(COC)c2ccccc12)NC(=O)[C@H](CC(C)(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1016/0960-894X(95)00084-7
9916235 9355 None 1 Human Functional pIC50 = 8.9 8.9 -4 4
Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin B receptor of chinese hamster ovary(CHO) cells.Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin B receptor of chinese hamster ovary(CHO) cells.
ChEMBL 578 14 1 7 4.6 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm970101g
CHEMBL111277 9355 None 1 Human Functional pIC50 = 8.9 8.9 -4 4
Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin B receptor of chinese hamster ovary(CHO) cells.Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin B receptor of chinese hamster ovary(CHO) cells.
ChEMBL 578 14 1 7 4.6 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm970101g
10651488 163474 None 0 Human Functional pIC50 = 8.8 8.8 -1 4
Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin B receptor of chinese hamster ovary(CHO) cells.Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin B receptor of chinese hamster ovary(CHO) cells.
ChEMBL 618 13 1 7 4.8 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCC(F)(F)F 10.1021/jm970101g
CHEMBL419367 163474 None 0 Human Functional pIC50 = 8.8 8.8 -1 4
Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin B receptor of chinese hamster ovary(CHO) cells.Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin B receptor of chinese hamster ovary(CHO) cells.
ChEMBL 618 13 1 7 4.8 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCC(F)(F)F 10.1021/jm970101g
11318978 168006 None 0 Human Functional pIC50 = 8.0 8.0 -7 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 560 7 2 6 4.8 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(F)cccc3Cl)c3ccccc32)n1 10.1021/jm031115r
CHEMBL431286 168006 None 0 Human Functional pIC50 = 8.0 8.0 -7 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 560 7 2 6 4.8 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(F)cccc3Cl)c3ccccc32)n1 10.1021/jm031115r
CHEMBL4533479 216452 None 1 Human Functional pIC50 = 6 6.0 1 2
Eurofins cellular functional assay - Antagonist (EDNRB)Eurofins cellular functional assay - Antagonist (EDNRB)
ChEMBL None None None CCCOc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(CC)cccc2CC)cc1 10.6019/CHEMBL4507261
11387205 111624 None 0 Human Functional pIC50 = 7.0 7.0 1 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 544 8 2 7 4.5 COc1ccc(CN2C(=O)CN[C@](C3CCCCC3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1 10.1021/jm031115r
CHEMBL328073 111624 None 0 Human Functional pIC50 = 7.0 7.0 1 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 544 8 2 7 4.5 COc1ccc(CN2C(=O)CN[C@](C3CCCCC3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1 10.1021/jm031115r
10298354 112069 None 0 Human Functional pIC50 = 7.0 7.0 -15 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 462 7 3 7 1.8 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(CCO)c3ccccc32)n1 10.1021/jm031115r
CHEMBL328878 112069 None 0 Human Functional pIC50 = 7.0 7.0 -15 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 462 7 3 7 1.8 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(CCO)c3ccccc32)n1 10.1021/jm031115r
10187313 107500 None 0 Human Functional pIC50 = 7.0 7.0 -18 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 544 7 2 6 4.3 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(F)cc3F)c3ccccc32)n1 10.1021/jm031115r
CHEMBL318247 107500 None 0 Human Functional pIC50 = 7.0 7.0 -18 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 544 7 2 6 4.3 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(F)cc3F)c3ccccc32)n1 10.1021/jm031115r
11169125 210018 None 0 Human Functional pIC50 = 7.0 7.0 -5 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 574 7 2 4 6.5 Cc1cc(C)cc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(Cl)cccc3Cl)c3ccccc32)c1 10.1021/jm031115r
CHEMBL94802 210018 None 0 Human Functional pIC50 = 7.0 7.0 -5 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 574 7 2 4 6.5 Cc1cc(C)cc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(Cl)cccc3Cl)c3ccccc32)c1 10.1021/jm031115r
10303258 161969 None 0 Human Functional pIC50 = 8.0 8.0 -3 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 564 10 2 6 5.3 CCCCc1ccc(CN2C(=O)CN[C@](c3ccccc3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1 10.1021/jm031115r
CHEMBL415010 161969 None 0 Human Functional pIC50 = 8.0 8.0 -3 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 564 10 2 6 5.3 CCCCc1ccc(CN2C(=O)CN[C@](c3ccccc3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1 10.1021/jm031115r
9957883 98710 None 0 Human Functional pIC50 = 6.0 6.0 -25 2
Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B receptor.Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B receptor.
ChEMBL 507 7 1 9 5.0 COc1cc2c(Sc3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OC 10.1016/0960-894X(96)00232-6
CHEMBL27732 98710 None 0 Human Functional pIC50 = 6.0 6.0 -25 2
Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B receptor.Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B receptor.
ChEMBL 507 7 1 9 5.0 COc1cc2c(Sc3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OC 10.1016/0960-894X(96)00232-6
9890440 8256 None 0 Human Functional pIC50 = 5.9 5.9 -301 2
Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).
ChEMBL 460 6 1 7 4.1 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(OC)c(C)c2)cc1 10.1021/jm00008a002
CHEMBL10924 8256 None 0 Human Functional pIC50 = 5.9 5.9 -301 2
Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).
ChEMBL 460 6 1 7 4.1 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(OC)c(C)c2)cc1 10.1021/jm00008a002
11753582 210047 None 0 Human Functional pIC50 = 6.9 6.9 -4 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 586 7 2 6 4.8 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(Br)cc3)c3ccccc32)n1 10.1021/jm031115r
CHEMBL94962 210047 None 0 Human Functional pIC50 = 6.9 6.9 -4 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 586 7 2 6 4.8 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(Br)cc3)c3ccccc32)n1 10.1021/jm031115r
3951 391 None 55 Human Functional pIC50 = 5.9 5.9 -47 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 378 7 1 5 3.5 COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1 10.1021/jm031115r
4337 391 None 55 Human Functional pIC50 = 5.9 5.9 -47 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 378 7 1 5 3.5 COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1 10.1021/jm031115r
6918493 391 None 55 Human Functional pIC50 = 5.9 5.9 -47 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 378 7 1 5 3.5 COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1 10.1021/jm031115r
6918493.0 391 None 55 Human Functional pIC50 = 5.9 5.9 -47 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 378 7 1 5 3.5 COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1 10.1021/jm031115r
CHEMBL1111 391 None 55 Human Functional pIC50 = 5.9 5.9 -47 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 378 7 1 5 3.5 COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1 10.1021/jm031115r
DB06403 391 None 55 Human Functional pIC50 = 5.9 5.9 -47 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 378 7 1 5 3.5 COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1 10.1021/jm031115r
11753090 106259 None 0 Human Functional pIC50 = 6.9 6.9 -7 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 542 7 2 6 4.7 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(Cl)cc3)c3ccccc32)n1 10.1021/jm031115r
CHEMBL313870 106259 None 0 Human Functional pIC50 = 6.9 6.9 -7 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 542 7 2 6 4.7 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(Cl)cc3)c3ccccc32)n1 10.1021/jm031115r
11398658 210058 None 0 Human Functional pIC50 = 7.9 7.9 -1 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 544 7 2 6 4.3 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3cc(F)cc(F)c3)c3ccccc32)n1 10.1021/jm031115r
CHEMBL95017 210058 None 0 Human Functional pIC50 = 7.9 7.9 -1 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 544 7 2 6 4.3 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3cc(F)cc(F)c3)c3ccccc32)n1 10.1021/jm031115r
10120430 209979 None 0 Human Functional pIC50 = 7.9 7.9 -5 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 562 7 2 6 4.4 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(F)ccc(F)c3F)c3ccccc32)n1 10.1021/jm031115r
CHEMBL94580 209979 None 0 Human Functional pIC50 = 7.9 7.9 -5 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 562 7 2 6 4.4 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(F)ccc(F)c3F)c3ccccc32)n1 10.1021/jm031115r
11330923 210281 None 0 Human Functional pIC50 = 7.9 7.9 1 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 606 10 2 6 6.3 CCCCc1cccc([C@]2([C@H](Oc3nc(C)cc(C)n3)C(=O)O)NCC(=O)N(Cc3c(C)cc(C)cc3C)c3ccccc32)c1 10.1021/jm031115r
CHEMBL96303 210281 None 0 Human Functional pIC50 = 7.9 7.9 1 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 606 10 2 6 6.3 CCCCc1cccc([C@]2([C@H](Oc3nc(C)cc(C)n3)C(=O)O)NCC(=O)N(Cc3c(C)cc(C)cc3C)c3ccccc32)c1 10.1021/jm031115r
CHEMBL96822 218410 None 0 Rat Functional pIC50 = 5.9 5.9 1 2
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing recombinant rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing recombinant rat ET- B receptors
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NS(C)(=O)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
11238540 209984 None 0 Human Functional pIC50 = 5.8 5.8 -11 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 576 8 2 5 5.9 COc1cccc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(Cl)cccc3Cl)c3ccccc32)c1 10.1021/jm031115r
CHEMBL94602 209984 None 0 Human Functional pIC50 = 5.8 5.8 -11 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 576 8 2 5 5.9 COc1cccc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(Cl)cccc3Cl)c3ccccc32)c1 10.1021/jm031115r
10166139 163439 None 0 Human Functional pIC50 = 7.8 7.8 -2 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 550 7 2 6 4.9 Cc1cc(C)c(CN2C(=O)CN[C@](c3ccccc3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)c(C)c1 10.1021/jm031115r
CHEMBL419136 163439 None 0 Human Functional pIC50 = 7.8 7.8 -2 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 550 7 2 6 4.9 Cc1cc(C)c(CN2C(=O)CN[C@](c3ccccc3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)c(C)c1 10.1021/jm031115r
11376627 107688 None 0 Human Functional pIC50 = 7.8 7.8 -1 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 576 7 2 6 5.0 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3cccc(C(F)(F)F)c3)c3ccccc32)n1 10.1021/jm031115r
CHEMBL319007 107688 None 0 Human Functional pIC50 = 7.8 7.8 -1 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 576 7 2 6 5.0 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3cccc(C(F)(F)F)c3)c3ccccc32)n1 10.1021/jm031115r
11386977 210006 None 0 Human Functional pIC50 = 6.8 6.8 -1 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 528 8 2 6 4.8 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(CCC3CCCCC3)c3ccccc32)n1 10.1021/jm031115r
CHEMBL94752 210006 None 0 Human Functional pIC50 = 6.8 6.8 -1 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 528 8 2 6 4.8 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(CCC3CCCCC3)c3ccccc32)n1 10.1021/jm031115r
9955200 9334 None 0 Human Functional pIC50 = 5.8 5.8 -380 3
Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).
ChEMBL 446 6 1 7 3.8 COc1ccc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc1 10.1021/jm00008a002
CHEMBL11115 9334 None 0 Human Functional pIC50 = 5.8 5.8 -380 3
Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).
ChEMBL 446 6 1 7 3.8 COc1ccc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc1 10.1021/jm00008a002
11318409 209914 None 0 Human Functional pIC50 = 7.8 7.8 -3 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 522 7 2 6 4.3 Cc1cccc(CN2C(=O)CN[C@](c3ccccc3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)c1 10.1021/jm031115r
CHEMBL94212 209914 None 0 Human Functional pIC50 = 7.8 7.8 -3 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 522 7 2 6 4.3 Cc1cccc(CN2C(=O)CN[C@](c3ccccc3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)c1 10.1021/jm031115r
CHEMBL413825 215547 None 0 Human Functional pIC50 = 4.8 4.8 4 2
Ability to block sarafotoxin-6c (SRTX-6c) stimulated arachidonic acid release in chinese hamster ovary (CHO) cells expressing recombinant rat endothelin B (ETB) receptorAbility to block sarafotoxin-6c (SRTX-6c) stimulated arachidonic acid release in chinese hamster ovary (CHO) cells expressing recombinant rat endothelin B (ETB) receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(N)=O)NC(=O)CNC(=O)[C@H](CC(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H]2CCCN2C1=O 10.1016/0960-894X(95)00084-7
10230737 112383 None 0 Human Functional pIC50 = 7.8 7.8 -16 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 544 7 2 6 4.3 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(F)cccc3F)c3ccccc32)n1 10.1021/jm031115r
CHEMBL329251 112383 None 0 Human Functional pIC50 = 7.8 7.8 -16 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 544 7 2 6 4.3 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(F)cccc3F)c3ccccc32)n1 10.1021/jm031115r
18995992 99892 None 0 Human Functional pIC50 = 6.8 6.8 -3 2
Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B receptor.Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B receptor.
ChEMBL 507 7 1 9 5.0 COc1ccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc4c(cc23)OCO4)cc1OC 10.1016/0960-894X(96)00232-6
CHEMBL28563 99892 None 0 Human Functional pIC50 = 6.8 6.8 -3 2
Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B receptor.Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B receptor.
ChEMBL 507 7 1 9 5.0 COc1ccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc4c(cc23)OCO4)cc1OC 10.1016/0960-894X(96)00232-6
18995991 100354 None 0 Human Functional pIC50 = 6.8 6.8 -9 2
Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B receptor.Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B receptor.
ChEMBL 537 8 1 10 5.0 COc1cc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc4c(cc23)OCO4)cc(OC)c1OC 10.1016/0960-894X(96)00232-6
CHEMBL28920 100354 None 0 Human Functional pIC50 = 6.8 6.8 -9 2
Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B receptor.Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B receptor.
ChEMBL 537 8 1 10 5.0 COc1cc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc4c(cc23)OCO4)cc(OC)c1OC 10.1016/0960-894X(96)00232-6
10342643 5159 None 0 Human Functional pIC50 = 5.8 5.8 -144 2
Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).
ChEMBL 430 5 1 6 4.1 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1C 10.1021/jm00008a002
CHEMBL10588 5159 None 0 Human Functional pIC50 = 5.8 5.8 -144 2
Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).
ChEMBL 430 5 1 6 4.1 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1C 10.1021/jm00008a002
11752174 172828 None 0 Human Functional pIC50 = 5.8 5.8 -4 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 489 8 2 7 2.4 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(CCN(C)C)c3ccccc32)n1 10.1021/jm031115r
CHEMBL450628 172828 None 0 Human Functional pIC50 = 5.8 5.8 -4 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 489 8 2 7 2.4 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(CCN(C)C)c3ccccc32)n1 10.1021/jm031115r
11410074 210249 None 0 Human Functional pIC50 = 7.7 7.7 -1 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 536 9 2 6 4.4 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(CCCc3ccccc3)c3ccccc32)n1 10.1021/jm031115r
CHEMBL96114 210249 None 0 Human Functional pIC50 = 7.7 7.7 -1 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 536 9 2 6 4.4 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(CCCc3ccccc3)c3ccccc32)n1 10.1021/jm031115r
11421392 209844 None 0 Human Functional pIC50 = 7.7 7.7 -5 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 544 7 2 6 4.3 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3cccc(F)c3F)c3ccccc32)n1 10.1021/jm031115r
CHEMBL93820 209844 None 0 Human Functional pIC50 = 7.7 7.7 -5 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 544 7 2 6 4.3 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3cccc(F)c3F)c3ccccc32)n1 10.1021/jm031115r
11387315 209893 None 0 Human Functional pIC50 = 6.7 6.7 1 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 552 8 2 7 4.3 COc1ccc(CN2C(=O)CN[C@](c3ccc(C)cc3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1 10.1021/jm031115r
CHEMBL94091 209893 None 0 Human Functional pIC50 = 6.7 6.7 1 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 552 8 2 7 4.3 COc1ccc(CN2C(=O)CN[C@](c3ccc(C)cc3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1 10.1021/jm031115r
11397857 210250 None 0 Human Functional pIC50 = 5.7 5.7 -6 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 496 7 2 6 3.7 COc1cc(OC)cc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3ccc(Cl)cc32)c1 10.1021/jm031115r
CHEMBL96125 210250 None 0 Human Functional pIC50 = 5.7 5.7 -6 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 496 7 2 6 3.7 COc1cc(OC)cc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3ccc(Cl)cc32)c1 10.1021/jm031115r
10224745 112753 None 0 Human Functional pIC50 = 6.7 6.7 -15 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 432 5 2 6 2.4 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3ccccc32)n1 10.1021/jm031115r
CHEMBL330425 112753 None 0 Human Functional pIC50 = 6.7 6.7 -15 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 432 5 2 6 2.4 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3ccccc32)n1 10.1021/jm031115r
11226740 210361 None 0 Human Functional pIC50 = 6.7 6.7 -9 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 558 7 2 4 6.0 Cc1cc(C)cc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(F)cccc3Cl)c3ccccc32)c1 10.1021/jm031115r
CHEMBL96704 210361 None 0 Human Functional pIC50 = 6.7 6.7 -9 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 558 7 2 4 6.0 Cc1cc(C)cc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(F)cccc3Cl)c3ccccc32)c1 10.1021/jm031115r
CHEMBL328942 213775 None 0 Rat Functional pIC50 = 7.7 7.7 -1 3
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL433406 216101 None 0 Rat Functional pIC50 = 7.7 7.7 9 2
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)NC)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
10187261 111603 None 0 Human Functional pIC50 = 7.7 7.7 -3 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 542 7 2 6 4.7 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3cccc(Cl)c3)c3ccccc32)n1 10.1021/jm031115r
CHEMBL327976 111603 None 0 Human Functional pIC50 = 7.7 7.7 -3 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 542 7 2 6 4.7 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3cccc(Cl)c3)c3ccccc32)n1 10.1021/jm031115r
11489318 210258 None 0 Human Functional pIC50 = 7.7 7.7 -5 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 522 8 2 6 4.0 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(CCc3ccccc3)c3ccccc32)n1 10.1021/jm031115r
CHEMBL96171 210258 None 0 Human Functional pIC50 = 7.7 7.7 -5 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 522 8 2 6 4.0 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(CCc3ccccc3)c3ccccc32)n1 10.1021/jm031115r
15289330 99856 None 0 Human Functional pIC50 = 6.7 6.7 -18 2
Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B receptor.Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B receptor.
ChEMBL 493 8 1 8 5.3 COc1cccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc(OC)c(OC)cc23)c1 10.1016/0960-894X(96)00232-6
CHEMBL285368 99856 None 0 Human Functional pIC50 = 6.7 6.7 -18 2
Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B receptor.Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B receptor.
ChEMBL 493 8 1 8 5.3 COc1cccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc(OC)c(OC)cc23)c1 10.1016/0960-894X(96)00232-6
10230546 107303 None 0 Human Functional pIC50 = 7.7 7.7 -4 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 538 8 2 7 4.0 COc1ccc(CN2C(=O)CN[C@](c3ccccc3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1 10.1021/jm031115r
CHEMBL316878 107303 None 0 Human Functional pIC50 = 7.7 7.7 -4 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 538 8 2 7 4.0 COc1ccc(CN2C(=O)CN[C@](c3ccccc3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1 10.1021/jm031115r
11273181 210325 None 0 Human Functional pIC50 = 7.7 7.7 4 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 576 7 2 6 5.0 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccccc3C(F)(F)F)c3ccccc32)n1 10.1021/jm031115r
CHEMBL96506 210325 None 0 Human Functional pIC50 = 7.7 7.7 4 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 576 7 2 6 5.0 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccccc3C(F)(F)F)c3ccccc32)n1 10.1021/jm031115r
44327659 109878 None 0 Rat Functional pIC50 = 6.7 6.7 1 2
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
ChEMBL 937 26 9 8 4.6 CCC(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC)[C@@H](C)CC)C(c1ccccc1)c1ccccc1 10.1021/jm00015a003
CHEMBL323331 109878 None 0 Rat Functional pIC50 = 6.7 6.7 1 2
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
ChEMBL 937 26 9 8 4.6 CCC(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC)[C@@H](C)CC)C(c1ccccc1)c1ccccc1 10.1021/jm00015a003
9955200 9334 None 0 Rat Functional pIC50 = 6.7 6.7 -53 3
Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.
ChEMBL 446 6 1 7 3.8 COc1ccc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc1 10.1021/jm00008a002
CHEMBL11115 9334 None 0 Rat Functional pIC50 = 6.7 6.7 -53 3
Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.
ChEMBL 446 6 1 7 3.8 COc1ccc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc1 10.1021/jm00008a002
345351 9361 None 3 Rat Functional pIC50 = 4.7 4.7 -24 3
Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.
ChEMBL 386 4 1 5 3.8 O=C1OC(O)(c2ccccc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2 10.1021/jm00008a002
CHEMBL11131 9361 None 3 Rat Functional pIC50 = 4.7 4.7 -24 3
Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.
ChEMBL 386 4 1 5 3.8 O=C1OC(O)(c2ccccc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2 10.1021/jm00008a002
11365059 210254 None 0 Human Functional pIC50 = 7.6 7.6 -1 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 564 7 2 6 5.3 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(C(C)(C)C)cc3)c3ccccc32)n1 10.1021/jm031115r
CHEMBL96154 210254 None 0 Human Functional pIC50 = 7.6 7.6 -1 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 564 7 2 6 5.3 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(C(C)(C)C)cc3)c3ccccc32)n1 10.1021/jm031115r
11467573 107296 None 0 Human Functional pIC50 = 6.6 6.6 -9 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 606 8 2 7 5.0 COc1ccc(CN2C(=O)CN[C@](c3cccc(C(F)(F)F)c3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1 10.1021/jm031115r
CHEMBL316851 107296 None 0 Human Functional pIC50 = 6.6 6.6 -9 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 606 8 2 7 5.0 COc1ccc(CN2C(=O)CN[C@](c3cccc(C(F)(F)F)c3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1 10.1021/jm031115r
11331242 107476 None 0 Human Functional pIC50 = 7.6 7.6 -1 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 652 8 2 6 7.0 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3cccc(-c4ccccc4)c3)NCC(=O)N(Cc3c(Cl)cccc3Cl)c3ccccc32)n1 10.1021/jm031115r
CHEMBL318086 107476 None 0 Human Functional pIC50 = 7.6 7.6 -1 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 652 8 2 6 7.0 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3cccc(-c4ccccc4)c3)NCC(=O)N(Cc3c(Cl)cccc3Cl)c3ccccc32)n1 10.1021/jm031115r
11342005 210008 None 0 Human Functional pIC50 = 7.6 7.6 -2 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 562 7 2 6 4.4 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3cc(F)c(F)c(F)c3)c3ccccc32)n1 10.1021/jm031115r
CHEMBL94766 210008 None 0 Human Functional pIC50 = 7.6 7.6 -2 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 562 7 2 6 4.4 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3cc(F)c(F)c(F)c3)c3ccccc32)n1 10.1021/jm031115r
11307805 107397 None 0 Human Functional pIC50 = 7.6 7.6 -3 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 586 7 2 6 4.8 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3cccc(Br)c3)c3ccccc32)n1 10.1021/jm031115r
CHEMBL317589 107397 None 0 Human Functional pIC50 = 7.6 7.6 -3 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 586 7 2 6 4.8 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3cccc(Br)c3)c3ccccc32)n1 10.1021/jm031115r
10226239 210347 None 0 Human Functional pIC50 = 6.6 6.6 -4 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 456 5 2 8 2.9 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCc3nnc(C)n3-c3ccccc32)n1 10.1021/jm031115r
CHEMBL96614 210347 None 0 Human Functional pIC50 = 6.6 6.6 -4 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 456 5 2 8 2.9 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCc3nnc(C)n3-c3ccccc32)n1 10.1021/jm031115r
44328057 96947 None 0 Rat Functional pIC50 = 5.6 5.6 7 2
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
ChEMBL 986 26 9 9 4.9 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)c1cccnc1)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL265734 96947 None 0 Rat Functional pIC50 = 5.6 5.6 7 2
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
ChEMBL 986 26 9 9 4.9 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)c1cccnc1)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
11156376 112729 None 0 Human Functional pIC50 = 6.6 6.6 -5 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 504 9 3 7 2.7 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(CCCC(=O)O)c3ccccc32)n1 10.1021/jm031115r
CHEMBL330359 112729 None 0 Human Functional pIC50 = 6.6 6.6 -5 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 504 9 3 7 2.7 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(CCCC(=O)O)c3ccccc32)n1 10.1021/jm031115r
11375934 210372 None 0 Human Functional pIC50 = 7.6 7.6 -3 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 526 7 2 6 4.1 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3cccc(F)c3)c3ccccc32)n1 10.1021/jm031115r
CHEMBL96746 210372 None 0 Human Functional pIC50 = 7.6 7.6 -3 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 526 7 2 6 4.1 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3cccc(F)c3)c3ccccc32)n1 10.1021/jm031115r
11156301 78695 None 0 Human Functional pIC50 = 6.6 6.6 -4 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 500 7 3 9 2.2 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCc3nnc(CC(=O)O)n3-c3ccccc32)n1 10.1021/jm031115r
CHEMBL2112377 78695 None 0 Human Functional pIC50 = 6.6 6.6 -4 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 500 7 3 9 2.2 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCc3nnc(CC(=O)O)n3-c3ccccc32)n1 10.1021/jm031115r
10070783 97109 None 0 Human Functional pIC50 = 5.6 5.6 -5 3
Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).
ChEMBL 420 4 1 5 4.5 O=C1OC(O)(c2ccc(Cl)cc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2 10.1021/jm00008a002
CHEMBL267094 97109 None 0 Human Functional pIC50 = 5.6 5.6 -5 3
Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).
ChEMBL 420 4 1 5 4.5 O=C1OC(O)(c2ccc(Cl)cc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2 10.1021/jm00008a002
11478911 156401 None 0 Human Functional pIC50 = 7.5 7.5 -4 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 598 7 2 6 4.7 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(F)c(F)c(F)c(F)c3F)c3ccccc32)n1 10.1021/jm031115r
CHEMBL406551 156401 None 0 Human Functional pIC50 = 7.5 7.5 -4 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 598 7 2 6 4.7 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(F)c(F)c(F)c(F)c3F)c3ccccc32)n1 10.1021/jm031115r
44327890 141499 None 0 Rat Functional pIC50 = 6.5 6.5 46 3
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
ChEMBL 985 26 9 8 5.5 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)c1ccccc1)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL384052 141499 None 0 Rat Functional pIC50 = 6.5 6.5 46 3
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
ChEMBL 985 26 9 8 5.5 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)c1ccccc1)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
44327656 141876 None 0 Rat Functional pIC50 = 6.5 6.5 1 2
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
ChEMBL 977 25 9 8 4.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C(F)(F)F)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL386181 141876 None 0 Rat Functional pIC50 = 6.5 6.5 1 2
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
ChEMBL 977 25 9 8 4.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C(F)(F)F)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
11421972 210304 None 0 Human Functional pIC50 = 7.5 7.5 -2 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 592 8 2 7 4.9 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3cccc(OC(F)(F)F)c3)c3ccccc32)n1 10.1021/jm031115r
CHEMBL96422 210304 None 0 Human Functional pIC50 = 7.5 7.5 -2 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 592 8 2 7 4.9 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3cccc(OC(F)(F)F)c3)c3ccccc32)n1 10.1021/jm031115r
345351 9361 None 3 Human Functional pIC50 = 4.5 4.5 -33 3
Tested for antagonistic activity against Endothelin B receptor in human (CHO expressed).Tested for antagonistic activity against Endothelin B receptor in human (CHO expressed).
ChEMBL 386 4 1 5 3.8 O=C1OC(O)(c2ccccc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2 10.1021/jm00008a002
CHEMBL11131 9361 None 3 Human Functional pIC50 = 4.5 4.5 -33 3
Tested for antagonistic activity against Endothelin B receptor in human (CHO expressed).Tested for antagonistic activity against Endothelin B receptor in human (CHO expressed).
ChEMBL 386 4 1 5 3.8 O=C1OC(O)(c2ccccc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2 10.1021/jm00008a002
11455999 210288 None 0 Human Functional pIC50 = 5.5 5.5 -31 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 580 7 2 4 6.6 O=C(O)[C@@H](Oc1cccc(Cl)c1)[C@@]1(c2ccccc2)NCC(=O)N(Cc2c(Cl)cccc2Cl)c2ccccc21 10.1021/jm031115r
CHEMBL96325 210288 None 0 Human Functional pIC50 = 5.5 5.5 -31 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 580 7 2 4 6.6 O=C(O)[C@@H](Oc1cccc(Cl)c1)[C@@]1(c2ccccc2)NCC(=O)N(Cc2c(Cl)cccc2Cl)c2ccccc21 10.1021/jm031115r
10282008 209539 None 0 Human Functional pIC50 = 7.5 7.5 -12 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 592 8 2 7 4.9 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(OC(F)(F)F)cc3)c3ccccc32)n1 10.1021/jm031115r
CHEMBL91873 209539 None 0 Human Functional pIC50 = 7.5 7.5 -12 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 592 8 2 7 4.9 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(OC(F)(F)F)cc3)c3ccccc32)n1 10.1021/jm031115r
11364770 163751 None 0 Human Functional pIC50 = 7.5 7.5 -5 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 544 7 2 6 4.3 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(F)c(F)c3)c3ccccc32)n1 10.1021/jm031115r
CHEMBL420435 163751 None 0 Human Functional pIC50 = 7.5 7.5 -5 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 544 7 2 6 4.3 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(F)c(F)c3)c3ccccc32)n1 10.1021/jm031115r
11191999 209958 None 0 Human Functional pIC50 = 7.5 7.5 -4 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 544 7 2 6 4.3 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3cc(F)ccc3F)c3ccccc32)n1 10.1021/jm031115r
CHEMBL94438 209958 None 0 Human Functional pIC50 = 7.5 7.5 -4 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 544 7 2 6 4.3 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3cc(F)ccc3F)c3ccccc32)n1 10.1021/jm031115r
11168474 210364 None 0 Human Functional pIC50 = 7.5 7.5 -9 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 526 7 2 6 4.1 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccccc3F)c3ccccc32)n1 10.1021/jm031115r
CHEMBL96723 210364 None 0 Human Functional pIC50 = 7.5 7.5 -9 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 526 7 2 6 4.1 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccccc3F)c3ccccc32)n1 10.1021/jm031115r
11308052 112728 None 0 Human Functional pIC50 = 7.5 7.5 -2 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 618 10 2 6 5.8 CCCCc1cccc([C@]2([C@H](Oc3nc(C)cc(C)n3)C(=O)O)NCC(=O)N(Cc3c(F)cc(F)cc3F)c3ccccc32)c1 10.1021/jm031115r
CHEMBL330354 112728 None 0 Human Functional pIC50 = 7.5 7.5 -2 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 618 10 2 6 5.8 CCCCc1cccc([C@]2([C@H](Oc3nc(C)cc(C)n3)C(=O)O)NCC(=O)N(Cc3c(F)cc(F)cc3F)c3ccccc32)c1 10.1021/jm031115r
11330570 210043 None 0 Human Functional pIC50 = 7.5 7.5 -4 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 570 8 2 7 4.5 COc1ccc(CN2C(=O)CN[C@](c3ccc(F)c(C)c3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1 10.1021/jm031115r
CHEMBL94934 210043 None 0 Human Functional pIC50 = 7.5 7.5 -4 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 570 8 2 7 4.5 COc1ccc(CN2C(=O)CN[C@](c3ccc(F)c(C)c3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1 10.1021/jm031115r
11432855 210313 None 0 Human Functional pIC50 = 5.5 5.5 -28 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 552 8 3 7 3.7 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(C(=O)O)cc3)c3ccccc32)n1 10.1021/jm031115r
CHEMBL96463 210313 None 0 Human Functional pIC50 = 5.5 5.5 -28 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 552 8 3 7 3.7 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(C(=O)O)cc3)c3ccccc32)n1 10.1021/jm031115r
11444738 164974 None 0 Human Functional pIC50 = 7.4 7.4 -4 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 594 11 2 7 5.4 CCCCc1cccc([C@]2([C@H](Oc3nc(C)cc(C)n3)C(=O)O)NCC(=O)N(Cc3ccc(OC)cc3)c3ccccc32)c1 10.1021/jm031115r
CHEMBL422068 164974 None 0 Human Functional pIC50 = 7.4 7.4 -4 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 594 11 2 7 5.4 CCCCc1cccc([C@]2([C@H](Oc3nc(C)cc(C)n3)C(=O)O)NCC(=O)N(Cc3ccc(OC)cc3)c3ccccc32)c1 10.1021/jm031115r
44327347 96816 None 0 Rat Functional pIC50 = 5.4 5.4 3 3
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
ChEMBL 1102 26 9 8 7.1 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C1c2ccccc2CCc2ccccc21)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL264579 96816 None 0 Rat Functional pIC50 = 5.4 5.4 3 3
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
ChEMBL 1102 26 9 8 7.1 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C1c2ccccc2CCc2ccccc21)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
11235126 210386 None 0 Human Functional pIC50 = 5.4 5.4 -52 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 405 5 2 6 2.9 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCCOc3ccccc32)n1 10.1021/jm031115r
CHEMBL96831 210386 None 0 Human Functional pIC50 = 5.4 5.4 -52 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 405 5 2 6 2.9 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCCOc3ccccc32)n1 10.1021/jm031115r
11786120 169271 None 0 Human Functional pIC50 = 5.4 5.4 -17 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 546 7 2 4 5.9 O=C(O)[C@@H](Oc1ccccc1)[C@@]1(c2ccccc2)NCC(=O)N(Cc2c(Cl)cccc2Cl)c2ccccc21 10.1021/jm031115r
CHEMBL440507 169271 None 0 Human Functional pIC50 = 5.4 5.4 -17 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 546 7 2 4 5.9 O=C(O)[C@@H](Oc1ccccc1)[C@@]1(c2ccccc2)NCC(=O)N(Cc2c(Cl)cccc2Cl)c2ccccc21 10.1021/jm031115r
11409474 210019 None 0 Human Functional pIC50 = 7.4 7.4 -1 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 502 10 2 6 4.4 CCCCCCN1C(=O)CN[C@](c2ccccc2)([C@H](Oc2nc(C)cc(C)n2)C(=O)O)c2ccccc21 10.1021/jm031115r
CHEMBL94810 210019 None 0 Human Functional pIC50 = 7.4 7.4 -1 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 502 10 2 6 4.4 CCCCCCN1C(=O)CN[C@](c2ccccc2)([C@H](Oc2nc(C)cc(C)n2)C(=O)O)c2ccccc21 10.1021/jm031115r
9845562 4743 None 0 Human Functional pIC50 = 6.4 6.4 -7 3
Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).
ChEMBL 430 5 1 6 4.1 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(C)cc2)cc1 10.1021/jm00008a002
CHEMBL10374 4743 None 0 Human Functional pIC50 = 6.4 6.4 -7 3
Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).
ChEMBL 430 5 1 6 4.1 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(C)cc2)cc1 10.1021/jm00008a002
11330927 209966 None 0 Human Functional pIC50 = 6.4 6.4 -8 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 606 9 2 6 5.9 COc1cc(OC)cc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(Cl)cccc3Cl)c3ccccc32)c1 10.1021/jm031115r
CHEMBL94488 209966 None 0 Human Functional pIC50 = 6.4 6.4 -8 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 606 9 2 6 5.9 COc1cc(OC)cc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(Cl)cccc3Cl)c3ccccc32)c1 10.1021/jm031115r
44283270 167984 None 0 Human Functional pIC50 = 8.4 8.4 -1 4
Functional inhibition of ET-1 induced [Ca2+] increase in human Girardi heart (hGH) cells, which express Endothelin B receptorFunctional inhibition of ET-1 induced [Ca2+] increase in human Girardi heart (hGH) cells, which express Endothelin B receptor
ChEMBL 580 12 5 5 3.8 CCCC[C@H](NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)C)C(=O)O 10.1016/0960-894X(95)00237-N
CHEMBL431124 167984 None 0 Human Functional pIC50 = 8.4 8.4 -1 4
Functional inhibition of ET-1 induced [Ca2+] increase in human Girardi heart (hGH) cells, which express Endothelin B receptorFunctional inhibition of ET-1 induced [Ca2+] increase in human Girardi heart (hGH) cells, which express Endothelin B receptor
ChEMBL 580 12 5 5 3.8 CCCC[C@H](NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)C)C(=O)O 10.1016/0960-894X(95)00237-N
44327881 161769 None 0 Rat Functional pIC50 = 5.4 5.4 2 2
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
ChEMBL 1044 26 9 8 6.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C12CC3CC(CC(C3)C1)C2)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL413179 161769 None 0 Rat Functional pIC50 = 5.4 5.4 2 2
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
ChEMBL 1044 26 9 8 6.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C12CC3CC(CC(C3)C1)C2)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
23670447 3029 None 2 Human Functional pIC50 = 6.4 6.4 -501 4
Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).
ChEMBL 528 10 0 9 0.1 COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+] 10.1021/jm00008a002
999 3029 None 2 Human Functional pIC50 = 6.4 6.4 -501 4
Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).
ChEMBL 528 10 0 9 0.1 COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+] 10.1021/jm00008a002
CHEMBL1204799 3029 None 2 Human Functional pIC50 = 6.4 6.4 -501 4
Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).
ChEMBL 528 10 0 9 0.1 COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+] 10.1021/jm00008a002
CHEMBL25438 3029 None 2 Human Functional pIC50 = 6.4 6.4 -501 4
Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).
ChEMBL 528 10 0 9 0.1 COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+] 10.1021/jm00008a002
9807691 100118 None 0 Human Functional pIC50 = 6.4 6.4 -134 2
Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B receptor.Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B receptor.
ChEMBL 553 10 1 10 5.3 COc1cc2c(Sc3cc(OC)c(OC)c(OC)c3)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OC 10.1016/0960-894X(96)00232-6
CHEMBL287169 100118 None 0 Human Functional pIC50 = 6.4 6.4 -134 2
Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B receptor.Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B receptor.
ChEMBL 553 10 1 10 5.3 COc1cc2c(Sc3cc(OC)c(OC)c(OC)c3)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OC 10.1016/0960-894X(96)00232-6
9845562 4743 None 0 Rat Functional pIC50 = 5.4 5.4 -87 3
Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.
ChEMBL 430 5 1 6 4.1 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(C)cc2)cc1 10.1021/jm00008a002
CHEMBL10374 4743 None 0 Rat Functional pIC50 = 5.4 5.4 -87 3
Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.
ChEMBL 430 5 1 6 4.1 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(C)cc2)cc1 10.1021/jm00008a002
9865706 98187 None 0 Rat Functional pIC50 = 5.4 5.4 -1 2
Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.
ChEMBL 400 4 1 5 4.1 Cc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1 10.1021/jm00008a002
CHEMBL273613 98187 None 0 Rat Functional pIC50 = 5.4 5.4 -1 2
Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.
ChEMBL 400 4 1 5 4.1 Cc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1 10.1021/jm00008a002
11742628 98288 None 0 Human Functional pIC50 = 5.3 5.3 -234 3
Tested for antagonistic activity against Endothelin B receptor in human (CHO expressed).Tested for antagonistic activity against Endothelin B receptor in human (CHO expressed).
ChEMBL 416 5 1 6 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1 10.1021/jm00008a002
CHEMBL274383 98288 None 0 Human Functional pIC50 = 5.3 5.3 -234 3
Tested for antagonistic activity against Endothelin B receptor in human (CHO expressed).Tested for antagonistic activity against Endothelin B receptor in human (CHO expressed).
ChEMBL 416 5 1 6 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1 10.1021/jm00008a002
10166981 209546 None 0 Human Functional pIC50 = 7.3 7.3 -2 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 576 7 2 6 5.0 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(C(F)(F)F)cc3)c3ccccc32)n1 10.1021/jm031115r
CHEMBL91926 209546 None 0 Human Functional pIC50 = 7.3 7.3 -2 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 576 7 2 6 5.0 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(C(F)(F)F)cc3)c3ccccc32)n1 10.1021/jm031115r
11283571 210057 None 0 Human Functional pIC50 = 7.3 7.3 -7 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 508 7 2 6 4.0 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccccc3)c3ccccc32)n1 10.1021/jm031115r
CHEMBL95013 210057 None 0 Human Functional pIC50 = 7.3 7.3 -7 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 508 7 2 6 4.0 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccccc3)c3ccccc32)n1 10.1021/jm031115r
11477664 168270 None 0 Human Functional pIC50 = 7.3 7.3 -6 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 506 10 2 8 2.4 COCCOCN1C(=O)CN[C@](c2ccccc2)([C@H](Oc2nc(C)cc(C)n2)C(=O)O)c2ccccc21 10.1021/jm031115r
CHEMBL433173 168270 None 0 Human Functional pIC50 = 7.3 7.3 -6 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 506 10 2 8 2.4 COCCOCN1C(=O)CN[C@](c2ccccc2)([C@H](Oc2nc(C)cc(C)n2)C(=O)O)c2ccccc21 10.1021/jm031115r
11408654 210395 None 0 Human Functional pIC50 = 6.3 6.3 -19 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 464 7 2 8 1.8 COc1cc(OC)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3ccccc32)n1 10.1021/jm031115r
CHEMBL96906 210395 None 0 Human Functional pIC50 = 6.3 6.3 -19 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 464 7 2 8 1.8 COc1cc(OC)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3ccccc32)n1 10.1021/jm031115r
10230703 210318 None 0 Human Functional pIC50 = 7.3 7.3 -4 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 542 7 2 6 4.7 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccccc3Cl)c3ccccc32)n1 10.1021/jm031115r
CHEMBL96472 210318 None 0 Human Functional pIC50 = 7.3 7.3 -4 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 542 7 2 6 4.7 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccccc3Cl)c3ccccc32)n1 10.1021/jm031115r
9870830 209172 None 29 Human Functional pIC50 = 6.3 6.3 -776 4
Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).
ChEMBL 506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1021/jm00008a002
CHEMBL8981 209172 None 29 Human Functional pIC50 = 6.3 6.3 -776 4
Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).
ChEMBL 506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1021/jm00008a002
11307457 210070 None 0 Human Functional pIC50 = 7.3 7.3 -5 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 556 8 2 7 4.2 COc1ccc(CN2C(=O)CN[C@](c3cccc(F)c3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1 10.1021/jm031115r
CHEMBL95095 210070 None 0 Human Functional pIC50 = 7.3 7.3 -5 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 556 8 2 7 4.2 COc1ccc(CN2C(=O)CN[C@](c3cccc(F)c3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1 10.1021/jm031115r
11785813 106978 None 0 Human Functional pIC50 = 7.3 7.3 -8 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 526 7 2 6 4.1 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(F)cc3)c3ccccc32)n1 10.1021/jm031115r
CHEMBL314755 106978 None 0 Human Functional pIC50 = 7.3 7.3 -8 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 526 7 2 6 4.1 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(F)cc3)c3ccccc32)n1 10.1021/jm031115r
10209814 209729 None 0 Human Functional pIC50 = 7.3 7.3 -7 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 562 7 2 6 4.4 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(F)c(F)c3F)c3ccccc32)n1 10.1021/jm031115r
CHEMBL93084 209729 None 0 Human Functional pIC50 = 7.3 7.3 -7 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 562 7 2 6 4.4 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(F)c(F)c3F)c3ccccc32)n1 10.1021/jm031115r
11284285 107385 None 0 Human Functional pIC50 = 7.3 7.3 -8 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 552 8 2 7 4.3 COc1ccc(CN2C(=O)CN[C@](c3cccc(C)c3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1 10.1021/jm031115r
CHEMBL317510 107385 None 0 Human Functional pIC50 = 7.3 7.3 -8 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 552 8 2 7 4.3 COc1ccc(CN2C(=O)CN[C@](c3cccc(C)c3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1 10.1021/jm031115r
11742628 98288 None 0 Rat Functional pIC50 = 6.3 6.3 -25 3
Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.
ChEMBL 416 5 1 6 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1 10.1021/jm00008a002
CHEMBL274383 98288 None 0 Rat Functional pIC50 = 6.3 6.3 -25 3
Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.
ChEMBL 416 5 1 6 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1 10.1021/jm00008a002
10070783 97109 None 0 Rat Functional pIC50 = 5.3 5.3 -3 3
Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.
ChEMBL 420 4 1 5 4.5 O=C1OC(O)(c2ccc(Cl)cc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2 10.1021/jm00008a002
CHEMBL267094 97109 None 0 Rat Functional pIC50 = 5.3 5.3 -3 3
Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.
ChEMBL 420 4 1 5 4.5 O=C1OC(O)(c2ccc(Cl)cc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2 10.1021/jm00008a002
11490160 209960 None 0 Human Functional pIC50 = 6.3 6.3 -5 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 584 8 2 6 5.7 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)n1 10.1021/jm031115r
CHEMBL94446 209960 None 0 Human Functional pIC50 = 6.3 6.3 -5 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 584 8 2 6 5.7 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)n1 10.1021/jm031115r
11432418 107004 None 0 Human Functional pIC50 = 7.3 7.3 -6 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 522 7 2 6 4.3 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccccc3C)c3ccccc32)n1 10.1021/jm031115r
CHEMBL314946 107004 None 0 Human Functional pIC50 = 7.3 7.3 -6 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 522 7 2 6 4.3 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccccc3C)c3ccccc32)n1 10.1021/jm031115r
10140418 106257 None 0 Human Functional pIC50 = 6.3 6.3 -43 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 476 7 3 7 1.9 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(CC(=O)O)c3ccccc32)n1 10.1021/jm031115r
CHEMBL313867 106257 None 0 Human Functional pIC50 = 6.3 6.3 -43 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 476 7 3 7 1.9 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(CC(=O)O)c3ccccc32)n1 10.1021/jm031115r
44327585 161877 None 0 Rat Functional pIC50 = 6.3 6.3 14 2
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
ChEMBL 992 26 9 8 5.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C1CCCCC1)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL414082 161877 None 0 Rat Functional pIC50 = 6.3 6.3 14 2
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
ChEMBL 992 26 9 8 5.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C1CCCCC1)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
11167889 210294 None 0 Human Functional pIC50 = 5.3 5.3 -1 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 496 7 2 6 3.7 COc1cc(OC)cc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3cc(Cl)ccc32)c1 10.1021/jm031115r
CHEMBL96351 210294 None 0 Human Functional pIC50 = 5.3 5.3 -1 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 496 7 2 6 3.7 COc1cc(OC)cc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3cc(Cl)ccc32)c1 10.1021/jm031115r
10347783 210293 None 0 Human Functional pIC50 = 6.3 6.3 -32 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 560 7 2 4 5.6 Cc1cc(C)cc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(F)cc(F)cc3F)c3ccccc32)c1 10.1021/jm031115r
CHEMBL96347 210293 None 0 Human Functional pIC50 = 6.3 6.3 -32 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 560 7 2 4 5.6 Cc1cc(C)cc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(F)cc(F)cc3F)c3ccccc32)c1 10.1021/jm031115r
1009 194 None 25 Human Functional pIC50 = 8.2 8.2 1479 2
Eurofins cellular functional assay - Antagonist (EDNRB)Eurofins cellular functional assay - Antagonist (EDNRB)
ChEMBL 558 11 2 6 5.8 CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2 10.6019/CHEMBL4507261
5310991 194 None 25 Human Functional pIC50 = 8.2 8.2 1479 2
Eurofins cellular functional assay - Antagonist (EDNRB)Eurofins cellular functional assay - Antagonist (EDNRB)
ChEMBL 558 11 2 6 5.8 CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2 10.6019/CHEMBL4507261
CHEMBL332794 194 None 25 Human Functional pIC50 = 8.2 8.2 1479 2
Eurofins cellular functional assay - Antagonist (EDNRB)Eurofins cellular functional assay - Antagonist (EDNRB)
ChEMBL 558 11 2 6 5.8 CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2 10.6019/CHEMBL4507261
9894443 112636 None 0 Human Functional pIC50 = 8.2 8.2 -3 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 576 7 2 6 5.3 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(Cl)cccc3Cl)c3ccccc32)n1 10.1021/jm031115r
CHEMBL330104 112636 None 0 Human Functional pIC50 = 8.2 8.2 -3 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 576 7 2 6 5.3 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(Cl)cccc3Cl)c3ccccc32)n1 10.1021/jm031115r
11385689 112859 None 0 Human Functional pIC50 = 5.2 5.2 -10 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 462 7 2 6 3.0 COc1cc(OC)cc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3ccccc32)c1 10.1021/jm031115r
CHEMBL330629 112859 None 0 Human Functional pIC50 = 5.2 5.2 -10 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 462 7 2 6 3.0 COc1cc(OC)cc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3ccccc32)c1 10.1021/jm031115r
10163956 210048 None 0 Human Functional pIC50 = 7.2 7.2 -10 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 500 7 3 9 1.5 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3nn[nH]n3)c3ccccc32)n1 10.1021/jm031115r
CHEMBL94964 210048 None 0 Human Functional pIC50 = 7.2 7.2 -10 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 500 7 3 9 1.5 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3nn[nH]n3)c3ccccc32)n1 10.1021/jm031115r
11224973 107506 None 0 Human Functional pIC50 = 6.2 6.2 -32 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 460 7 2 6 2.9 CCc1cc(CC)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3ccccc32)n1 10.1021/jm031115r
CHEMBL318270 107506 None 0 Human Functional pIC50 = 6.2 6.2 -32 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 460 7 2 6 2.9 CCc1cc(CC)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3ccccc32)n1 10.1021/jm031115r
11353580 210397 None 0 Human Functional pIC50 = 7.2 7.2 -21 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 566 9 2 7 4.6 CCc1cccc([C@]2([C@H](Oc3nc(C)cc(C)n3)C(=O)O)NCC(=O)N(Cc3ccc(OC)cc3)c3ccccc32)c1 10.1021/jm031115r
CHEMBL96932 210397 None 0 Human Functional pIC50 = 7.2 7.2 -21 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 566 9 2 7 4.6 CCc1cccc([C@]2([C@H](Oc3nc(C)cc(C)n3)C(=O)O)NCC(=O)N(Cc3ccc(OC)cc3)c3ccccc32)c1 10.1021/jm031115r
11156692 167979 None 0 Human Functional pIC50 = 7.2 7.2 -2 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 522 7 2 6 4.3 Cc1ccc(CN2C(=O)CN[C@](c3ccccc3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1 10.1021/jm031115r
CHEMBL431087 167979 None 0 Human Functional pIC50 = 7.2 7.2 -2 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 522 7 2 6 4.3 Cc1ccc(CN2C(=O)CN[C@](c3ccccc3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1 10.1021/jm031115r
11204331 112642 None 0 Human Functional pIC50 = 8.2 8.2 1 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 616 10 2 6 6.1 CCCCc1cccc([C@]2([C@H](Oc3nc(C)cc(C)n3)C(=O)O)NCC(=O)N(Cc3c(F)cccc3Cl)c3ccccc32)c1 10.1021/jm031115r
CHEMBL330135 112642 None 0 Human Functional pIC50 = 8.2 8.2 1 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 616 10 2 6 6.1 CCCCc1cccc([C@]2([C@H](Oc3nc(C)cc(C)n3)C(=O)O)NCC(=O)N(Cc3c(F)cccc3Cl)c3ccccc32)c1 10.1021/jm031115r
10303311 107218 None 0 Human Functional pIC50 = 7.2 7.2 -9 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 566 8 2 8 3.8 COC(=O)c1ccc(CN2C(=O)CN[C@](c3ccccc3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1 10.1021/jm031115r
CHEMBL316301 107218 None 0 Human Functional pIC50 = 7.2 7.2 -9 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 566 8 2 8 3.8 COC(=O)c1ccc(CN2C(=O)CN[C@](c3ccccc3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1 10.1021/jm031115r
11202819 112627 None 0 Human Functional pIC50 = 6.2 6.2 -1 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 499 6 3 8 3.2 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCc3c(C(=O)O)nc(C)n3-c3ccccc32)n1 10.1021/jm031115r
CHEMBL330045 112627 None 0 Human Functional pIC50 = 6.2 6.2 -1 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 499 6 3 8 3.2 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCc3c(C(=O)O)nc(C)n3-c3ccccc32)n1 10.1021/jm031115r
11478553 163545 None 0 Human Functional pIC50 = 7.1 7.1 -10 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 562 7 2 6 4.4 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3cc(F)c(F)cc3F)c3ccccc32)n1 10.1021/jm031115r
CHEMBL419879 163545 None 0 Human Functional pIC50 = 7.1 7.1 -10 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 562 7 2 6 4.4 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3cc(F)c(F)cc3F)c3ccccc32)n1 10.1021/jm031115r
11744509 5432 None 0 Rat Functional pIC50 = 6.1 6.1 -5 2
Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.
ChEMBL 450 5 1 6 4.5 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(Cl)cc2)cc1 10.1021/jm00008a002
CHEMBL10733 5432 None 0 Rat Functional pIC50 = 6.1 6.1 -5 2
Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.
ChEMBL 450 5 1 6 4.5 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(Cl)cc2)cc1 10.1021/jm00008a002
11307120 112467 None 0 Human Functional pIC50 = 7.1 7.1 4 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 532 11 2 7 4.5 CCCCC[C@]1([C@H](Oc2nc(C)cc(C)n2)C(=O)O)NCC(=O)N(Cc2ccc(OC)cc2)c2ccccc21 10.1021/jm031115r
CHEMBL329744 112467 None 0 Human Functional pIC50 = 7.1 7.1 4 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 532 11 2 7 4.5 CCCCC[C@]1([C@H](Oc2nc(C)cc(C)n2)C(=O)O)NCC(=O)N(Cc2ccc(OC)cc2)c2ccccc21 10.1021/jm031115r
11456110 210298 None 0 Human Functional pIC50 = 7.1 7.1 1 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 592 8 2 7 4.9 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccccc3OC(F)(F)F)c3ccccc32)n1 10.1021/jm031115r
CHEMBL96387 210298 None 0 Human Functional pIC50 = 7.1 7.1 1 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 592 8 2 7 4.9 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccccc3OC(F)(F)F)c3ccccc32)n1 10.1021/jm031115r
18995989 100609 None 0 Human Functional pIC50 = 6.1 6.1 2 2
Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B receptor.Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B receptor.
ChEMBL 583 9 1 9 6.6 COc1cc2c(Sc3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OCc1ccccc1 10.1016/0960-894X(96)00232-6
CHEMBL29147 100609 None 0 Human Functional pIC50 = 6.1 6.1 2 2
Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B receptor.Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin B receptor.
ChEMBL 583 9 1 9 6.6 COc1cc2c(Sc3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OCc1ccccc1 10.1016/0960-894X(96)00232-6
11318559 210261 None 0 Human Functional pIC50 = 6.1 6.1 -5 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 531 8 2 8 2.1 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(CCN3CCOCC3)c3ccccc32)n1 10.1021/jm031115r
CHEMBL96193 210261 None 0 Human Functional pIC50 = 6.1 6.1 -5 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 531 8 2 8 2.1 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(CCN3CCOCC3)c3ccccc32)n1 10.1021/jm031115r
11410410 210009 None 0 Human Functional pIC50 = 6.1 6.1 -25 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 560 7 2 4 6.2 Cc1cccc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(Cl)cccc3Cl)c3ccccc32)c1 10.1021/jm031115r
CHEMBL94769 210009 None 0 Human Functional pIC50 = 6.1 6.1 -25 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 560 7 2 4 6.2 Cc1cccc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(Cl)cccc3Cl)c3ccccc32)c1 10.1021/jm031115r
CHEMBL413825 215547 None 0 Human Functional pIC50 = 5.1 5.1 4 2
Ability to block endothelin-1 (ET-1) stimulated arachidonic acid release in rabbit renal vascular smooth muscle cells (AARA) expressing recombinant rat endothelin B (ETB) receptorAbility to block endothelin-1 (ET-1) stimulated arachidonic acid release in rabbit renal vascular smooth muscle cells (AARA) expressing recombinant rat endothelin B (ETB) receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(N)=O)NC(=O)CNC(=O)[C@H](CC(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H]2CCCN2C1=O 10.1016/0960-894X(95)00084-7
11489946 209806 None 0 Human Functional pIC50 = 6.1 6.1 -2 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 566 8 2 7 4.6 COc1ccc(CN2C(=O)CN[C@](c3cc(C)cc(C)c3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1 10.1021/jm031115r
CHEMBL93612 209806 None 0 Human Functional pIC50 = 6.1 6.1 -2 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 566 8 2 7 4.6 COc1ccc(CN2C(=O)CN[C@](c3cc(C)cc(C)c3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1 10.1021/jm031115r
11785180 111571 None 0 Human Functional pIC50 = 5.1 5.1 -1 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 492 8 2 7 3.1 COc1cc(OC)cc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3cc(OC)ccc32)c1 10.1021/jm031115r
CHEMBL327823 111571 None 0 Human Functional pIC50 = 5.1 5.1 -1 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 492 8 2 7 3.1 COc1cc(OC)cc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3cc(OC)ccc32)c1 10.1021/jm031115r
11238500 210283 None 0 Human Functional pIC50 = 7.1 7.1 -3 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 572 8 2 7 4.7 COc1ccc(CN2C(=O)CN[C@](c3cccc(Cl)c3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1 10.1021/jm031115r
CHEMBL96313 210283 None 0 Human Functional pIC50 = 7.1 7.1 -3 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 572 8 2 7 4.7 COc1ccc(CN2C(=O)CN[C@](c3cccc(Cl)c3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1 10.1021/jm031115r
11441050 210290 None 0 Human Functional pIC50 = 5.1 5.1 -85 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 403 5 2 5 3.4 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCCCc3ccccc32)n1 10.1021/jm031115r
CHEMBL96331 210290 None 0 Human Functional pIC50 = 5.1 5.1 -85 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 403 5 2 5 3.4 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCCCc3ccccc32)n1 10.1021/jm031115r
11398818 168034 None 0 Human Functional pIC50 = 7.1 7.1 -2 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 556 8 2 7 4.2 COc1ccc(CN2C(=O)CN[C@](c3ccccc3F)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1 10.1021/jm031115r
CHEMBL431460 168034 None 0 Human Functional pIC50 = 7.1 7.1 -2 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 556 8 2 7 4.2 COc1ccc(CN2C(=O)CN[C@](c3ccccc3F)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1 10.1021/jm031115r
11168401 112367 None 0 Human Functional pIC50 = 5.1 5.1 -18 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 522 9 2 8 3.1 COc1cc(OC)cc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3cc(OC)c(OC)cc32)c1 10.1021/jm031115r
CHEMBL329132 112367 None 0 Human Functional pIC50 = 5.1 5.1 -18 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 522 9 2 8 3.1 COc1cc(OC)cc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3cc(OC)c(OC)cc32)c1 10.1021/jm031115r
11489174 112611 None 0 Human Functional pIC50 = 7.1 7.1 1 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 514 7 2 6 4.4 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(CC3CCCCC3)c3ccccc32)n1 10.1021/jm031115r
CHEMBL329943 112611 None 0 Human Functional pIC50 = 7.1 7.1 1 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 514 7 2 6 4.4 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(CC3CCCCC3)c3ccccc32)n1 10.1021/jm031115r
10166543 112425 None 0 Human Functional pIC50 = 7.1 7.1 -33 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 562 7 2 6 4.4 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(F)cc(F)cc3F)c3ccccc32)n1 10.1021/jm031115r
CHEMBL329477 112425 None 0 Human Functional pIC50 = 7.1 7.1 -33 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 562 7 2 6 4.4 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(F)cc(F)cc3F)c3ccccc32)n1 10.1021/jm031115r
11387934 107233 None 0 Human Functional pIC50 = 7.1 7.1 -28 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 614 9 2 7 5.7 COc1ccc(CN2C(=O)CN[C@](c3cccc(-c4ccccc4)c3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1 10.1021/jm031115r
CHEMBL316453 107233 None 0 Human Functional pIC50 = 7.1 7.1 -28 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 614 9 2 7 5.7 COc1ccc(CN2C(=O)CN[C@](c3cccc(-c4ccccc4)c3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1 10.1021/jm031115r
11157599 163578 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 588 8 2 4 7.0 CC(C)c1ccc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(Cl)cccc3Cl)c3ccccc32)cc1 10.1021/jm031115r
CHEMBL420072 163578 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 588 8 2 4 7.0 CC(C)c1ccc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(Cl)cccc3Cl)c3ccccc32)cc1 10.1021/jm031115r
11155687 210286 None 0 Human Functional pIC50 = 7.1 7.1 -12 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 472 7 2 6 3.2 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(CC3CC3)c3ccccc32)n1 10.1021/jm031115r
CHEMBL96318 210286 None 0 Human Functional pIC50 = 7.1 7.1 -12 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 472 7 2 6 3.2 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(CC3CC3)c3ccccc32)n1 10.1021/jm031115r
11377200 108354 None 0 Human Functional pIC50 = 7.1 7.1 -11 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 638 8 2 6 6.1 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3cccc(-c4ccccc4)c3)NCC(=O)N(Cc3c(F)cc(F)cc3F)c3ccccc32)n1 10.1021/jm031115r
CHEMBL319754 108354 None 0 Human Functional pIC50 = 7.1 7.1 -11 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 638 8 2 6 6.1 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3cccc(-c4ccccc4)c3)NCC(=O)N(Cc3c(F)cc(F)cc3F)c3ccccc32)n1 10.1021/jm031115r
44327466 96504 None 0 Rat Functional pIC50 = 6.1 6.1 16 2
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
ChEMBL 966 25 9 8 5.2 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C(C)(C)C)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL262229 96504 None 0 Rat Functional pIC50 = 6.1 6.1 16 2
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
ChEMBL 966 25 9 8 5.2 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C(C)(C)C)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL319537 213678 None 0 Rat Functional pIC50 = 5.0 5.0 -2 2
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
11362537 107577 None 0 Human Functional pIC50 = 5.0 5.0 -24 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 434 6 2 7 1.8 COc1cnc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3ccccc32)nc1 10.1021/jm031115r
CHEMBL318683 107577 None 0 Human Functional pIC50 = 5.0 5.0 -24 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 434 6 2 7 1.8 COc1cnc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3ccccc32)nc1 10.1021/jm031115r
44327348 162001 None 0 Rat Functional pIC50 = 5.0 5.0 -1 2
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
ChEMBL 1076 28 9 8 7.0 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL415238 162001 None 0 Rat Functional pIC50 = 5.0 5.0 -1 2
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
ChEMBL 1076 28 9 8 7.0 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL407933 215154 None 0 Rat Functional pIC50 = 5.0 5.0 -1 2
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptorsInhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)NC1CCCCC1)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
11342089 107264 None 0 Human Functional pIC50 = 7.0 7.0 -9 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 568 9 2 8 4.0 COc1ccc(CN2C(=O)CN[C@](c3cccc(OC)c3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1 10.1021/jm031115r
CHEMBL316629 107264 None 0 Human Functional pIC50 = 7.0 7.0 -9 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 568 9 2 8 4.0 COc1ccc(CN2C(=O)CN[C@](c3cccc(OC)c3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1 10.1021/jm031115r
11488556 210328 None 0 Human Functional pIC50 = 5.0 5.0 -10 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 482 5 2 6 2.6 CN1C(=O)CN[C@](c2ccccc2)([C@H](Oc2ncc(Br)cn2)C(=O)O)c2ccccc21 10.1021/jm031115r
CHEMBL96520 210328 None 0 Human Functional pIC50 = 5.0 5.0 -10 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 482 5 2 6 2.6 CN1C(=O)CN[C@](c2ccccc2)([C@H](Oc2ncc(Br)cn2)C(=O)O)c2ccccc21 10.1021/jm031115r
11226767 209985 None 0 Human Functional pIC50 = 6.0 6.0 -6 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 560 7 2 4 6.2 Cc1ccc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(Cl)cccc3Cl)c3ccccc32)cc1 10.1021/jm031115r
CHEMBL94606 209985 None 0 Human Functional pIC50 = 6.0 6.0 -6 2
Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
ChEMBL 560 7 2 4 6.2 Cc1ccc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(Cl)cccc3Cl)c3ccccc32)cc1 10.1021/jm031115r
9809919 206867 None 0 Rat Functional pKd = 6 6.0 - 2
In vitro functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETB receptors)In vitro functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETB receptors)
ChEMBL 665 13 2 13 4.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
CHEMBL72037 206867 None 0 Rat Functional pKd = 6 6.0 - 2
In vitro functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETB receptors)In vitro functional inhibitory potency prevention of ET-1 induced constriction of rat aortic rings (ETB receptors)
ChEMBL 665 13 2 13 4.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
18184194 130630 None 0 Rat Functional pKd = 7.0 7.0 - 2
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)
ChEMBL 712 15 2 12 4.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCCNS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(02)01083-1
CHEMBL368107 130630 None 0 Rat Functional pKd = 7.0 7.0 - 2
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)
ChEMBL 712 15 2 12 4.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCCNS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(02)01083-1
9831249 59717 None 0 Rat Functional pKd = 8.0 8.0 - 2
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)
ChEMBL 672 14 2 10 6.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C2CC2)nc1OCCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
CHEMBL172297 59717 None 0 Rat Functional pKd = 8.0 8.0 - 2
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)
ChEMBL 672 14 2 10 6.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C2CC2)nc1OCCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
9985589 168346 None 0 Human Functional pKd = 6.9 6.9 - 1
In vitro antagonistic activity against endothelin B receptor in isolated rabbit jugularis veinIn vitro antagonistic activity against endothelin B receptor in isolated rabbit jugularis vein
ChEMBL 576 9 1 8 5.0 CCN(c1ccc2c(c1)oc1c(-c3ccc(OC)cc3)c(C(=O)O)c(=O)n(Cc3ccccc3OC)c12)S(C)(=O)=O 10.1016/s0960-894x(99)00040-2
CHEMBL433700 168346 None 0 Human Functional pKd = 6.9 6.9 - 1
In vitro antagonistic activity against endothelin B receptor in isolated rabbit jugularis veinIn vitro antagonistic activity against endothelin B receptor in isolated rabbit jugularis vein
ChEMBL 576 9 1 8 5.0 CCN(c1ccc2c(c1)oc1c(-c3ccc(OC)cc3)c(C(=O)O)c(=O)n(Cc3ccccc3OC)c12)S(C)(=O)=O 10.1016/s0960-894x(99)00040-2
104865 706 None 60 Rat Functional pKd = 5.8 5.8 -11 5
Compound was evaluated for in vitro functional inhibitory potency for prevention of sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptors)Compound was evaluated for in vitro functional inhibitory potency for prevention of sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptors)
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/S0960-894X(97)00400-9
104865.0 706 None 60 Rat Functional pKd = 5.8 5.8 -11 5
Compound was evaluated for in vitro functional inhibitory potency for prevention of sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptors)Compound was evaluated for in vitro functional inhibitory potency for prevention of sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptors)
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/S0960-894X(97)00400-9
3494 706 None 60 Rat Functional pKd = 5.8 5.8 -11 5
Compound was evaluated for in vitro functional inhibitory potency for prevention of sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptors)Compound was evaluated for in vitro functional inhibitory potency for prevention of sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptors)
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/S0960-894X(97)00400-9
392 706 None 60 Rat Functional pKd = 5.8 5.8 -11 5
Compound was evaluated for in vitro functional inhibitory potency for prevention of sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptors)Compound was evaluated for in vitro functional inhibitory potency for prevention of sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptors)
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/S0960-894X(97)00400-9
CHEMBL957 706 None 60 Rat Functional pKd = 5.8 5.8 -11 5
Compound was evaluated for in vitro functional inhibitory potency for prevention of sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptors)Compound was evaluated for in vitro functional inhibitory potency for prevention of sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptors)
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/S0960-894X(97)00400-9
DB00559 706 None 60 Rat Functional pKd = 5.8 5.8 -11 5
Compound was evaluated for in vitro functional inhibitory potency for prevention of sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptors)Compound was evaluated for in vitro functional inhibitory potency for prevention of sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptors)
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/S0960-894X(97)00400-9
9848132 210036 None 0 Human Functional pKd = 5.8 5.8 - 2
Compound was evaluated for the antagonism at the Endothelin B receptor in isolated rabbit jugularis veinCompound was evaluated for the antagonism at the Endothelin B receptor in isolated rabbit jugularis vein
ChEMBL 483 6 1 8 2.8 Cc1cc(C)c(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)n1 10.1016/S0960-894X(96)00617-8
CHEMBL94918 210036 None 0 Human Functional pKd = 5.8 5.8 - 2
Compound was evaluated for the antagonism at the Endothelin B receptor in isolated rabbit jugularis veinCompound was evaluated for the antagonism at the Endothelin B receptor in isolated rabbit jugularis vein
ChEMBL 483 6 1 8 2.8 Cc1cc(C)c(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)n1 10.1016/S0960-894X(96)00617-8
9961131 132225 None 0 Rat Functional pKd = 6.6 6.6 - 2
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)
ChEMBL 650 15 2 12 3.1 CCCS(=O)(=O)NCCOc1nc(N2CCOCC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
CHEMBL369676 132225 None 0 Rat Functional pKd = 6.6 6.6 - 2
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)
ChEMBL 650 15 2 12 3.1 CCCS(=O)(=O)NCCOc1nc(N2CCOCC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
9809919 206867 None 0 Rat Functional pKd = 7.6 7.6 - 2
Compound was evaluated for in vitro functional inhibitory potency for prevention of sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptors)Compound was evaluated for in vitro functional inhibitory potency for prevention of sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptors)
ChEMBL 665 13 2 13 4.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
CHEMBL72037 206867 None 0 Rat Functional pKd = 7.6 7.6 - 2
Compound was evaluated for in vitro functional inhibitory potency for prevention of sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptors)Compound was evaluated for in vitro functional inhibitory potency for prevention of sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptors)
ChEMBL 665 13 2 13 4.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
9809270 131408 None 0 Rat Functional pKd = 5.6 5.6 - 2
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)
ChEMBL 622 14 2 12 2.3 CCCS(=O)(=O)NCCOc1nc(N2CCOCC2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
CHEMBL368738 131408 None 0 Rat Functional pKd = 5.6 5.6 - 2
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)
ChEMBL 622 14 2 12 2.3 CCCS(=O)(=O)NCCOc1nc(N2CCOCC2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
9873255 59653 None 0 Rat Functional pKd = 6.6 6.6 - 2
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)
ChEMBL 591 14 2 10 3.8 CCS(=O)(=O)NCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
CHEMBL172071 59653 None 0 Rat Functional pKd = 6.6 6.6 - 2
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)
ChEMBL 591 14 2 10 3.8 CCS(=O)(=O)NCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
18184234 62229 None 0 Rat Functional pKd = 6.6 6.6 - 2
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)
ChEMBL 605 15 2 10 4.2 CCS(=O)(=O)NCCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
CHEMBL177802 62229 None 0 Rat Functional pKd = 6.6 6.6 - 2
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)
ChEMBL 605 15 2 10 4.2 CCS(=O)(=O)NCCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
9807691 100118 None 0 Human Functional pKd = 5.5 5.5 -134 2
Inhibition of sarafotoxin-6c stimulated vasoconstriction in rabbit pulmonary artery.Inhibition of sarafotoxin-6c stimulated vasoconstriction in rabbit pulmonary artery.
ChEMBL 553 10 1 10 5.3 COc1cc2c(Sc3cc(OC)c(OC)c(OC)c3)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OC 10.1016/0960-894X(96)00232-6
CHEMBL287169 100118 None 0 Human Functional pKd = 5.5 5.5 -134 2
Inhibition of sarafotoxin-6c stimulated vasoconstriction in rabbit pulmonary artery.Inhibition of sarafotoxin-6c stimulated vasoconstriction in rabbit pulmonary artery.
ChEMBL 553 10 1 10 5.3 COc1cc2c(Sc3cc(OC)c(OC)c(OC)c3)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OC 10.1016/0960-894X(96)00232-6
9810571 61406 None 0 Rat Functional pKd = 7.5 7.5 - 2
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)
ChEMBL 731 18 2 13 5.0 CCCS(=O)(=O)NCCOc1nc(-c2cc(OC)c(OC)c(OC)c2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
CHEMBL176997 61406 None 0 Rat Functional pKd = 7.5 7.5 - 2
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)
ChEMBL 731 18 2 13 5.0 CCCS(=O)(=O)NCCOc1nc(-c2cc(OC)c(OC)c(OC)c2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
9897092 59956 None 0 Rat Functional pKd = 7.5 7.5 - 2
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)
ChEMBL 779 17 2 13 6.0 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2cc(OC)c(OC)c(OC)c2)nc1OCCNS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(02)01083-1
CHEMBL173201 59956 None 0 Rat Functional pKd = 7.5 7.5 - 2
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)
ChEMBL 779 17 2 13 6.0 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2cc(OC)c(OC)c(OC)c2)nc1OCCNS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(02)01083-1
18184229 59627 None 0 Rat Functional pKd = 6.4 6.4 - 2
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)
ChEMBL 605 15 2 10 4.2 CCCS(=O)(=O)NCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
CHEMBL171950 59627 None 0 Rat Functional pKd = 6.4 6.4 - 2
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)
ChEMBL 605 15 2 10 4.2 CCCS(=O)(=O)NCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
9853680 98701 None 0 Rat Functional pKd = 7.4 7.4 - 2
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)
ChEMBL 771 17 2 14 5.7 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2cc(OC)c(OC)c(OC)c2)nc1OCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
CHEMBL277275 98701 None 0 Rat Functional pKd = 7.4 7.4 - 2
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)
ChEMBL 771 17 2 14 5.7 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2cc(OC)c(OC)c(OC)c2)nc1OCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
9830773 130294 None 0 Rat Functional pKd = 6.4 6.4 - 2
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)
ChEMBL 636 14 2 12 2.8 CCS(=O)(=O)NCCOc1nc(N2CCOCC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
CHEMBL367958 130294 None 0 Rat Functional pKd = 6.4 6.4 - 2
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)
ChEMBL 636 14 2 12 2.8 CCS(=O)(=O)NCCOc1nc(N2CCOCC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
9874557 129806 None 0 Rat Functional pKd = 7.3 7.3 - 2
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)
ChEMBL 667 15 2 10 5.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(C2CC2)nc1OCCCNS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(02)01083-1
CHEMBL367443 129806 None 0 Rat Functional pKd = 7.3 7.3 - 2
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)
ChEMBL 667 15 2 10 5.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(C2CC2)nc1OCCCNS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(02)01083-1
9831527 129550 None 0 Rat Functional pKd = 7.3 7.3 - 2
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)
ChEMBL 698 14 2 12 4.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCNS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(02)01083-1
CHEMBL367274 129550 None 0 Rat Functional pKd = 7.3 7.3 - 2
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)
ChEMBL 698 14 2 12 4.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCNS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(02)01083-1
9957883 98710 None 0 Human Functional pKd = 6.2 6.2 -25 2
Inhibition of sarafotoxin-6c stimulated vasoconstriction in rabbit pulmonary artery.Inhibition of sarafotoxin-6c stimulated vasoconstriction in rabbit pulmonary artery.
ChEMBL 507 7 1 9 5.0 COc1cc2c(Sc3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OC 10.1016/0960-894X(96)00232-6
CHEMBL27732 98710 None 0 Human Functional pKd = 6.2 6.2 -25 2
Inhibition of sarafotoxin-6c stimulated vasoconstriction in rabbit pulmonary artery.Inhibition of sarafotoxin-6c stimulated vasoconstriction in rabbit pulmonary artery.
ChEMBL 507 7 1 9 5.0 COc1cc2c(Sc3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OC 10.1016/0960-894X(96)00232-6
18995992 99892 None 0 Human Functional pKd = 6.2 6.2 -3 2
Inhibition of sarafotoxin-6c stimulated vasoconstriction in rabbit pulmonary artery.Inhibition of sarafotoxin-6c stimulated vasoconstriction in rabbit pulmonary artery.
ChEMBL 507 7 1 9 5.0 COc1ccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc4c(cc23)OCO4)cc1OC 10.1016/0960-894X(96)00232-6
CHEMBL28563 99892 None 0 Human Functional pKd = 6.2 6.2 -3 2
Inhibition of sarafotoxin-6c stimulated vasoconstriction in rabbit pulmonary artery.Inhibition of sarafotoxin-6c stimulated vasoconstriction in rabbit pulmonary artery.
ChEMBL 507 7 1 9 5.0 COc1ccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc4c(cc23)OCO4)cc1OC 10.1016/0960-894X(96)00232-6
9917072 62123 None 0 Rat Functional pKd = 7.2 7.2 - 2
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)
ChEMBL 619 16 2 10 4.6 CCCS(=O)(=O)NCCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
CHEMBL177538 62123 None 0 Rat Functional pKd = 7.2 7.2 - 2
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)
ChEMBL 619 16 2 10 4.6 CCCS(=O)(=O)NCCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
9853077 59646 None 0 Rat Functional pKd = 7.2 7.2 - 2
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)
ChEMBL 696 13 2 12 5.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
CHEMBL172030 59646 None 0 Rat Functional pKd = 7.2 7.2 - 2
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)
ChEMBL 696 13 2 12 5.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
9917706 129807 None 0 Rat Functional pKd = 8.0 8.0 - 2
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)
ChEMBL 659 15 2 11 5.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(C2CC2)nc1OCCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
CHEMBL367444 129807 None 0 Rat Functional pKd = 8.0 8.0 - 2
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)
ChEMBL 659 15 2 11 5.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(C2CC2)nc1OCCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
13016 670 None 14 Human Functional pKi = 4.7 4.7 - 0
Inhibitory concentration against endotheline ETB receptorInhibitory concentration against endotheline ETB receptor
ChEMBL 395 5 1 6 4.4 CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4 10.1021/jm030480f
9843631 670 None 14 Human Functional pKi = 4.7 4.7 - 0
Inhibitory concentration against endotheline ETB receptorInhibitory concentration against endotheline ETB receptor
ChEMBL 395 5 1 6 4.4 CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4 10.1021/jm030480f
CHEMBL24461 670 None 14 Human Functional pKi = 4.7 4.7 - 0
Inhibitory concentration against endotheline ETB receptorInhibitory concentration against endotheline ETB receptor
ChEMBL 395 5 1 6 4.4 CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4 10.1021/jm030480f
10096179 177125 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity against human Endothelin B receptor expressed in CHO cellsAntagonist activity against human Endothelin B receptor expressed in CHO cells
ChEMBL 468 9 1 5 5.7 CCOc1ccc(-c2cc(C)nc(OC(C(=O)O)C(C)(c3ccccc3)c3ccccc3)n2)cc1 10.1016/s0960-894x(03)00236-1
CHEMBL46311 177125 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity against human Endothelin B receptor expressed in CHO cellsAntagonist activity against human Endothelin B receptor expressed in CHO cells
ChEMBL 468 9 1 5 5.7 CCOc1ccc(-c2cc(C)nc(OC(C(=O)O)C(C)(c3ccccc3)c3ccccc3)n2)cc1 10.1016/s0960-894x(03)00236-1
10070 449 None 43 Human Functional pA2 = 5.5 5.5 -109 2
UnclassifiedUnclassified
Guide to Pharmacology 544 8 2 8 2.5 Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N 18780830
25099191 449 None 43 Human Functional pA2 = 5.5 5.5 -109 2
UnclassifiedUnclassified
Guide to Pharmacology 544 8 2 8 2.5 Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N 18780830
25099191.0 449 None 43 Human Functional pA2 = 5.5 5.5 -109 2
UnclassifiedUnclassified
Guide to Pharmacology 544 8 2 8 2.5 Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N 18780830
CHEMBL2165326 449 None 43 Human Functional pA2 = 5.5 5.5 -109 2
UnclassifiedUnclassified
Guide to Pharmacology 544 8 2 8 2.5 Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N 18780830
DB15059 449 None 43 Human Functional pA2 = 5.5 5.5 -109 2
UnclassifiedUnclassified
Guide to Pharmacology 544 8 2 8 2.5 Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N 18780830
104865 706 None 60 Rat Functional pA2 = 6 6.0 -11 5
UnclassifiedUnclassified
Guide to Pharmacology 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 8035319
104865.0 706 None 60 Rat Functional pA2 = 6 6.0 -11 5
UnclassifiedUnclassified
Guide to Pharmacology 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 8035319
3494 706 None 60 Rat Functional pA2 = 6 6.0 -11 5
UnclassifiedUnclassified
Guide to Pharmacology 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 8035319
392 706 None 60 Rat Functional pA2 = 6 6.0 -11 5
UnclassifiedUnclassified
Guide to Pharmacology 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 8035319
CHEMBL957 706 None 60 Rat Functional pA2 = 6 6.0 -11 5
UnclassifiedUnclassified
Guide to Pharmacology 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 8035319
DB00559 706 None 60 Rat Functional pA2 = 6 6.0 -11 5
UnclassifiedUnclassified
Guide to Pharmacology 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 8035319
3913 3737 None 0 Rat Functional pA2 = 8.4 8.4 1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7780649
5311469 3737 None 0 Rat Functional pA2 = 8.4 8.4 1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7780649
104865 706 None 60 Rat Functional pIC50 = 8.2 8.2 -11 5
NoneNone
Drug Central 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
104865.0 706 None 60 Rat Functional pIC50 = 8.2 8.2 -11 5
NoneNone
Drug Central 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
3494 706 None 60 Rat Functional pIC50 = 8.2 8.2 -11 5
NoneNone
Drug Central 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
392 706 None 60 Rat Functional pIC50 = 8.2 8.2 -11 5
NoneNone
Drug Central 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
CHEMBL957 706 None 60 Rat Functional pIC50 = 8.2 8.2 -11 5
NoneNone
Drug Central 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
DB00559 706 None 60 Rat Functional pIC50 = 8.2 8.2 -11 5
NoneNone
Drug Central 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
3951 391 None 55 Human Functional pIC50 = 5.9 5.9 -47 2
UnclassifiedUnclassified
Guide to Pharmacology 378 7 1 5 3.5 COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1 15139756
4337 391 None 55 Human Functional pIC50 = 5.9 5.9 -47 2
UnclassifiedUnclassified
Guide to Pharmacology 378 7 1 5 3.5 COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1 15139756
6918493 391 None 55 Human Functional pIC50 = 5.9 5.9 -47 2
UnclassifiedUnclassified
Guide to Pharmacology 378 7 1 5 3.5 COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1 15139756
6918493.0 391 None 55 Human Functional pIC50 = 5.9 5.9 -47 2
UnclassifiedUnclassified
Guide to Pharmacology 378 7 1 5 3.5 COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1 15139756
CHEMBL1111 391 None 55 Human Functional pIC50 = 5.9 5.9 -47 2
UnclassifiedUnclassified
Guide to Pharmacology 378 7 1 5 3.5 COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1 15139756
DB06403 391 None 55 Human Functional pIC50 = 5.9 5.9 -47 2
UnclassifiedUnclassified
Guide to Pharmacology 378 7 1 5 3.5 COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1 15139756
10070 449 None 43 Human Functional pIC50 = 6.0 6.0 -109 2
UnclassifiedUnclassified
Guide to Pharmacology 544 8 2 8 2.5 Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N 18780830
25099191 449 None 43 Human Functional pIC50 = 6.0 6.0 -109 2
UnclassifiedUnclassified
Guide to Pharmacology 544 8 2 8 2.5 Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N 18780830
25099191.0 449 None 43 Human Functional pIC50 = 6.0 6.0 -109 2
UnclassifiedUnclassified
Guide to Pharmacology 544 8 2 8 2.5 Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N 18780830
CHEMBL2165326 449 None 43 Human Functional pIC50 = 6.0 6.0 -109 2
UnclassifiedUnclassified
Guide to Pharmacology 544 8 2 8 2.5 Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N 18780830
DB15059 449 None 43 Human Functional pIC50 = 6.0 6.0 -109 2
UnclassifiedUnclassified
Guide to Pharmacology 544 8 2 8 2.5 Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N 18780830
16004692 2454 None 59 Human Functional pIC50 = 6.4 6.4 -107 2
UnclassifiedUnclassified
Guide to Pharmacology 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 22862294
16004692.0 2454 None 59 Human Functional pIC50 = 6.4 6.4 -107 2
UnclassifiedUnclassified
Guide to Pharmacology 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 22862294
4809 2454 None 59 Human Functional pIC50 = 6.4 6.4 -107 2
UnclassifiedUnclassified
Guide to Pharmacology 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 22862294
7352 2454 None 59 Human Functional pIC50 = 6.4 6.4 -107 2
UnclassifiedUnclassified
Guide to Pharmacology 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 22862294
CHEMBL2103873 2454 None 59 Human Functional pIC50 = 6.4 6.4 -107 2
UnclassifiedUnclassified
Guide to Pharmacology 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 22862294
DB08932 2454 None 59 Human Functional pIC50 = 6.4 6.4 -107 2
UnclassifiedUnclassified
Guide to Pharmacology 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 22862294
1011 3352 None 26 Human Functional pIC50 = 7.2 7.2 102 2
UnclassifiedUnclassified
Guide to Pharmacology 609 12 3 10 4.8 OC[C@H](COc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ccc(cc1)OC)O 8612786
5312146 3352 None 26 Human Functional pIC50 = 7.2 7.2 102 2
UnclassifiedUnclassified
Guide to Pharmacology 609 12 3 10 4.8 OC[C@H](COc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ccc(cc1)OC)O 8612786
CHEMBL1628620 3352 None 26 Human Functional pIC50 = 7.2 7.2 102 2
UnclassifiedUnclassified
Guide to Pharmacology 609 12 3 10 4.8 OC[C@H](COc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ccc(cc1)OC)O 8612786
3911 3317 None 0 Human Functional pIC50 = 8 8.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8183252
CHEMBL429908 3317 None 0 Human Functional pIC50 = 8 8.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8183252
9651 2174 None 0 Human Functional pIC50 = 8.2 8.2 - 1
UnclassifiedUnclassified
Guide to Pharmacology 682 12 2 10 6.9 COc1ccccc1Oc1c(OCCC(=O)Nc2c(C)cccc2C)nc(nc1NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 28805809
9810112 2174 None 0 Human Functional pIC50 = 8.2 8.2 - 1
UnclassifiedUnclassified
Guide to Pharmacology 682 12 2 10 6.9 COc1ccccc1Oc1c(OCCC(=O)Nc2c(C)cccc2C)nc(nc1NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 28805809
108002 3494 None 22 Rat Functional pKB = 9.4 9.4 1 2
UnclassifiedUnclassified
Guide to Pharmacology 520 10 2 7 4.7 CCCOc1ccc2c(c1)[C@H]([C@@H]([C@H]2c1ccc2c(c1)OCO2)C(=O)O)c1ccc(cc1OCC(=O)O)OC 8201588
3528 3494 None 22 Rat Functional pKB = 9.4 9.4 1 2
UnclassifiedUnclassified
Guide to Pharmacology 520 10 2 7 4.7 CCCOc1ccc2c(c1)[C@H]([C@@H]([C@H]2c1ccc2c(c1)OCO2)C(=O)O)c1ccc(cc1OCC(=O)O)OC 8201588
CHEMBL8823 3494 None 22 Rat Functional pKB = 9.4 9.4 1 2
UnclassifiedUnclassified
Guide to Pharmacology 520 10 2 7 4.7 CCCOc1ccc2c(c1)[C@H]([C@@H]([C@H]2c1ccc2c(c1)OCO2)C(=O)O)c1ccc(cc1OCC(=O)O)OC 8201588




Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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DOI

4236 28104 None 33 Human Binding pAC50 = 4.6 4.6 - 1
Binding affinity towards human EDNRB in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human EDNRB in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 273 5 1 2 2.0 NC(=O)C[S+]([O-])C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1373 28104 None 33 Human Binding pAC50 = 4.6 4.6 - 1
Binding affinity towards human EDNRB in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human EDNRB in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 273 5 1 2 2.0 NC(=O)C[S+]([O-])C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
104865 706 None 60 Human Binding pAC50 = 6.6 6.6 -6 4
Binding affinity towards human EDNRB in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human EDNRB in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1038/s41467-023-40064-9
104865.0 706 None 60 Human Binding pAC50 = 6.6 6.6 -6 4
Binding affinity towards human EDNRB in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human EDNRB in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1038/s41467-023-40064-9
3494 706 None 60 Human Binding pAC50 = 6.6 6.6 -6 4
Binding affinity towards human EDNRB in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human EDNRB in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1038/s41467-023-40064-9
392 706 None 60 Human Binding pAC50 = 6.6 6.6 -6 4
Binding affinity towards human EDNRB in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human EDNRB in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1038/s41467-023-40064-9
CHEMBL957 706 None 60 Human Binding pAC50 = 6.6 6.6 -6 4
Binding affinity towards human EDNRB in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human EDNRB in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1038/s41467-023-40064-9
DB00559 706 None 60 Human Binding pAC50 = 6.6 6.6 -6 4
Binding affinity towards human EDNRB in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human EDNRB in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1038/s41467-023-40064-9
4020 207608 None 20 Human Binding pAC50 = 4.5 4.5 - 1
Binding affinity towards human EDNRB in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human EDNRB in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 1 1 3 2.6 OC1(c2ccc(Cl)cc2)c2ccccc2C2=NCCN21 10.1038/s41467-023-40064-9
CHEMBL781 207608 None 20 Human Binding pAC50 = 4.5 4.5 - 1
Binding affinity towards human EDNRB in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human EDNRB in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 1 1 3 2.6 OC1(c2ccc(Cl)cc2)c2ccccc2C2=NCCN21 10.1038/s41467-023-40064-9
CHEMBL2370066 212236 None 0 Rat Binding pEC50 = 6.8 6.8 - 0
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCN)NC(=O)[C@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00070a001
CHEMBL2370067 212237 None 0 Rat Binding pEC50 = 5.7 5.7 - 0
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](N)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@H](C=O)Cc1c[nH]c2ccccc12)[C@@H](C)CC 10.1021/jm00070a001
CHEMBL315841 213652 None 0 Rat Binding pEC50 = 7.3 7.3 - 0
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00070a001
CHEMBL407269 215111 None 0 Rat Binding pEC50 = 7.3 7.3 - 0
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00070a001
CHEMBL387200 214868 None 0 Rat Binding pEC50 = 7.2 7.2 - 0
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00070a001
CHEMBL86703 218379 None 0 Rat Binding pEC50 = 5.2 5.2 - 0
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)C(C)C 10.1021/jm00070a001
CHEMBL313344 213571 None 0 Rat Binding pEC50 = 5.2 5.2 - 0
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)CC 10.1021/jm00070a001
CHEMBL1790180 211342 None 0 Human Binding pIC50 = 10.5 10.5 -1 3
Binding affinity to human ETB receptor by radioligand displacement assayBinding affinity to human ETB receptor by radioligand displacement assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CCc3ccc(O)cc3)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H](Cc3ccccc3)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/j.ejmech.2013.01.044
CHEMBL1790180 211342 None 0 Human Binding pIC50 = 10.4 10.4 -1 3
Binding affinity to human ETB receptor by radioligand displacement assayBinding affinity to human ETB receptor by radioligand displacement assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CCc3ccc(O)cc3)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H](Cc3ccccc3)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/j.bmc.2013.03.016
CHEMBL1790180 211342 None 0 Human Binding pIC50 = 10.0 10.0 -1 3
Displacement of radiolabeled endothelin-3 from human endothelin ETB receptorDisplacement of radiolabeled endothelin-3 from human endothelin ETB receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CCc3ccc(O)cc3)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H](Cc3ccccc3)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm8007618
44284481 216186 None 0 Human Binding pIC50 = 9.9 9.9 -4 5
Displacement of [125I]Endothelin-1 from human recombinant ETB receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Endothelin-1 from human recombinant ETB receptor expressed in CHOK1 cells after 2 hrs
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/j.bmcl.2013.01.025
CHEMBL437472 216186 None 0 Human Binding pIC50 = 9.9 9.9 -4 5
Displacement of [125I]Endothelin-1 from human recombinant ETB receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Endothelin-1 from human recombinant ETB receptor expressed in CHOK1 cells after 2 hrs
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/j.bmcl.2013.01.025
10603409 110667 None 0 Human Binding pIC50 = 9.9 9.9 - 0
Binding assay performed using human Endothelin B receptor (hETB) expressed in chinese hamster ovary cells(CHO)Binding assay performed using human Endothelin B receptor (hETB) expressed in chinese hamster ovary cells(CHO)
ChEMBL 584 13 1 7 4.1 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCCl 10.1021/jm970101g
CHEMBL325581 110667 None 0 Human Binding pIC50 = 9.9 9.9 - 0
Binding assay performed using human Endothelin B receptor (hETB) expressed in chinese hamster ovary cells(CHO)Binding assay performed using human Endothelin B receptor (hETB) expressed in chinese hamster ovary cells(CHO)
ChEMBL 584 13 1 7 4.1 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCCl 10.1021/jm970101g
10603409 110667 None 0 Pig Binding pIC50 = 9.7 9.7 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 584 13 1 7 4.1 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCCl 10.1021/jm970101g
CHEMBL325581 110667 None 0 Pig Binding pIC50 = 9.7 9.7 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 584 13 1 7 4.1 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCCl 10.1021/jm970101g
10651488 163474 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Binding assay performed using human Endothelin B receptor (hETB) expressed in chinese hamster ovary cells(CHO)Binding assay performed using human Endothelin B receptor (hETB) expressed in chinese hamster ovary cells(CHO)
ChEMBL 618 13 1 7 4.8 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCC(F)(F)F 10.1021/jm970101g
CHEMBL419367 163474 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Binding assay performed using human Endothelin B receptor (hETB) expressed in chinese hamster ovary cells(CHO)Binding assay performed using human Endothelin B receptor (hETB) expressed in chinese hamster ovary cells(CHO)
ChEMBL 618 13 1 7 4.8 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCC(F)(F)F 10.1021/jm970101g
44284481 216186 None 0 Human Binding pIC50 = 9.7 9.7 -4 5
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(97)00400-9
CHEMBL437472 216186 None 0 Human Binding pIC50 = 9.7 9.7 -4 5
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(97)00400-9
CHEMBL2165327 211791 None 5 Human Binding pIC50 = 9.7 9.7 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC2=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm3009103
10839947 117366 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 530 9 2 6 5.0 CCc1cccc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm990170q
CHEMBL339657 117366 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 530 9 2 6 5.0 CCc1cccc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm990170q
9916235 9355 None 1 Human Binding pIC50 = 9.6 9.6 - 0
Binding assay performed using human Endothelin B receptor (hETB) expressed in chinese hamster ovary cells(CHO)Binding assay performed using human Endothelin B receptor (hETB) expressed in chinese hamster ovary cells(CHO)
ChEMBL 578 14 1 7 4.6 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm970101g
CHEMBL111277 9355 None 1 Human Binding pIC50 = 9.6 9.6 - 0
Binding assay performed using human Endothelin B receptor (hETB) expressed in chinese hamster ovary cells(CHO)Binding assay performed using human Endothelin B receptor (hETB) expressed in chinese hamster ovary cells(CHO)
ChEMBL 578 14 1 7 4.6 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm970101g
9916235 9355 None 1 Pig Binding pIC50 = 9.5 9.5 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 578 14 1 7 4.6 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm970101g
CHEMBL111277 9355 None 1 Pig Binding pIC50 = 9.5 9.5 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 578 14 1 7 4.6 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm970101g
10187997 110028 None 0 Pig Binding pIC50 = 9.5 9.5 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 564 13 1 7 4.2 CCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm970101g
CHEMBL323464 110028 None 0 Pig Binding pIC50 = 9.5 9.5 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 564 13 1 7 4.2 CCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm970101g
10651488 163474 None 0 Pig Binding pIC50 = 9.5 9.5 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 618 13 1 7 4.8 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCC(F)(F)F 10.1021/jm970101g
CHEMBL419367 163474 None 0 Pig Binding pIC50 = 9.5 9.5 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 618 13 1 7 4.8 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCC(F)(F)F 10.1021/jm970101g
10210629 8766 None 0 Pig Binding pIC50 = 9.5 9.5 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 592 15 1 7 5.0 CCCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm970101g
CHEMBL109644 8766 None 0 Pig Binding pIC50 = 9.5 9.5 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 592 15 1 7 5.0 CCCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm970101g
10187997 110028 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Binding assay performed using human Endothelin B receptor (hETB) expressed in chinese hamster ovary cells(CHO)Binding assay performed using human Endothelin B receptor (hETB) expressed in chinese hamster ovary cells(CHO)
ChEMBL 564 13 1 7 4.2 CCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm970101g
CHEMBL323464 110028 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Binding assay performed using human Endothelin B receptor (hETB) expressed in chinese hamster ovary cells(CHO)Binding assay performed using human Endothelin B receptor (hETB) expressed in chinese hamster ovary cells(CHO)
ChEMBL 564 13 1 7 4.2 CCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm970101g
10210629 8766 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Binding assay performed using human Endothelin B receptor (hETB) expressed in chinese hamster ovary cells(CHO)Binding assay performed using human Endothelin B receptor (hETB) expressed in chinese hamster ovary cells(CHO)
ChEMBL 592 15 1 7 5.0 CCCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm970101g
CHEMBL109644 8766 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Binding assay performed using human Endothelin B receptor (hETB) expressed in chinese hamster ovary cells(CHO)Binding assay performed using human Endothelin B receptor (hETB) expressed in chinese hamster ovary cells(CHO)
ChEMBL 592 15 1 7 5.0 CCCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm970101g
10555806 12126 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 616 12 2 7 6.0 CC(C)OCCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)(C)C)cc1 10.1021/jm990171i
CHEMBL1184095 12126 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 616 12 2 7 6.0 CC(C)OCCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)(C)C)cc1 10.1021/jm990171i
CHEMBL332289 12126 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 616 12 2 7 6.0 CC(C)OCCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)(C)C)cc1 10.1021/jm990171i
1009 194 None 25 Human Binding pIC50 = 9.1 9.1 676 2
Affinity On-target Cellular interaction (EDNRB-dependent phosphatidylinositol hydrolysis assay (CHO cells transfected with human EDNRBA)) EUB0000350a EDNRBAffinity On-target Cellular interaction (EDNRB-dependent phosphatidylinositol hydrolysis assay (CHO cells transfected with human EDNRBA)) EUB0000350a EDNRB
ChEMBL 558 11 2 6 5.8 CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2 10.6019/CHEMBL5210121
5310991 194 None 25 Human Binding pIC50 = 9.1 9.1 676 2
Affinity On-target Cellular interaction (EDNRB-dependent phosphatidylinositol hydrolysis assay (CHO cells transfected with human EDNRBA)) EUB0000350a EDNRBAffinity On-target Cellular interaction (EDNRB-dependent phosphatidylinositol hydrolysis assay (CHO cells transfected with human EDNRBA)) EUB0000350a EDNRB
ChEMBL 558 11 2 6 5.8 CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2 10.6019/CHEMBL5210121
CHEMBL332794 194 None 25 Human Binding pIC50 = 9.1 9.1 676 2
Affinity On-target Cellular interaction (EDNRB-dependent phosphatidylinositol hydrolysis assay (CHO cells transfected with human EDNRBA)) EUB0000350a EDNRBAffinity On-target Cellular interaction (EDNRB-dependent phosphatidylinositol hydrolysis assay (CHO cells transfected with human EDNRBA)) EUB0000350a EDNRB
ChEMBL 558 11 2 6 5.8 CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2 10.6019/CHEMBL5210121
10792711 114855 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 548 9 2 6 5.2 CCc1cc(F)cc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm990170q
CHEMBL333972 114855 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 548 9 2 6 5.2 CCc1cc(F)cc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm990170q
44314619 207144 None 0 Pig Binding pIC50 = 9.1 9.1 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 631 12 5 4 4.5 CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)O 10.1021/jm9600914
CHEMBL73925 207144 None 0 Pig Binding pIC50 = 9.1 9.1 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 631 12 5 4 4.5 CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)O 10.1021/jm9600914
CHEMBL284250 213319 None 0 Pig Binding pIC50 = 9.1 9.1 - 0
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranesInhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranes
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)[C@@H](NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)O 10.1016/0960-894X(95)00237-N
9916235 9355 None 1 Pig Binding pIC50 = 9.1 9.1 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 578 14 1 7 4.6 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm970101g
CHEMBL111277 9355 None 1 Pig Binding pIC50 = 9.1 9.1 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 578 14 1 7 4.6 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm970101g
10816963 113392 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 574 12 2 7 5.0 CCc1cccc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCOC)cc1 10.1021/jm990170q
CHEMBL331625 113392 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 574 12 2 7 5.0 CCc1cccc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCOC)cc1 10.1021/jm990170q
9896468 170772 None 0 Pig Binding pIC50 = 9.1 9.1 - 0
Displacement of 125I-ET1 from pig ETB receptor transfected in grivet COS7 cellsDisplacement of 125I-ET1 from pig ETB receptor transfected in grivet COS7 cells
ChEMBL 703 13 2 10 6.7 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(N2CCOCC2)nc1OCCC(=O)Nc1ccccc1C(C)C 10.1016/j.bmcl.2016.06.014
CHEMBL4451582 170772 None 0 Pig Binding pIC50 = 9.1 9.1 - 0
Displacement of 125I-ET1 from pig ETB receptor transfected in grivet COS7 cellsDisplacement of 125I-ET1 from pig ETB receptor transfected in grivet COS7 cells
ChEMBL 703 13 2 10 6.7 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(N2CCOCC2)nc1OCCC(=O)Nc1ccccc1C(C)C 10.1016/j.bmcl.2016.06.014
10626362 11455 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 544 8 2 6 5.2 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)(C)C)cc1 10.1021/jm990171i
CHEMBL1180351 11455 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 544 8 2 6 5.2 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)(C)C)cc1 10.1021/jm990171i
CHEMBL123316 11455 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 544 8 2 6 5.2 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)(C)C)cc1 10.1021/jm990171i
10651488 163474 None 0 Pig Binding pIC50 = 9.0 9.0 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 618 13 1 7 4.8 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCC(F)(F)F 10.1021/jm970101g
CHEMBL419367 163474 None 0 Pig Binding pIC50 = 9.0 9.0 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 618 13 1 7 4.8 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCC(F)(F)F 10.1021/jm970101g
10187997 110028 None 0 Pig Binding pIC50 = 9 9.0 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 564 13 1 7 4.2 CCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm970101g
CHEMBL323464 110028 None 0 Pig Binding pIC50 = 9 9.0 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 564 13 1 7 4.2 CCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm970101g
10603409 110667 None 0 Pig Binding pIC50 = 9 9.0 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 584 13 1 7 4.1 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCCl 10.1021/jm970101g
CHEMBL325581 110667 None 0 Pig Binding pIC50 = 9 9.0 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 584 13 1 7 4.1 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCCl 10.1021/jm970101g
10698065 12117 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 558 11 2 6 5.6 CCC(CC)C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1 10.1021/jm990171i
CHEMBL1184065 12117 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 558 11 2 6 5.6 CCC(CC)C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1 10.1021/jm990171i
CHEMBL330895 12117 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 558 11 2 6 5.6 CCC(CC)C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1 10.1021/jm990171i
10841170 12123 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 592 9 2 6 5.8 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2C)c2ccccc2C)cc1 10.1021/jm990171i
CHEMBL1184090 12123 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 592 9 2 6 5.8 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2C)c2ccccc2C)cc1 10.1021/jm990171i
CHEMBL332109 12123 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 592 9 2 6 5.8 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2C)c2ccccc2C)cc1 10.1021/jm990171i
44314619 207144 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Binding affinity towards Endothelin B receptor in human girardi heart cell membranesBinding affinity towards Endothelin B receptor in human girardi heart cell membranes
ChEMBL 631 12 5 4 4.5 CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)O 10.1021/jm9600914
CHEMBL73925 207144 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Binding affinity towards Endothelin B receptor in human girardi heart cell membranesBinding affinity towards Endothelin B receptor in human girardi heart cell membranes
ChEMBL 631 12 5 4 4.5 CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)O 10.1021/jm9600914
10816963 113392 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 574 12 2 7 5.0 CCc1cccc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCOC)cc1 10.1021/jm990170q
CHEMBL331625 113392 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 574 12 2 7 5.0 CCc1cccc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCOC)cc1 10.1021/jm990170q
10167052 109695 None 0 Pig Binding pIC50 = 8.9 8.9 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 578 13 1 7 4.5 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCC(C)C 10.1021/jm970101g
CHEMBL322297 109695 None 0 Pig Binding pIC50 = 8.9 8.9 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 578 13 1 7 4.5 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCC(C)C 10.1021/jm970101g
137630807 161206 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 641 12 4 7 4.8 CCCC[C@@H](NC(=O)[C@@H](Cc1cc2ccccc2n1C(=O)OC)NC(=O)[C@H](CC(C)(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1016/j.bmcl.2017.04.049
CHEMBL4075238 161206 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 641 12 4 7 4.8 CCCC[C@@H](NC(=O)[C@@H](Cc1cc2ccccc2n1C(=O)OC)NC(=O)[C@H](CC(C)(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1016/j.bmcl.2017.04.049
CHEMBL4117106 161206 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 641 12 4 7 4.8 CCCC[C@@H](NC(=O)[C@@H](Cc1cc2ccccc2n1C(=O)OC)NC(=O)[C@H](CC(C)(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1016/j.bmcl.2017.04.049
10792636 168618 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 544 10 2 6 5.4 CCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(CC)cccc2CC)cc1 10.1021/jm990170q
CHEMBL435385 168618 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 544 10 2 6 5.4 CCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(CC)cccc2CC)cc1 10.1021/jm990170q
CHEMBL2370534 212328 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]1CCCCNC(=O)CC[C@@H](NC(=O)[C@H](CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](N)Cc2ccccc2)C(C)C)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](C)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@H](C(N)=O)[C@@H](C)CC)[C@@H](C)CC 10.1021/jm990170q
155560344 176608 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]ET-1 from ET-B receptor in human Girardi heart cells incubated for 4 hrs by gamma counting methodDisplacement of [125I]ET-1 from ET-B receptor in human Girardi heart cells incubated for 4 hrs by gamma counting method
ChEMBL 641 12 4 7 4.8 CCCC[C@H](NC(=O)[C@@H](Cc1cn(C(=O)OC)c2ccccc12)NC(=O)[C@@H](CC(C)(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/acs.jmedchem.5b01781
CHEMBL4568795 176608 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]ET-1 from ET-B receptor in human Girardi heart cells incubated for 4 hrs by gamma counting methodDisplacement of [125I]ET-1 from ET-B receptor in human Girardi heart cells incubated for 4 hrs by gamma counting method
ChEMBL 641 12 4 7 4.8 CCCC[C@H](NC(=O)[C@@H](Cc1cn(C(=O)OC)c2ccccc12)NC(=O)[C@@H](CC(C)(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/acs.jmedchem.5b01781
CHEMBL4596821 176608 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]ET-1 from ET-B receptor in human Girardi heart cells incubated for 4 hrs by gamma counting methodDisplacement of [125I]ET-1 from ET-B receptor in human Girardi heart cells incubated for 4 hrs by gamma counting method
ChEMBL 641 12 4 7 4.8 CCCC[C@H](NC(=O)[C@@H](Cc1cn(C(=O)OC)c2ccccc12)NC(=O)[C@@H](CC(C)(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/acs.jmedchem.5b01781
44283453 138864 None 0 Pig Binding pIC50 = 8.9 8.9 - 0
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranesInhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranes
ChEMBL 641 12 4 7 4.8 CCCC[C@H](NC(=O)[C@@H](Cc1cn(C(=O)OC)c2ccccc12)NC(=O)C(CC(C)(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1016/0960-894X(95)00237-N
CHEMBL37807 138864 None 0 Pig Binding pIC50 = 8.9 8.9 - 0
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranesInhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranes
ChEMBL 641 12 4 7 4.8 CCCC[C@H](NC(=O)[C@@H](Cc1cn(C(=O)OC)c2ccccc12)NC(=O)C(CC(C)(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1016/0960-894X(95)00237-N
44314620 103200 None 0 Pig Binding pIC50 = 8.9 8.9 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 587 12 5 4 4.4 CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)O 10.1021/jm9600914
CHEMBL307903 103200 None 0 Pig Binding pIC50 = 8.9 8.9 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 587 12 5 4 4.4 CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)O 10.1021/jm9600914
3887 2072 None 35 Human Binding pIC50 = 8.9 8.9 -7 4
Displacement of [125I]ET-1 from human ET-B receptor expressed in CHO cell membrane incubated for 2 hrsDisplacement of [125I]ET-1 from human ET-B receptor expressed in CHO cell membrane incubated for 2 hrs
ChEMBL None None None None 10.1021/acs.jmedchem.5b01781
5311192 2072 None 35 Human Binding pIC50 = 8.9 8.9 -7 4
Displacement of [125I]ET-1 from human ET-B receptor expressed in CHO cell membrane incubated for 2 hrsDisplacement of [125I]ET-1 from human ET-B receptor expressed in CHO cell membrane incubated for 2 hrs
ChEMBL None None None None 10.1021/acs.jmedchem.5b01781
CHEMBL72410 2072 None 35 Human Binding pIC50 = 8.9 8.9 -7 4
Displacement of [125I]ET-1 from human ET-B receptor expressed in CHO cell membrane incubated for 2 hrsDisplacement of [125I]ET-1 from human ET-B receptor expressed in CHO cell membrane incubated for 2 hrs
ChEMBL None None None None 10.1021/acs.jmedchem.5b01781
10839947 117366 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 530 9 2 6 5.0 CCc1cccc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm990170q
CHEMBL339657 117366 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 530 9 2 6 5.0 CCc1cccc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm990170q
10210629 8766 None 0 Pig Binding pIC50 = 8.8 8.8 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 592 15 1 7 5.0 CCCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm970101g
CHEMBL109644 8766 None 0 Pig Binding pIC50 = 8.8 8.8 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 592 15 1 7 5.0 CCCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm970101g
10792934 164008 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 558 10 2 6 5.6 CCc1cc(CC)c(NC(=O)CN2C[C@H](c3ccc4c(c3)OCO4)[C@@H](C(=O)O)[C@@H]2c2ccc(OC)cc2)c(CC)c1 10.1021/jm990170q
CHEMBL420729 164008 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 558 10 2 6 5.6 CCc1cc(CC)c(NC(=O)CN2C[C@H](c3ccc4c(c3)OCO4)[C@@H](C(=O)O)[C@@H]2c2ccc(OC)cc2)c(CC)c1 10.1021/jm990170q
10120499 109812 None 0 Pig Binding pIC50 = 8.8 8.8 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 564 12 1 7 4.1 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CC(C)C 10.1021/jm970101g
CHEMBL323055 109812 None 0 Pig Binding pIC50 = 8.8 8.8 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 564 12 1 7 4.1 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CC(C)C 10.1021/jm970101g
44314472 103853 None 0 Pig Binding pIC50 = 8.8 8.8 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 594 13 5 5 4.2 CCCCC(NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
CHEMBL309003 103853 None 0 Pig Binding pIC50 = 8.8 8.8 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 594 13 5 5 4.2 CCCCC(NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
44284481 216186 None 0 Rat Binding pIC50 = 8.8 8.8 3 5
Inhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar membranesInhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar membranes
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00095a029
CHEMBL437472 216186 None 0 Rat Binding pIC50 = 8.8 8.8 3 5
Inhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar membranesInhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar membranes
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00095a029
44283420 161886 None 0 Pig Binding pIC50 = 8.8 8.8 - 0
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranesInhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranes
ChEMBL 594 13 5 5 4.2 CCCC[C@H](NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1016/0960-894X(95)00237-N
CHEMBL414175 161886 None 0 Pig Binding pIC50 = 8.8 8.8 - 0
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranesInhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranes
ChEMBL 594 13 5 5 4.2 CCCC[C@H](NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1016/0960-894X(95)00237-N
10604119 11461 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 636 12 2 7 5.8 COCCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2C)c2ccccc2C)cc1 10.1021/jm990171i
CHEMBL1180361 11461 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 636 12 2 7 5.8 COCCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2C)c2ccccc2C)cc1 10.1021/jm990171i
CHEMBL123654 11461 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 636 12 2 7 5.8 COCCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2C)c2ccccc2C)cc1 10.1021/jm990171i
9846994 106045 None 0 Rat Binding pIC50 = 8.8 8.8 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 458 6 1 6 5.9 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2cccs2)nn1CC1CCCCC1 10.1016/s0960-894x(00)00513-8
CHEMBL313153 106045 None 0 Rat Binding pIC50 = 8.8 8.8 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 458 6 1 6 5.9 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2cccs2)nn1CC1CCCCC1 10.1016/s0960-894x(00)00513-8
44315008 102886 None 0 Pig Binding pIC50 = 8.7 8.7 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 665 13 5 5 4.7 CCSCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
CHEMBL305524 102886 None 0 Pig Binding pIC50 = 8.7 8.7 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 665 13 5 5 4.7 CCSCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
9961347 11966 None 1 Human Binding pIC50 = 8.7 8.7 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 664 13 2 7 6.6 Cc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCOC(C)C)cc1)c1ccccc1C 10.1021/jm990171i
CHEMBL1182945 11966 None 1 Human Binding pIC50 = 8.7 8.7 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 664 13 2 7 6.6 Cc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCOC(C)C)cc1)c1ccccc1C 10.1021/jm990171i
CHEMBL273642 11966 None 1 Human Binding pIC50 = 8.7 8.7 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 664 13 2 7 6.6 Cc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCOC(C)C)cc1)c1ccccc1C 10.1021/jm990171i
44315007 207006 None 0 Pig Binding pIC50 = 8.7 8.7 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 679 14 5 5 5.1 CCCSCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
CHEMBL72891 207006 None 0 Pig Binding pIC50 = 8.7 8.7 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 679 14 5 5 5.1 CCCSCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
CHEMBL405599 215028 None 0 Rat Binding pIC50 = 8 8.0 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL413825 215547 None 0 Human Binding pIC50 = 8 8.0 - 0
Binding affinity in Chinese hamster ovary (CHO) cells stably transfected with human endothelin B (ETB) receptorBinding affinity in Chinese hamster ovary (CHO) cells stably transfected with human endothelin B (ETB) receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(N)=O)NC(=O)CNC(=O)[C@H](CC(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H]2CCCN2C1=O 10.1016/0960-894X(95)00084-7
10627805 16586 None 0 Human Binding pIC50 = 8 8.0 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 630 7 2 6 5.4 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(Br)cccc2Br)cc1 10.1021/jm990170q
CHEMBL123926 16586 None 0 Human Binding pIC50 = 8 8.0 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 630 7 2 6 5.4 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(Br)cccc2Br)cc1 10.1021/jm990170q
22004774 100863 None 0 Pig Binding pIC50 = 7 7.0 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 442 8 1 6 5.7 CCCCSC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL293192 100863 None 0 Pig Binding pIC50 = 7 7.0 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 442 8 1 6 5.7 CCCCSC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
10146305 174375 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 656 14 2 13 4.2 COc1ccccc1Oc1c(NS(=O)(=O)CCc2cccs2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1 10.1016/j.bmcl.2016.06.014
CHEMBL4549357 174375 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 656 14 2 13 4.2 COc1ccccc1Oc1c(NS(=O)(=O)CCc2cccs2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1 10.1016/j.bmcl.2016.06.014
44385008 131429 None 0 Human Binding pIC50 = 7 7.0 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 574 10 2 9 4.9 C#CCOc1nc(-c2ccnc(CO)c2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL368829 131429 None 0 Human Binding pIC50 = 7 7.0 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 574 10 2 9 4.9 C#CCOc1nc(-c2ccnc(CO)c2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
44333867 4644 None 0 Human Binding pIC50 = 7 7.0 - 0
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B receptor
ChEMBL 403 4 1 5 4.1 COc1ccc([C@@H]2c3nc(C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1016/s0960-894x(02)00663-7
CHEMBL103001 4644 None 0 Human Binding pIC50 = 7 7.0 - 0
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B receptor
ChEMBL 403 4 1 5 4.1 COc1ccc([C@@H]2c3nc(C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1016/s0960-894x(02)00663-7
44284196 100577 None 0 Human Binding pIC50 = 7 7.0 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 504 9 2 7 5.4 CCCOc1cc(OC)ccc1[C@@H]1c2nc(NC(C)C)ccc2[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O 10.1016/j.bmcl.2004.01.008
CHEMBL291247 100577 None 0 Human Binding pIC50 = 7 7.0 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 504 9 2 7 5.4 CCCOc1cc(OC)ccc1[C@@H]1c2nc(NC(C)C)ccc2[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O 10.1016/j.bmcl.2004.01.008
9853025 59837 None 0 Human Binding pIC50 = 7 7.0 - 0
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 690 14 2 13 3.9 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
CHEMBL172759 59837 None 0 Human Binding pIC50 = 7 7.0 - 0
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 690 14 2 13 3.9 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
104865 706 None 60 Human Binding pIC50 = 6 6.0 -6 4
Antagonist activity at ETB receptor (unknown origin) assessed as effect on G protein-mediated smooth muscle contractionAntagonist activity at ETB receptor (unknown origin) assessed as effect on G protein-mediated smooth muscle contraction
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/acs.jmedchem.8b00435
104865.0 706 None 60 Human Binding pIC50 = 6 6.0 -6 4
Antagonist activity at ETB receptor (unknown origin) assessed as effect on G protein-mediated smooth muscle contractionAntagonist activity at ETB receptor (unknown origin) assessed as effect on G protein-mediated smooth muscle contraction
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/acs.jmedchem.8b00435
3494 706 None 60 Human Binding pIC50 = 6 6.0 -6 4
Antagonist activity at ETB receptor (unknown origin) assessed as effect on G protein-mediated smooth muscle contractionAntagonist activity at ETB receptor (unknown origin) assessed as effect on G protein-mediated smooth muscle contraction
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/acs.jmedchem.8b00435
392 706 None 60 Human Binding pIC50 = 6 6.0 -6 4
Antagonist activity at ETB receptor (unknown origin) assessed as effect on G protein-mediated smooth muscle contractionAntagonist activity at ETB receptor (unknown origin) assessed as effect on G protein-mediated smooth muscle contraction
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/acs.jmedchem.8b00435
CHEMBL957 706 None 60 Human Binding pIC50 = 6 6.0 -6 4
Antagonist activity at ETB receptor (unknown origin) assessed as effect on G protein-mediated smooth muscle contractionAntagonist activity at ETB receptor (unknown origin) assessed as effect on G protein-mediated smooth muscle contraction
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/acs.jmedchem.8b00435
DB00559 706 None 60 Human Binding pIC50 = 6 6.0 -6 4
Antagonist activity at ETB receptor (unknown origin) assessed as effect on G protein-mediated smooth muscle contractionAntagonist activity at ETB receptor (unknown origin) assessed as effect on G protein-mediated smooth muscle contraction
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/acs.jmedchem.8b00435
10814440 98200 None 0 Human Binding pIC50 = 6 6.0 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 476 7 1 8 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)ccc2OC)cc1 10.1021/jm9606507
CHEMBL273723 98200 None 0 Human Binding pIC50 = 6 6.0 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 476 7 1 8 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)ccc2OC)cc1 10.1021/jm9606507
44279383 100048 None 0 Human Binding pIC50 = 6 6.0 - 0
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB receptor
ChEMBL 398 3 2 3 4.2 O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(-c3ccccc3)cc21 10.1016/0960-894X(95)00230-Q
CHEMBL286687 100048 None 0 Human Binding pIC50 = 6 6.0 - 0
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB receptor
ChEMBL 398 3 2 3 4.2 O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(-c3ccccc3)cc21 10.1016/0960-894X(95)00230-Q
122044 10175 None 42 Rat Binding pIC50 = 6 6.0 - 0
Displacement of 125I-ET1 from rat aortic ring ETB receptorDisplacement of 125I-ET1 from rat aortic ring ETB receptor
ChEMBL 473 9 2 8 3.7 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCO)c1 10.1016/j.bmcl.2016.06.014
CHEMBL115951 10175 None 42 Rat Binding pIC50 = 6 6.0 - 0
Displacement of 125I-ET1 from rat aortic ring ETB receptorDisplacement of 125I-ET1 from rat aortic ring ETB receptor
ChEMBL 473 9 2 8 3.7 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCO)c1 10.1016/j.bmcl.2016.06.014
17869373 14640 None 0 Pig Binding pIC50 = 6 6.0 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 460 8 1 7 4.7 COc1ccc(C(=O)/C(Cc2cccc(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL1205094 14640 None 0 Pig Binding pIC50 = 6 6.0 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 460 8 1 7 4.7 COc1ccc(C(=O)/C(Cc2cccc(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL51890 14640 None 0 Pig Binding pIC50 = 6 6.0 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 460 8 1 7 4.7 COc1ccc(C(=O)/C(Cc2cccc(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
44276969 106895 None 0 Rat Binding pIC50 = 6 6.0 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 506 7 1 5 4.8 COc1cccc(Cn2[nH]c(C(F)(F)C(F)(F)C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2=O)c1 10.1016/s0960-894x(00)00232-8
CHEMBL3144607 106895 None 0 Rat Binding pIC50 = 6 6.0 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 506 7 1 5 4.8 COc1cccc(Cn2[nH]c(C(F)(F)C(F)(F)C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2=O)c1 10.1016/s0960-894x(00)00232-8
44311225 207165 None 0 Human Binding pIC50 = 6 6.0 - 0
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 581 11 1 10 5.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCOC(=O)c1ccoc1 10.1016/S0960-894X(97)00400-9
CHEMBL74118 207165 None 0 Human Binding pIC50 = 6 6.0 - 0
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 581 11 1 10 5.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCOC(=O)c1ccoc1 10.1016/S0960-894X(97)00400-9
CHEMBL269428 213246 None 0 Rat Binding pIC50 = 5 5.0 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)C(c1ccccc1)(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
44267002 98612 None 0 Human Binding pIC50 = 5 5.0 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 546 5 1 7 5.2 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc3c2CCc2ccccc2C3=O)cc1 10.1021/jm9606507
CHEMBL276601 98612 None 0 Human Binding pIC50 = 5 5.0 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 546 5 1 7 5.2 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc3c2CCc2ccccc2C3=O)cc1 10.1021/jm9606507
10552883 110060 None 0 Human Binding pIC50 = 5 5.0 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 484 13 1 5 4.8 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC=C1CC1 10.1021/jm980217s
CHEMBL323485 110060 None 0 Human Binding pIC50 = 5 5.0 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 484 13 1 5 4.8 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC=C1CC1 10.1021/jm980217s
11100307 205659 None 0 Pig Binding pIC50 = 5 5.0 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 354 5 1 5 3.8 CCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccccc21 10.1021/jm010382z
CHEMBL64340 205659 None 0 Pig Binding pIC50 = 5 5.0 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 354 5 1 5 3.8 CCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccccc21 10.1021/jm010382z
CHEMBL289687 213334 None 0 Rat Binding pIC50 = 5 5.0 - 0
Displacement of [125I]ET1 from Endothelin B receptor of rat cerebellumDisplacement of [125I]ET1 from Endothelin B receptor of rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]cn1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)81215-4
10453733 112374 None 0 Rat Binding pIC50 = 5 5.0 - 0
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.
ChEMBL 402 9 1 5 4.8 Cc1ccccc1[C@@H](CCC(=O)O)Oc1cc(OCc2cccnc2)ccc1C#N 10.1021/jm9707131
CHEMBL329181 112374 None 0 Rat Binding pIC50 = 5 5.0 - 0
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.
ChEMBL 402 9 1 5 4.8 Cc1ccccc1[C@@H](CCC(=O)O)Oc1cc(OCc2cccnc2)ccc1C#N 10.1021/jm9707131
11797717 209519 None 0 Rat Binding pIC50 = 5 5.0 - 0
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.
ChEMBL 448 10 2 5 6.0 Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1-c1cc[nH]n1 10.1021/jm9707131
CHEMBL91753 209519 None 0 Rat Binding pIC50 = 5 5.0 - 0
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.
ChEMBL 448 10 2 5 6.0 Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1-c1cc[nH]n1 10.1021/jm9707131
10668808 209619 None 0 Rat Binding pIC50 = 5 5.0 - 0
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.
ChEMBL 402 9 1 5 4.8 Cc1ccccc1[C@@H](CCC(=O)O)Oc1cc(OCc2ccncc2)ccc1C#N 10.1021/jm9707131
CHEMBL92353 209619 None 0 Rat Binding pIC50 = 5 5.0 - 0
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.
ChEMBL 402 9 1 5 4.8 Cc1ccccc1[C@@H](CCC(=O)O)Oc1cc(OCc2ccncc2)ccc1C#N 10.1021/jm9707131
10504148 209717 None 0 Rat Binding pIC50 = 5 5.0 - 0
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.
ChEMBL 459 10 1 5 6.7 Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1-c1ccccn1 10.1021/jm9707131
CHEMBL92965 209717 None 0 Rat Binding pIC50 = 5 5.0 - 0
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.
ChEMBL 459 10 1 5 6.7 Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1-c1ccccn1 10.1021/jm9707131
10599453 209730 None 0 Rat Binding pIC50 = 5 5.0 - 0
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.
ChEMBL 445 9 1 6 5.2 Cc1ccccc1[C@@H](CCC(=O)O)Oc1cc(OCc2ccc3c(c2)OCO3)ccc1C#N 10.1021/jm9707131
CHEMBL93097 209730 None 0 Rat Binding pIC50 = 5 5.0 - 0
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.
ChEMBL 445 9 1 6 5.2 Cc1ccccc1[C@@H](CCC(=O)O)Oc1cc(OCc2ccc3c(c2)OCO3)ccc1C#N 10.1021/jm9707131
10740214 209763 None 0 Rat Binding pIC50 = 5 5.0 - 0
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.
ChEMBL 408 9 1 6 4.9 Cc1ccccc1[C@@H](CCC(=O)O)Oc1cc(OCc2cnsc2)ccc1C#N 10.1021/jm9707131
CHEMBL93331 209763 None 0 Rat Binding pIC50 = 5 5.0 - 0
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.
ChEMBL 408 9 1 6 4.9 Cc1ccccc1[C@@H](CCC(=O)O)Oc1cc(OCc2cnsc2)ccc1C#N 10.1021/jm9707131
10693679 209832 None 0 Rat Binding pIC50 = 5 5.0 - 0
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.
ChEMBL 425 10 2 5 4.7 Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1C(N)=O 10.1021/jm9707131
CHEMBL93749 209832 None 0 Rat Binding pIC50 = 5 5.0 - 0
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.
ChEMBL 425 10 2 5 4.7 Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1C(N)=O 10.1021/jm9707131
11796594 209837 None 0 Rat Binding pIC50 = 5 5.0 - 0
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.
ChEMBL 424 10 1 5 5.8 CC(=O)c1ccc(OCc2ccsc2)cc1OC(CCC(=O)O)c1ccccc1C 10.1021/jm9707131
CHEMBL93776 209837 None 0 Rat Binding pIC50 = 5 5.0 - 0
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.
ChEMBL 424 10 1 5 5.8 CC(=O)c1ccc(OCc2ccsc2)cc1OC(CCC(=O)O)c1ccccc1C 10.1021/jm9707131
10669120 209904 None 0 Rat Binding pIC50 = 5 5.0 - 0
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.
ChEMBL 407 9 1 5 5.5 Cc1ccccc1[C@H](CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1C#N 10.1021/jm9707131
CHEMBL94141 209904 None 0 Rat Binding pIC50 = 5 5.0 - 0
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.
ChEMBL 407 9 1 5 5.5 Cc1ccccc1[C@H](CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1C#N 10.1021/jm9707131
10694804 210279 None 0 Rat Binding pIC50 = 5 5.0 - 0
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.
ChEMBL 449 10 1 6 6.3 Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1-c1ncco1 10.1021/jm9707131
CHEMBL96301 210279 None 0 Rat Binding pIC50 = 5 5.0 - 0
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.
ChEMBL 449 10 1 6 6.3 Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1-c1ncco1 10.1021/jm9707131
CHEMBL289687 213334 None 0 Rat Binding pIC50 = 5 5.0 - 0
Inhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar membranesInhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar membranes
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]cn1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00095a029
137661460 159469 None 0 Human Binding pIC50 = 6 6.0 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 565 10 2 9 4.4 C=CCOc1ccc2c(c1)c(=O)c(Cc1cccc(-c3nnn[nH]3)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL4100579 159469 None 0 Human Binding pIC50 = 6 6.0 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 565 10 2 9 4.4 C=CCOc1ccc2c(c1)c(=O)c(Cc1cccc(-c3nnn[nH]3)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2017.04.049
9852624 128749 None 0 Human Binding pIC50 = 7 7.0 - 0
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 656 14 2 11 4.5 CCS(=O)(=O)NCCCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
CHEMBL366872 128749 None 0 Human Binding pIC50 = 7 7.0 - 0
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 656 14 2 11 4.5 CCS(=O)(=O)NCCCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
10502577 12408 None 0 Human Binding pIC50 = 5 5.0 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 426 7 1 7 3.9 COc1ccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)cc1 10.1021/jm9700068
CHEMBL1185771 12408 None 0 Human Binding pIC50 = 5 5.0 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 426 7 1 7 3.9 COc1ccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)cc1 10.1021/jm9700068
CHEMBL432109 12408 None 0 Human Binding pIC50 = 5 5.0 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 426 7 1 7 3.9 COc1ccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)cc1 10.1021/jm9700068
10814776 99527 None 0 Human Binding pIC50 = 5 5.0 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 485 5 2 8 3.6 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc3c(c2)OCO3)c1Br 10.1021/jm9608366
10814776 99527 None 0 Human Binding pIC50 = 5 5.0 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 485 5 2 8 3.6 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc3c(c2)OCO3)c1Br 10.1021/jm9700068
CHEMBL283136 99527 None 0 Human Binding pIC50 = 5 5.0 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 485 5 2 8 3.6 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc3c(c2)OCO3)c1Br 10.1021/jm9608366
CHEMBL283136 99527 None 0 Human Binding pIC50 = 5 5.0 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 485 5 2 8 3.6 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc3c(c2)OCO3)c1Br 10.1021/jm9700068
18184234 62229 None 0 Human Binding pIC50 = 7.0 7.0 - 2
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 605 15 2 10 4.2 CCS(=O)(=O)NCCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
CHEMBL177802 62229 None 0 Human Binding pIC50 = 7.0 7.0 - 2
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 605 15 2 10 4.2 CCS(=O)(=O)NCCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
9961131 132225 None 0 Human Binding pIC50 = 7.0 7.0 - 2
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 650 15 2 12 3.1 CCCS(=O)(=O)NCCOc1nc(N2CCOCC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
CHEMBL369676 132225 None 0 Human Binding pIC50 = 7.0 7.0 - 2
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 650 15 2 12 3.1 CCCS(=O)(=O)NCCOc1nc(N2CCOCC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
42630654 18411 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
ChEMBL 545 10 2 8 4.3 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCOC)ccc31)OCO2 10.1016/j.bmcl.2010.08.074
CHEMBL1271531 18411 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
ChEMBL 545 10 2 8 4.3 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCOC)ccc31)OCO2 10.1016/j.bmcl.2010.08.074
10210086 61301 None 0 Human Binding pIC50 = 6.0 6.0 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 571 10 2 12 3.0 C#CCOc1nc(-c2ccnc(-c3nn[nH]n3)c2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL176664 61301 None 0 Human Binding pIC50 = 6.0 6.0 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 571 10 2 12 3.0 C#CCOc1nc(-c2ccnc(-c3nn[nH]n3)c2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
42630654 18411 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 545 10 2 8 4.3 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCOC)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL1271531 18411 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 545 10 2 8 4.3 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCOC)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
11071347 117870 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
ChEMBL 516 11 1 5 5.0 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(F)c(F)c1 10.1021/jm010237l
CHEMBL340190 117870 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
ChEMBL 516 11 1 5 5.0 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(F)c(F)c1 10.1021/jm010237l
44279677 102281 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB receptor
ChEMBL 478 2 2 3 4.0 O=C1c2cc(Br)ccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(Br)cc21 10.1016/0960-894X(95)00230-Q
CHEMBL30297 102281 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB receptor
ChEMBL 478 2 2 3 4.0 O=C1c2cc(Br)ccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(Br)cc21 10.1016/0960-894X(95)00230-Q
10504475 209410 None 0 Pig Binding pIC50 = 6.0 6.0 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 468 8 1 6 3.4 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(C)CC(C)C)cc1 10.1021/jm9505369
CHEMBL9119 209410 None 0 Pig Binding pIC50 = 6.0 6.0 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 468 8 1 6 3.4 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(C)CC(C)C)cc1 10.1021/jm9505369
44458669 84707 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
ChEMBL 505 6 2 7 3.0 Cc1ccccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(N)=O)ccc12 10.1016/s0960-894x(01)00660-6
CHEMBL22249 84707 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
ChEMBL 505 6 2 7 3.0 Cc1ccccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(N)=O)ccc12 10.1016/s0960-894x(01)00660-6
10168939 131436 None 0 Human Binding pIC50 = 6.0 6.0 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 695 11 2 12 5.9 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCC#CCOC(=O)Nc1ccccn1 10.1016/s0960-894x(02)01084-3
CHEMBL368860 131436 None 0 Human Binding pIC50 = 6.0 6.0 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 695 11 2 12 5.9 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCC#CCOC(=O)Nc1ccccn1 10.1016/s0960-894x(02)01084-3
76320429 85875 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]ET-1 from ETB receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hrDisplacement of [125I]ET-1 from ETB receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hr
ChEMBL 324 4 1 6 3.6 Cc1c(C(=O)O)oc2cccc(OCc3ccc4nonc4c3)c12 10.1007/s00044-013-0542-3
CHEMBL2296900 85875 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]ET-1 from ETB receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hrDisplacement of [125I]ET-1 from ETB receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hr
ChEMBL 324 4 1 6 3.6 Cc1c(C(=O)O)oc2cccc(OCc3ccc4nonc4c3)c12 10.1007/s00044-013-0542-3
10625633 209597 None 0 Pig Binding pIC50 = 6.0 6.0 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 514 12 1 8 2.4 COCCN(CCOC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL9223 209597 None 0 Pig Binding pIC50 = 6.0 6.0 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 514 12 1 8 2.4 COCCN(CCOC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
10817024 12132 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 578 10 2 6 5.2 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NCC(c2ccccc2)c2ccccc2)cc1 10.1021/jm990171i
CHEMBL1184112 12132 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 578 10 2 6 5.2 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NCC(c2ccccc2)c2ccccc2)cc1 10.1021/jm990171i
CHEMBL332808 12132 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 578 10 2 6 5.2 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NCC(c2ccccc2)c2ccccc2)cc1 10.1021/jm990171i
11798504 97176 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Radioligand binding selectivity to human Endothelin B receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin B receptor in chinese hamster ovary cells
ChEMBL 468 9 1 6 3.5 CCCCN(C)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL267695 97176 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Radioligand binding selectivity to human Endothelin B receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin B receptor in chinese hamster ovary cells
ChEMBL 468 9 1 6 3.5 CCCCN(C)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
71458721 81732 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 642 14 2 10 4.6 COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)nc(C2CC2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
CHEMBL2163726 81732 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 642 14 2 10 4.6 COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)nc(C2CC2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
CHEMBL2304010 211925 None 0 Pig Binding pIC50 = 8.0 8.0 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL None None None CSC(C)(C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc2c(Cl)[nH]c3ccccc23)NC(=O)[C@@H](C(C)C)NC1=O 10.1021/jm9600914
44320192 107112 None 0 Rat Binding pIC50 = 8.0 8.0 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 480 6 1 5 5.9 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1Cc1cccc(Cl)c1 10.1016/s0960-894x(00)00513-8
CHEMBL315622 107112 None 0 Rat Binding pIC50 = 8.0 8.0 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 480 6 1 5 5.9 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1Cc1cccc(Cl)c1 10.1016/s0960-894x(00)00513-8
10321290 4638 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B receptor
ChEMBL 445 7 1 5 5.1 CCCCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(02)00663-7
CHEMBL102969 4638 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B receptor
ChEMBL 445 7 1 5 5.1 CCCCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(02)00663-7
44284287 161341 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 532 10 3 7 5.2 CCC(CO)Cc1cc(OC)ccc1[C@@H]1c2nc(NC(C)C)ccc2[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O 10.1016/j.bmcl.2004.01.008
CHEMBL411925 161341 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 532 10 3 7 5.2 CCC(CO)Cc1cc(OC)ccc1[C@@H]1c2nc(NC(C)C)ccc2[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O 10.1016/j.bmcl.2004.01.008
44314657 103258 None 0 Pig Binding pIC50 = 7.0 7.0 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 619 13 5 4 4.3 CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1CCCCC1)C(=O)O 10.1021/jm9600914
CHEMBL308383 103258 None 0 Pig Binding pIC50 = 7.0 7.0 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 619 13 5 4 4.3 CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1CCCCC1)C(=O)O 10.1021/jm9600914
159594 522 None 36 Pig Binding pIC50 = 7.0 7.0 - 3
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1016/s0960-894x(98)00301-1
159594.0 522 None 36 Pig Binding pIC50 = 7.0 7.0 - 3
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1016/s0960-894x(98)00301-1
3487 522 None 36 Pig Binding pIC50 = 7.0 7.0 - 3
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1016/s0960-894x(98)00301-1
CHEMBL9194 522 None 36 Pig Binding pIC50 = 7.0 7.0 - 3
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1016/s0960-894x(98)00301-1
DB06199 522 None 36 Pig Binding pIC50 = 7.0 7.0 - 3
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1016/s0960-894x(98)00301-1
122044 10175 None 42 Human Binding pIC50 = 6.0 6.0 - 0
Ability to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptorAbility to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptor
ChEMBL 473 9 2 8 3.7 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCO)c1 10.1021/jm0102304
CHEMBL115951 10175 None 42 Human Binding pIC50 = 6.0 6.0 - 0
Ability to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptorAbility to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptor
ChEMBL 473 9 2 8 3.7 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCO)c1 10.1021/jm0102304
15289330 99856 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 493 8 1 8 5.3 COc1cccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc(OC)c(OC)cc23)c1 10.1016/0960-894X(96)00232-6
CHEMBL285368 99856 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 493 8 1 8 5.3 COc1cccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc(OC)c(OC)cc23)c1 10.1016/0960-894X(96)00232-6
18995998 162485 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 523 9 1 9 5.3 COc1cccc(Sc2c(C(=O)O)n(Cc3cc(OC)c4c(c3)OCO4)c3cc(OC)c(OC)cc23)c1 10.1016/0960-894X(96)00232-6
CHEMBL416570 162485 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 523 9 1 9 5.3 COc1cccc(Sc2c(C(=O)O)n(Cc3cc(OC)c4c(c3)OCO4)c3cc(OC)c(OC)cc23)c1 10.1016/0960-894X(96)00232-6
CHEMBL438768 216257 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Binding affinity against Endothelin B receptor in rat cerebellar membrane (ET-B) from adult blue laurie ratBinding affinity against Endothelin B receptor in rat cerebellar membrane (ET-B) from adult blue laurie rat
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](CCC(=O)O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)80156-6
15453179 207939 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 392 4 1 4 4.2 Cc1noc(NS(=O)(=O)c2cccc(-c3ccccc3)c2)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL80538 207939 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 392 4 1 4 4.2 Cc1noc(NS(=O)(=O)c2cccc(-c3ccccc3)c2)c1Br 10.1016/0960-894X(96)00441-6
11783885 100941 None 0 Pig Binding pIC50 = 6.0 6.0 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 382 7 1 5 4.6 CCCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccccc21 10.1021/jm010382z
CHEMBL293702 100941 None 0 Pig Binding pIC50 = 6.0 6.0 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 382 7 1 5 4.6 CCCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccccc21 10.1021/jm010382z
44279350 168279 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB receptor
ChEMBL 428 4 2 4 4.2 COc1cccc(-c2ccc3c(c2)C(=O)c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@H]32)c1 10.1016/0960-894X(95)00230-Q
CHEMBL433229 168279 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB receptor
ChEMBL 428 4 2 4 4.2 COc1cccc(-c2ccc3c(c2)C(=O)c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@H]32)c1 10.1016/0960-894X(95)00230-Q
44314609 207206 None 0 Pig Binding pIC50 = 6.0 6.0 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 720 12 6 4 5.6 CC(C)CC(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)N[C@H](Cc1c(Br)[nH]c2ccccc12)C(=O)NC(Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm9600914
CHEMBL74471 207206 None 0 Pig Binding pIC50 = 6.0 6.0 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 720 12 6 4 5.6 CC(C)CC(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)N[C@H](Cc1c(Br)[nH]c2ccccc12)C(=O)NC(Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm9600914
44458999 168331 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
ChEMBL 525 6 2 7 3.3 Cn1cc(C(C(=O)NS(=O)(=O)c2ccc(Cl)cc2)c2ccc3c(c2)OCO3)c2ccc(C(N)=O)cc21 10.1016/s0960-894x(01)00660-6
CHEMBL433619 168331 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
ChEMBL 525 6 2 7 3.3 Cn1cc(C(C(=O)NS(=O)(=O)c2ccc(Cl)cc2)c2ccc3c(c2)OCO3)c2ccc(C(N)=O)cc21 10.1016/s0960-894x(01)00660-6
44266552 4515 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 473 7 1 7 5.3 CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2c(c1)OCO2 10.1016/0960-894X(96)00170-9
CHEMBL10218 4515 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 473 7 1 7 5.3 CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2c(c1)OCO2 10.1016/0960-894X(96)00170-9
44317109 104948 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 472 3 1 4 4.1 Cc1noc(NS(=O)(=O)c2cc(Br)ccc2Br)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL311216 104948 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 472 3 1 4 4.1 Cc1noc(NS(=O)(=O)c2cc(Br)ccc2Br)c1Br 10.1016/0960-894X(96)00441-6
10694591 9228 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 444 6 1 6 4.6 CC(C)Oc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1 10.1021/jm9606507
CHEMBL11064 9228 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 444 6 1 6 4.6 CC(C)Oc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1 10.1021/jm9606507
10551532 110647 None 0 Pig Binding pIC50 = 5.0 5.0 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 450 8 1 4 3.9 CCCN(C)C(=O)CN1C[C@H](c2ccc3c(c2)CCC3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL325444 110647 None 0 Pig Binding pIC50 = 5.0 5.0 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 450 8 1 4 3.9 CCCN(C)C(=O)CN1C[C@H](c2ccc3c(c2)CCC3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
10791702 198272 None 0 Pig Binding pIC50 = 5.0 5.0 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 506 12 1 5 5.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2cccc3occc23)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL558148 198272 None 0 Pig Binding pIC50 = 5.0 5.0 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 506 12 1 5 5.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2cccc3occc23)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
15340612 106888 None 1 Rat Binding pIC50 = 5.0 5.0 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 406 5 1 5 3.6 COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2=O)c1 10.1016/s0960-894x(00)00232-8
CHEMBL3144599 106888 None 1 Rat Binding pIC50 = 5.0 5.0 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 406 5 1 5 3.6 COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2=O)c1 10.1016/s0960-894x(00)00232-8
CHEMBL2367550 212043 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
Inhibition of binding to Endothelin B receptor of rat cerebellar membranes.Inhibition of binding to Endothelin B receptor of rat cerebellar membranes.
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N(C)[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm970161m
44439103 91985 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]ET1 from human ETB receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETB receptor expressed in CHO cells
ChEMBL 859 27 2 14 5.3 CC(=O)CC(=O)CCc1ccc(NC(=O)CCOCCOCCOCCOCC(=O)N(C)Cc2cc(-c3ncco3)ccc2-c2ccccc2S(=O)(=O)Nc2ccno2)cc1 10.1016/j.bmcl.2006.10.009
CHEMBL241460 91985 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]ET1 from human ETB receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETB receptor expressed in CHO cells
ChEMBL 859 27 2 14 5.3 CC(=O)CC(=O)CCc1ccc(NC(=O)CCOCCOCCOCCOCC(=O)N(C)Cc2cc(-c3ncco3)ccc2-c2ccccc2S(=O)(=O)Nc2ccno2)cc1 10.1016/j.bmcl.2006.10.009
10836835 97154 None 0 Pig Binding pIC50 = 5.0 5.0 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 440 7 2 5 3.8 CCCCNC(=O)N1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL267483 97154 None 0 Pig Binding pIC50 = 5.0 5.0 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 440 7 2 5 3.8 CCCCNC(=O)N1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
44351961 18843 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
ChEMBL 522 13 1 5 5.6 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CCC)cc1 10.1021/jm010237l
CHEMBL128061 18843 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
ChEMBL 522 13 1 5 5.6 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CCC)cc1 10.1021/jm010237l
10218058 81700 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Antagonist activity at ETB receptor (unknown origin)Antagonist activity at ETB receptor (unknown origin)
ChEMBL 523 12 2 10 3.1 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCO 10.1016/j.bmcl.2016.06.014
CHEMBL2163695 81700 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Antagonist activity at ETB receptor (unknown origin)Antagonist activity at ETB receptor (unknown origin)
ChEMBL 523 12 2 10 3.1 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCO 10.1016/j.bmcl.2016.06.014
42630532 18406 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
ChEMBL 541 10 2 7 4.9 C=CCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2010.08.074
CHEMBL1271479 18406 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
ChEMBL 541 10 2 7 4.9 C=CCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2010.08.074
10218058 81700 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 523 12 2 10 3.1 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCO 10.1021/jm3009103
CHEMBL2163695 81700 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 523 12 2 10 3.1 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCO 10.1021/jm3009103
42630532 18406 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 541 10 2 7 4.9 C=CCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL1271479 18406 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 541 10 2 7 4.9 C=CCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2017.04.049
22467230 85389 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cells
ChEMBL 536 8 1 8 4.0 COCc1ccc2c(C(C(=O)NS(=O)(=O)c3ccc(C)cc3OC)c3ccc4c(c3)OCO4)cn(C)c2c1 10.1007/s00044-004-0021-y
CHEMBL2261601 85389 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cells
ChEMBL 536 8 1 8 4.0 COCc1ccc2c(C(C(=O)NS(=O)(=O)c3ccc(C)cc3OC)c3ccc4c(c3)OCO4)cn(C)c2c1 10.1007/s00044-004-0021-y
10281943 60084 None 0 Human Binding pIC50 = 5.9 5.9 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 589 10 1 10 4.9 COCC#CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL173743 60084 None 0 Human Binding pIC50 = 5.9 5.9 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 589 10 1 10 4.9 COCC#CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
71460536 81717 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 589 11 1 12 3.1 COc1ccccc1Oc1c(NS(C)(=O)=O)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
CHEMBL2163712 81717 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 589 11 1 12 3.1 COc1ccccc1Oc1c(NS(C)(=O)=O)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
23445593 60255 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 440 6 1 5 4.7 Cc1ccc(CCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(97)00133-9
CHEMBL174086 60255 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 440 6 1 5 4.7 Cc1ccc(CCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(97)00133-9
10553017 98160 None 0 Pig Binding pIC50 = 5.9 5.9 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 488 7 1 6 3.9 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(C)c2ccccc2)cc1 10.1021/jm9505369
CHEMBL273476 98160 None 0 Pig Binding pIC50 = 5.9 5.9 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 488 7 1 6 3.9 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(C)c2ccccc2)cc1 10.1021/jm9505369
9807456 60493 None 0 Human Binding pIC50 = 5.9 5.9 - 1
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 545 9 1 9 4.8 C#CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL175435 60493 None 0 Human Binding pIC50 = 5.9 5.9 - 1
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 545 9 1 9 4.8 C#CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
9852318 9616 None 8 Human Binding pIC50 = 7.9 7.9 -2691 2
Antagonist activity at ET-B receptor (unknown origin)Antagonist activity at ET-B receptor (unknown origin)
ChEMBL 613 11 2 9 4.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/acs.jmedchem.5b01781
CHEMBL112624 9616 None 8 Human Binding pIC50 = 7.9 7.9 -2691 2
Antagonist activity at ET-B receptor (unknown origin)Antagonist activity at ET-B receptor (unknown origin)
ChEMBL 613 11 2 9 4.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/acs.jmedchem.5b01781
CHEMBL1627022 9616 None 8 Human Binding pIC50 = 7.9 7.9 -2691 2
Antagonist activity at ET-B receptor (unknown origin)Antagonist activity at ET-B receptor (unknown origin)
ChEMBL 613 11 2 9 4.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/acs.jmedchem.5b01781
CHEMBL385492 214812 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00015a003
1009 194 None 25 Human Binding pIC50 = 7.9 7.9 676 2
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 558 11 2 6 5.8 CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2 10.1021/jm990170q
5310991 194 None 25 Human Binding pIC50 = 7.9 7.9 676 2
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 558 11 2 6 5.8 CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2 10.1021/jm990170q
CHEMBL332794 194 None 25 Human Binding pIC50 = 7.9 7.9 676 2
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 558 11 2 6 5.8 CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2 10.1021/jm990170q
9852318 9616 None 8 Human Binding pIC50 = 7.9 7.9 -2691 2
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 613 11 2 9 4.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm3009103
CHEMBL112624 9616 None 8 Human Binding pIC50 = 7.9 7.9 -2691 2
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 613 11 2 9 4.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm3009103
CHEMBL1627022 9616 None 8 Human Binding pIC50 = 7.9 7.9 -2691 2
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 613 11 2 9 4.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm3009103
21462932 49149 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 548 8 2 8 4.6 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2cc(NS(C)(=O)=O)ccc23)cc1 10.1016/s0960-894x(99)00040-2
CHEMBL156194 49149 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 548 8 2 8 4.6 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2cc(NS(C)(=O)=O)ccc23)cc1 10.1016/s0960-894x(99)00040-2
10173807 50897 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 455 6 1 6 5.2 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(99)00040-2
CHEMBL157742 50897 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 455 6 1 6 5.2 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(99)00040-2
9825494 205067 None 0 Pig Binding pIC50 = 6.9 6.9 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 460 6 1 6 5.2 COc1ccc(C2=C(C(=O)O)[C@@H](c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
CHEMBL61211 205067 None 0 Pig Binding pIC50 = 6.9 6.9 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 460 6 1 6 5.2 COc1ccc(C2=C(C(=O)O)[C@@H](c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
CHEMBL2304007 211922 None 0 Pig Binding pIC50 = 6.9 6.9 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL None None None Cc1[nH]c2ccccc2c1C[C@@H]1NC(=O)[C@@H](C(C)C)NC(=O)[C@H](C2CCCC2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC1=O 10.1021/jm9600914
155551580 174097 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 526 12 2 10 3.0 CCNS(=O)(=O)Nc1ncnc(OCCOc2cc(OC)ccc2Cl)c1-c1ncc(SC)cn1 10.1016/j.bmcl.2016.06.014
CHEMBL4542394 174097 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 526 12 2 10 3.0 CCNS(=O)(=O)Nc1ncnc(OCCOc2cc(OC)ccc2Cl)c1-c1ncc(SC)cn1 10.1016/j.bmcl.2016.06.014
11757759 174550 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 570 13 2 10 2.8 COCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Br)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL4553625 174550 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 570 13 2 10 2.8 COCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Br)cc1 10.1016/j.bmcl.2016.06.014
9870830 209172 None 29 Human Binding pIC50 = 6.9 6.9 -66 2
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors / CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors / CHO-K1 cells
ChEMBL 506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1021/jm9606507
CHEMBL8981 209172 None 29 Human Binding pIC50 = 6.9 6.9 -66 2
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors / CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors / CHO-K1 cells
ChEMBL 506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1021/jm9606507
44311135 206648 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 607 11 2 10 5.7 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
CHEMBL70800 206648 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 607 11 2 10 5.7 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
8260 531 None 42 Human Binding pIC50 = 5.9 5.9 - 0
Antagonist activity at ETB receptor (unknown origin) in presence of ET1Antagonist activity at ETB receptor (unknown origin) in presence of ET1
ChEMBL 479 8 1 9 3.9 COc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cn1)C)c1ccncc1 10.1016/j.bmcl.2016.06.014
9912992 531 None 42 Human Binding pIC50 = 5.9 5.9 - 0
Antagonist activity at ETB receptor (unknown origin) in presence of ET1Antagonist activity at ETB receptor (unknown origin) in presence of ET1
ChEMBL 479 8 1 9 3.9 COc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cn1)C)c1ccncc1 10.1016/j.bmcl.2016.06.014
CHEMBL3989834 531 None 42 Human Binding pIC50 = 5.9 5.9 - 0
Antagonist activity at ETB receptor (unknown origin) in presence of ET1Antagonist activity at ETB receptor (unknown origin) in presence of ET1
ChEMBL 479 8 1 9 3.9 COc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cn1)C)c1ccncc1 10.1016/j.bmcl.2016.06.014
15453180 105281 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 348 4 1 4 4.1 Cc1noc(NS(=O)(=O)c2cccc(-c3ccccc3)c2)c1Cl 10.1016/0960-894X(96)00441-6
CHEMBL311510 105281 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 348 4 1 4 4.1 Cc1noc(NS(=O)(=O)c2cccc(-c3ccccc3)c2)c1Cl 10.1016/0960-894X(96)00441-6
10288020 14635 None 0 Pig Binding pIC50 = 5.9 5.9 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 430 7 1 6 4.7 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL1205067 14635 None 0 Pig Binding pIC50 = 5.9 5.9 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 430 7 1 6 4.7 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL48881 14635 None 0 Pig Binding pIC50 = 5.9 5.9 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 430 7 1 6 4.7 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
44266646 98618 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptor
ChEMBL 475 6 1 8 4.5 COc1cc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OC 10.1016/s0960-894x(97)10151-2
CHEMBL276638 98618 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptor
ChEMBL 475 6 1 8 4.5 COc1cc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OC 10.1016/s0960-894x(97)10151-2
10310877 206347 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptor
ChEMBL 473 8 1 7 5.9 CCCOc1ccc2c(c1)c(-c1ccc(OC)cc1)c(C(=O)O)n2Cc1ccc2nsnc2c1 10.1016/s0960-894x(97)10151-2
CHEMBL68896 206347 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptor
ChEMBL 473 8 1 7 5.9 CCCOc1ccc2c(c1)c(-c1ccc(OC)cc1)c(C(=O)O)n2Cc1ccc2nsnc2c1 10.1016/s0960-894x(97)10151-2
10769526 102755 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.
ChEMBL 578 12 2 10 4.1 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCCC(=O)O)c2)cc1 10.1021/jm980504w
CHEMBL304762 102755 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.
ChEMBL 578 12 2 10 4.1 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCCC(=O)O)c2)cc1 10.1021/jm980504w
44211959 55452 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) receptor expressed in CHO cells
ChEMBL 620 12 1 9 5.5 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)NS(C)(=O)=O)c1ccc2c(c1)OCO2 10.1016/0960-894X(95)00186-W
CHEMBL16197 55452 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) receptor expressed in CHO cells
ChEMBL 620 12 1 9 5.5 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)NS(C)(=O)=O)c1ccc2c(c1)OCO2 10.1016/0960-894X(95)00186-W
44327412 210040 None 0 Pig Binding pIC50 = 5.9 5.9 - 0
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranes
ChEMBL 497 5 1 8 3.0 Cc1cc(C)c(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c2ccc3c(c2)OCO3)n1 10.1016/S0960-894X(96)00617-8
CHEMBL94929 210040 None 0 Pig Binding pIC50 = 5.9 5.9 - 0
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranes
ChEMBL 497 5 1 8 3.0 Cc1cc(C)c(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c2ccc3c(c2)OCO3)n1 10.1016/S0960-894X(96)00617-8
11038320 18880 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
ChEMBL 492 11 1 4 5.2 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(C)cc1 10.1021/jm010237l
CHEMBL128240 18880 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
ChEMBL 492 11 1 4 5.2 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(C)cc1 10.1021/jm010237l
10501279 98271 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 402 6 1 5 4.1 COc1ccc(C2(O)OC(=O)C(c3cccc(OC)c3)=C2Cc2ccccc2)cc1 10.1021/jm9606507
CHEMBL274307 98271 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 402 6 1 5 4.1 COc1ccc(C2(O)OC(=O)C(c3cccc(OC)c3)=C2Cc2ccccc2)cc1 10.1021/jm9606507
44277368 106901 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 480 8 2 7 3.0 COc1ccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2=O)c(OCC(=O)O)c1 10.1016/s0960-894x(00)00232-8
CHEMBL3144733 106901 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 480 8 2 7 3.0 COc1ccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2=O)c(OCC(=O)O)c1 10.1016/s0960-894x(00)00232-8
44386144 62004 None 0 Pig Binding pIC50 = 4.9 4.9 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 555 9 3 7 5.2 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)n2ccc3ccccc32)nc1C(=O)O 10.1021/jm950592+
CHEMBL177431 62004 None 0 Pig Binding pIC50 = 4.9 4.9 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 555 9 3 7 5.2 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)n2ccc3ccccc32)nc1C(=O)O 10.1021/jm950592+
44266575 4645 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 459 6 1 7 5.2 CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2-c1ccc2c(c1)OCO2 10.1016/0960-894X(96)00170-9
CHEMBL10302 4645 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 459 6 1 7 5.2 CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2-c1ccc2c(c1)OCO2 10.1016/0960-894X(96)00170-9
9830773 130294 None 0 Human Binding pIC50 = 6.9 6.9 - 2
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 636 14 2 12 2.8 CCS(=O)(=O)NCCOc1nc(N2CCOCC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
CHEMBL367958 130294 None 0 Human Binding pIC50 = 6.9 6.9 - 2
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 636 14 2 12 2.8 CCS(=O)(=O)NCCOc1nc(N2CCOCC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
44291897 101347 None 0 Human Binding pIC50 = 4.9 4.9 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 482 7 2 9 3.6 COc1cc(C#N)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(OC)c1 10.1021/jm9608366
CHEMBL296456 101347 None 0 Human Binding pIC50 = 4.9 4.9 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 482 7 2 9 3.6 COc1cc(C#N)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(OC)c1 10.1021/jm9608366
9956918 170986 None 0 Human Binding pIC50 = 4.9 4.9 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 482 7 2 9 3.6 COc1cc(C#N)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)cc1OC 10.1021/jm9700068
CHEMBL44544 170986 None 0 Human Binding pIC50 = 4.9 4.9 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 482 7 2 9 3.6 COc1cc(C#N)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)cc1OC 10.1021/jm9700068
10190108 130766 None 0 Human Binding pIC50 = 6.9 6.9 - 1
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 681 12 2 12 5.7 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccncc2)nc1OCC#CCOC(=O)Nc1ccccn1 10.1016/s0960-894x(02)01084-3
CHEMBL368386 130766 None 0 Human Binding pIC50 = 6.9 6.9 - 1
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 681 12 2 12 5.7 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccncc2)nc1OCC#CCOC(=O)Nc1ccccn1 10.1016/s0960-894x(02)01084-3
19432672 206679 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 606 11 3 9 5.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCNC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
CHEMBL70924 206679 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 606 11 3 9 5.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCNC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
23445333 127873 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 484 6 1 7 4.4 Cc1cc2c(cc1CCc1ccsc1S(=O)(=O)Nc1onc(C)c1Br)OCO2 10.1016/S0960-894X(97)00133-9
CHEMBL366378 127873 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 484 6 1 7 4.4 Cc1cc2c(cc1CCc1ccsc1S(=O)(=O)Nc1onc(C)c1Br)OCO2 10.1016/S0960-894X(97)00133-9
10599829 97182 None 0 Pig Binding pIC50 = 5.9 5.9 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 454 9 2 6 3.2 CCCCNC(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL267761 97182 None 0 Pig Binding pIC50 = 5.9 5.9 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 454 9 2 6 3.2 CCCCNC(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
44368390 45320 None 0 Pig Binding pIC50 = 4.9 4.9 - 0
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 475 9 2 6 3.9 COc1ccc(CN(C(=O)/C=C/c2ccc3c(c2)OCO3)C(Cc2ccc(O)cc2)C(=O)O)cc1 10.1016/s0960-894x(01)00009-9
CHEMBL152654 45320 None 0 Pig Binding pIC50 = 4.9 4.9 - 0
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 475 9 2 6 3.9 COc1ccc(CN(C(=O)/C=C/c2ccc3c(c2)OCO3)C(Cc2ccc(O)cc2)C(=O)O)cc1 10.1016/s0960-894x(01)00009-9
71462321 82038 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 584 12 2 8 4.2 CCc1ccc(-c2c(NS(=O)(=O)NCc3ccccc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm3009103
CHEMBL2165335 82038 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 584 12 2 8 4.2 CCc1ccc(-c2c(NS(=O)(=O)NCc3ccccc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm3009103
10577111 209355 None 0 Pig Binding pIC50 = 4.9 4.9 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 493 7 1 6 4.0 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2C(=O)COc2ccc(F)cc2)cc1 10.1021/jm9505369
CHEMBL9084 209355 None 0 Pig Binding pIC50 = 4.9 4.9 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 493 7 1 6 4.0 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2C(=O)COc2ccc(F)cc2)cc1 10.1021/jm9505369
44371495 54261 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 590 10 1 8 5.4 CCCN(c1ccc2c(c1)oc1c(-c3ccc(OC)cc3)c(C(=O)O)c(=O)n(Cc3ccccc3OC)c12)S(C)(=O)=O 10.1016/s0960-894x(99)00040-2
CHEMBL160768 54261 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 590 10 1 8 5.4 CCCN(c1ccc2c(c1)oc1c(-c3ccc(OC)cc3)c(C(=O)O)c(=O)n(Cc3ccccc3OC)c12)S(C)(=O)=O 10.1016/s0960-894x(99)00040-2
44314575 103627 None 0 Pig Binding pIC50 = 7.9 7.9 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 601 13 5 5 4.2 CSCCC(NC(=O)[C@@H](Cc1c(C)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
CHEMBL308584 103627 None 0 Pig Binding pIC50 = 7.9 7.9 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 601 13 5 5 4.2 CSCCC(NC(=O)[C@@H](Cc1c(C)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
44314723 207456 None 0 Pig Binding pIC50 = 7.9 7.9 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 583 13 5 4 4.7 CCCCC(NC(=O)[C@@H](Cc1c(C)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
CHEMBL76735 207456 None 0 Pig Binding pIC50 = 7.9 7.9 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 583 13 5 4 4.7 CCCCC(NC(=O)[C@@H](Cc1c(C)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
44386169 131457 None 0 Human Binding pIC50 = 7.9 7.9 - 1
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 690 12 2 14 3.9 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1cnccn1 10.1016/s0960-894x(02)01084-3
CHEMBL368996 131457 None 0 Human Binding pIC50 = 7.9 7.9 - 1
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 690 12 2 14 3.9 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1cnccn1 10.1016/s0960-894x(02)01084-3
123883 14650 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Ability to displace endothelin ([125I]ET1) from human Endothelin B receptorAbility to displace endothelin ([125I]ET1) from human Endothelin B receptor
ChEMBL 927 12 9 11 0.8 CC(C)C[C@@H]1NC(=O)[C@@H](c2cccs2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)N2CCN(c3ccccc3)CC2)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm970101g
CHEMBL1205177 14650 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Ability to displace endothelin ([125I]ET1) from human Endothelin B receptorAbility to displace endothelin ([125I]ET1) from human Endothelin B receptor
ChEMBL 927 12 9 11 0.8 CC(C)C[C@@H]1NC(=O)[C@@H](c2cccs2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)N2CCN(c3ccccc3)CC2)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm970101g
CHEMBL61425 14650 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Ability to displace endothelin ([125I]ET1) from human Endothelin B receptorAbility to displace endothelin ([125I]ET1) from human Endothelin B receptor
ChEMBL 927 12 9 11 0.8 CC(C)C[C@@H]1NC(=O)[C@@H](c2cccs2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)N2CCN(c3ccccc3)CC2)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm970101g
11102201 205681 None 0 Pig Binding pIC50 = 6.9 6.9 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 438 9 1 6 5.1 C=CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL64447 205681 None 0 Pig Binding pIC50 = 6.9 6.9 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 438 9 1 6 5.1 C=CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
11005243 205839 None 0 Pig Binding pIC50 = 6.9 6.9 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 474 8 1 6 5.6 CCCCOc1ccc2c(c1)C(c1ccc(OC)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
CHEMBL65337 205839 None 0 Pig Binding pIC50 = 6.9 6.9 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 474 8 1 6 5.6 CCCCOc1ccc2c(c1)C(c1ccc(OC)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
CHEMBL2304015 211930 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding affinity towards Endothelin B receptor in human girardi heart cell membranesBinding affinity towards Endothelin B receptor in human girardi heart cell membranes
ChEMBL None None None Cc1[nH]c2ccccc2c1C[C@@H]1NC(=O)[C@@H](C2CC2)NC(=O)[C@H](C2CCCC2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC1=O 10.1021/jm9600914
10505755 14590 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cells
ChEMBL 506 10 1 8 4.4 COc1ccc(C(=O)/C(Cc2ccc(OC)c(OC)c2OC)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1021/jm9606507
CHEMBL10832 14590 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cells
ChEMBL 506 10 1 8 4.4 COc1ccc(C(=O)/C(Cc2ccc(OC)c(OC)c2OC)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1021/jm9606507
CHEMBL1204670 14590 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cells
ChEMBL 506 10 1 8 4.4 COc1ccc(C(=O)/C(Cc2ccc(OC)c(OC)c2OC)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1021/jm9606507
44334053 4553 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B receptor
ChEMBL 465 5 1 5 5.5 COc1ccc([C@@H]2c3nc(-c4ccccc4)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1016/s0960-894x(02)00663-7
CHEMBL102411 4553 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B receptor
ChEMBL 465 5 1 5 5.5 COc1ccc([C@@H]2c3nc(-c4ccccc4)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1016/s0960-894x(02)00663-7
CHEMBL328942 213775 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Inhibitory concentration was evaluated by measuring the binding affinity at the Endothelin B receptor in rat cerebellar membranesInhibitory concentration was evaluated by measuring the binding affinity at the Endothelin B receptor in rat cerebellar membranes
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm970161m
44371516 51000 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 469 7 1 6 5.6 CCOc1ccccc1Cn1c(=O)c(C(=O)O)c(-c2ccc(OC)cc2)c2oc3ccccc3c21 10.1016/s0960-894x(99)00040-2
CHEMBL157827 51000 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 469 7 1 6 5.6 CCOc1ccccc1Cn1c(=O)c(C(=O)O)c(-c2ccc(OC)cc2)c2oc3ccccc3c21 10.1016/s0960-894x(99)00040-2
44351968 118144 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
ChEMBL 508 12 1 5 5.2 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CC)cc1 10.1021/jm010237l
CHEMBL340575 118144 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
ChEMBL 508 12 1 5 5.2 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CC)cc1 10.1021/jm010237l
44327348 162001 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL 1076 28 9 8 7.0 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL415238 162001 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL 1076 28 9 8 7.0 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL407933 215154 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)NC1CCCCC1)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
10503067 8172 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 436 5 1 6 4.9 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2CC2CCCCCC2)cc1 10.1021/jm9606507
CHEMBL10919 8172 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 436 5 1 6 4.9 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2CC2CCCCCC2)cc1 10.1021/jm9606507
15411005 4762 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Binding affinity for human endothelin B receptor expressed in CHO-K1 cells.Binding affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 677 13 1 12 5.2 CCOC(=O)C(NC(=O)OC1(c2ccc(OC)cc2)OC(=O)C(c2ccc3c(c2)OCO3)=C1Cc1cc(OC)c(OC)c(OC)c1)C(C)C 10.1016/S0960-894X(97)00002-4
CHEMBL103846 4762 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Binding affinity for human endothelin B receptor expressed in CHO-K1 cells.Binding affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 677 13 1 12 5.2 CCOC(=O)C(NC(=O)OC1(c2ccc(OC)cc2)OC(=O)C(c2ccc3c(c2)OCO3)=C1Cc1cc(OC)c(OC)c(OC)c1)C(C)C 10.1016/S0960-894X(97)00002-4
11026025 205343 None 0 Pig Binding pIC50 = 5.9 5.9 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 412 7 1 6 4.6 CCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL62669 205343 None 0 Pig Binding pIC50 = 5.9 5.9 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 412 7 1 6 4.6 CCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
11762081 205777 None 0 Pig Binding pIC50 = 5.9 5.9 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 446 7 1 5 5.5 COc1ccc(C2=C(C(=O)O)C(c3ccc(OC)cc3)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
CHEMBL64851 205777 None 0 Pig Binding pIC50 = 5.9 5.9 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 446 7 1 5 5.5 COc1ccc(C2=C(C(=O)O)C(c3ccc(OC)cc3)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
CHEMBL147908 211240 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]ET1 from Endothelin B receptor of rat cerebellumDisplacement of [125I]ET1 from Endothelin B receptor of rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)81215-4
10649086 175357 None 0 Human Binding pIC50 = 5.9 5.9 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 500 5 3 8 4.0 Cc1noc(NS(=O)(=O)c2ccsc2NC(=O)Nc2ccc3c(c2)OCO3)c1Br 10.1021/jm9700068
CHEMBL45723 175357 None 0 Human Binding pIC50 = 5.9 5.9 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 500 5 3 8 4.0 Cc1noc(NS(=O)(=O)c2ccsc2NC(=O)Nc2ccc3c(c2)OCO3)c1Br 10.1021/jm9700068
44299023 198954 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membranesInhibition of [125I]ET1 binding to porcine kidney inner medulla membranes
ChEMBL 457 6 1 6 4.7 CCc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)c(=O)n2Cc1ccccc1OC 10.1016/S0960-894X(97)00319-3
CHEMBL56343 198954 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membranesInhibition of [125I]ET1 binding to porcine kidney inner medulla membranes
ChEMBL 457 6 1 6 4.7 CCc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)c(=O)n2Cc1ccccc1OC 10.1016/S0960-894X(97)00319-3
56681797 63344 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibition of binding to Endothelin B receptor of rat cerebellar membranes.Inhibition of binding to Endothelin B receptor of rat cerebellar membranes.
ChEMBL 937 26 9 9 3.6 CC[C@H](C)[C@H](NC(=O)[C@@H](N)Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)[C@H](C)CC 10.1021/jm970161m
CHEMBL1793924 63344 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibition of binding to Endothelin B receptor of rat cerebellar membranes.Inhibition of binding to Endothelin B receptor of rat cerebellar membranes.
ChEMBL 937 26 9 9 3.6 CC[C@H](C)[C@H](NC(=O)[C@@H](N)Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)[C@H](C)CC 10.1021/jm970161m
44270523 48630 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) receptor expressed in CHO cells
ChEMBL 724 14 1 9 8.0 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2 10.1016/0960-894X(95)00186-W
CHEMBL15573 48630 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) receptor expressed in CHO cells
ChEMBL 724 14 1 9 8.0 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2 10.1016/0960-894X(95)00186-W
15453178 104809 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 348 4 1 4 4.1 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2)c1Cl 10.1016/0960-894X(96)00441-6
CHEMBL310739 104809 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 348 4 1 4 4.1 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2)c1Cl 10.1016/0960-894X(96)00441-6
18617303 105851 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 330 3 1 4 2.9 Cc1cccc(S(=O)(=O)Nc2onc(C)c2Br)c1 10.1016/0960-894X(96)00441-6
CHEMBL312685 105851 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 330 3 1 4 2.9 Cc1cccc(S(=O)(=O)Nc2onc(C)c2Br)c1 10.1016/0960-894X(96)00441-6
18617389 163573 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 408 3 1 4 3.6 Cc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL420029 163573 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 408 3 1 4 3.6 Cc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/0960-894X(96)00441-6
18617374 207974 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 350 3 1 4 3.2 Cc1noc(NS(=O)(=O)c2cccc(Cl)c2)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL80808 207974 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 350 3 1 4 3.2 Cc1noc(NS(=O)(=O)c2cccc(Cl)c2)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL414917 215620 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Binding affinity in Chinese hamster ovary (CHO) cells stably transfected with human endothelin B (ETB) receptorBinding affinity in Chinese hamster ovary (CHO) cells stably transfected with human endothelin B (ETB) receptor
ChEMBL None None None NC(=O)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)C1c2ccccc2CCc2ccccc21)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(95)00084-7
10575552 111372 None 0 Pig Binding pIC50 = 4.9 4.9 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 450 8 1 5 4.2 CCCN(C)C(=O)CN1C[C@H](c2ccc3ccoc3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL326690 111372 None 0 Pig Binding pIC50 = 4.9 4.9 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 450 8 1 5 4.2 CCCN(C)C(=O)CN1C[C@H](c2ccc3ccoc3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL2369710 212112 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Inhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellumInhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(95)00152-J
9915028 9413 None 19 Human Binding pIC50 = 4.9 4.9 -28183 3
Inhibitory activity against human endothelin B receptorInhibitory activity against human endothelin B receptor
ChEMBL 532 15 1 6 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC 10.1021/jm010237l
CHEMBL111612 9413 None 19 Human Binding pIC50 = 4.9 4.9 -28183 3
Inhibitory activity against human endothelin B receptorInhibitory activity against human endothelin B receptor
ChEMBL 532 15 1 6 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC 10.1021/jm010237l
CHEMBL4761843 9413 None 19 Human Binding pIC50 = 4.9 4.9 -28183 3
Inhibitory activity against human endothelin B receptorInhibitory activity against human endothelin B receptor
ChEMBL 532 15 1 6 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC 10.1021/jm010237l
44385621 128263 None 0 Pig Binding pIC50 = 4.9 4.9 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 550 10 5 5 4.6 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2C)nc1C(=O)O 10.1021/jm950592+
CHEMBL366544 128263 None 0 Pig Binding pIC50 = 4.9 4.9 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 550 10 5 5 4.6 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2C)nc1C(=O)O 10.1021/jm950592+
23445537 61165 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B receptor
ChEMBL 514 8 1 8 4.9 CCCc1cc2c(cc1OCc1ccsc1S(=O)(=O)Nc1onc(C)c1Br)OCO2 10.1016/S0960-894X(97)00132-7
CHEMBL176538 61165 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B receptor
ChEMBL 514 8 1 8 4.9 CCCc1cc2c(cc1OCc1ccsc1S(=O)(=O)Nc1onc(C)c1Br)OCO2 10.1016/S0960-894X(97)00132-7
44320488 107041 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 438 5 1 5 5.7 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1C1CCCCC1 10.1016/s0960-894x(00)00513-8
CHEMBL315175 107041 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 438 5 1 5 5.7 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1C1CCCCC1 10.1016/s0960-894x(00)00513-8
23445547 112405 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 398 4 1 5 4.3 Cc1noc(NS(=O)(=O)c2cc(-c3ccccc3)cs2)c1Br 10.1016/S0960-894X(96)00496-9
CHEMBL329375 112405 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 398 4 1 5 4.3 Cc1noc(NS(=O)(=O)c2cc(-c3ccccc3)cs2)c1Br 10.1016/S0960-894X(96)00496-9
137652304 157318 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 544 10 3 8 3.7 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCCN)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL4076290 157318 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 544 10 3 8 3.7 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCCN)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
10119105 101502 None 0 Human Binding pIC50 = 4.9 4.9 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 526 7 2 9 3.1 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2CC(=O)N(C)C)OCO3)c1Cl 10.1021/jm9608366
CHEMBL297618 101502 None 0 Human Binding pIC50 = 4.9 4.9 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 526 7 2 9 3.1 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2CC(=O)N(C)C)OCO3)c1Cl 10.1021/jm9608366
11798504 97176 None 0 Pig Binding pIC50 = 5.9 5.9 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 468 9 1 6 3.5 CCCCN(C)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL267695 97176 None 0 Pig Binding pIC50 = 5.9 5.9 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 468 9 1 6 3.5 CCCCN(C)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
23445336 60196 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 468 6 1 5 5.3 Cc1cc(C)c(CCc2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00133-9
CHEMBL173977 60196 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 468 6 1 5 5.3 Cc1cc(C)c(CCc2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00133-9
44314890 105132 None 0 Pig Binding pIC50 = 7.9 7.9 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 647 12 5 4 5.0 CC(C)CC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
CHEMBL311384 105132 None 0 Pig Binding pIC50 = 7.9 7.9 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 647 12 5 4 5.0 CC(C)CC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
44334128 4407 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B receptor
ChEMBL 443 7 1 5 4.9 C=CCCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(02)00663-7
CHEMBL101424 4407 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B receptor
ChEMBL 443 7 1 5 4.9 C=CCCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(02)00663-7
44334145 4654 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B receptor
ChEMBL 460 6 1 6 4.6 COc1ccc([C@@H]2c3nc(N(C)C(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1016/s0960-894x(02)00663-7
CHEMBL103090 4654 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B receptor
ChEMBL 460 6 1 6 4.6 COc1ccc([C@@H]2c3nc(N(C)C(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1016/s0960-894x(02)00663-7
44284292 168215 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 518 8 3 7 4.9 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(C)(C)O)c1 10.1016/j.bmcl.2004.01.008
CHEMBL432856 168215 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 518 8 3 7 4.9 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(C)(C)O)c1 10.1016/j.bmcl.2004.01.008
44311346 103218 None 0 Human Binding pIC50 = 7.9 7.9 - 1
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 681 13 2 13 5.2 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCSCC2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
CHEMBL308088 103218 None 0 Human Binding pIC50 = 7.9 7.9 - 1
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 681 13 2 13 5.2 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCSCC2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
17885912 107155 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 496 7 2 6 5.1 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1CC1CCCC(C(=O)O)C1 10.1016/s0960-894x(00)00513-8
CHEMBL315936 107155 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 496 7 2 6 5.1 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1CC1CCCC(C(=O)O)C1 10.1016/s0960-894x(00)00513-8
CHEMBL433406 216101 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)NC)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
15453172 207443 None 3 Human Binding pIC50 = 6.9 6.9 - 0
Binding affinity against human ETB receptor in transfected COS 7 cell membrane preparationBinding affinity against human ETB receptor in transfected COS 7 cell membrane preparation
ChEMBL 392 4 1 4 4.2 Cc1noc(NS(=O)(=O)c2ccc(-c3ccccc3)cc2)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL76623 207443 None 3 Human Binding pIC50 = 6.9 6.9 - 0
Binding affinity against human ETB receptor in transfected COS 7 cell membrane preparationBinding affinity against human ETB receptor in transfected COS 7 cell membrane preparation
ChEMBL 392 4 1 4 4.2 Cc1noc(NS(=O)(=O)c2ccc(-c3ccccc3)cc2)c1Br 10.1016/0960-894X(96)00441-6
44298381 198360 None 0 Pig Binding pIC50 = 6.9 6.9 - 0
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptor
ChEMBL 476 9 2 7 4.9 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCO)c1 10.1016/s0960-894x(00)00366-8
CHEMBL55909 198360 None 0 Pig Binding pIC50 = 6.9 6.9 - 0
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptor
ChEMBL 476 9 2 7 4.9 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCO)c1 10.1016/s0960-894x(00)00366-8
CHEMBL2304009 211924 None 0 Pig Binding pIC50 = 6.9 6.9 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc2c(Br)[nH]c3ccccc23)NC(=O)[C@@H](C(C)C)NC1=O 10.1021/jm9600914
CHEMBL86814 218382 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]ET1 from Endothelin B receptor of rat cerebellumDisplacement of [125I]ET1 from Endothelin B receptor of rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)81215-4
44333721 167896 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B receptor
ChEMBL 447 7 1 6 4.3 CCOCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(02)00663-7
CHEMBL430506 167896 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B receptor
ChEMBL 447 7 1 6 4.3 CCOCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(02)00663-7
CHEMBL436899 216155 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Binding affinity against Endothelin B receptor in rat cerebellar membrane (ET-B) from adult blue laurie ratBinding affinity against Endothelin B receptor in rat cerebellar membrane (ET-B) from adult blue laurie rat
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)80156-6
10916428 162790 None 0 Pig Binding pIC50 = 5.9 5.9 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 402 4 1 5 4.4 COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccccc32)cc1 10.1021/jm010382z
CHEMBL417050 162790 None 0 Pig Binding pIC50 = 5.9 5.9 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 402 4 1 5 4.4 COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccccc32)cc1 10.1021/jm010382z
44295106 14748 None 0 Pig Binding pIC50 = 5.9 5.9 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 472 7 1 7 4.6 COc1ccc(C(=O)/C(Cc2ccc3c(c2)CCO3)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL1206319 14748 None 0 Pig Binding pIC50 = 5.9 5.9 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 472 7 1 7 4.6 COc1ccc(C(=O)/C(Cc2ccc3c(c2)CCO3)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL262000 14748 None 0 Pig Binding pIC50 = 5.9 5.9 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 472 7 1 7 4.6 COc1ccc(C(=O)/C(Cc2ccc3c(c2)CCO3)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
10212163 130164 None 0 Human Binding pIC50 = 5.9 5.9 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 696 11 2 13 5.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCC#CCOC(=O)Nc1cnccn1 10.1016/s0960-894x(02)01084-3
CHEMBL367767 130164 None 0 Human Binding pIC50 = 5.9 5.9 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 696 11 2 13 5.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCC#CCOC(=O)Nc1cnccn1 10.1016/s0960-894x(02)01084-3
44266646 98618 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 475 6 1 8 4.5 COc1cc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OC 10.1016/0960-894X(96)00170-9
CHEMBL276638 98618 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 475 6 1 8 4.5 COc1cc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OC 10.1016/0960-894X(96)00170-9
122272 97150 None 32 Human Binding pIC50 = 4.9 4.9 - 2
Binding affinity against human ETB receptor in transfected COS 7 cell membrane preparationBinding affinity against human ETB receptor in transfected COS 7 cell membrane preparation
ChEMBL 345 4 1 5 3.3 Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C 10.1016/0960-894X(96)00441-6
CHEMBL267458 97150 None 32 Human Binding pIC50 = 4.9 4.9 - 2
Binding affinity against human ETB receptor in transfected COS 7 cell membrane preparationBinding affinity against human ETB receptor in transfected COS 7 cell membrane preparation
ChEMBL 345 4 1 5 3.3 Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C 10.1016/0960-894X(96)00441-6
18617345 105260 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 384 3 1 4 3.9 Cc1noc(NS(=O)(=O)c2cc(Cl)cc(Cl)c2)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL311461 105260 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 384 3 1 4 3.9 Cc1noc(NS(=O)(=O)c2cc(Cl)cc(Cl)c2)c1Br 10.1016/0960-894X(96)00441-6
18617314 207690 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 334 3 1 4 2.7 Cc1noc(NS(=O)(=O)c2ccc(F)cc2)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL78734 207690 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 334 3 1 4 2.7 Cc1noc(NS(=O)(=O)c2ccc(F)cc2)c1Br 10.1016/0960-894X(96)00441-6
3811690 207868 None 1 Human Binding pIC50 = 4.9 4.9 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 330 3 1 4 2.9 Cc1noc(NS(=O)(=O)c2ccc(Br)cc2)c1C 10.1016/0960-894X(96)00441-6
CHEMBL80129 207868 None 1 Human Binding pIC50 = 4.9 4.9 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 330 3 1 4 2.9 Cc1noc(NS(=O)(=O)c2ccc(Br)cc2)c1C 10.1016/0960-894X(96)00441-6
CHEMBL441006 216336 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Binding affinity in Chinese hamster ovary (CHO) cells stably transfected with human endothelin B (ETB) receptorBinding affinity in Chinese hamster ovary (CHO) cells stably transfected with human endothelin B (ETB) receptor
ChEMBL None None None CC(=O)[C@H](Cc1c[nH]c2ccccc12)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(95)00084-7
44277035 106908 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 410 4 1 4 4.2 O=c1c(Cc2ccc3c(c2)OCO3)c(C(F)(F)F)[nH]n1Cc1cccc(Cl)c1 10.1016/s0960-894x(00)00232-8
CHEMBL3144806 106908 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 410 4 1 4 4.2 O=c1c(Cc2ccc3c(c2)OCO3)c(C(F)(F)F)[nH]n1Cc1cccc(Cl)c1 10.1016/s0960-894x(00)00232-8
10646831 184026 None 0 Human Binding pIC50 = 4.9 4.9 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 441 6 2 7 4.1 COc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1 10.1021/jm9608366
10646831 184026 None 0 Human Binding pIC50 = 4.9 4.9 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 441 6 2 7 4.1 COc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1 10.1021/jm9700068
CHEMBL48134 184026 None 0 Human Binding pIC50 = 4.9 4.9 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 441 6 2 7 4.1 COc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1 10.1021/jm9608366
CHEMBL48134 184026 None 0 Human Binding pIC50 = 4.9 4.9 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 441 6 2 7 4.1 COc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1 10.1021/jm9700068
CHEMBL1791277 211377 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Inhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellumInhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O)[C@H](C)CC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(95)00152-J
10625530 209498 None 2 Pig Binding pIC50 = 4.9 4.9 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 510 12 1 6 4.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL9162 209498 None 2 Pig Binding pIC50 = 4.9 4.9 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 510 12 1 6 4.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
44266595 4394 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 507 6 1 7 6.0 O=C(O)c1c(-c2ccc3c(c2)OCO3)c2cc(OCc3ccccc3)ccc2n1-c1ccc2c(c1)OCO2 10.1016/0960-894X(96)00170-9
CHEMBL10136 4394 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 507 6 1 7 6.0 O=C(O)c1c(-c2ccc3c(c2)OCO3)c2cc(OCc3ccccc3)ccc2n1-c1ccc2c(c1)OCO2 10.1016/0960-894X(96)00170-9
10766385 98481 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 460 6 1 7 4.1 COc1ccc(C2(O)OC(=O)C(c3cc(OC)c4c(c3)OCO4)=C2Cc2ccccc2)cc1C 10.1021/jm9606507
CHEMBL275559 98481 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 460 6 1 7 4.1 COc1ccc(C2(O)OC(=O)C(c3cc(OC)c4c(c3)OCO4)=C2Cc2ccccc2)cc1C 10.1021/jm9606507
9870959 8919 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 509 13 1 6 4.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1ccccn1 10.1021/jm980217s
CHEMBL109778 8919 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 509 13 1 6 4.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1ccccn1 10.1021/jm980217s
10811595 98821 None 0 Human Binding pIC50 = 4.9 4.9 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 411 5 2 6 4.1 Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)cc1 10.1021/jm9608366
10811595 98821 None 0 Human Binding pIC50 = 4.9 4.9 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 411 5 2 6 4.1 Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)cc1 10.1021/jm9700068
CHEMBL278114 98821 None 0 Human Binding pIC50 = 4.9 4.9 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 411 5 2 6 4.1 Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)cc1 10.1021/jm9608366
CHEMBL278114 98821 None 0 Human Binding pIC50 = 4.9 4.9 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 411 5 2 6 4.1 Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)cc1 10.1021/jm9700068
155562688 175284 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 554 13 2 10 2.9 CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC 10.1016/j.bmcl.2016.06.014
CHEMBL4570529 175284 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 554 13 2 10 2.9 CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC 10.1016/j.bmcl.2016.06.014
44352026 117549 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
ChEMBL 548 11 1 5 5.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(C(F)(F)F)cc1 10.1021/jm010237l
CHEMBL339969 117549 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
ChEMBL 548 11 1 5 5.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(C(F)(F)F)cc1 10.1021/jm010237l
137633653 156688 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 593 10 2 9 5.0 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(-c4nnn[nH]4)c3)c(=O)c3cc(OCC4CCC4)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL4068786 156688 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 593 10 2 9 5.0 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(-c4nnn[nH]4)c3)c(=O)c3cc(OCC4CCC4)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
44311283 102388 None 0 Human Binding pIC50 = 6.8 6.8 - 1
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 649 11 2 10 6.7 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C(C)(C)C)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
CHEMBL303649 102388 None 0 Human Binding pIC50 = 6.8 6.8 - 1
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 649 11 2 10 6.7 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C(C)(C)C)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
10553490 181222 None 0 Human Binding pIC50 = 4.8 4.8 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 501 8 3 10 2.9 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2OCCO)OCO3)c1Cl 10.1021/jm9608366
CHEMBL47604 181222 None 0 Human Binding pIC50 = 4.8 4.8 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 501 8 3 10 2.9 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2OCCO)OCO3)c1Cl 10.1021/jm9608366
71455062 81710 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 669 14 1 12 5.0 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(C(F)(F)F)cn1 10.1021/jm3009103
CHEMBL2163705 81710 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 669 14 1 12 5.0 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(C(F)(F)F)cn1 10.1021/jm3009103
44266538 5467 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 371 4 1 4 4.8 O=C(O)c1c(-c2ccc3c(c2)OCO3)c2ccccc2n1Cc1ccccc1 10.1016/0960-894X(96)00170-9
CHEMBL10750 5467 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 371 4 1 4 4.8 O=C(O)c1c(-c2ccc3c(c2)OCO3)c2ccccc2n1Cc1ccccc1 10.1016/0960-894X(96)00170-9
52950137 18441 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
ChEMBL 559 10 3 8 3.8 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCC(=O)O)ccc31)OCO2 10.1016/j.bmcl.2010.08.074
CHEMBL1271863 18441 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
ChEMBL 559 10 3 8 3.8 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCC(=O)O)ccc31)OCO2 10.1016/j.bmcl.2010.08.074
71456863 81721 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Antagonist activity at ETB receptor (unknown origin)Antagonist activity at ETB receptor (unknown origin)
ChEMBL 680 14 2 12 4.2 COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1016/j.bmcl.2016.06.014
CHEMBL2163716 81721 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Antagonist activity at ETB receptor (unknown origin)Antagonist activity at ETB receptor (unknown origin)
ChEMBL 680 14 2 12 4.2 COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1016/j.bmcl.2016.06.014
71456863 81721 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 680 14 2 12 4.2 COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
CHEMBL2163716 81721 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 680 14 2 12 4.2 COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
10625083 209104 None 0 Pig Binding pIC50 = 5.8 5.8 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 496 10 1 5 5.3 CCCCN(CCCC)C(=O)N1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL8925 209104 None 0 Pig Binding pIC50 = 5.8 5.8 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 496 10 1 5 5.3 CCCCN(CCCC)C(=O)N1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
71460537 81728 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 660 12 1 13 2.7 COc1ccccc1Oc1c(NS(=O)(=O)N2CCOCC2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
CHEMBL2163722 81728 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 660 12 1 13 2.7 COc1ccccc1Oc1c(NS(=O)(=O)N2CCOCC2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
21041266 82043 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 584 10 2 8 3.3 O=S(=O)(Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1)NC1CC1 10.1021/jm3009103
CHEMBL2165340 82043 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 584 10 2 8 3.3 O=S(=O)(Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1)NC1CC1 10.1021/jm3009103
44304492 96613 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL 949 23 9 8 4.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL262993 96613 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL 949 23 9 8 4.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL2304006 211921 None 0 Pig Binding pIC50 = 7.8 7.8 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL None None None O=C(O)C[C@H]1NC(=O)[C@H](Cc2c(Br)[nH]c3ccccc23)NC(=O)[C@@H](C2CC2)NC(=O)[C@H](C2CCCC2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/jm9600914
22467235 96578 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cells
ChEMBL 533 7 2 7 3.8 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(C(N)=O)ccc23)cc1 10.1007/s00044-004-0021-y
CHEMBL262784 96578 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cells
ChEMBL 533 7 2 7 3.8 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(C(N)=O)ccc23)cc1 10.1007/s00044-004-0021-y
23288645 169830 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta cell membranes
ChEMBL 580 12 3 8 5.6 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(SC)cc3)cc(C(=O)Nc3ccccc3)cc2OCCO)c1 10.1016/j.bmcl.2016.06.014
CHEMBL4438411 169830 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta cell membranes
ChEMBL 580 12 3 8 5.6 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(SC)cc3)cc(C(=O)Nc3ccccc3)cc2OCCO)c1 10.1016/j.bmcl.2016.06.014
9917072 62123 None 0 Human Binding pIC50 = 7.8 7.8 - 2
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 619 16 2 10 4.6 CCCS(=O)(=O)NCCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
CHEMBL177538 62123 None 0 Human Binding pIC50 = 7.8 7.8 - 2
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 619 16 2 10 4.6 CCCS(=O)(=O)NCCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
44304492 96613 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
Inhibitory concentration was evaluated by measuring the binding affinity at the Endothelin B receptor in rat cerebellar membranesInhibitory concentration was evaluated by measuring the binding affinity at the Endothelin B receptor in rat cerebellar membranes
ChEMBL 949 23 9 8 4.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm970161m
CHEMBL262993 96613 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
Inhibitory concentration was evaluated by measuring the binding affinity at the Endothelin B receptor in rat cerebellar membranesInhibitory concentration was evaluated by measuring the binding affinity at the Endothelin B receptor in rat cerebellar membranes
ChEMBL 949 23 9 8 4.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm970161m
44284287 161341 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 532 10 3 7 5.2 CCC(CO)Cc1cc(OC)ccc1[C@@H]1c2nc(NC(C)C)ccc2[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O 10.1016/j.bmcl.2004.01.008
CHEMBL411925 161341 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 532 10 3 7 5.2 CCC(CO)Cc1cc(OC)ccc1[C@@H]1c2nc(NC(C)C)ccc2[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O 10.1016/j.bmcl.2004.01.008
CHEMBL94983 218406 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCN)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
10983045 205364 None 0 Pig Binding pIC50 = 6.8 6.8 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 440 9 1 6 5.3 CCCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL62762 205364 None 0 Pig Binding pIC50 = 6.8 6.8 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 440 9 1 6 5.3 CCCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
11144344 205470 None 0 Pig Binding pIC50 = 6.8 6.8 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 424 8 1 5 5.8 CCCCCC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL63267 205470 None 0 Pig Binding pIC50 = 6.8 6.8 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 424 8 1 5 5.8 CCCCCC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
104865 706 None 60 Human Binding pIC50 = 6.8 6.8 -6 4
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta cell membranes
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.bmcl.2016.06.014
104865.0 706 None 60 Human Binding pIC50 = 6.8 6.8 -6 4
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta cell membranes
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.bmcl.2016.06.014
3494 706 None 60 Human Binding pIC50 = 6.8 6.8 -6 4
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta cell membranes
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.bmcl.2016.06.014
392 706 None 60 Human Binding pIC50 = 6.8 6.8 -6 4
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta cell membranes
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.bmcl.2016.06.014
CHEMBL957 706 None 60 Human Binding pIC50 = 6.8 6.8 -6 4
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta cell membranes
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.bmcl.2016.06.014
DB00559 706 None 60 Human Binding pIC50 = 6.8 6.8 -6 4
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta cell membranes
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.bmcl.2016.06.014
CHEMBL89736 218391 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)CC 10.1021/jm00070a001
CHEMBL328942 213775 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Inhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar membranesInhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar membranes
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00095a029
104865 706 None 60 Human Binding pIC50 = 6.8 6.8 -6 4
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/S0960-894X(97)00400-9
104865.0 706 None 60 Human Binding pIC50 = 6.8 6.8 -6 4
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/S0960-894X(97)00400-9
3494 706 None 60 Human Binding pIC50 = 6.8 6.8 -6 4
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/S0960-894X(97)00400-9
392 706 None 60 Human Binding pIC50 = 6.8 6.8 -6 4
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/S0960-894X(97)00400-9
CHEMBL957 706 None 60 Human Binding pIC50 = 6.8 6.8 -6 4
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/S0960-894X(97)00400-9
DB00559 706 None 60 Human Binding pIC50 = 6.8 6.8 -6 4
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/S0960-894X(97)00400-9
10671649 98619 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 460 5 1 8 3.6 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc3c(c2)OCO3)cc1 10.1021/jm9606507
CHEMBL276639 98619 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 460 5 1 8 3.6 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc3c(c2)OCO3)cc1 10.1021/jm9606507
10961546 96812 None 0 Pig Binding pIC50 = 5.8 5.8 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 460 6 1 6 5.2 COc1ccc(C2=C(C(=O)O)[C@H](c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
CHEMBL264543 96812 None 0 Pig Binding pIC50 = 5.8 5.8 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 460 6 1 6 5.2 COc1ccc(C2=C(C(=O)O)[C@H](c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
18738881 79614 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
ChEMBL 534 7 2 7 4.4 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(C(=O)O)ccc23)cc1 10.1016/s0960-894x(01)00660-6
CHEMBL2114305 79614 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
ChEMBL 534 7 2 7 4.4 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(C(=O)O)ccc23)cc1 10.1016/s0960-894x(01)00660-6
19363918 14642 None 0 Pig Binding pIC50 = 5.8 5.8 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 474 7 1 8 4.4 COc1ccc(C(=O)/C(Cc2ccc3c(c2)OCO3)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL1205106 14642 None 0 Pig Binding pIC50 = 5.8 5.8 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 474 7 1 8 4.4 COc1ccc(C(=O)/C(Cc2ccc3c(c2)OCO3)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL52535 14642 None 0 Pig Binding pIC50 = 5.8 5.8 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 474 7 1 8 4.4 COc1ccc(C(=O)/C(Cc2ccc3c(c2)OCO3)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL1793934 211391 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibition of binding to Endothelin B receptor of rat cerebellar membranes.Inhibition of binding to Endothelin B receptor of rat cerebellar membranes.
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)N(C)C(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)[C@@H](C)CC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm970161m
18995988 100391 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 389 6 1 4 5.5 COc1cccc(Sc2c(C(=O)O)n(Cc3ccccc3)c3ccccc23)c1 10.1016/0960-894X(96)00232-6
CHEMBL28948 100391 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 389 6 1 4 5.5 COc1cccc(Sc2c(C(=O)O)n(Cc3ccccc3)c3ccccc23)c1 10.1016/0960-894X(96)00232-6
44317215 207721 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 266 3 1 4 2.4 Cc1ccc(S(=O)(=O)Nc2onc(C)c2C)cc1 10.1016/0960-894X(96)00441-6
CHEMBL78952 207721 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 266 3 1 4 2.4 Cc1ccc(S(=O)(=O)Nc2onc(C)c2C)cc1 10.1016/0960-894X(96)00441-6
18617377 207932 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 344 3 1 4 3.2 Cc1ccc(C)c(S(=O)(=O)Nc2onc(C)c2Br)c1 10.1016/0960-894X(96)00441-6
CHEMBL80484 207932 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 344 3 1 4 3.2 Cc1ccc(C)c(S(=O)(=O)Nc2onc(C)c2Br)c1 10.1016/0960-894X(96)00441-6
10665805 98231 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 354 4 1 6 3.0 CCC1=C(c2ccc3c(c2)OCO3)C(=O)OC1(O)c1ccc(OC)cc1 10.1021/jm9606507
CHEMBL273951 98231 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 354 4 1 6 3.0 CCC1=C(c2ccc3c(c2)OCO3)C(=O)OC1(O)c1ccc(OC)cc1 10.1021/jm9606507
CHEMBL413880 215554 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Binding affinity in Chinese hamster ovary (CHO) cells stably transfected with human endothelin B (ETB) receptorBinding affinity in Chinese hamster ovary (CHO) cells stably transfected with human endothelin B (ETB) receptor
ChEMBL None None None NC(=O)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)N[C@H](Cc1c[nH]c2ccccc12)C(=O)O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(95)00084-7
10882352 205441 None 0 Pig Binding pIC50 = 4.8 4.8 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 340 4 1 5 3.4 CCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccccc21 10.1021/jm010382z
CHEMBL63099 205441 None 0 Pig Binding pIC50 = 4.8 4.8 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 340 4 1 5 3.4 CCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccccc21 10.1021/jm010382z
44276577 106913 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 459 7 1 7 4.1 COc1cccc(Cn2[nH]c(-c3ccc([N+](=O)[O-])cc3)c(Cc3ccc4c(c3)OCO4)c2=O)c1 10.1016/s0960-894x(00)00232-8
CHEMBL3144850 106913 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 459 7 1 7 4.1 COc1cccc(Cn2[nH]c(-c3ccc([N+](=O)[O-])cc3)c(Cc3ccc4c(c3)OCO4)c2=O)c1 10.1016/s0960-894x(00)00232-8
44266592 5377 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 431 4 1 7 4.5 COc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2-c1ccc2c(c1)OCO2 10.1016/0960-894X(96)00170-9
CHEMBL10699 5377 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 431 4 1 7 4.5 COc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2-c1ccc2c(c1)OCO2 10.1016/0960-894X(96)00170-9
71458718 81705 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 615 14 1 12 4.3 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(C)cn1 10.1021/jm3009103
CHEMBL2163700 81705 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 615 14 1 12 4.3 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(C)cn1 10.1021/jm3009103
23445250 168209 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 468 6 1 5 5.8 Cc1cc(CC(C)C)ccc1-c1ccsc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/S0960-894X(96)00496-9
CHEMBL432815 168209 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 468 6 1 5 5.8 Cc1cc(CC(C)C)ccc1-c1ccsc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/S0960-894X(96)00496-9
10302118 60444 None 0 Human Binding pIC50 = 5.8 5.8 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 533 9 2 10 3.2 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2ccncc2)nc1OCC#CCO 10.1016/s0960-894x(02)01084-3
CHEMBL175111 60444 None 0 Human Binding pIC50 = 5.8 5.8 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 533 9 2 10 3.2 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2ccncc2)nc1OCC#CCO 10.1016/s0960-894x(02)01084-3
18184249 128539 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 662 13 2 11 4.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2ccncc2)nc1OCCNS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(02)01083-1
CHEMBL366628 128539 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 662 13 2 11 4.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2ccncc2)nc1OCCNS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(02)01083-1
10528383 11239 None 0 Human Binding pIC50 = 4.8 4.8 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 470 5 1 8 3.6 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)c2ccc3c(c2)OCO3)c1Br 10.1021/jm9700068
CHEMBL1178854 11239 None 0 Human Binding pIC50 = 4.8 4.8 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 470 5 1 8 3.6 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)c2ccc3c(c2)OCO3)c1Br 10.1021/jm9700068
CHEMBL46357 11239 None 0 Human Binding pIC50 = 4.8 4.8 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 470 5 1 8 3.6 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)c2ccc3c(c2)OCO3)c1Br 10.1021/jm9700068
9915028 9413 None 19 Human Binding pIC50 = 4.8 4.8 -28183 3
Inhibition of [125I]-endothelin-3 binding to EDNRBInhibition of [125I]-endothelin-3 binding to EDNRB
ChEMBL 532 15 1 6 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC 10.6019/CHEMBL4507258
CHEMBL111612 9413 None 19 Human Binding pIC50 = 4.8 4.8 -28183 3
Inhibition of [125I]-endothelin-3 binding to EDNRBInhibition of [125I]-endothelin-3 binding to EDNRB
ChEMBL 532 15 1 6 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC 10.6019/CHEMBL4507258
CHEMBL4761843 9413 None 19 Human Binding pIC50 = 4.8 4.8 -28183 3
Inhibition of [125I]-endothelin-3 binding to EDNRBInhibition of [125I]-endothelin-3 binding to EDNRB
ChEMBL 532 15 1 6 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC 10.6019/CHEMBL4507258
9915028 9413 None 19 Human Binding pIC50 = 4.8 4.8 -28183 3
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)
ChEMBL 532 15 1 6 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC 10.1021/jm980217s
CHEMBL111612 9413 None 19 Human Binding pIC50 = 4.8 4.8 -28183 3
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)
ChEMBL 532 15 1 6 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC 10.1021/jm980217s
CHEMBL4761843 9413 None 19 Human Binding pIC50 = 4.8 4.8 -28183 3
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)
ChEMBL 532 15 1 6 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC 10.1021/jm980217s
9955200 9334 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 446 6 1 7 3.8 COc1ccc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc1 10.1021/jm9606507
CHEMBL11115 9334 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 446 6 1 7 3.8 COc1ccc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc1 10.1021/jm9606507
24997097 18480 None 3 Human Binding pIC50 = 4.8 4.8 - 0
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
ChEMBL 501 7 3 7 4.0 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(O)ccc31)OCO2 10.1016/j.bmcl.2010.08.074
CHEMBL1272137 18480 None 3 Human Binding pIC50 = 4.8 4.8 - 0
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
ChEMBL 501 7 3 7 4.0 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(O)ccc31)OCO2 10.1016/j.bmcl.2010.08.074
23445507 59780 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B receptor
ChEMBL 442 6 1 6 4.5 Cc1ccc(OCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(97)00132-7
CHEMBL172538 59780 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B receptor
ChEMBL 442 6 1 6 4.5 Cc1ccc(OCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(97)00132-7
24997097 18480 None 3 Human Binding pIC50 = 4.8 4.8 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 501 7 3 7 4.0 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(O)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL1272137 18480 None 3 Human Binding pIC50 = 4.8 4.8 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 501 7 3 7 4.0 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(O)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
11797486 12047 None 1 Human Binding pIC50 = 4.8 4.8 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 442 6 2 8 3.5 Cc1noc(NS(=O)(=O)c2ccsc2C(O)Cc2ccc3c(c2)OCO3)c1Cl 10.1021/jm9700068
CHEMBL1183448 12047 None 1 Human Binding pIC50 = 4.8 4.8 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 442 6 2 8 3.5 Cc1noc(NS(=O)(=O)c2ccsc2C(O)Cc2ccc3c(c2)OCO3)c1Cl 10.1021/jm9700068
CHEMBL297557 12047 None 1 Human Binding pIC50 = 4.8 4.8 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 442 6 2 8 3.5 Cc1noc(NS(=O)(=O)c2ccsc2C(O)Cc2ccc3c(c2)OCO3)c1Cl 10.1021/jm9700068
10671037 131512 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cells
ChEMBL 446 8 1 6 4.4 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1 10.1021/jm9606507
CHEMBL273660 131512 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cells
ChEMBL 446 8 1 6 4.4 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1 10.1021/jm9606507
CHEMBL369085 131512 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cells
ChEMBL 446 8 1 6 4.4 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1 10.1021/jm9606507
21041264 82042 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 600 12 2 8 4.0 CCCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1 10.1021/jm3009103
CHEMBL2165339 82042 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 600 12 2 8 4.0 CCCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1 10.1021/jm3009103
10554539 101297 None 0 Human Binding pIC50 = 4.8 4.8 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 543 9 2 11 3.4 CC(=O)OCCOc1cc2c(cc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl)OCO2 10.1021/jm9608366
CHEMBL296129 101297 None 0 Human Binding pIC50 = 4.8 4.8 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 543 9 2 11 3.4 CC(=O)OCCOc1cc2c(cc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl)OCO2 10.1021/jm9608366
10743872 97260 None 0 Pig Binding pIC50 = 5.8 5.8 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 496 13 1 6 5.2 CCCCN(CCCC)CCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL268432 97260 None 0 Pig Binding pIC50 = 5.8 5.8 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 496 13 1 6 5.2 CCCCN(CCCC)CCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL319719 213680 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
10625270 113438 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 502 7 2 6 4.5 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(C)cccc2C)cc1 10.1021/jm990170q
CHEMBL331767 113438 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 502 7 2 6 4.5 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(C)cccc2C)cc1 10.1021/jm990170q
177236 1325 None 32 Human Binding pIC50 = 7.8 7.8 -134 3
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
ChEMBL 410 9 1 7 2.9 COC([C@@H](C(=O)O)Oc1nc(OC)cc(n1)OC)(c1ccccc1)c1ccccc1 10.1016/s0960-894x(01)00660-6
3508 1325 None 32 Human Binding pIC50 = 7.8 7.8 -134 3
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
ChEMBL 410 9 1 7 2.9 COC([C@@H](C(=O)O)Oc1nc(OC)cc(n1)OC)(c1ccccc1)c1ccccc1 10.1016/s0960-894x(01)00660-6
CHEMBL23261 1325 None 32 Human Binding pIC50 = 7.8 7.8 -134 3
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
ChEMBL 410 9 1 7 2.9 COC([C@@H](C(=O)O)Oc1nc(OC)cc(n1)OC)(c1ccccc1)c1ccccc1 10.1016/s0960-894x(01)00660-6
DB04883 1325 None 32 Human Binding pIC50 = 7.8 7.8 -134 3
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
ChEMBL 410 9 1 7 2.9 COC([C@@H](C(=O)O)Oc1nc(OC)cc(n1)OC)(c1ccccc1)c1ccccc1 10.1016/s0960-894x(01)00660-6
9853077 59646 None 0 Human Binding pIC50 = 7.8 7.8 - 2
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 696 13 2 12 5.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
CHEMBL172030 59646 None 0 Human Binding pIC50 = 7.8 7.8 - 2
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 696 13 2 12 5.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
10950843 205410 None 0 Pig Binding pIC50 = 6.8 6.8 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 474 8 1 6 5.6 CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1cccc(OC)c1)O2 10.1021/jm010382z
CHEMBL62951 205410 None 0 Pig Binding pIC50 = 6.8 6.8 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 474 8 1 6 5.6 CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1cccc(OC)c1)O2 10.1021/jm010382z
10152810 14792 None 2 Pig Binding pIC50 = 6.8 6.8 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 538 10 1 9 4.8 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1F 10.1016/s0960-894x(98)00301-1
CHEMBL1206706 14792 None 2 Pig Binding pIC50 = 6.8 6.8 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 538 10 1 9 4.8 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1F 10.1016/s0960-894x(98)00301-1
CHEMBL298725 14792 None 2 Pig Binding pIC50 = 6.8 6.8 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 538 10 1 9 4.8 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1F 10.1016/s0960-894x(98)00301-1
44311284 206703 None 0 Human Binding pIC50 = 6.8 6.8 - 1
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 635 12 2 10 6.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C(C)C)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
CHEMBL71070 206703 None 0 Human Binding pIC50 = 6.8 6.8 - 1
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 635 12 2 10 6.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C(C)C)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
44371532 51490 None 1 Human Binding pIC50 = 5.8 5.8 - 0
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 455 6 1 6 5.2 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3cccc(OC)c3)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(99)00040-2
CHEMBL158239 51490 None 1 Human Binding pIC50 = 5.8 5.8 - 0
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 455 6 1 6 5.2 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3cccc(OC)c3)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(99)00040-2
44278161 99858 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 569 10 1 8 6.9 COc1cccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc(OCc4ccccc4)c(OC)cc23)c1 10.1016/0960-894X(96)00232-6
CHEMBL285380 99858 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 569 10 1 8 6.9 COc1cccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc(OCc4ccccc4)c(OC)cc23)c1 10.1016/0960-894X(96)00232-6
CHEMBL2370247 212272 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](C(c2ccccc2)c2ccccc2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]([C@@H](C)CC)NC1=O 10.1021/jm00015a003
10790686 5252 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 474 5 1 8 3.6 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc3c(c2)OCCO3)cc1 10.1021/jm9606507
CHEMBL10635 5252 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 474 5 1 8 3.6 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc3c(c2)OCCO3)cc1 10.1021/jm9606507
10552007 6325 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 462 8 1 7 4.1 COc1ccc(C2(O)OC(=O)C(c3cc(OC)c(OC)c(OC)c3)=C2Cc2ccccc2)cc1 10.1021/jm9606507
CHEMBL10819 6325 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 462 8 1 7 4.1 COc1ccc(C2(O)OC(=O)C(c3cc(OC)c(OC)c(OC)c3)=C2Cc2ccccc2)cc1 10.1021/jm9606507
11058717 205274 None 0 Pig Binding pIC50 = 5.8 5.8 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 412 8 1 6 4.6 CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OCC)cc21 10.1021/jm010382z
CHEMBL62348 205274 None 0 Pig Binding pIC50 = 5.8 5.8 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 412 8 1 6 4.6 CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OCC)cc21 10.1021/jm010382z
10951244 205411 None 0 Pig Binding pIC50 = 5.8 5.8 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 504 9 1 7 5.6 CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1cc(OC)ccc1OC)O2 10.1021/jm010382z
CHEMBL62962 205411 None 0 Pig Binding pIC50 = 5.8 5.8 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 504 9 1 7 5.6 CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1cc(OC)ccc1OC)O2 10.1021/jm010382z
44294580 14641 None 0 Pig Binding pIC50 = 5.8 5.8 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 502 8 1 7 5.8 COc1ccc(C(=O)/C(Cc2ccc(OC(C)(C)C)cc2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL1205104 14641 None 0 Pig Binding pIC50 = 5.8 5.8 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 502 8 1 7 5.8 COc1ccc(C(=O)/C(Cc2ccc(OC(C)(C)C)cc2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL52338 14641 None 0 Pig Binding pIC50 = 5.8 5.8 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 502 8 1 7 5.8 COc1ccc(C(=O)/C(Cc2ccc(OC(C)(C)C)cc2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
44266552 4515 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptor
ChEMBL 473 7 1 7 5.3 CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2c(c1)OCO2 10.1016/s0960-894x(97)10151-2
CHEMBL10218 4515 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptor
ChEMBL 473 7 1 7 5.3 CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2c(c1)OCO2 10.1016/s0960-894x(97)10151-2
44310016 206297 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptor
ChEMBL 489 6 1 9 4.8 COc1cc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4nsnc4c3)c2cc1OC 10.1016/s0960-894x(97)10151-2
CHEMBL68557 206297 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptor
ChEMBL 489 6 1 9 4.8 COc1cc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4nsnc4c3)c2cc1OC 10.1016/s0960-894x(97)10151-2
10195727 206385 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptor
ChEMBL 487 7 1 8 5.6 CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2nsnc2c1 10.1016/s0960-894x(97)10151-2
CHEMBL69150 206385 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptor
ChEMBL 487 7 1 8 5.6 CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2nsnc2c1 10.1016/s0960-894x(97)10151-2
9809526 14865 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.
ChEMBL 614 12 2 11 3.5 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCCS(=O)(=O)O)c2)cc1 10.1021/jm980504w
CHEMBL1207463 14865 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.
ChEMBL 614 12 2 11 3.5 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCCS(=O)(=O)O)c2)cc1 10.1021/jm980504w
CHEMBL408055 14865 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.
ChEMBL 614 12 2 11 3.5 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCCS(=O)(=O)O)c2)cc1 10.1021/jm980504w
19010508 56361 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) receptor expressed in CHO cells
ChEMBL 501 9 1 7 5.5 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)ccc1OC(C(=O)O)c1ccc2c(c1)OCO2 10.1016/0960-894X(95)00186-W
CHEMBL16306 56361 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) receptor expressed in CHO cells
ChEMBL 501 9 1 7 5.5 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)ccc1OC(C(=O)O)c1ccc2c(c1)OCO2 10.1016/0960-894X(95)00186-W
22616262 207997 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Binding affinity against human ETB receptor in transfected COS 7 cell membrane preparationBinding affinity against human ETB receptor in transfected COS 7 cell membrane preparation
ChEMBL 366 3 1 4 3.7 Cc1noc(NS(=O)(=O)c2cccc3ccccc23)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL80980 207997 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Binding affinity against human ETB receptor in transfected COS 7 cell membrane preparationBinding affinity against human ETB receptor in transfected COS 7 cell membrane preparation
ChEMBL 366 3 1 4 3.7 Cc1noc(NS(=O)(=O)c2cccc3ccccc23)c1Br 10.1016/0960-894X(96)00441-6
10505209 9319 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 490 6 1 9 3.6 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c3c(c2)OCO3)cc1 10.1021/jm9606507
CHEMBL11106 9319 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 490 6 1 9 3.6 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c3c(c2)OCO3)cc1 10.1021/jm9606507
10767210 111378 None 0 Pig Binding pIC50 = 4.8 4.8 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 484 12 1 4 5.1 CCCCN(CCCC)C(=O)CN1C[C@H](c2cccc(F)c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL326719 111378 None 0 Pig Binding pIC50 = 4.8 4.8 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 484 12 1 4 5.1 CCCCN(CCCC)C(=O)CN1C[C@H](c2cccc(F)c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
10813007 113383 None 0 Pig Binding pIC50 = 4.8 4.8 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 440 9 1 5 3.4 CCCN(C)C(=O)CN1C[C@H](c2ccc(OC)cc2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL331577 113383 None 0 Pig Binding pIC50 = 4.8 4.8 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 440 9 1 5 3.4 CCCN(C)C(=O)CN1C[C@H](c2ccc(OC)cc2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
137655525 159083 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 525 7 3 9 3.5 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(-c4nnn[nH]4)c3)c(=O)c3cc(O)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL4096346 159083 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 525 7 3 9 3.5 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(-c4nnn[nH]4)c3)c(=O)c3cc(O)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
71462247 81729 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 680 14 2 12 4.2 COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)nc(-c2cnccn2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
CHEMBL2163723 81729 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 680 14 2 12 4.2 COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)nc(-c2cnccn2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
71455063 81726 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 646 15 2 12 3.8 CCCCNS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC 10.1021/jm3009103
CHEMBL2163720 81726 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 646 15 2 12 3.8 CCCCNS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC 10.1021/jm3009103
10304227 130076 None 0 Human Binding pIC50 = 5.8 5.8 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 603 10 2 13 4.2 C#CCOc1nc(-c2ccnc(-c3noc(S)n3)c2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL367686 130076 None 0 Human Binding pIC50 = 5.8 5.8 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 603 10 2 13 4.2 C#CCOc1nc(-c2ccnc(-c3noc(S)n3)c2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
9915028 9413 None 19 Human Binding pIC50 = 4.8 4.8 -28183 3
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 532 15 1 6 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC 10.1021/jm980217s
CHEMBL111612 9413 None 19 Human Binding pIC50 = 4.8 4.8 -28183 3
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 532 15 1 6 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC 10.1021/jm980217s
CHEMBL4761843 9413 None 19 Human Binding pIC50 = 4.8 4.8 -28183 3
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 532 15 1 6 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC 10.1021/jm980217s
10744041 97355 None 0 Pig Binding pIC50 = 5.8 5.8 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 502 8 1 6 3.9 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(C)Cc2ccccc2)cc1 10.1021/jm9505369
CHEMBL269108 97355 None 0 Pig Binding pIC50 = 5.8 5.8 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 502 8 1 6 3.9 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(C)Cc2ccccc2)cc1 10.1021/jm9505369
10140965 101226 None 0 Human Binding pIC50 = 4.8 4.8 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 485 7 3 9 3.0 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2CCO)OCO3)c1Cl 10.1021/jm9608366
CHEMBL295588 101226 None 0 Human Binding pIC50 = 4.8 4.8 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 485 7 3 9 3.0 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2CCO)OCO3)c1Cl 10.1021/jm9608366
44371357 119803 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 515 8 1 8 5.2 COc1ccccc1Cn1c(=O)c(C(=O)O)c(-c2cc(OC)c(OC)c(OC)c2)c2oc3ccccc3c21 10.1016/s0960-894x(99)00040-2
CHEMBL347680 119803 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 515 8 1 8 5.2 COc1ccccc1Cn1c(=O)c(C(=O)O)c(-c2cc(OC)c(OC)c(OC)c2)c2oc3ccccc3c21 10.1016/s0960-894x(99)00040-2
18995992 99892 None 0 Human Binding pIC50 = 6.8 6.8 - 1
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 507 7 1 9 5.0 COc1ccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc4c(cc23)OCO4)cc1OC 10.1016/0960-894X(96)00232-6
CHEMBL28563 99892 None 0 Human Binding pIC50 = 6.8 6.8 - 1
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 507 7 1 9 5.0 COc1ccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc4c(cc23)OCO4)cc1OC 10.1016/0960-894X(96)00232-6
10994373 162549 None 0 Pig Binding pIC50 = 6.8 6.8 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 474 5 1 7 5.0 CC(C)Oc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
CHEMBL416675 162549 None 0 Pig Binding pIC50 = 6.8 6.8 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 474 5 1 7 5.0 CC(C)Oc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
11102844 205699 None 0 Pig Binding pIC50 = 6.8 6.8 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 476 7 2 7 4.2 COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)CO)cc32)cc1 10.1021/jm010382z
CHEMBL64536 205699 None 0 Pig Binding pIC50 = 6.8 6.8 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 476 7 2 7 4.2 COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)CO)cc32)cc1 10.1021/jm010382z
44314581 104933 None 0 Pig Binding pIC50 = 6.8 6.8 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 591 11 6 5 2.8 Cc1[nH]c2ccccc2c1C[C@@H](NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)NC(Cc1c[nH]cn1)C(=O)O 10.1021/jm9600914
CHEMBL311134 104933 None 0 Pig Binding pIC50 = 6.8 6.8 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 591 11 6 5 2.8 Cc1[nH]c2ccccc2c1C[C@@H](NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)NC(Cc1c[nH]cn1)C(=O)O 10.1021/jm9600914
CHEMBL2304014 211929 None 0 Pig Binding pIC50 = 6.8 6.8 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc2c(C#N)[nH]c3ccccc23)NC(=O)[C@@H](C(C)C)NC1=O 10.1021/jm9600914
44311233 206567 None 0 Human Binding pIC50 = 6.8 6.8 - 1
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 630 12 2 13 4.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2ncccn2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
CHEMBL70303 206567 None 0 Human Binding pIC50 = 6.8 6.8 - 1
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 630 12 2 13 4.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2ncccn2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
CHEMBL408141 215163 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Binding affinity against Endothelin B receptor in rat cerebellar membrane (ET-B) from adult blue laurie ratBinding affinity against Endothelin B receptor in rat cerebellar membrane (ET-B) from adult blue laurie rat
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)80156-6
CHEMBL436884 216151 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Binding affinity against Endothelin B receptor in rat cerebellar membrane (ET-B) from adult blue laurie ratBinding affinity against Endothelin B receptor in rat cerebellar membrane (ET-B) from adult blue laurie rat
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)80156-6
44327726 210351 None 0 Pig Binding pIC50 = 5.8 5.8 - 0
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranes
ChEMBL 495 6 1 8 2.7 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)n2nc3c(cc2=O)CCC3)cc1 10.1016/S0960-894X(96)00617-8
CHEMBL96644 210351 None 0 Pig Binding pIC50 = 5.8 5.8 - 0
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranes
ChEMBL 495 6 1 8 2.7 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)n2nc3c(cc2=O)CCC3)cc1 10.1016/S0960-894X(96)00617-8
18617393 207735 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 308 5 1 4 3.2 CCc1ccc(CC)c(S(=O)(=O)Nc2onc(C)c2C)c1 10.1016/0960-894X(96)00441-6
CHEMBL79066 207735 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 308 5 1 4 3.2 CCc1ccc(CC)c(S(=O)(=O)Nc2onc(C)c2C)c1 10.1016/0960-894X(96)00441-6
10623877 8490 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 461 6 1 8 3.7 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc([N+](=O)[O-])cc2)cc1 10.1021/jm9606507
CHEMBL10940 8490 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 461 6 1 8 3.7 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc([N+](=O)[O-])cc2)cc1 10.1021/jm9606507
10649122 9741 None 0 Pig Binding pIC50 = 4.8 4.8 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 502 12 1 4 5.2 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc(F)c(F)c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL113400 9741 None 0 Pig Binding pIC50 = 4.8 4.8 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 502 12 1 4 5.2 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc(F)c(F)c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
15340616 106890 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 420 4 1 6 3.3 O=c1c(Cc2ccc3c(c2)OCO3)c(C(F)(F)F)[nH]n1Cc1ccc2c(c1)OCO2 10.1016/s0960-894x(00)00232-8
CHEMBL3144602 106890 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 420 4 1 6 3.3 O=c1c(Cc2ccc3c(c2)OCO3)c(C(F)(F)F)[nH]n1Cc1ccc2c(c1)OCO2 10.1016/s0960-894x(00)00232-8
10344511 59703 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 466 5 1 5 5.7 Cc1cc(C)c(/C=C/c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00133-9
CHEMBL172248 59703 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 466 5 1 5 5.7 Cc1cc(C)c(/C=C/c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00133-9
10525281 182956 None 0 Human Binding pIC50 = 4.8 4.8 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 404 6 1 6 4.2 Cc1ccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2C)c(C)c1 10.1021/jm9700068
CHEMBL47915 182956 None 0 Human Binding pIC50 = 4.8 4.8 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 404 6 1 6 4.2 Cc1ccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2C)c(C)c1 10.1021/jm9700068
12286 948 None 29 Human Binding pIC50 = 6.8 6.8 -1348 2
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta cell membranes
ChEMBL 577 11 3 13 2.4 Cc1cnc(cc1)S(=O)(=O)Nc1c(c(nc(n1)c1cc(ncc1)c1n[nH]nn1)OCCO)Oc1ccccc1OC 10.1016/j.bmcl.2016.06.014
6433095 948 None 29 Human Binding pIC50 = 6.8 6.8 -1348 2
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta cell membranes
ChEMBL 577 11 3 13 2.4 Cc1cnc(cc1)S(=O)(=O)Nc1c(c(nc(n1)c1cc(ncc1)c1n[nH]nn1)OCCO)Oc1ccccc1OC 10.1016/j.bmcl.2016.06.014
6433095.0 948 None 29 Human Binding pIC50 = 6.8 6.8 -1348 2
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta cell membranes
ChEMBL 577 11 3 13 2.4 Cc1cnc(cc1)S(=O)(=O)Nc1c(c(nc(n1)c1cc(ncc1)c1n[nH]nn1)OCCO)Oc1ccccc1OC 10.1016/j.bmcl.2016.06.014
CHEMBL109648 948 None 29 Human Binding pIC50 = 6.8 6.8 -1348 2
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta cell membranes
ChEMBL 577 11 3 13 2.4 Cc1cnc(cc1)S(=O)(=O)Nc1c(c(nc(n1)c1cc(ncc1)c1n[nH]nn1)OCCO)Oc1ccccc1OC 10.1016/j.bmcl.2016.06.014
DB06677 948 None 29 Human Binding pIC50 = 6.8 6.8 -1348 2
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta cell membranes
ChEMBL 577 11 3 13 2.4 Cc1cnc(cc1)S(=O)(=O)Nc1c(c(nc(n1)c1cc(ncc1)c1n[nH]nn1)OCCO)Oc1ccccc1OC 10.1016/j.bmcl.2016.06.014
10342643 5159 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 430 5 1 6 4.1 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1C 10.1021/jm9606507
CHEMBL10588 5159 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 430 5 1 6 4.1 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1C 10.1021/jm9606507
71455061 81704 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 511 11 1 12 2.4 COc1ccccc1Oc1c(NS(C)(=O)=O)nc(-c2ncccn2)nc1OCCOc1ncccn1 10.1021/jm3009103
CHEMBL2163699 81704 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 511 11 1 12 2.4 COc1ccccc1Oc1c(NS(C)(=O)=O)nc(-c2ncccn2)nc1OCCOc1ncccn1 10.1021/jm3009103
5310990 166926 None 8 Pig Binding pIC50 = 5.8 5.8 - 2
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 510 12 1 6 4.7 CCCCN(CCCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL428504 166926 None 8 Pig Binding pIC50 = 5.8 5.8 - 2
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 510 12 1 6 4.7 CCCCN(CCCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
10741025 181787 None 0 Human Binding pIC50 = 4.8 4.8 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 424 6 1 6 4.5 Cc1cc(C)cc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c1 10.1021/jm9700068
CHEMBL47765 181787 None 0 Human Binding pIC50 = 4.8 4.8 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 424 6 1 6 4.5 Cc1cc(C)cc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c1 10.1021/jm9700068
44320782 107128 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 482 7 1 6 5.8 COc1ccc(-c2nn(CC3CCCCC3)c(C(=O)O)c2Cc2cc3c(cc2Cl)OCO3)cc1 10.1016/s0960-894x(00)00513-8
CHEMBL315788 107128 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 482 7 1 6 5.8 COc1ccc(-c2nn(CC3CCCCC3)c(C(=O)O)c2Cc2cc3c(cc2Cl)OCO3)cc1 10.1016/s0960-894x(00)00513-8
23445438 61519 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 470 6 1 7 4.1 Cc1noc(NS(=O)(=O)c2sccc2CCc2ccc3c(c2)OCO3)c1Br 10.1016/S0960-894X(97)00133-9
CHEMBL177070 61519 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 470 6 1 7 4.1 Cc1noc(NS(=O)(=O)c2sccc2CCc2ccc3c(c2)OCO3)c1Br 10.1016/S0960-894X(97)00133-9
10815726 11452 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 516 8 2 6 4.5 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(C)c2ccccc2C)cc1 10.1021/jm990171i
CHEMBL1180348 11452 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 516 8 2 6 4.5 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(C)c2ccccc2C)cc1 10.1021/jm990171i
CHEMBL123146 11452 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 516 8 2 6 4.5 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(C)c2ccccc2C)cc1 10.1021/jm990171i
10122442 130765 None 0 Human Binding pIC50 = 7.8 7.8 - 1
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 660 14 2 11 5.6 CCCCNC(=O)OCC#CCOc1nc(-c2ccncc2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL368383 130765 None 0 Human Binding pIC50 = 7.8 7.8 - 1
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 660 14 2 11 5.6 CCCCNC(=O)OCC#CCOc1nc(-c2ccncc2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
10602743 7159 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 550 9 1 10 4.2 COc1ccc(C2(O)OC(=O)C(c3cc(OC)c4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1C 10.1021/jm9606507
CHEMBL10854 7159 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 550 9 1 10 4.2 COc1ccc(C2(O)OC(=O)C(c3cc(OC)c4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1C 10.1021/jm9606507
9933950 205284 None 0 Pig Binding pIC50 = 6.8 6.8 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 460 6 1 6 5.2 COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
CHEMBL62395 205284 None 0 Pig Binding pIC50 = 6.8 6.8 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 460 6 1 6 5.2 COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
44295173 14639 None 0 Pig Binding pIC50 = 6.8 6.8 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 554 10 1 9 5.3 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1Cl 10.1016/s0960-894x(98)00301-1
CHEMBL1205090 14639 None 0 Pig Binding pIC50 = 6.8 6.8 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 554 10 1 9 5.3 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1Cl 10.1016/s0960-894x(98)00301-1
CHEMBL51234 14639 None 0 Pig Binding pIC50 = 6.8 6.8 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 554 10 1 9 5.3 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1Cl 10.1016/s0960-894x(98)00301-1
9868822 8593 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 459 6 1 7 3.9 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(N(C)C)cc2)cc1 10.1021/jm9606507
CHEMBL10948 8593 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 459 6 1 7 3.9 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(N(C)C)cc2)cc1 10.1021/jm9606507
9960931 108077 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity for human endothelin B receptor expressed in CHO-K1 cells.Binding affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 635 12 1 12 4.1 CCOC(=O)CNC(=O)OC1(c2ccc(OC)cc2)OC(=O)C(c2ccc3c(c2)OCO3)=C1Cc1cc(OC)c(OC)c(OC)c1 10.1016/S0960-894X(97)00002-4
CHEMBL319452 108077 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity for human endothelin B receptor expressed in CHO-K1 cells.Binding affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 635 12 1 12 4.1 CCOC(=O)CNC(=O)OC1(c2ccc(OC)cc2)OC(=O)C(c2ccc3c(c2)OCO3)=C1Cc1cc(OC)c(OC)c(OC)c1 10.1016/S0960-894X(97)00002-4
CHEMBL433349 216098 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity measured in CHO cells stably transfected with the human endothelin B receptorBinding affinity measured in CHO cells stably transfected with the human endothelin B receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
9868379 100837 None 0 Pig Binding pIC50 = 5.8 5.8 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 450 5 1 6 5.6 Cc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)s1 10.1021/jm010382z
CHEMBL293012 100837 None 0 Pig Binding pIC50 = 5.8 5.8 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 450 5 1 6 5.6 Cc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)s1 10.1021/jm010382z
11733232 205322 None 0 Pig Binding pIC50 = 5.8 5.8 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 460 7 1 6 5.2 CCCOc1cccc2c1C(c1ccc(OC)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
CHEMBL62586 205322 None 0 Pig Binding pIC50 = 5.8 5.8 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 460 7 1 6 5.2 CCCOc1cccc2c1C(c1ccc(OC)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
11826062 205447 None 0 Pig Binding pIC50 = 5.8 5.8 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 426 8 2 6 4.3 CC(C)Oc1ccc2c(c1)C(CCCCO)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
CHEMBL63113 205447 None 0 Pig Binding pIC50 = 5.8 5.8 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 426 8 2 6 4.3 CC(C)Oc1ccc2c(c1)C(CCCCO)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
9868379 100837 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 450 5 1 6 5.6 Cc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)s1 10.1016/j.bmcl.2016.06.014
CHEMBL293012 100837 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 450 5 1 6 5.6 Cc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)s1 10.1016/j.bmcl.2016.06.014
44295032 14796 None 0 Pig Binding pIC50 = 5.8 5.8 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 520 10 1 9 4.7 COc1cccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)c1 10.1016/s0960-894x(98)00301-1
CHEMBL1206717 14796 None 0 Pig Binding pIC50 = 5.8 5.8 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 520 10 1 9 4.7 COc1cccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)c1 10.1016/s0960-894x(98)00301-1
CHEMBL299572 14796 None 0 Pig Binding pIC50 = 5.8 5.8 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 520 10 1 9 4.7 COc1cccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)c1 10.1016/s0960-894x(98)00301-1
44294929 14800 None 0 Pig Binding pIC50 = 5.8 5.8 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 460 8 1 7 4.7 COc1ccc(C/C(C(=O)c2ccc(OC)cc2)=C(/C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL1206731 14800 None 0 Pig Binding pIC50 = 5.8 5.8 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 460 8 1 7 4.7 COc1ccc(C/C(C(=O)c2ccc(OC)cc2)=C(/C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL301971 14800 None 0 Pig Binding pIC50 = 5.8 5.8 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 460 8 1 7 4.7 COc1ccc(C/C(C(=O)c2ccc(OC)cc2)=C(/C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL317064 213656 None 12 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar membranesInhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar membranes
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00095a029
11798999 210044 None 0 Pig Binding pIC50 = 5.8 5.8 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 482 7 1 6 3.8 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(C)CC(C)(C)C)cc1 10.1021/jm9505369
CHEMBL9495 210044 None 0 Pig Binding pIC50 = 5.8 5.8 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 482 7 1 6 3.8 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(C)CC(C)(C)C)cc1 10.1021/jm9505369
CHEMBL303185 213376 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Binding activity against Endothelin B receptor 0f Porcine cerebellum membranesBinding activity against Endothelin B receptor 0f Porcine cerebellum membranes
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00089a028
10647021 6976 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 446 6 1 7 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1OC 10.1021/jm9606507
CHEMBL10846 6976 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 446 6 1 7 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1OC 10.1021/jm9606507
10740614 98361 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 416 5 1 6 3.8 COc1cccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)c1 10.1021/jm9606507
CHEMBL274857 98361 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 416 5 1 6 3.8 COc1cccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)c1 10.1021/jm9606507
CHEMBL303185 213376 None 0 Pig Binding pIC50 = 4.8 4.8 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm9600914
443289 711 None 39 Pig Binding pIC50 = 4.8 4.8 - 3
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranesInhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranes
ChEMBL None None None None 10.1016/0960-894X(95)00237-N
997 711 None 39 Pig Binding pIC50 = 4.8 4.8 - 3
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranesInhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranes
ChEMBL None None None None 10.1016/0960-894X(95)00237-N
CHEMBL314691 711 None 39 Pig Binding pIC50 = 4.8 4.8 - 3
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranesInhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranes
ChEMBL None None None None 10.1016/0960-894X(95)00237-N
DB12054 711 None 39 Pig Binding pIC50 = 4.8 4.8 - 3
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranesInhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranes
ChEMBL None None None None 10.1016/0960-894X(95)00237-N
CHEMBL336033 214033 None 0 Pig Binding pIC50 = 4.8 4.8 - 0
Inhibitory effect against porcine Endothelin B receptorInhibitory effect against porcine Endothelin B receptor
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
9806559 9152 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)
ChEMBL 515 13 1 6 3.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCN1CCCC1=O 10.1021/jm980217s
CHEMBL110053 9152 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)
ChEMBL 515 13 1 6 3.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCN1CCCC1=O 10.1021/jm980217s
10224228 179718 None 0 Human Binding pIC50 = 4.7 4.7 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 424 6 1 6 4.5 Cc1ccc(C)c(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c1 10.1021/jm9700068
CHEMBL47424 179718 None 0 Human Binding pIC50 = 4.7 4.7 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 424 6 1 6 4.5 Cc1ccc(C)c(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c1 10.1021/jm9700068
10601795 97025 None 0 Pig Binding pIC50 = 5.7 5.7 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 510 10 1 6 4.4 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(CC(C)C)CC(C)C)cc1 10.1021/jm9505369
CHEMBL266354 97025 None 0 Pig Binding pIC50 = 5.7 5.7 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 510 10 1 6 4.4 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(CC(C)C)CC(C)C)cc1 10.1021/jm9505369
73669994 117694 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]ET-1 from rat ETB receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETB receptor after 1 hr by Lowry method
ChEMBL 429 9 1 7 4.7 N#Cc1ccc(OCc2ccc3nonc3c2)cc1OC(CCC(=O)O)c1ccccc1 10.1016/j.bmc.2015.01.003
CHEMBL3400996 117694 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]ET-1 from rat ETB receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETB receptor after 1 hr by Lowry method
ChEMBL 429 9 1 7 4.7 N#Cc1ccc(OCc2ccc3nonc3c2)cc1OC(CCC(=O)O)c1ccccc1 10.1016/j.bmc.2015.01.003
10140871 59269 None 0 Human Binding pIC50 = 6.7 6.7 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 484 9 2 9 3.0 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)ncnc1OCC#CCO 10.1016/s0960-894x(02)01084-3
CHEMBL170342 59269 None 0 Human Binding pIC50 = 6.7 6.7 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 484 9 2 9 3.0 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)ncnc1OCC#CCO 10.1016/s0960-894x(02)01084-3
10224745 112753 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 432 5 2 6 2.4 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3ccccc32)n1 10.1016/j.bmcl.2016.06.014
CHEMBL330425 112753 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 432 5 2 6 2.4 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3ccccc32)n1 10.1016/j.bmcl.2016.06.014
10647373 97024 None 0 Pig Binding pIC50 = 6.7 6.7 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 454 8 2 6 3.0 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)NCC(C)C)cc1 10.1021/jm9505369
CHEMBL266337 97024 None 0 Pig Binding pIC50 = 6.7 6.7 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 454 8 2 6 3.0 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)NCC(C)C)cc1 10.1021/jm9505369
CHEMBL273391 213268 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Displacement of [125I]ET1 from Endothelin B receptor of rat cerebellumDisplacement of [125I]ET1 from Endothelin B receptor of rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)81215-4
CHEMBL273391 213268 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00070a001
44284238 100181 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 490 8 3 7 4.2 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CCO)c1 10.1016/j.bmcl.2004.01.008
CHEMBL287622 100181 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 490 8 3 7 4.2 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CCO)c1 10.1016/j.bmcl.2004.01.008
9874557 129806 None 0 Human Binding pIC50 = 7.7 7.7 - 2
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 667 15 2 10 5.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(C2CC2)nc1OCCCNS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(02)01083-1
CHEMBL367443 129806 None 0 Human Binding pIC50 = 7.7 7.7 - 2
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 667 15 2 10 5.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(C2CC2)nc1OCCCNS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(02)01083-1
44311516 206576 None 0 Human Binding pIC50 = 7.7 7.7 - 1
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 678 12 2 12 5.2 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
CHEMBL70339 206576 None 0 Human Binding pIC50 = 7.7 7.7 - 1
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 678 12 2 12 5.2 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
71453357 81713 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 707 12 1 12 5.8 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
CHEMBL2163708 81713 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 707 12 1 12 5.8 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
44328057 96947 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL 986 26 9 9 4.9 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)c1cccnc1)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL265734 96947 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL 986 26 9 9 4.9 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)c1cccnc1)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
11732966 205629 None 0 Pig Binding pIC50 = 6.7 6.7 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 444 5 1 5 5.6 COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(C(C)C)cc32)cc1 10.1021/jm010382z
CHEMBL64244 205629 None 0 Pig Binding pIC50 = 6.7 6.7 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 444 5 1 5 5.6 COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(C(C)C)cc32)cc1 10.1021/jm010382z
44279309 161911 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB receptor
ChEMBL 412 3 2 3 4.5 Cc1ccc(-c2ccc3c(c2)C(=O)c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@H]32)cc1 10.1016/0960-894X(95)00230-Q
CHEMBL414408 161911 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB receptor
ChEMBL 412 3 2 3 4.5 Cc1ccc(-c2ccc3c(c2)C(=O)c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@H]32)cc1 10.1016/0960-894X(95)00230-Q
44334097 110125 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B receptor
ChEMBL 447 7 2 6 3.7 COc1ccc([C@@H]2c3nc(CCCO)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1016/s0960-894x(02)00663-7
CHEMBL323561 110125 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B receptor
ChEMBL 447 7 2 6 3.7 COc1ccc([C@@H]2c3nc(CCCO)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1016/s0960-894x(02)00663-7
44371460 49544 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 469 5 1 7 4.9 COc1ccccc1Cn1c(=O)c(C(=O)O)c(-c2ccc3c(c2)OCO3)c2oc3ccccc3c21 10.1016/s0960-894x(99)00040-2
CHEMBL156539 49544 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 469 5 1 7 4.9 COc1ccccc1Cn1c(=O)c(C(=O)O)c(-c2ccc3c(c2)OCO3)c2oc3ccccc3c21 10.1016/s0960-894x(99)00040-2
CHEMBL319537 213678 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
10815005 9750 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 492 6 1 6 5.5 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(-c3ccccc3)cc2)cc1 10.1021/jm9606507
CHEMBL11345 9750 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 492 6 1 6 5.5 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(-c3ccccc3)cc2)cc1 10.1021/jm9606507
54587165 60329 None 0 Pig Binding pIC50 = 5.7 5.7 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 675 15 5 4 5.9 CCCCCC[C@@H](NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
CHEMBL1744023 60329 None 0 Pig Binding pIC50 = 5.7 5.7 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 675 15 5 4 5.9 CCCCCC[C@@H](NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
CHEMBL315047 213645 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00070a001
44295114 14886 None 0 Pig Binding pIC50 = 5.7 5.7 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 556 11 1 9 5.3 COc1cc(C/C(C(=O)c2ccc(OC(F)F)cc2)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC 10.1016/s0960-894x(98)00301-1
CHEMBL1207717 14886 None 0 Pig Binding pIC50 = 5.7 5.7 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 556 11 1 9 5.3 COc1cc(C/C(C(=O)c2ccc(OC(F)F)cc2)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC 10.1016/s0960-894x(98)00301-1
CHEMBL433090 14886 None 0 Pig Binding pIC50 = 5.7 5.7 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 556 11 1 9 5.3 COc1cc(C/C(C(=O)c2ccc(OC(F)F)cc2)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC 10.1016/s0960-894x(98)00301-1
10768294 14594 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cells
ChEMBL 520 10 1 8 4.7 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1C 10.1021/jm9606507
CHEMBL10922 14594 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cells
ChEMBL 520 10 1 8 4.7 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1C 10.1021/jm9606507
CHEMBL1204674 14594 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cells
ChEMBL 520 10 1 8 4.7 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1C 10.1021/jm9606507
19010490 53551 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) receptor expressed in CHO cells
ChEMBL 648 13 1 9 6.3 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)NS(=O)(=O)C(C)C)c1ccc2c(c1)OCO2 10.1016/0960-894X(95)00186-W
CHEMBL16018 53551 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) receptor expressed in CHO cells
ChEMBL 648 13 1 9 6.3 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)NS(=O)(=O)C(C)C)c1ccc2c(c1)OCO2 10.1016/0960-894X(95)00186-W
44368480 44622 None 0 Pig Binding pIC50 = 4.7 4.7 - 0
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 495 13 1 7 4.4 COc1ccc(CC(C(=O)O)N(Cc2ccc(OC)cc2)Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1016/s0960-894x(01)00009-9
CHEMBL152034 44622 None 0 Pig Binding pIC50 = 4.7 4.7 - 0
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 495 13 1 7 4.4 COc1ccc(CC(C(=O)O)N(Cc2ccc(OC)cc2)Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1016/s0960-894x(01)00009-9
10837347 8871 None 0 Pig Binding pIC50 = 4.7 4.7 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 452 8 1 5 3.3 CCCN(C)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL109736 8871 None 0 Pig Binding pIC50 = 4.7 4.7 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 452 8 1 5 3.3 CCCN(C)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
10841134 60468 None 0 Pig Binding pIC50 = 4.7 4.7 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 589 10 4 6 5.3 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC23CC4CC(CC(C4)C2)C3)nc1C(=O)O 10.1021/jm950592+
CHEMBL175277 60468 None 0 Pig Binding pIC50 = 4.7 4.7 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 589 10 4 6 5.3 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC23CC4CC(CC(C4)C2)C3)nc1C(=O)O 10.1021/jm950592+
CHEMBL414165 215575 None 0 Pig Binding pIC50 = 4.7 4.7 - 0
Inhibitory effect against porcine Endothelin B receptorInhibitory effect against porcine Endothelin B receptor
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](c2cccs2)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
159594 522 None 36 Pig Binding pIC50 = 6.7 6.7 - 3
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm9505369
159594.0 522 None 36 Pig Binding pIC50 = 6.7 6.7 - 3
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm9505369
3487 522 None 36 Pig Binding pIC50 = 6.7 6.7 - 3
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm9505369
CHEMBL9194 522 None 36 Pig Binding pIC50 = 6.7 6.7 - 3
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm9505369
DB06199 522 None 36 Pig Binding pIC50 = 6.7 6.7 - 3
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm9505369
44439111 97229 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]ET1 from human ETB receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETB receptor expressed in CHO cells
ChEMBL 979 31 2 15 7.0 CC(=O)CC(=O)CCc1ccc(NC(=O)CCOCCOCCOCCOCCOc2ccc(CC(=O)N(C)Cc3cc(-c4ncco4)ccc3-c3ccccc3S(=O)(=O)Nc3ccno3)cc2)cc1 10.1016/j.bmcl.2006.10.009
CHEMBL268201 97229 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]ET1 from human ETB receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETB receptor expressed in CHO cells
ChEMBL 979 31 2 15 7.0 CC(=O)CC(=O)CCc1ccc(NC(=O)CCOCCOCCOCCOCCOc2ccc(CC(=O)N(C)Cc3cc(-c4ncco4)ccc3-c3ccccc3S(=O)(=O)Nc3ccno3)cc2)cc1 10.1016/j.bmcl.2006.10.009
10622380 101510 None 0 Human Binding pIC50 = 4.7 4.7 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 426 7 1 7 3.9 COc1cccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c1 10.1021/jm9700068
CHEMBL297679 101510 None 0 Human Binding pIC50 = 4.7 4.7 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 426 7 1 7 3.9 COc1cccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c1 10.1021/jm9700068
21041372 81731 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 687 14 2 12 3.6 COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)nc(N2CCOCC2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
CHEMBL2163725 81731 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 687 14 2 12 3.6 COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)nc(N2CCOCC2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
71462246 81722 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 604 12 2 12 2.6 CNS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC 10.1021/jm3009103
CHEMBL2163717 81722 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 604 12 2 12 2.6 CNS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC 10.1021/jm3009103
3951 391 None 55 Human Binding pIC50 = 6.7 6.7 1 2
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 378 7 1 5 3.5 COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2016.06.014
4337 391 None 55 Human Binding pIC50 = 6.7 6.7 1 2
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 378 7 1 5 3.5 COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2016.06.014
6918493 391 None 55 Human Binding pIC50 = 6.7 6.7 1 2
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 378 7 1 5 3.5 COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2016.06.014
6918493.0 391 None 55 Human Binding pIC50 = 6.7 6.7 1 2
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 378 7 1 5 3.5 COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2016.06.014
CHEMBL1111 391 None 55 Human Binding pIC50 = 6.7 6.7 1 2
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 378 7 1 5 3.5 COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2016.06.014
DB06403 391 None 55 Human Binding pIC50 = 6.7 6.7 1 2
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 378 7 1 5 3.5 COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2016.06.014
44384766 59685 None 0 Human Binding pIC50 = 5.7 5.7 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 532 10 1 10 4.1 C#CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL172184 59685 None 0 Human Binding pIC50 = 5.7 5.7 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 532 10 1 10 4.1 C#CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
10576888 170948 None 0 Human Binding pIC50 = 4.7 4.7 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 485 6 3 7 3.6 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccccc2C(=O)O)c1Br 10.1021/jm9608366
CHEMBL44539 170948 None 0 Human Binding pIC50 = 4.7 4.7 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 485 6 3 7 3.6 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccccc2C(=O)O)c1Br 10.1021/jm9608366
10211781 129809 None 0 Human Binding pIC50 = 6.7 6.7 - 1
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 661 11 2 13 3.6 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccccn1 10.1016/s0960-894x(02)01084-3
CHEMBL367453 129809 None 0 Human Binding pIC50 = 6.7 6.7 - 1
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 661 11 2 13 3.6 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccccn1 10.1016/s0960-894x(02)01084-3
73669820 117692 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]ET-1 from rat ETB receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETB receptor after 1 hr by Lowry method
ChEMBL 462 10 1 7 5.5 CC(=O)c1ccc(OCc2ccc3nsnc3c2)cc1OC(CCC(=O)O)c1ccccc1 10.1016/j.bmc.2015.01.003
CHEMBL3400989 117692 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]ET-1 from rat ETB receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETB receptor after 1 hr by Lowry method
ChEMBL 462 10 1 7 5.5 CC(=O)c1ccc(OCc2ccc3nsnc3c2)cc1OC(CCC(=O)O)c1ccccc1 10.1016/j.bmc.2015.01.003
10697883 11243 None 0 Human Binding pIC50 = 4.7 4.7 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 548 8 3 10 2.5 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2CNS(C)(=O)=O)OCO3)c1Cl 10.1021/jm9608366
CHEMBL1178885 11243 None 0 Human Binding pIC50 = 4.7 4.7 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 548 8 3 10 2.5 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2CNS(C)(=O)=O)OCO3)c1Cl 10.1021/jm9608366
CHEMBL47828 11243 None 0 Human Binding pIC50 = 4.7 4.7 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 548 8 3 10 2.5 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2CNS(C)(=O)=O)OCO3)c1Cl 10.1021/jm9608366
137639474 156989 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 607 10 2 9 5.4 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(-c4nnn[nH]4)c3)c(=O)c3cc(OCC4CCCC4)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL4072165 156989 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 607 10 2 9 5.4 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(-c4nnn[nH]4)c3)c(=O)c3cc(OCC4CCCC4)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
52949155 18418 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
ChEMBL 557 10 2 7 5.4 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCC(C)C)ccc31)OCO2 10.1016/j.bmcl.2010.08.074
CHEMBL1271640 18418 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
ChEMBL 557 10 2 7 5.4 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCC(C)C)ccc31)OCO2 10.1016/j.bmcl.2010.08.074
10122495 30879 None 0 Human Binding pIC50 = 6.7 6.7 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 665 12 1 10 6.4 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCC#CCOCc1ccccc1 10.1016/s0960-894x(02)01084-3
CHEMBL139734 30879 None 0 Human Binding pIC50 = 6.7 6.7 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 665 12 1 10 6.4 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCC#CCOCc1ccccc1 10.1016/s0960-894x(02)01084-3
9870117 195547 None 0 Pig Binding pIC50 = 8.7 8.7 - 0
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptor
ChEMBL 488 10 1 7 5.5 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCC=O)c1 10.1016/s0960-894x(00)00366-8
CHEMBL54057 195547 None 0 Pig Binding pIC50 = 8.7 8.7 - 0
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptor
ChEMBL 488 10 1 7 5.5 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCC=O)c1 10.1016/s0960-894x(00)00366-8
9870117 195547 None 0 Pig Binding pIC50 = 8.7 8.7 - 0
Displacement of 125I-ET1 from pig ETB receptor transfected in grivet COS7 cellsDisplacement of 125I-ET1 from pig ETB receptor transfected in grivet COS7 cells
ChEMBL 488 10 1 7 5.5 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCC=O)c1 10.1016/j.bmcl.2016.06.014
CHEMBL54057 195547 None 0 Pig Binding pIC50 = 8.7 8.7 - 0
Displacement of 125I-ET1 from pig ETB receptor transfected in grivet COS7 cellsDisplacement of 125I-ET1 from pig ETB receptor transfected in grivet COS7 cells
ChEMBL 488 10 1 7 5.5 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCC=O)c1 10.1016/j.bmcl.2016.06.014
9831249 59717 None 0 Human Binding pIC50 = 8.7 8.7 - 2
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 672 14 2 10 6.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C2CC2)nc1OCCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
CHEMBL172297 59717 None 0 Human Binding pIC50 = 8.7 8.7 - 2
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 672 14 2 10 6.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C2CC2)nc1OCCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
10720982 127884 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 530 9 2 6 4.8 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)C)cc1 10.1021/jm990171i
CHEMBL121647 127884 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 530 9 2 6 4.8 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)C)cc1 10.1021/jm990171i
CHEMBL366441 127884 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 530 9 2 6 4.8 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)C)cc1 10.1021/jm990171i
44314889 103797 None 0 Pig Binding pIC50 = 8.7 8.7 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 633 12 5 4 4.7 CCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
CHEMBL308815 103797 None 0 Pig Binding pIC50 = 8.7 8.7 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 633 12 5 4 4.7 CCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
9808545 11456 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 588 11 2 7 5.2 COCCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)(C)C)cc1 10.1021/jm990171i
CHEMBL1180353 11456 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 588 11 2 7 5.2 COCCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)(C)C)cc1 10.1021/jm990171i
CHEMBL123408 11456 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 588 11 2 7 5.2 COCCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)(C)C)cc1 10.1021/jm990171i
44314579 102972 None 0 Pig Binding pIC50 = 8.6 8.6 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 580 12 5 5 3.8 CCCCC(NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)C)C(=O)O 10.1021/jm9600914
CHEMBL306123 102972 None 0 Pig Binding pIC50 = 8.6 8.6 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 580 12 5 5 3.8 CCCCC(NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)C)C(=O)O 10.1021/jm9600914
44283270 167984 None 0 Pig Binding pIC50 = 8.6 8.6 - 0
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranesInhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranes
ChEMBL 580 12 5 5 3.8 CCCC[C@H](NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)C)C(=O)O 10.1016/0960-894X(95)00237-N
CHEMBL431124 167984 None 0 Pig Binding pIC50 = 8.6 8.6 - 0
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranesInhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranes
ChEMBL 580 12 5 5 3.8 CCCC[C@H](NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)C)C(=O)O 10.1016/0960-894X(95)00237-N
44314750 165747 None 0 Pig Binding pIC50 = 8.6 8.6 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 647 13 5 4 5.1 CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
CHEMBL424422 165747 None 0 Pig Binding pIC50 = 8.6 8.6 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 647 13 5 4 5.1 CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
44283419 100371 None 0 Pig Binding pIC50 = 8.6 8.6 - 0
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranesInhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranes
ChEMBL 647 13 5 4 5.1 CCCC[C@H](NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1016/0960-894X(95)00237-N
CHEMBL289349 100371 None 0 Pig Binding pIC50 = 8.6 8.6 - 0
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranesInhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranes
ChEMBL 647 13 5 4 5.1 CCCC[C@H](NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1016/0960-894X(95)00237-N
10603546 110510 None 0 Pig Binding pIC50 = 8.6 8.6 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 592 15 1 7 5.0 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCC)c(F)c1 10.1021/jm970101g
CHEMBL324639 110510 None 0 Pig Binding pIC50 = 8.6 8.6 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 592 15 1 7 5.0 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCC)c(F)c1 10.1021/jm970101g
10625694 11450 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 516 9 2 6 4.5 CCC(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1 10.1021/jm990171i
CHEMBL1180344 11450 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 516 9 2 6 4.5 CCC(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1 10.1021/jm990171i
CHEMBL123107 11450 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 516 9 2 6 4.5 CCC(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1 10.1021/jm990171i
11123269 208758 None 0 Rat Binding pIC50 = 8.6 8.6 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 452 6 1 5 5.8 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1CC1CCCCC1 10.1016/s0960-894x(00)00513-8
CHEMBL87070 208758 None 0 Rat Binding pIC50 = 8.6 8.6 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 452 6 1 5 5.8 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1CC1CCCCC1 10.1016/s0960-894x(00)00513-8
44314664 207154 None 0 Pig Binding pIC50 = 8.6 8.6 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 615 12 5 4 5.1 CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CCCC1)C(=O)O 10.1021/jm9600914
CHEMBL74000 207154 None 0 Pig Binding pIC50 = 8.6 8.6 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 615 12 5 4 5.1 CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CCCC1)C(=O)O 10.1021/jm9600914
10555516 9243 None 0 Pig Binding pIC50 = 8.5 8.5 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 598 12 1 7 4.6 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)Cc1ccccc1 10.1021/jm970101g
CHEMBL110700 9243 None 0 Pig Binding pIC50 = 8.5 8.5 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 598 12 1 7 4.6 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)Cc1ccccc1 10.1021/jm970101g
44314904 103202 None 0 Pig Binding pIC50 = 8.5 8.5 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 585 12 5 5 3.6 CSCCC(NC(=O)[C@@H](Cc1c(C)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)O 10.1021/jm9600914
CHEMBL307936 103202 None 0 Pig Binding pIC50 = 8.5 8.5 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 585 12 5 5 3.6 CSCCC(NC(=O)[C@@H](Cc1c(C)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)O 10.1021/jm9600914
44314905 207505 None 0 Pig Binding pIC50 = 8.5 8.5 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 567 12 5 4 4.0 CCCCC(NC(=O)[C@@H](Cc1c(C)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)O 10.1021/jm9600914
CHEMBL77083 207505 None 0 Pig Binding pIC50 = 8.5 8.5 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 567 12 5 4 4.0 CCCCC(NC(=O)[C@@H](Cc1c(C)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)O 10.1021/jm9600914
10649119 11442 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 502 8 2 6 4.1 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(C)c2ccccc2)cc1 10.1021/jm990171i
CHEMBL1180318 11442 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 502 8 2 6 4.1 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(C)c2ccccc2)cc1 10.1021/jm990171i
CHEMBL121761 11442 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 502 8 2 6 4.1 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(C)c2ccccc2)cc1 10.1021/jm990171i
CHEMBL317099 213657 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
44298382 197508 None 0 Pig Binding pIC50 = 7.7 7.7 - 0
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptor
ChEMBL 502 11 1 7 5.8 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCCC=O)c1 10.1016/s0960-894x(00)00366-8
CHEMBL54998 197508 None 0 Pig Binding pIC50 = 7.7 7.7 - 0
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptor
ChEMBL 502 11 1 7 5.8 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCCC=O)c1 10.1016/s0960-894x(00)00366-8
10792316 168585 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 530 8 2 6 5.3 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(C)cccc2C(C)C)cc1 10.1021/jm990170q
CHEMBL435185 168585 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 530 8 2 6 5.3 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(C)cccc2C(C)C)cc1 10.1021/jm990170q
CHEMBL313984 213582 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00070a001
56671734 63349 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Inhibition of binding to Endothelin B receptor of rat cerebellar membranes.Inhibition of binding to Endothelin B receptor of rat cerebellar membranes.
ChEMBL 937 26 9 9 3.6 CC[C@H](C)[C@H](NC(=O)[C@@H](N)Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)NCC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)[C@@H](C)CC 10.1021/jm970161m
CHEMBL1793932 63349 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Inhibition of binding to Endothelin B receptor of rat cerebellar membranes.Inhibition of binding to Endothelin B receptor of rat cerebellar membranes.
ChEMBL 937 26 9 9 3.6 CC[C@H](C)[C@H](NC(=O)[C@@H](N)Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)NCC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)[C@@H](C)CC 10.1021/jm970161m
44284236 122389 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 504 9 3 7 4.5 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CCCO)c1 10.1016/j.bmcl.2004.01.008
CHEMBL35984 122389 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 504 9 3 7 4.5 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CCCO)c1 10.1016/j.bmcl.2004.01.008
21462927 120306 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 500 7 1 8 5.1 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2cc([N+](=O)[O-])ccc23)cc1 10.1016/s0960-894x(99)00040-2
CHEMBL352241 120306 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 500 7 1 8 5.1 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2cc([N+](=O)[O-])ccc23)cc1 10.1016/s0960-894x(99)00040-2
9825494 205067 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding affinity at human Endothelin B receptorBinding affinity at human Endothelin B receptor
ChEMBL 460 6 1 6 5.2 COc1ccc(C2=C(C(=O)O)[C@@H](c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
CHEMBL61211 205067 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding affinity at human Endothelin B receptorBinding affinity at human Endothelin B receptor
ChEMBL 460 6 1 6 5.2 COc1ccc(C2=C(C(=O)O)[C@@H](c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
10896413 100661 None 0 Pig Binding pIC50 = 6.7 6.7 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 504 9 1 7 5.4 COc1ccc(CCOC2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
CHEMBL291841 100661 None 0 Pig Binding pIC50 = 6.7 6.7 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 504 9 1 7 5.4 COc1ccc(CCOC2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
11755275 202465 None 0 Human Binding pIC50 = 6.7 6.7 - 1
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membranesInhibition of [125I]ET1 binding to porcine kidney inner medulla membranes
ChEMBL 489 9 1 7 4.8 CCOc1ccc2c(c1)c(-c1ccc(OC)cc1)c(C(=O)O)c(=O)n2Cc1cc(OC)ccc1OC 10.1016/S0960-894X(97)00319-3
CHEMBL59537 202465 None 0 Human Binding pIC50 = 6.7 6.7 - 1
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membranesInhibition of [125I]ET1 binding to porcine kidney inner medulla membranes
ChEMBL 489 9 1 7 4.8 CCOc1ccc2c(c1)c(-c1ccc(OC)cc1)c(C(=O)O)c(=O)n2Cc1cc(OC)ccc1OC 10.1016/S0960-894X(97)00319-3
10627272 206514 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.
ChEMBL 592 12 1 11 4.2 COC(=O)CCCOc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc(OC)c1OC 10.1021/jm980504w
CHEMBL69986 206514 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.
ChEMBL 592 12 1 11 4.2 COC(=O)CCCOc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc(OC)c1OC 10.1021/jm980504w
44311527 206581 None 0 Human Binding pIC50 = 6.7 6.7 - 1
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 675 12 2 11 7.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2cccs2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
CHEMBL70365 206581 None 0 Human Binding pIC50 = 6.7 6.7 - 1
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 675 12 2 11 7.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2cccs2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
44327868 111507 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL 906 24 9 8 3.9 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC12CC3CC(CC(C3)C1)C2)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL327523 111507 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL 906 24 9 8 3.9 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC12CC3CC(CC(C3)C1)C2)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
10791694 98253 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(OC)c(OC)c2OC)cc1 10.1021/jm9606507
CHEMBL274175 98253 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(OC)c(OC)c2OC)cc1 10.1021/jm9606507
9934580 163025 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 474 6 1 8 3.6 COC(=O)c1ccc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc1 10.1021/jm9606507
CHEMBL417428 163025 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 474 6 1 8 3.6 COC(=O)c1ccc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc1 10.1021/jm9606507
10765057 163255 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 430 4 1 7 3.5 O=C1OC(O)(c2ccc3c(c2)OCO3)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2 10.1021/jm9606507
CHEMBL417978 163255 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 430 4 1 7 3.5 O=C1OC(O)(c2ccc3c(c2)OCO3)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2 10.1021/jm9606507
171348836 193851 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Binding affinity to human placenta ETBBinding affinity to human placenta ETB
ChEMBL 439 7 2 6 3.3 O=S(=O)(Nc1ncnc(OCCO)c1-c1ccccc1)c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.0c01093
CHEMBL5272983 193851 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Binding affinity to human placenta ETBBinding affinity to human placenta ETB
ChEMBL 439 7 2 6 3.3 O=S(=O)(Nc1ncnc(OCCO)c1-c1ccccc1)c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.0c01093
19735343 176155 None 0 Human Binding pIC50 = 5.7 5.7 - 1
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta cell membranes
ChEMBL 473 7 2 6 4.0 O=S(=O)(Nc1ncnc(OCCO)c1-c1ccc(Cl)cc1)c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL4590568 176155 None 0 Human Binding pIC50 = 5.7 5.7 - 1
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta cell membranes
ChEMBL 473 7 2 6 4.0 O=S(=O)(Nc1ncnc(OCCO)c1-c1ccc(Cl)cc1)c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL86814 218382 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00070a001
CHEMBL1791279 211378 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellumInhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)[C@H](C)CC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(95)00152-J
44383753 60086 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 466 5 1 5 5.7 Cc1cc(C)c(/C=C/c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00133-9
CHEMBL173761 60086 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 466 5 1 5 5.7 Cc1cc(C)c(/C=C/c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00133-9
44327661 164685 None 0 Pig Binding pIC50 = 5.7 5.7 - 0
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranes
ChEMBL 483 5 1 8 2.7 Cc1ccc(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c2ccc3c(c2)OCO3)n1 10.1016/S0960-894X(96)00617-8
CHEMBL421563 164685 None 0 Pig Binding pIC50 = 5.7 5.7 - 0
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranes
ChEMBL 483 5 1 8 2.7 Cc1ccc(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c2ccc3c(c2)OCO3)n1 10.1016/S0960-894X(96)00617-8
44316515 207462 None 1 Human Binding pIC50 = 4.7 4.7 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 360 4 1 5 2.9 COc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1C 10.1016/0960-894X(96)00441-6
CHEMBL76779 207462 None 1 Human Binding pIC50 = 4.7 4.7 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 360 4 1 5 2.9 COc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1C 10.1016/0960-894X(96)00441-6
18617288 207604 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 316 3 1 4 2.5 Cc1noc(NS(=O)(=O)c2ccccc2)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL78080 207604 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 316 3 1 4 2.5 Cc1noc(NS(=O)(=O)c2ccccc2)c1Br 10.1016/0960-894X(96)00441-6
11800804 161930 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Inhibitory activity was evaluated against human Endothelin B receptorInhibitory activity was evaluated against human Endothelin B receptor
ChEMBL 550 10 4 5 4.7 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N(C)C2CCCCC2)nc1C(=O)O 10.1021/jm9505932
CHEMBL414605 161930 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Inhibitory activity was evaluated against human Endothelin B receptorInhibitory activity was evaluated against human Endothelin B receptor
ChEMBL 550 10 4 5 4.7 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N(C)C2CCCCC2)nc1C(=O)O 10.1021/jm9505932
104865 706 None 60 Human Binding pIC50 = 6.7 6.7 -6 4
Antagonist activity at ET-B receptor (unknown origin)Antagonist activity at ET-B receptor (unknown origin)
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/acs.jmedchem.5b01781
104865.0 706 None 60 Human Binding pIC50 = 6.7 6.7 -6 4
Antagonist activity at ET-B receptor (unknown origin)Antagonist activity at ET-B receptor (unknown origin)
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/acs.jmedchem.5b01781
3494 706 None 60 Human Binding pIC50 = 6.7 6.7 -6 4
Antagonist activity at ET-B receptor (unknown origin)Antagonist activity at ET-B receptor (unknown origin)
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/acs.jmedchem.5b01781
392 706 None 60 Human Binding pIC50 = 6.7 6.7 -6 4
Antagonist activity at ET-B receptor (unknown origin)Antagonist activity at ET-B receptor (unknown origin)
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/acs.jmedchem.5b01781
CHEMBL957 706 None 60 Human Binding pIC50 = 6.7 6.7 -6 4
Antagonist activity at ET-B receptor (unknown origin)Antagonist activity at ET-B receptor (unknown origin)
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/acs.jmedchem.5b01781
DB00559 706 None 60 Human Binding pIC50 = 6.7 6.7 -6 4
Antagonist activity at ET-B receptor (unknown origin)Antagonist activity at ET-B receptor (unknown origin)
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/acs.jmedchem.5b01781
104865 706 None 60 Human Binding pIC50 = 6.7 6.7 -6 4
Displacement of 125I-ET1 from human placenta ETB receptorDisplacement of 125I-ET1 from human placenta ETB receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.bmcl.2016.06.014
104865.0 706 None 60 Human Binding pIC50 = 6.7 6.7 -6 4
Displacement of 125I-ET1 from human placenta ETB receptorDisplacement of 125I-ET1 from human placenta ETB receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.bmcl.2016.06.014
3494 706 None 60 Human Binding pIC50 = 6.7 6.7 -6 4
Displacement of 125I-ET1 from human placenta ETB receptorDisplacement of 125I-ET1 from human placenta ETB receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.bmcl.2016.06.014
392 706 None 60 Human Binding pIC50 = 6.7 6.7 -6 4
Displacement of 125I-ET1 from human placenta ETB receptorDisplacement of 125I-ET1 from human placenta ETB receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.bmcl.2016.06.014
CHEMBL957 706 None 60 Human Binding pIC50 = 6.7 6.7 -6 4
Displacement of 125I-ET1 from human placenta ETB receptorDisplacement of 125I-ET1 from human placenta ETB receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.bmcl.2016.06.014
DB00559 706 None 60 Human Binding pIC50 = 6.7 6.7 -6 4
Displacement of 125I-ET1 from human placenta ETB receptorDisplacement of 125I-ET1 from human placenta ETB receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.bmcl.2016.06.014
104865 706 None 60 Human Binding pIC50 = 6.7 6.7 -6 4
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm3009103
104865.0 706 None 60 Human Binding pIC50 = 6.7 6.7 -6 4
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm3009103
3494 706 None 60 Human Binding pIC50 = 6.7 6.7 -6 4
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm3009103
392 706 None 60 Human Binding pIC50 = 6.7 6.7 -6 4
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm3009103
CHEMBL957 706 None 60 Human Binding pIC50 = 6.7 6.7 -6 4
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm3009103
DB00559 706 None 60 Human Binding pIC50 = 6.7 6.7 -6 4
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm3009103
10122033 81708 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 631 15 1 13 4.0 COc1cnc(OCCOc2nc(-c3ncccn3)nc(NS(=O)(=O)CCc3ccccc3)c2Oc2ccccc2OC)nc1 10.1021/jm3009103
CHEMBL2163703 81708 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 631 15 1 13 4.0 COc1cnc(OCCOc2nc(-c3ncccn3)nc(NS(=O)(=O)CCc3ccccc3)c2Oc2ccccc2OC)nc1 10.1021/jm3009103
58688005 175064 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 540 11 2 9 3.1 CCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Br)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL4565926 175064 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 540 11 2 9 3.1 CCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Br)cc1 10.1016/j.bmcl.2016.06.014
10144372 166149 None 0 Human Binding pIC50 = 5.7 5.7 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 562 10 2 11 3.4 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ncccn2)nc1OCC#CCO 10.1016/s0960-894x(02)01084-3
CHEMBL425682 166149 None 0 Human Binding pIC50 = 5.7 5.7 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 562 10 2 11 3.4 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ncccn2)nc1OCC#CCO 10.1016/s0960-894x(02)01084-3
22467229 99011 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
ChEMBL 519 7 2 7 4.1 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(CN)ccc23)cc1 10.1016/s0960-894x(01)00660-6
CHEMBL279703 99011 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
ChEMBL 519 7 2 7 4.1 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(CN)ccc23)cc1 10.1016/s0960-894x(01)00660-6
44320338 107030 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 490 7 2 6 5.0 O=C(O)c1ccc(Cn2nc(-c3ccccc3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)cc1 10.1016/s0960-894x(00)00513-8
CHEMBL315087 107030 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 490 7 2 6 5.0 O=C(O)c1ccc(Cn2nc(-c3ccccc3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)cc1 10.1016/s0960-894x(00)00513-8
10281192 61097 None 0 Human Binding pIC50 = 6.7 6.7 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 561 11 2 10 4.2 C#CCOc1nc(-c2ccnc(CO)c2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL176482 61097 None 0 Human Binding pIC50 = 6.7 6.7 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 561 11 2 10 4.2 C#CCOc1nc(-c2ccnc(CO)c2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
10211543 131453 None 0 Human Binding pIC50 = 6.7 6.7 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 640 13 2 12 3.5 CCCCNC(=O)OCC#CCOc1nc(N2CCOCC2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL368989 131453 None 0 Human Binding pIC50 = 6.7 6.7 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 640 13 2 12 3.5 CCCCNC(=O)OCC#CCOc1nc(N2CCOCC2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
71462245 81697 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 588 13 2 10 3.6 CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1Oc1cc(OC)ccc1Cl 10.1021/jm3009103
CHEMBL2163692 81697 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 588 13 2 10 3.6 CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1Oc1cc(OC)ccc1Cl 10.1021/jm3009103
44177614 129719 None 0 Human Binding pIC50 = 5.7 5.7 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 547 10 1 9 5.4 C=CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL367339 129719 None 0 Human Binding pIC50 = 5.7 5.7 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 547 10 1 9 5.4 C=CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
10479787 59634 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 468 6 1 5 5.3 Cc1cc(C)c(CCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00133-9
CHEMBL171972 59634 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 468 6 1 5 5.3 Cc1cc(C)c(CCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00133-9
151174 205177 None 35 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta cell membranes
ChEMBL 605 12 3 13 3.2 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccnc(-c3nn[nH]n3)c2)nc1OCCO 10.1016/j.bmcl.2016.06.014
CHEMBL61780 205177 None 35 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta cell membranes
ChEMBL 605 12 3 13 3.2 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccnc(-c3nn[nH]n3)c2)nc1OCCO 10.1016/j.bmcl.2016.06.014
44334130 4511 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B receptor
ChEMBL 458 5 1 6 4.4 COc1ccc([C@@H]2c3nc(N4CCCC4)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1016/s0960-894x(02)00663-7
CHEMBL102173 4511 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B receptor
ChEMBL 458 5 1 6 4.4 COc1ccc([C@@H]2c3nc(N4CCCC4)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1016/s0960-894x(02)00663-7
10745564 6227 None 0 Pig Binding pIC50 = 6.7 6.7 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 566 11 1 7 4.4 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)c1ccccc1 10.1021/jm970101g
CHEMBL108142 6227 None 0 Pig Binding pIC50 = 6.7 6.7 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 566 11 1 7 4.4 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)c1ccccc1 10.1021/jm970101g
CHEMBL263295 213024 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00015a003
44304492 96613 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding affinity measured in CHO cells stably transfected with the human endothelin B receptorBinding affinity measured in CHO cells stably transfected with the human endothelin B receptor
ChEMBL 949 23 9 8 4.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL262993 96613 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding affinity measured in CHO cells stably transfected with the human endothelin B receptorBinding affinity measured in CHO cells stably transfected with the human endothelin B receptor
ChEMBL 949 23 9 8 4.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
18738880 168277 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
ChEMBL 561 8 2 7 4.5 CCn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c2ccc(C(=O)NC)cc21 10.1016/s0960-894x(01)00660-6
CHEMBL433221 168277 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
ChEMBL 561 8 2 7 4.5 CCn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c2ccc(C(=O)NC)cc21 10.1016/s0960-894x(01)00660-6
21041283 173250 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 552 13 2 9 3.2 CCCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(OC)cn2)c1-c1ccc(Br)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL4521348 173250 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 552 13 2 9 3.2 CCCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(OC)cn2)c1-c1ccc(Br)cc1 10.1016/j.bmcl.2016.06.014
10960638 101122 None 0 Pig Binding pIC50 = 5.7 5.7 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 414 4 1 4 5.6 CC(C)c1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccccc32)cc1 10.1021/jm010382z
CHEMBL294793 101122 None 0 Pig Binding pIC50 = 5.7 5.7 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 414 4 1 4 5.6 CC(C)c1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccccc32)cc1 10.1021/jm010382z
44279371 99978 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB receptor
ChEMBL 466 3 2 3 5.5 O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(-c3cc(Cl)cc(Cl)c3)cc21 10.1016/0960-894X(95)00230-Q
CHEMBL286214 99978 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB receptor
ChEMBL 466 3 2 3 5.5 O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(-c3cc(Cl)cc(Cl)c3)cc21 10.1016/0960-894X(95)00230-Q
10814743 179477 None 0 Human Binding pIC50 = 5.7 5.7 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 484 6 1 9 3.7 Cc1noc(NS(=O)(=O)c2ccsc2C2(Cc3ccc4c(c3)OCO4)OCCO2)c1Cl 10.1021/jm9700068
CHEMBL47383 179477 None 0 Human Binding pIC50 = 5.7 5.7 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 484 6 1 9 3.7 Cc1noc(NS(=O)(=O)c2ccsc2C2(Cc3ccc4c(c3)OCO4)OCCO2)c1Cl 10.1021/jm9700068
10555424 206494 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.
ChEMBL 592 13 2 10 4.5 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCCCC(=O)O)c2)cc1 10.1021/jm980504w
CHEMBL69832 206494 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.
ChEMBL 592 13 2 10 4.5 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCCCC(=O)O)c2)cc1 10.1021/jm980504w
44266568 98150 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 493 7 1 6 6.3 COc1ccc(-c2c(C(=O)O)n(-c3ccc4c(c3)OCO4)c3ccc(OCc4ccccc4)cc23)cc1 10.1016/0960-894X(96)00170-9
CHEMBL273410 98150 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 493 7 1 6 6.3 COc1ccc(-c2c(C(=O)O)n(-c3ccc4c(c3)OCO4)c3ccc(OCc4ccccc4)cc23)cc1 10.1016/0960-894X(96)00170-9
CHEMBL133257 211174 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Inhibitory effect against Human Endothelin B receptorInhibitory effect against Human Endothelin B receptor
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C2CCCC2)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
44383537 59267 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Tested for binding affinity towards rabbit Endothelin B receptorTested for binding affinity towards rabbit Endothelin B receptor
ChEMBL 388 4 2 5 3.4 C/C=C/C=C/C=C/C(=O)O[C@@H]1C=C2COC(O)[C@]2(O)[C@@]2(C)CCCC(C)(C)C12 10.1016/s0960-894x(00)00136-0
CHEMBL170335 59267 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Tested for binding affinity towards rabbit Endothelin B receptorTested for binding affinity towards rabbit Endothelin B receptor
ChEMBL 388 4 2 5 3.4 C/C=C/C=C/C=C/C(=O)O[C@@H]1C=C2COC(O)[C@]2(O)[C@@]2(C)CCCC(C)(C)C12 10.1016/s0960-894x(00)00136-0
10648937 209765 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Radioligand binding selectivity to human Endothelin B receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin B receptor in chinese hamster ovary cells
ChEMBL 496 11 1 6 4.3 CCCCN(CCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL9334 209765 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Radioligand binding selectivity to human Endothelin B receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin B receptor in chinese hamster ovary cells
ChEMBL 496 11 1 6 4.3 CCCCN(CCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
44385412 131446 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 711 14 2 13 4.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(Cc2ccc3c(c2)OCO3)nc1OCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
CHEMBL368945 131446 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 711 14 2 13 4.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(Cc2ccc3c(c2)OCO3)nc1OCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
23445358 111626 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 412 4 1 5 4.6 Cc1cccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c1 10.1016/S0960-894X(96)00496-9
CHEMBL328089 111626 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 412 4 1 5 4.6 Cc1cccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c1 10.1016/S0960-894X(96)00496-9
44352079 116605 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
ChEMBL 494 11 1 5 5.0 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(C)cc1 10.1021/jm010237l
CHEMBL336272 116605 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
ChEMBL 494 11 1 5 5.0 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(C)cc1 10.1021/jm010237l
137649809 157479 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 583 10 2 7 5.9 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCC4CCCC4)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL4078297 157479 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 583 10 2 7 5.9 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCC4CCCC4)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
23548253 81707 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Antagonist activity at ETB receptor (unknown origin)Antagonist activity at ETB receptor (unknown origin)
ChEMBL 679 14 1 12 4.7 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1016/j.bmcl.2016.06.014
CHEMBL2163702 81707 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Antagonist activity at ETB receptor (unknown origin)Antagonist activity at ETB receptor (unknown origin)
ChEMBL 679 14 1 12 4.7 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1016/j.bmcl.2016.06.014
23548253 81707 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 679 14 1 12 4.7 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
CHEMBL2163702 81707 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 679 14 1 12 4.7 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
76330201 85383 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cells
ChEMBL 526 6 1 7 4.5 COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(Cl)ccc12 10.1007/s00044-004-0021-y
CHEMBL2261363 85383 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cells
ChEMBL 526 6 1 7 4.5 COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(Cl)ccc12 10.1007/s00044-004-0021-y
44214320 85384 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cells
ChEMBL 510 6 1 7 4.0 COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(F)ccc12 10.1007/s00044-004-0021-y
CHEMBL2261364 85384 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cells
ChEMBL 510 6 1 7 4.0 COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(F)ccc12 10.1007/s00044-004-0021-y
CHEMBL2304017 211932 None 0 Pig Binding pIC50 = 7.7 7.7 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL None None None CSC(C)(C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc2c(C#N)[nH]c3ccccc23)NC(=O)[C@@H](C(C)C)NC1=O 10.1021/jm9600914
11059576 205751 None 0 Pig Binding pIC50 = 6.7 6.7 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 460 7 1 6 5.2 CCCOc1ccc2c(c1)C(c1ccc(OC)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
CHEMBL64726 205751 None 0 Pig Binding pIC50 = 6.7 6.7 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 460 7 1 6 5.2 CCCOc1ccc2c(c1)C(c1ccc(OC)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
44295097 14769 None 0 Pig Binding pIC50 = 6.7 6.7 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 604 13 1 9 7.0 COc1ccc(C(=O)/C(Cc2cc(OC(C)C)c(OC(C)C)c(OC(C)C)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL1206461 14769 None 0 Pig Binding pIC50 = 6.7 6.7 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 604 13 1 9 7.0 COc1ccc(C(=O)/C(Cc2cc(OC(C)C)c(OC(C)C)c(OC(C)C)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL276362 14769 None 0 Pig Binding pIC50 = 6.7 6.7 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 604 13 1 9 7.0 COc1ccc(C(=O)/C(Cc2cc(OC(C)C)c(OC(C)C)c(OC(C)C)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
11827880 10228 None 0 Human Binding pIC50 = 6.7 6.7 - 0
In vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptorIn vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptor
ChEMBL 565 10 1 9 5.5 CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccc(C)cc2)nc1 10.1021/jm0102304
CHEMBL116046 10228 None 0 Human Binding pIC50 = 6.7 6.7 - 0
In vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptorIn vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptor
ChEMBL 565 10 1 9 5.5 CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccc(C)cc2)nc1 10.1021/jm0102304
CHEMBL177979 10228 None 0 Human Binding pIC50 = 6.7 6.7 - 0
In vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptorIn vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptor
ChEMBL 565 10 1 9 5.5 CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccc(C)cc2)nc1 10.1021/jm0102304
10552548 98575 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 476 7 1 8 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OC)c2OC)cc1 10.1021/jm9606507
CHEMBL276252 98575 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 476 7 1 8 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OC)c2OC)cc1 10.1021/jm9606507
11145841 101009 None 0 Pig Binding pIC50 = 5.7 5.7 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 528 9 1 6 6.9 CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc(OC3CCCC3)cc1)O2 10.1021/jm010382z
CHEMBL294127 101009 None 0 Pig Binding pIC50 = 5.7 5.7 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 528 9 1 6 6.9 CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc(OC3CCCC3)cc1)O2 10.1021/jm010382z
18738879 90267 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
ChEMBL 548 8 2 7 4.8 CCn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c2ccc(C(=O)O)cc21 10.1016/s0960-894x(01)00660-6
CHEMBL23833 90267 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
ChEMBL 548 8 2 7 4.8 CCn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c2ccc(C(=O)O)cc21 10.1016/s0960-894x(01)00660-6
15340617 99291 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 464 8 1 7 3.7 COc1cccc(Cn2nc(C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2OCC(=O)O)c1 10.1016/s0960-894x(00)00232-8
CHEMBL281677 99291 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 464 8 1 7 3.7 COc1cccc(Cn2nc(C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2OCC(=O)O)c1 10.1016/s0960-894x(00)00232-8
18617379 207682 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 364 3 1 4 3.5 Cc1noc(NS(=O)(=O)c2cccc(Cl)c2C)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL78669 207682 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 364 3 1 4 3.5 Cc1noc(NS(=O)(=O)c2cccc(Cl)c2C)c1Br 10.1016/0960-894X(96)00441-6
44276948 106892 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 396 5 1 3 4.5 COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccc(Cl)cc3)c2=O)c1 10.1016/s0960-894x(00)00232-8
CHEMBL3144604 106892 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 396 5 1 3 4.5 COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccc(Cl)cc3)c2=O)c1 10.1016/s0960-894x(00)00232-8
9845967 11097 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cells
ChEMBL 416 7 1 5 4.4 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1021/jm9606507
CHEMBL10801 11097 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cells
ChEMBL 416 7 1 5 4.4 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1021/jm9606507
CHEMBL1178000 11097 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cells
ChEMBL 416 7 1 5 4.4 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1021/jm9606507
CHEMBL51530 11097 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cells
ChEMBL 416 7 1 5 4.4 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1021/jm9606507
44385941 130744 None 0 Pig Binding pIC50 = 4.7 4.7 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 550 10 5 5 4.6 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCC(C)C2)nc1C(=O)O 10.1021/jm950592+
CHEMBL368286 130744 None 0 Pig Binding pIC50 = 4.7 4.7 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 550 10 5 5 4.6 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCC(C)C2)nc1C(=O)O 10.1021/jm950592+
44266532 4503 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 401 3 1 6 4.5 O=C(O)c1c(-c2ccc3c(c2)OCO3)c2ccccc2n1-c1ccc2c(c1)OCO2 10.1016/0960-894X(96)00170-9
CHEMBL10211 4503 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 401 3 1 6 4.5 O=C(O)c1c(-c2ccc3c(c2)OCO3)c2ccccc2n1-c1ccc2c(c1)OCO2 10.1016/0960-894X(96)00170-9
10282163 60433 None 0 Human Binding pIC50 = 6.7 6.7 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 599 11 2 12 3.9 C#CCOc1nc(-c2ccnc(-c3nn[nH]n3)c2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL175057 60433 None 0 Human Binding pIC50 = 6.7 6.7 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 599 11 2 12 3.9 C#CCOc1nc(-c2ccnc(-c3nn[nH]n3)c2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
9932004 98230 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 422 5 1 6 4.6 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2CC2CCCCC2)cc1 10.1021/jm9606507
CHEMBL273948 98230 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 422 5 1 6 4.6 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2CC2CCCCC2)cc1 10.1021/jm9606507
44458604 98666 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
ChEMBL 559 6 2 7 3.7 Cn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(F)(F)F)cc2)c2ccc3c(c2)OCO3)c2ccc(C(N)=O)cc21 10.1016/s0960-894x(01)00660-6
CHEMBL276982 98666 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
ChEMBL 559 6 2 7 3.7 Cn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(F)(F)F)cc2)c2ccc3c(c2)OCO3)c2ccc(C(N)=O)cc21 10.1016/s0960-894x(01)00660-6
44386161 61296 None 0 Human Binding pIC50 = 5.6 5.6 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 573 9 1 9 5.6 CCC#CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL176650 61296 None 0 Human Binding pIC50 = 5.6 5.6 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 573 9 1 9 5.6 CCC#CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL2304008 211923 None 0 Pig Binding pIC50 = 7.6 7.6 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL None None None CSC(C)(C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc2c(Br)[nH]c3ccccc23)NC(=O)[C@@H](C(C)C)NC1=O 10.1021/jm9600914
44284391 139388 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 532 9 3 7 5.3 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CCC(C)(C)O)c1 10.1016/j.bmcl.2004.01.008
CHEMBL37920 139388 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 532 9 3 7 5.3 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CCC(C)(C)O)c1 10.1016/j.bmcl.2004.01.008
18995991 100354 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 537 8 1 10 5.0 COc1cc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc4c(cc23)OCO4)cc(OC)c1OC 10.1016/0960-894X(96)00232-6
CHEMBL28920 100354 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 537 8 1 10 5.0 COc1cc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc4c(cc23)OCO4)cc(OC)c1OC 10.1016/0960-894X(96)00232-6
44279127 99542 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB receptor
ChEMBL 432 3 2 3 4.8 O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(-c3ccc(Cl)cc3)cc21 10.1016/0960-894X(95)00230-Q
CHEMBL283200 99542 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB receptor
ChEMBL 432 3 2 3 4.8 O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(-c3ccc(Cl)cc3)cc21 10.1016/0960-894X(95)00230-Q
19010493 98409 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) receptor expressed in CHO cells
ChEMBL 543 11 1 7 6.5 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)O)c1ccc2c(c1)OCO2 10.1016/0960-894X(95)00186-W
CHEMBL275179 98409 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) receptor expressed in CHO cells
ChEMBL 543 11 1 7 6.5 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)O)c1ccc2c(c1)OCO2 10.1016/0960-894X(95)00186-W
11048815 102370 None 0 Pig Binding pIC50 = 5.6 5.6 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 460 7 1 6 5.2 CCCOc1ccc2c(c1)OC(c1ccc3c(c1)OCO3)C(C(=O)O)=C2c1ccc(OC)cc1 10.1021/jm010382z
CHEMBL303531 102370 None 0 Pig Binding pIC50 = 5.6 5.6 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 460 7 1 6 5.2 CCCOc1ccc2c(c1)OC(c1ccc3c(c1)OCO3)C(C(=O)O)=C2c1ccc(OC)cc1 10.1021/jm010382z
10862228 205419 None 0 Pig Binding pIC50 = 5.6 5.6 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 398 7 1 6 4.2 CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC)cc21 10.1021/jm010382z
CHEMBL63000 205419 None 0 Pig Binding pIC50 = 5.6 5.6 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 398 7 1 6 4.2 CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC)cc21 10.1021/jm010382z
10722371 102283 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.
ChEMBL 605 11 1 11 3.6 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCN3CCOCC3)c2)cc1 10.1021/jm980504w
CHEMBL302974 102283 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.
ChEMBL 605 11 1 11 3.6 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCN3CCOCC3)c2)cc1 10.1021/jm980504w
44316768 207701 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 358 4 1 4 3.4 CCc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1C 10.1016/0960-894X(96)00441-6
CHEMBL78830 207701 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 358 4 1 4 3.4 CCc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1C 10.1016/0960-894X(96)00441-6
443289 711 None 39 Pig Binding pIC50 = 4.6 4.6 - 3
Compound was evaluated for the binding affinity to Endothelin B receptor in the porcine cerebellum.Compound was evaluated for the binding affinity to Endothelin B receptor in the porcine cerebellum.
ChEMBL None None None None 10.1021/jm00087a001
997 711 None 39 Pig Binding pIC50 = 4.6 4.6 - 3
Compound was evaluated for the binding affinity to Endothelin B receptor in the porcine cerebellum.Compound was evaluated for the binding affinity to Endothelin B receptor in the porcine cerebellum.
ChEMBL None None None None 10.1021/jm00087a001
CHEMBL314691 711 None 39 Pig Binding pIC50 = 4.6 4.6 - 3
Compound was evaluated for the binding affinity to Endothelin B receptor in the porcine cerebellum.Compound was evaluated for the binding affinity to Endothelin B receptor in the porcine cerebellum.
ChEMBL None None None None 10.1021/jm00087a001
DB12054 711 None 39 Pig Binding pIC50 = 4.6 4.6 - 3
Compound was evaluated for the binding affinity to Endothelin B receptor in the porcine cerebellum.Compound was evaluated for the binding affinity to Endothelin B receptor in the porcine cerebellum.
ChEMBL None None None None 10.1021/jm00087a001
10478562 131866 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B receptor
ChEMBL 442 6 1 6 4.5 Cc1ccc(OCc2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(97)00132-7
CHEMBL369359 131866 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B receptor
ChEMBL 442 6 1 6 4.5 Cc1ccc(OCc2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(97)00132-7
10717279 97100 None 0 Pig Binding pIC50 = 4.6 4.6 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 425 9 1 5 4.8 CCCCCCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL266996 97100 None 0 Pig Binding pIC50 = 4.6 4.6 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 425 9 1 5 4.8 CCCCCCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
10122675 98525 None 0 Human Binding pIC50 = 6.6 6.6 - 1
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 682 12 2 13 5.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccncc2)nc1OCC#CCOC(=O)Nc1cnccn1 10.1016/s0960-894x(02)01084-3
CHEMBL275897 98525 None 0 Human Binding pIC50 = 6.6 6.6 - 1
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 682 12 2 13 5.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccncc2)nc1OCC#CCOC(=O)Nc1cnccn1 10.1016/s0960-894x(02)01084-3
10742024 96996 None 0 Pig Binding pIC50 = 5.6 5.6 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 446 7 1 6 3.9 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CCc2ccccn2)cc1 10.1021/jm9505369
CHEMBL266143 96996 None 0 Pig Binding pIC50 = 5.6 5.6 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 446 7 1 6 3.9 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CCc2ccccn2)cc1 10.1021/jm9505369
135884434 130633 None 0 Human Binding pIC50 = 6.6 6.6 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 628 10 2 12 5.2 C#CCOc1nc(-c2ccnc(-c3noc(O)n3)c2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL368117 130633 None 0 Human Binding pIC50 = 6.6 6.6 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 628 10 2 12 5.2 C#CCOc1nc(-c2ccnc(-c3noc(O)n3)c2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
9810571 61406 None 0 Human Binding pIC50 = 7.6 7.6 - 2
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 731 18 2 13 5.0 CCCS(=O)(=O)NCCOc1nc(-c2cc(OC)c(OC)c(OC)c2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
CHEMBL176997 61406 None 0 Human Binding pIC50 = 7.6 7.6 - 2
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 731 18 2 13 5.0 CCCS(=O)(=O)NCCOc1nc(-c2cc(OC)c(OC)c(OC)c2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
18184194 130630 None 0 Human Binding pIC50 = 7.6 7.6 - 2
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 712 15 2 12 4.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCCNS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(02)01083-1
CHEMBL368107 130630 None 0 Human Binding pIC50 = 7.6 7.6 - 2
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 712 15 2 12 4.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCCNS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(02)01083-1
44368819 168995 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
Binding affinity against Endothelin B receptor in rat cerebellar membrane (ET-B) from adult blue laurie ratBinding affinity against Endothelin B receptor in rat cerebellar membrane (ET-B) from adult blue laurie rat
ChEMBL 1637 31 19 20 1.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)NCCCCCCCC(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)80156-6
77282140 168995 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
Binding affinity against Endothelin B receptor in rat cerebellar membrane (ET-B) from adult blue laurie ratBinding affinity against Endothelin B receptor in rat cerebellar membrane (ET-B) from adult blue laurie rat
ChEMBL 1637 31 19 20 1.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)NCCCCCCCC(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)80156-6
CHEMBL438380 168995 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
Binding affinity against Endothelin B receptor in rat cerebellar membrane (ET-B) from adult blue laurie ratBinding affinity against Endothelin B receptor in rat cerebellar membrane (ET-B) from adult blue laurie rat
ChEMBL 1637 31 19 20 1.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)NCCCCCCCC(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)80156-6
10815823 9799 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 520 8 1 9 4.2 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1C 10.1021/jm9606507
CHEMBL11369 9799 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 520 8 1 9 4.2 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1C 10.1021/jm9606507
44298304 101610 None 0 Pig Binding pIC50 = 6.6 6.6 - 0
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptor
ChEMBL 503 10 2 7 4.7 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCC(N)=O)c1 10.1016/s0960-894x(00)00366-8
CHEMBL298395 101610 None 0 Pig Binding pIC50 = 6.6 6.6 - 0
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptor
ChEMBL 503 10 2 7 4.7 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCC(N)=O)c1 10.1016/s0960-894x(00)00366-8
44298409 197242 None 0 Pig Binding pIC50 = 6.6 6.6 - 0
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptor
ChEMBL 490 10 2 7 5.2 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCCO)c1 10.1016/s0960-894x(00)00366-8
CHEMBL54770 197242 None 0 Pig Binding pIC50 = 6.6 6.6 - 0
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptor
ChEMBL 490 10 2 7 5.2 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCCO)c1 10.1016/s0960-894x(00)00366-8
CHEMBL2304018 211933 None 0 Pig Binding pIC50 = 6.6 6.6 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc2c(Cl)[nH]c3ccccc23)NC(=O)[C@@H](C(C)C)NC1=O 10.1021/jm9600914
76319370 85390 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cells
ChEMBL 564 8 1 9 4.0 CCOC(=O)c1ccc2c(C(C(=O)NS(=O)(=O)c3ccc(C)cc3OC)c3ccc4c(c3)OCO4)cn(C)c2c1 10.1007/s00044-004-0021-y
CHEMBL2261602 85390 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cells
ChEMBL 564 8 1 9 4.0 CCOC(=O)c1ccc2c(C(C(=O)NS(=O)(=O)c3ccc(C)cc3OC)c3ccc4c(c3)OCO4)cn(C)c2c1 10.1007/s00044-004-0021-y
10886132 9811 None 0 Human Binding pIC50 = 6.6 6.6 - 0
In vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptorIn vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptor
ChEMBL 549 10 1 9 4.8 COc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccc(C)cc2)nc1 10.1021/jm0102304
CHEMBL113757 9811 None 0 Human Binding pIC50 = 6.6 6.6 - 0
In vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptorIn vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptor
ChEMBL 549 10 1 9 4.8 COc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccc(C)cc2)nc1 10.1021/jm0102304
CHEMBL368796 9811 None 0 Human Binding pIC50 = 6.6 6.6 - 0
In vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptorIn vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptor
ChEMBL 549 10 1 9 4.8 COc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccc(C)cc2)nc1 10.1021/jm0102304
10440821 209997 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL 918 24 9 8 4.1 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c(C)c(C)c(C)c(C)c1C)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL94689 209997 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL 918 24 9 8 4.1 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c(C)c(C)c(C)c(C)c1C)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
44279351 99998 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB receptor
ChEMBL 412 3 2 3 4.5 Cc1ccccc1-c1ccc2c(c1)C(=O)c1ccccc1[C@@H]1[C@H](C(=O)O)[C@H](C(=O)O)[C@H]21 10.1016/0960-894X(95)00230-Q
CHEMBL286333 99998 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB receptor
ChEMBL 412 3 2 3 4.5 Cc1ccccc1-c1ccc2c(c1)C(=O)c1ccccc1[C@@H]1[C@H](C(=O)O)[C@H](C(=O)O)[C@H]21 10.1016/0960-894X(95)00230-Q
44279129 107051 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB receptor
ChEMBL 428 4 2 4 4.2 COc1ccccc1-c1ccc2c(c1)C(=O)c1ccccc1[C@@H]1[C@H](C(=O)O)[C@H](C(=O)O)[C@H]21 10.1016/0960-894X(95)00230-Q
CHEMBL31524 107051 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB receptor
ChEMBL 428 4 2 4 4.2 COc1ccccc1-c1ccc2c(c1)C(=O)c1ccccc1[C@@H]1[C@H](C(=O)O)[C@H](C(=O)O)[C@H]21 10.1016/0960-894X(95)00230-Q
22998446 106688 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 398 4 1 5 4.3 Cc1noc(NS(=O)(=O)c2ccc(-c3ccccc3)s2)c1Br 10.1016/S0960-894X(96)00496-9
CHEMBL314320 106688 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 398 4 1 5 4.3 Cc1noc(NS(=O)(=O)c2ccc(-c3ccccc3)s2)c1Br 10.1016/S0960-894X(96)00496-9
44277263 106893 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 440 5 1 5 4.2 COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3cc4c(cc3Cl)OCO4)c2=O)c1 10.1016/s0960-894x(00)00232-8
CHEMBL3144605 106893 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 440 5 1 5 4.2 COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3cc4c(cc3Cl)OCO4)c2=O)c1 10.1016/s0960-894x(00)00232-8
10744085 102925 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.
ChEMBL 503 9 1 8 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OCCN(C)C)c2)cc1 10.1021/jm980504w
CHEMBL305777 102925 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.
ChEMBL 503 9 1 8 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OCCN(C)C)c2)cc1 10.1021/jm980504w
44327727 168300 None 0 Pig Binding pIC50 = 5.6 5.6 - 0
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranes
ChEMBL 503 6 1 8 3.0 Cc1ccc(=O)n(C(C(=O)NS(=O)(=O)c2ccc(-c3ccccc3)cc2)c2ccc3c(c2)OCO3)n1 10.1016/S0960-894X(96)00617-8
CHEMBL433373 168300 None 0 Pig Binding pIC50 = 5.6 5.6 - 0
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranes
ChEMBL 503 6 1 8 3.0 Cc1ccc(=O)n(C(C(=O)NS(=O)(=O)c2ccc(-c3ccccc3)cc2)c2ccc3c(c2)OCO3)n1 10.1016/S0960-894X(96)00617-8
44386536 130781 None 0 Pig Binding pIC50 = 5.6 5.6 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 549 10 4 6 4.9 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)Nc2ccccc2F)nc1C(=O)O 10.1021/jm950592+
CHEMBL368461 130781 None 0 Pig Binding pIC50 = 5.6 5.6 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 549 10 4 6 4.9 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)Nc2ccccc2F)nc1C(=O)O 10.1021/jm950592+
44266655 5045 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 445 5 1 7 4.5 COc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2c(c1)OCO2 10.1016/0960-894X(96)00170-9
CHEMBL10523 5045 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 445 5 1 7 4.5 COc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2c(c1)OCO2 10.1016/0960-894X(96)00170-9
18617363 164655 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 384 3 1 4 3.9 Cc1noc(NS(=O)(=O)c2ccc(Cl)cc2Cl)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL421523 164655 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 384 3 1 4 3.9 Cc1noc(NS(=O)(=O)c2ccc(Cl)cc2Cl)c1Br 10.1016/0960-894X(96)00441-6
5344 173577 None 67 Human Binding pIC50 = 4.6 4.6 - 1
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 267 3 2 5 1.7 Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C 10.1016/0960-894X(96)00441-6
CHEMBL453 173577 None 67 Human Binding pIC50 = 4.6 4.6 - 1
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 267 3 2 5 1.7 Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C 10.1016/0960-894X(96)00441-6
15453210 207704 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 376 5 1 6 2.6 COc1ccc(S(=O)(=O)Nc2onc(C)c2Br)cc1OC 10.1016/0960-894X(96)00441-6
CHEMBL78853 207704 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 376 5 1 6 2.6 COc1ccc(S(=O)(=O)Nc2onc(C)c2Br)cc1OC 10.1016/0960-894X(96)00441-6
44276596 106898 None 0 Rat Binding pIC50 = 4.6 4.6 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 458 8 1 6 4.2 COc1ccc(Cc2[nH]n(Cc3cccc(OC)c3)c(=O)c2Cc2ccc3c(c2)OCO3)cc1 10.1016/s0960-894x(00)00232-8
CHEMBL3144728 106898 None 0 Rat Binding pIC50 = 4.6 4.6 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 458 8 1 6 4.2 COc1ccc(Cc2[nH]n(Cc3cccc(OC)c3)c(=O)c2Cc2ccc3c(c2)OCO3)cc1 10.1016/s0960-894x(00)00232-8
44276907 106911 None 0 Rat Binding pIC50 = 4.6 4.6 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 376 4 1 4 3.6 O=c1c(Cc2ccc3c(c2)OCO3)c(C(F)(F)F)[nH]n1Cc1ccccc1 10.1016/s0960-894x(00)00232-8
CHEMBL3144845 106911 None 0 Rat Binding pIC50 = 4.6 4.6 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 376 4 1 4 3.6 O=c1c(Cc2ccc3c(c2)OCO3)c(C(F)(F)F)[nH]n1Cc1ccccc1 10.1016/s0960-894x(00)00232-8
10146377 60434 None 0 Human Binding pIC50 = 6.6 6.6 - 1
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 662 11 2 14 3.0 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1cnccn1 10.1016/s0960-894x(02)01084-3
CHEMBL175058 60434 None 0 Human Binding pIC50 = 6.6 6.6 - 1
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 662 11 2 14 3.0 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1cnccn1 10.1016/s0960-894x(02)01084-3
71449713 81699 None 25 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 585 11 1 8 4.5 CCCCS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1 10.1021/jm3009103
CHEMBL2163694 81699 None 25 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 585 11 1 8 4.5 CCCCS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1 10.1021/jm3009103
10575061 209351 None 0 Pig Binding pIC50 = 5.6 5.6 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 439 9 1 6 4.0 CCCCC(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL9082 209351 None 0 Pig Binding pIC50 = 5.6 5.6 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 439 9 1 6 4.0 CCCCC(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
22467266 85380 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cells
ChEMBL 522 7 2 8 3.4 COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(CO)ccc12 10.1007/s00044-004-0021-y
CHEMBL2261360 85380 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cells
ChEMBL 522 7 2 8 3.4 COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(CO)ccc12 10.1007/s00044-004-0021-y
23445366 106239 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 482 7 1 5 6.2 Cc1cc(CCC(C)C)ccc1-c1ccsc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/S0960-894X(96)00496-9
CHEMBL313801 106239 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 482 7 1 5 6.2 Cc1cc(CCC(C)C)ccc1-c1ccsc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/S0960-894X(96)00496-9
CHEMBL2370070 212238 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCN)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00070a001
71455140 82039 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 598 12 2 8 4.7 CC(C)c1ccc(-c2c(NS(=O)(=O)NCc3ccccc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm3009103
CHEMBL2165336 82039 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 598 12 2 8 4.7 CC(C)c1ccc(-c2c(NS(=O)(=O)NCc3ccccc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm3009103
71456865 81733 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 632 14 2 11 3.7 COc1nc(NS(=O)(=O)NCc2ccccc2)c(Oc2ccccc2OC)c(OCCOc2ncc(Br)cn2)n1 10.1021/jm3009103
CHEMBL2163727 81733 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 632 14 2 11 3.7 COc1nc(NS(=O)(=O)NCc2ccccc2)c(Oc2ccccc2OC)c(OCCOc2ncc(Br)cn2)n1 10.1021/jm3009103
44284405 100410 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 532 10 2 7 5.4 COCC(C)Cc1cc(OC)ccc1[C@@H]1c2nc(NC(C)C)ccc2[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O 10.1016/j.bmcl.2004.01.008
CHEMBL289634 100410 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 532 10 2 7 5.4 COCC(C)Cc1cc(OC)ccc1[C@@H]1c2nc(NC(C)C)ccc2[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O 10.1016/j.bmcl.2004.01.008
44284328 127608 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 476 7 2 7 4.6 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(OC)c1 10.1016/j.bmcl.2004.01.008
CHEMBL36627 127608 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 476 7 2 7 4.6 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(OC)c1 10.1016/j.bmcl.2004.01.008
9939238 206586 None 0 Human Binding pIC50 = 7.6 7.6 - 1
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 637 12 2 13 3.6 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
CHEMBL70385 206586 None 0 Human Binding pIC50 = 7.6 7.6 - 1
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 637 12 2 13 3.6 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
44311345 206675 None 0 Human Binding pIC50 = 7.6 7.6 - 1
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 663 13 3 12 5.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(C2CCNCC2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
CHEMBL70895 206675 None 0 Human Binding pIC50 = 7.6 7.6 - 1
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 663 13 3 12 5.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(C2CCNCC2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
CHEMBL85341 218378 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00070a001
15411009 107246 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Binding affinity for human endothelin B receptor expressed in CHO-K1 cells.Binding affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 691 14 1 12 5.6 CCOC(=O)C(CC(C)C)NC(=O)OC1(c2ccc(OC)cc2)OC(=O)C(c2ccc3c(c2)OCO3)=C1Cc1cc(OC)c(OC)c(OC)c1 10.1016/S0960-894X(97)00002-4
CHEMBL316523 107246 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Binding affinity for human endothelin B receptor expressed in CHO-K1 cells.Binding affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 691 14 1 12 5.6 CCOC(=O)C(CC(C)C)NC(=O)OC1(c2ccc(OC)cc2)OC(=O)C(c2ccc3c(c2)OCO3)=C1Cc1cc(OC)c(OC)c(OC)c1 10.1016/S0960-894X(97)00002-4
10938122 163101 None 0 Pig Binding pIC50 = 5.6 5.6 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 396 5 1 5 4.8 CC(C)Oc1ccc2c(c1)C(C(C)C)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
CHEMBL417555 163101 None 0 Pig Binding pIC50 = 5.6 5.6 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 396 5 1 5 4.8 CC(C)Oc1ccc2c(c1)C(C(C)C)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
135415889 59287 None 0 Human Binding pIC50 = 5.6 5.6 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 587 10 2 13 3.6 C#CCOc1nc(-c2ccnc(-c3noc(O)n3)c2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL170401 59287 None 0 Human Binding pIC50 = 5.6 5.6 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 587 10 2 13 3.6 C#CCOc1nc(-c2ccnc(-c3noc(O)n3)c2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
44266542 162905 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 521 7 1 7 6.1 O=C(O)c1c(-c2ccc3c(c2)OCO3)c2cc(OCc3ccccc3)ccc2n1Cc1ccc2c(c1)OCO2 10.1016/0960-894X(96)00170-9
CHEMBL417246 162905 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 521 7 1 7 6.1 O=C(O)c1c(-c2ccc3c(c2)OCO3)c2cc(OCc3ccccc3)ccc2n1Cc1ccc2c(c1)OCO2 10.1016/0960-894X(96)00170-9
18617351 104164 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 384 3 1 4 3.9 Cc1noc(NS(=O)(=O)c2cc(Cl)ccc2Cl)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL309397 104164 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 384 3 1 4 3.9 Cc1noc(NS(=O)(=O)c2cc(Cl)ccc2Cl)c1Br 10.1016/0960-894X(96)00441-6
18617407 207438 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 320 3 1 4 3.4 Cc1noc(NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1C 10.1016/0960-894X(96)00441-6
CHEMBL76576 207438 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 320 3 1 4 3.4 Cc1noc(NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1C 10.1016/0960-894X(96)00441-6
10788853 6112 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 432 7 1 6 4.1 COc1ccc(C2(O)OC(=O)C(c3ccc(OC)cc3OC)=C2Cc2ccccc2)cc1 10.1021/jm9606507
CHEMBL10808 6112 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 432 7 1 6 4.1 COc1ccc(C2(O)OC(=O)C(c3ccc(OC)cc3OC)=C2Cc2ccccc2)cc1 10.1021/jm9606507
10766396 110642 None 0 Pig Binding pIC50 = 4.6 4.6 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 460 8 1 4 4.6 CCCN(C)C(=O)CN1C[C@H](c2ccc3ccccc3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL325418 110642 None 0 Pig Binding pIC50 = 4.6 4.6 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 460 8 1 4 4.6 CCCN(C)C(=O)CN1C[C@H](c2ccc3ccccc3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
44276886 106889 None 0 Rat Binding pIC50 = 4.6 4.6 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 410 4 1 4 4.2 O=c1c(Cc2ccc3c(c2)OCO3)c(C(F)(F)F)[nH]n1Cc1ccccc1Cl 10.1016/s0960-894x(00)00232-8
CHEMBL3144600 106889 None 0 Rat Binding pIC50 = 4.6 4.6 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 410 4 1 4 4.2 O=c1c(Cc2ccc3c(c2)OCO3)c(C(F)(F)F)[nH]n1Cc1ccccc1Cl 10.1016/s0960-894x(00)00232-8
44459272 91274 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
ChEMBL 491 6 2 7 2.6 Cn1cc(C(C(=O)NS(=O)(=O)c2ccccc2)c2ccc3c(c2)OCO3)c2ccc(C(N)=O)cc21 10.1016/s0960-894x(01)00660-6
CHEMBL24015 91274 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
ChEMBL 491 6 2 7 2.6 Cn1cc(C(C(=O)NS(=O)(=O)c2ccccc2)c2ccc3c(c2)OCO3)c2ccc(C(N)=O)cc21 10.1016/s0960-894x(01)00660-6
10279940 101406 None 0 Human Binding pIC50 = 4.6 4.6 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 527 8 2 10 3.6 CC(=O)OCCc1cc2c(cc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl)OCO2 10.1021/jm9608366
CHEMBL296927 101406 None 0 Human Binding pIC50 = 4.6 4.6 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 527 8 2 10 3.6 CC(=O)OCCc1cc2c(cc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl)OCO2 10.1021/jm9608366
10504920 163205 None 0 Human Binding pIC50 = 4.6 4.6 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 480 6 2 9 3.5 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2CC#N)OCO3)c1Cl 10.1021/jm9608366
CHEMBL417719 163205 None 0 Human Binding pIC50 = 4.6 4.6 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 480 6 2 9 3.5 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2CC#N)OCO3)c1Cl 10.1021/jm9608366
44384611 128721 None 0 Human Binding pIC50 = 6.6 6.6 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 644 10 2 12 5.8 C#CCOc1nc(-c2ccnc(-c3noc(S)n3)c2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL366797 128721 None 0 Human Binding pIC50 = 6.6 6.6 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 644 10 2 12 5.8 C#CCOc1nc(-c2ccnc(-c3noc(S)n3)c2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
44314647 207543 None 0 Pig Binding pIC50 = 7.6 7.6 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 647 13 5 4 5.1 CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1CCCCCCC1)C(=O)O 10.1021/jm9600914
CHEMBL77468 207543 None 0 Pig Binding pIC50 = 7.6 7.6 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 647 13 5 4 5.1 CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1CCCCCCC1)C(=O)O 10.1021/jm9600914
10745418 114056 None 1 Human Binding pIC50 = 7.6 7.6 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 558 9 2 6 6.2 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(C(C)C)cccc2C(C)C)cc1 10.1021/jm990170q
CHEMBL332627 114056 None 1 Human Binding pIC50 = 7.6 7.6 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 558 9 2 6 6.2 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(C(C)C)cccc2C(C)C)cc1 10.1021/jm990170q
44320461 106405 None 0 Rat Binding pIC50 = 7.6 7.6 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 514 6 1 5 6.6 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1Cc1ccc(Cl)c(Cl)c1 10.1016/s0960-894x(00)00513-8
CHEMBL313920 106405 None 0 Rat Binding pIC50 = 7.6 7.6 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 514 6 1 5 6.6 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1Cc1ccc(Cl)c(Cl)c1 10.1016/s0960-894x(00)00513-8
10118046 9438 None 0 Pig Binding pIC50 = 6.6 6.6 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 504 10 1 7 2.9 CCCS(=O)(=O)N(C)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm970101g
CHEMBL111728 9438 None 0 Pig Binding pIC50 = 6.6 6.6 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 504 10 1 7 2.9 CCCS(=O)(=O)N(C)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm970101g
44327659 109878 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL 937 26 9 8 4.6 CCC(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC)[C@@H](C)CC)C(c1ccccc1)c1ccccc1 10.1021/jm00015a003
CHEMBL323331 109878 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL 937 26 9 8 4.6 CCC(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC)[C@@H](C)CC)C(c1ccccc1)c1ccccc1 10.1021/jm00015a003
CHEMBL96822 218410 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NS(C)(=O)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
10789524 5194 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 446 6 1 7 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OC)c2)cc1 10.1021/jm9606507
CHEMBL10607 5194 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 446 6 1 7 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OC)c2)cc1 10.1021/jm9606507
10530409 5708 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 536 9 1 10 3.9 COc1ccc(C2(O)OC(=O)C(c3cc(OC)c4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1021/jm9606507
CHEMBL10781 5708 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 536 9 1 10 3.9 COc1ccc(C2(O)OC(=O)C(c3cc(OC)c4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1021/jm9606507
73669821 117691 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
Displacement of S6c from rat ETB receptor after 1 hr by Lowry methodDisplacement of S6c from rat ETB receptor after 1 hr by Lowry method
ChEMBL 448 10 1 6 5.2 CC(=O)c1ccc(OCc2ccc3c(c2)OCO3)cc1OC(CCC(=O)O)c1ccccc1 10.1016/j.bmc.2015.01.003
CHEMBL3400988 117691 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
Displacement of S6c from rat ETB receptor after 1 hr by Lowry methodDisplacement of S6c from rat ETB receptor after 1 hr by Lowry method
ChEMBL 448 10 1 6 5.2 CC(=O)c1ccc(OCc2ccc3c(c2)OCO3)cc1OC(CCC(=O)O)c1ccccc1 10.1016/j.bmc.2015.01.003
44295177 14787 None 0 Pig Binding pIC50 = 6.6 6.6 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 534 10 1 9 5.0 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1C 10.1016/s0960-894x(98)00301-1
CHEMBL1206680 14787 None 0 Pig Binding pIC50 = 6.6 6.6 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 534 10 1 9 5.0 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1C 10.1016/s0960-894x(98)00301-1
CHEMBL295483 14787 None 0 Pig Binding pIC50 = 6.6 6.6 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 534 10 1 9 5.0 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1C 10.1016/s0960-894x(98)00301-1
10789525 61790 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibitory concentration against Endothelin B receptorInhibitory concentration against Endothelin B receptor
ChEMBL 446 8 1 6 4.4 COc1ccc(C(=O)/C(Cc2cccc(OC)c2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1021/jm031041j
CHEMBL177221 61790 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibitory concentration against Endothelin B receptorInhibitory concentration against Endothelin B receptor
ChEMBL 446 8 1 6 4.4 COc1ccc(C(=O)/C(Cc2cccc(OC)c2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1021/jm031041j
10346184 9198 None 0 Pig Binding pIC50 = 5.6 5.6 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 508 12 1 5 4.9 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL110366 9198 None 0 Pig Binding pIC50 = 5.6 5.6 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 508 12 1 5 4.9 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL315328 213648 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](N)Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00070a001
CHEMBL87252 218384 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
ChEMBL None None None None 10.1021/jm00070a001
18936171 198962 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membranesInhibition of [125I]ET1 binding to porcine kidney inner medulla membranes
ChEMBL 489 7 1 8 4.2 COc1ccccc1Cn1c(=O)c(C(=O)O)c(-c2ccc3c(c2)OCO3)c2c(OC)c(OC)ccc21 10.1016/S0960-894X(97)00319-3
CHEMBL56348 198962 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membranesInhibition of [125I]ET1 binding to porcine kidney inner medulla membranes
ChEMBL 489 7 1 8 4.2 COc1ccccc1Cn1c(=O)c(C(=O)O)c(-c2ccc3c(c2)OCO3)c2c(OC)c(OC)ccc21 10.1016/S0960-894X(97)00319-3
44327252 209992 None 0 Pig Binding pIC50 = 5.6 5.6 - 0
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranes
ChEMBL 495 7 1 8 3.1 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)n2nc(C3CC3)ccc2=O)cc1 10.1016/S0960-894X(96)00617-8
CHEMBL94654 209992 None 0 Pig Binding pIC50 = 5.6 5.6 - 0
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranes
ChEMBL 495 7 1 8 3.1 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)n2nc(C3CC3)ccc2=O)cc1 10.1016/S0960-894X(96)00617-8
44327226 210374 None 0 Pig Binding pIC50 = 5.6 5.6 - 0
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranes
ChEMBL 497 7 1 8 3.1 CCc1cc(C)nn(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c1=O 10.1016/S0960-894X(96)00617-8
CHEMBL96762 210374 None 0 Pig Binding pIC50 = 5.6 5.6 - 0
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranes
ChEMBL 497 7 1 8 3.1 CCc1cc(C)nn(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c1=O 10.1016/S0960-894X(96)00617-8
22616258 105462 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 372 5 1 4 3.8 CCCc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1C 10.1016/0960-894X(96)00441-6
CHEMBL311781 105462 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 372 5 1 4 3.8 CCCc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1C 10.1016/0960-894X(96)00441-6
9870959 8919 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 509 13 1 6 4.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1ccccn1 10.1021/jm980217s
CHEMBL109778 8919 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 509 13 1 6 4.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1ccccn1 10.1021/jm980217s
10625152 110522 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 498 13 1 6 4.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1ccoc1 10.1021/jm980217s
CHEMBL324685 110522 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 498 13 1 6 4.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1ccoc1 10.1021/jm980217s
44386621 61297 None 0 Pig Binding pIC50 = 4.6 4.6 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 549 10 4 6 4.5 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CC3CCC2C3)nc1C(=O)O 10.1021/jm950592+
CHEMBL176653 61297 None 0 Pig Binding pIC50 = 4.6 4.6 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 549 10 4 6 4.5 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CC3CCC2C3)nc1C(=O)O 10.1021/jm950592+
11801544 61797 None 0 Pig Binding pIC50 = 4.6 4.6 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 589 10 4 6 5.1 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2C3CC4CC(C3)CC2C4)nc1C(=O)O 10.1021/jm950592+
CHEMBL177261 61797 None 0 Pig Binding pIC50 = 4.6 4.6 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 589 10 4 6 5.1 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2C3CC4CC(C3)CC2C4)nc1C(=O)O 10.1021/jm950592+
44385805 61316 None 0 Human Binding pIC50 = 5.6 5.6 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 532 10 1 10 4.1 C#CCOc1nc(-c2cnccn2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL176698 61316 None 0 Human Binding pIC50 = 5.6 5.6 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 532 10 1 10 4.1 C#CCOc1nc(-c2cnccn2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
10552413 110731 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 472 13 1 5 4.7 C/C=C\CC[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC 10.1021/jm980217s
CHEMBL325935 110731 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 472 13 1 5 4.7 C/C=C\CC[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC 10.1021/jm980217s
10346184 9198 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
ChEMBL 508 12 1 5 4.9 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm010237l
CHEMBL110366 9198 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
ChEMBL 508 12 1 5 4.9 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm010237l
21462925 120003 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 470 6 2 7 4.8 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2cc(N)ccc23)cc1 10.1016/s0960-894x(99)00040-2
CHEMBL349556 120003 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 470 6 2 7 4.8 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2cc(N)ccc23)cc1 10.1016/s0960-894x(99)00040-2
CHEMBL2304011 211926 None 0 Pig Binding pIC50 = 6.6 6.6 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL None None None Cc1[nH]c2ccccc2c1C[C@@H]1NC(=O)[C@@H](C2CC2)NC(=O)[C@H](C(C)C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC1=O 10.1021/jm9600914
CHEMBL2369709 212111 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
Inhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellumInhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(95)00152-J
44371421 51450 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 459 5 1 5 5.8 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3Cl)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(99)00040-2
CHEMBL158204 51450 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 459 5 1 5 5.8 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3Cl)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(99)00040-2
10412464 9139 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 470 6 1 5 5.4 COc1ccc(CC2=C(c3ccc(Cl)c(Cl)c3)C(=O)OC2(O)c2ccc(OC)cc2)cc1 10.1021/jm9606507
CHEMBL10996 9139 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 470 6 1 5 5.4 COc1ccc(CC2=C(c3ccc(Cl)c(Cl)c3)C(=O)OC2(O)c2ccc(OC)cc2)cc1 10.1021/jm9606507
10961720 205942 None 0 Pig Binding pIC50 = 5.6 5.6 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 472 6 1 5 6.3 CC(C)Oc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc(C(C)C)cc1)O2 10.1021/jm010382z
CHEMBL66094 205942 None 0 Pig Binding pIC50 = 5.6 5.6 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 472 6 1 5 6.3 CC(C)Oc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc(C(C)C)cc1)O2 10.1021/jm010382z
44314461 207237 None 0 Pig Binding pIC50 = 5.6 5.6 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 605 13 5 4 3.9 CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1CCCC1)C(=O)O 10.1021/jm9600914
CHEMBL74837 207237 None 0 Pig Binding pIC50 = 5.6 5.6 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 605 13 5 4 3.9 CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1CCCC1)C(=O)O 10.1021/jm9600914
10767778 16409 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 502 7 2 6 4.5 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2cc(C)cc(C)c2)cc1 10.1021/jm990170q
CHEMBL123077 16409 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 502 7 2 6 4.5 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2cc(C)cc(C)c2)cc1 10.1021/jm990170q
10216862 198868 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membranesInhibition of [125I]ET1 binding to porcine kidney inner medulla membranes
ChEMBL 443 4 1 7 3.9 O=C(O)c1c(-c2ccc3c(c2)OCO3)c2ccccc2n(Cc2ccc3c(c2)OCO3)c1=O 10.1016/S0960-894X(97)00319-3
CHEMBL56286 198868 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membranesInhibition of [125I]ET1 binding to porcine kidney inner medulla membranes
ChEMBL 443 4 1 7 3.9 O=C(O)c1c(-c2ccc3c(c2)OCO3)c2ccccc2n(Cc2ccc3c(c2)OCO3)c1=O 10.1016/S0960-894X(97)00319-3
CHEMBL265066 96868 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
Tested for its inhibitory activity against Endothelin B receptorTested for its inhibitory activity against Endothelin B receptor
ChEMBL 646 8 2 13 5.8 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC(=O)C2=C(C)N=C(C)/C(=C(/O)OC)[C@@H]2c2cccc([N+](=O)[O-])c2)[C@H]1c1cccc([N+](=O)[O-])c1 10.1016/S0960-894X(01)81025-8
22616257 207472 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Binding affinity against human ETB receptor in transfected COS 7 cell membrane preparationBinding affinity against human ETB receptor in transfected COS 7 cell membrane preparation
ChEMBL 272 3 1 4 2.4 Cc1noc(NS(=O)(=O)c2ccccc2)c1Cl 10.1016/0960-894X(96)00441-6
CHEMBL76860 207472 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Binding affinity against human ETB receptor in transfected COS 7 cell membrane preparationBinding affinity against human ETB receptor in transfected COS 7 cell membrane preparation
ChEMBL 272 3 1 4 2.4 Cc1noc(NS(=O)(=O)c2ccccc2)c1Cl 10.1016/0960-894X(96)00441-6
44316831 207973 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 358 4 1 4 3.4 CCc1ccc(Br)c(S(=O)(=O)Nc2onc(C)c2C)c1 10.1016/0960-894X(96)00441-6
CHEMBL80807 207973 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 358 4 1 4 3.4 CCc1ccc(Br)c(S(=O)(=O)Nc2onc(C)c2C)c1 10.1016/0960-894X(96)00441-6
10070783 97109 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 420 4 1 5 4.5 O=C1OC(O)(c2ccc(Cl)cc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2 10.1021/jm9606507
CHEMBL267094 97109 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 420 4 1 5 4.5 O=C1OC(O)(c2ccc(Cl)cc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2 10.1021/jm9606507
10502226 101583 None 0 Human Binding pIC50 = 4.6 4.6 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 420 6 1 8 3.3 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Cc2ccc3c(c2)OCO3)c1C 10.1021/jm9700068
CHEMBL298203 101583 None 0 Human Binding pIC50 = 4.6 4.6 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 420 6 1 8 3.3 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Cc2ccc3c(c2)OCO3)c1C 10.1021/jm9700068
10719007 11245 None 0 Human Binding pIC50 = 4.6 4.6 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 465 6 1 9 3.7 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)C(C#N)c2ccc3c(c2)OCO3)c1Cl 10.1021/jm9700068
CHEMBL1178895 11245 None 0 Human Binding pIC50 = 4.6 4.6 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 465 6 1 9 3.7 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)C(C#N)c2ccc3c(c2)OCO3)c1Cl 10.1021/jm9700068
CHEMBL48448 11245 None 0 Human Binding pIC50 = 4.6 4.6 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 465 6 1 9 3.7 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)C(C#N)c2ccc3c(c2)OCO3)c1Cl 10.1021/jm9700068
10646637 209506 None 0 Pig Binding pIC50 = 4.6 4.6 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 437 8 1 5 4.9 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2C/C=C/CC(C)C)cc1 10.1021/jm9505369
CHEMBL9168 209506 None 0 Pig Binding pIC50 = 4.6 4.6 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 437 8 1 5 4.9 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2C/C=C/CC(C)C)cc1 10.1021/jm9505369
10347080 85261 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cells
ChEMBL 535 7 2 8 3.0 COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(N)=O)ccc12 10.1007/s00044-004-0021-y
CHEMBL22562 85261 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cells
ChEMBL 535 7 2 8 3.0 COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(N)=O)ccc12 10.1007/s00044-004-0021-y
44314646 207497 None 0 Pig Binding pIC50 = 7.6 7.6 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 633 13 5 4 4.7 CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1CCCCCC1)C(=O)O 10.1021/jm9600914
CHEMBL77033 207497 None 0 Pig Binding pIC50 = 7.6 7.6 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 633 13 5 4 4.7 CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1CCCCCC1)C(=O)O 10.1021/jm9600914
11766844 109837 None 0 Human Binding pIC50 = 7.6 7.6 - 0
In vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptorIn vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptor
ChEMBL 553 9 1 8 5.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Cl)cn2)cc1 10.1021/jm0102304
CHEMBL176272 109837 None 0 Human Binding pIC50 = 7.6 7.6 - 0
In vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptorIn vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptor
ChEMBL 553 9 1 8 5.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Cl)cn2)cc1 10.1021/jm0102304
CHEMBL323243 109837 None 0 Human Binding pIC50 = 7.6 7.6 - 0
In vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptorIn vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptor
ChEMBL 553 9 1 8 5.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Cl)cn2)cc1 10.1021/jm0102304
10212088 96749 None 0 Human Binding pIC50 = 7.6 7.6 - 1
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 688 12 2 12 5.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccccc1 10.1016/s0960-894x(02)01084-3
CHEMBL264035 96749 None 0 Human Binding pIC50 = 7.6 7.6 - 1
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 688 12 2 12 5.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccccc1 10.1016/s0960-894x(02)01084-3
9957883 98710 None 0 Human Binding pIC50 = 6.6 6.6 - 1
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 507 7 1 9 5.0 COc1cc2c(Sc3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OC 10.1016/0960-894X(96)00232-6
CHEMBL27732 98710 None 0 Human Binding pIC50 = 6.6 6.6 - 1
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 507 7 1 9 5.0 COc1cc2c(Sc3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OC 10.1016/0960-894X(96)00232-6
44279370 107262 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB receptor
ChEMBL 426 4 2 3 4.7 CCc1ccc(-c2ccc3c(c2)C(=O)c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@H]32)cc1 10.1016/0960-894X(95)00230-Q
CHEMBL31662 107262 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB receptor
ChEMBL 426 4 2 3 4.7 CCc1ccc(-c2ccc3c(c2)C(=O)c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@H]32)cc1 10.1016/0960-894X(95)00230-Q
104865 706 None 60 Human Binding pIC50 = 6.6 6.6 -6 4
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/s0960-894x(02)01084-3
104865.0 706 None 60 Human Binding pIC50 = 6.6 6.6 -6 4
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/s0960-894x(02)01084-3
3494 706 None 60 Human Binding pIC50 = 6.6 6.6 -6 4
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/s0960-894x(02)01084-3
392 706 None 60 Human Binding pIC50 = 6.6 6.6 -6 4
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/s0960-894x(02)01084-3
CHEMBL957 706 None 60 Human Binding pIC50 = 6.6 6.6 -6 4
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/s0960-894x(02)01084-3
DB00559 706 None 60 Human Binding pIC50 = 6.6 6.6 -6 4
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/s0960-894x(02)01084-3
11091217 101121 None 0 Pig Binding pIC50 = 5.6 5.6 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 426 9 1 6 5.0 CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2cc(OCCC)ccc21 10.1021/jm010382z
CHEMBL294787 101121 None 0 Pig Binding pIC50 = 5.6 5.6 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 426 9 1 6 5.0 CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2cc(OCCC)ccc21 10.1021/jm010382z
11014820 205370 None 0 Pig Binding pIC50 = 5.6 5.6 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 398 6 1 6 4.2 CCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL62780 205370 None 0 Pig Binding pIC50 = 5.6 5.6 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 398 6 1 6 4.2 CCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
10894688 205964 None 0 Pig Binding pIC50 = 5.6 5.6 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 402 4 1 5 4.4 COc1cccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccccc32)c1 10.1021/jm010382z
CHEMBL66246 205964 None 0 Pig Binding pIC50 = 5.6 5.6 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 402 4 1 5 4.4 COc1cccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccccc32)c1 10.1021/jm010382z
44298325 198133 None 0 Pig Binding pIC50 = 5.6 5.6 - 0
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptor
ChEMBL 446 7 1 6 5.5 CCc1onc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Sc1cccc(OC)c1 10.1016/s0960-894x(00)00366-8
CHEMBL55664 198133 None 0 Pig Binding pIC50 = 5.6 5.6 - 0
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptor
ChEMBL 446 7 1 6 5.5 CCc1onc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Sc1cccc(OC)c1 10.1016/s0960-894x(00)00366-8
44311218 103182 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 607 11 2 10 5.7 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCOC(=O)Nc1ccncc1 10.1016/S0960-894X(97)00400-9
CHEMBL307803 103182 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 607 11 2 10 5.7 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCOC(=O)Nc1ccncc1 10.1016/S0960-894X(97)00400-9
10278777 168235 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)
ChEMBL 502 14 1 5 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC 10.1021/jm980217s
CHEMBL432974 168235 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)
ChEMBL 502 14 1 5 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC 10.1021/jm980217s
23445284 112865 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 440 5 1 5 5.4 Cc1noc(NS(=O)(=O)c2sccc2-c2ccc(C(C)C)cc2)c1Br 10.1016/S0960-894X(96)00496-9
CHEMBL330674 112865 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 440 5 1 5 5.4 Cc1noc(NS(=O)(=O)c2sccc2-c2ccc(C(C)C)cc2)c1Br 10.1016/S0960-894X(96)00496-9
71455060 81694 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 614 9 1 9 2.9 O=S(=O)(Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1)N1CCOCC1 10.1021/jm3009103
CHEMBL2163689 81694 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 614 9 1 9 2.9 O=S(=O)(Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1)N1CCOCC1 10.1021/jm3009103
44265861 97261 None 0 Pig Binding pIC50 = 6.6 6.6 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 481 11 1 6 5.1 CCCC(CCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL268433 97261 None 0 Pig Binding pIC50 = 6.6 6.6 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 481 11 1 6 5.1 CCCC(CCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
10553384 109724 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 498 13 1 7 3.6 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCn1cccn1 10.1021/jm980217s
CHEMBL322537 109724 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 498 13 1 7 3.6 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCn1cccn1 10.1021/jm980217s
25211074 18492 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 543 10 2 7 5.1 CCCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL1272244 18492 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 543 10 2 7 5.1 CCCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2017.04.049
25211074 18492 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in membranes by radioligand assayAntagonist activity at ETB receptor (unknown origin) expressed in membranes by radioligand assay
ChEMBL 543 10 2 7 5.1 CCCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL1272244 18492 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in membranes by radioligand assayAntagonist activity at ETB receptor (unknown origin) expressed in membranes by radioligand assay
ChEMBL 543 10 2 7 5.1 CCCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2017.04.049
44215416 175184 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 649 11 2 13 5.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2ccnc(-c3noc(=S)[nH]3)c2)nc1OCC1CCCO1 10.1016/j.bmcl.2016.06.014
CHEMBL4568468 175184 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 649 11 2 13 5.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2ccnc(-c3noc(=S)[nH]3)c2)nc1OCC1CCCO1 10.1016/j.bmcl.2016.06.014
10205429 61626 None 0 Human Binding pIC50 = 5.5 5.5 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 470 8 2 9 2.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(C)nc1OCC#CCO 10.1016/s0960-894x(02)01084-3
CHEMBL177111 61626 None 0 Human Binding pIC50 = 5.5 5.5 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 470 8 2 9 2.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(C)nc1OCC#CCO 10.1016/s0960-894x(02)01084-3
23445408 111698 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 454 6 1 5 5.5 Cc1noc(NS(=O)(=O)c2sccc2-c2ccc(CC(C)C)cc2)c1Br 10.1016/S0960-894X(96)00496-9
CHEMBL328517 111698 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 454 6 1 5 5.5 Cc1noc(NS(=O)(=O)c2sccc2-c2ccc(CC(C)C)cc2)c1Br 10.1016/S0960-894X(96)00496-9
CHEMBL2304006 211921 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Binding affinity towards Endothelin B receptor in human girardi heart cell membranesBinding affinity towards Endothelin B receptor in human girardi heart cell membranes
ChEMBL None None None O=C(O)C[C@H]1NC(=O)[C@H](Cc2c(Br)[nH]c3ccccc23)NC(=O)[C@@H](C2CC2)NC(=O)[C@H](C2CCCC2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/jm9600914
CHEMBL2304017 211932 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Binding affinity towards Endothelin B receptor in human girardi heart cell membranesBinding affinity towards Endothelin B receptor in human girardi heart cell membranes
ChEMBL None None None CSC(C)(C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc2c(C#N)[nH]c3ccccc23)NC(=O)[C@@H](C(C)C)NC1=O 10.1021/jm9600914
70240112 171706 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 626 10 2 11 5.0 CC#CCOc1nc(-c2ccnc(-c3nnn[nH]3)c2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/j.bmcl.2016.06.014
CHEMBL4465332 171706 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 626 10 2 11 5.0 CC#CCOc1nc(-c2ccnc(-c3nnn[nH]3)c2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/j.bmcl.2016.06.014
21041288 174030 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 526 10 2 9 2.8 CNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Br)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL4540866 174030 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 526 10 2 9 2.8 CNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Br)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL406279 215062 None 0 Rat Binding pIC50 = 6.5 6.5 - 0
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00070a001
44294712 14798 None 0 Pig Binding pIC50 = 6.5 6.5 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 566 11 1 9 5.6 COc1cc(C/C(C(=O)c2ccc(OC(C)C)c(F)c2)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC 10.1016/s0960-894x(98)00301-1
CHEMBL1206722 14798 None 0 Pig Binding pIC50 = 6.5 6.5 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 566 11 1 9 5.6 COc1cc(C/C(C(=O)c2ccc(OC(C)C)c(F)c2)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC 10.1016/s0960-894x(98)00301-1
CHEMBL300201 14798 None 0 Pig Binding pIC50 = 6.5 6.5 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 566 11 1 9 5.6 COc1cc(C/C(C(=O)c2ccc(OC(C)C)c(F)c2)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC 10.1016/s0960-894x(98)00301-1
44284381 128576 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 462 6 3 7 4.3 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(O)c1 10.1016/j.bmcl.2004.01.008
CHEMBL36671 128576 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 462 6 3 7 4.3 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(O)c1 10.1016/j.bmcl.2004.01.008
17869371 14795 None 0 Pig Binding pIC50 = 5.5 5.5 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 478 8 1 7 4.8 COc1ccc(C(=O)/C(Cc2ccc(OC)c(F)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL1206716 14795 None 0 Pig Binding pIC50 = 5.5 5.5 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 478 8 1 7 4.8 COc1ccc(C(=O)/C(Cc2ccc(OC)c(F)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL299521 14795 None 0 Pig Binding pIC50 = 5.5 5.5 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 478 8 1 7 4.8 COc1ccc(C(=O)/C(Cc2ccc(OC)c(F)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
10457385 112751 None 0 Pig Binding pIC50 = 5.5 5.5 - 1
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranes
ChEMBL 469 6 1 8 2.5 Cc1ccc(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)n1 10.1016/S0960-894X(96)00617-8
CHEMBL330424 112751 None 0 Pig Binding pIC50 = 5.5 5.5 - 1
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranes
ChEMBL 469 6 1 8 2.5 Cc1ccc(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)n1 10.1016/S0960-894X(96)00617-8
10527706 97054 None 0 Pig Binding pIC50 = 5.5 5.5 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 454 8 1 6 3.1 CCCN(C)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL266594 97054 None 0 Pig Binding pIC50 = 5.5 5.5 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 454 8 1 6 3.1 CCCN(C)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
18995990 99410 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 507 7 1 9 5.0 COc1cccc(Sc2c(C(=O)O)n(Cc3cc(OC)c4c(c3)OCO4)c3cc4c(cc23)OCO4)c1 10.1016/0960-894X(96)00232-6
CHEMBL282426 99410 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 507 7 1 9 5.0 COc1cccc(Sc2c(C(=O)O)n(Cc3cc(OC)c4c(c3)OCO4)c3cc4c(cc23)OCO4)c1 10.1016/0960-894X(96)00232-6
18617385 207670 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 286 3 1 4 2.7 Cc1noc(NS(=O)(=O)c2ccc(Cl)cc2)c1C 10.1016/0960-894X(96)00441-6
CHEMBL78601 207670 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 286 3 1 4 2.7 Cc1noc(NS(=O)(=O)c2ccc(Cl)cc2)c1C 10.1016/0960-894X(96)00441-6
44277387 106906 None 0 Rat Binding pIC50 = 4.5 4.5 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 450 7 2 6 3.0 O=C(O)COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2=O)c1 10.1016/s0960-894x(00)00232-8
CHEMBL3144800 106906 None 0 Rat Binding pIC50 = 4.5 4.5 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 450 7 2 6 3.0 O=C(O)COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2=O)c1 10.1016/s0960-894x(00)00232-8
10366742 107164 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 454 6 1 5 5.5 CCCc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(96)00496-9
CHEMBL316012 107164 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 454 6 1 5 5.5 CCCc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(96)00496-9
10715441 176030 None 0 Human Binding pIC50 = 4.5 4.5 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 390 6 1 6 3.9 Cc1ccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1021/jm9700068
CHEMBL45875 176030 None 0 Human Binding pIC50 = 4.5 4.5 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 390 6 1 6 3.9 Cc1ccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1021/jm9700068
10697636 167923 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 536 13 1 7 4.9 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC1SCCS1 10.1021/jm980217s
CHEMBL430683 167923 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 536 13 1 7 4.9 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC1SCCS1 10.1021/jm980217s
135512539 128541 None 0 Human Binding pIC50 = 6.5 6.5 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 615 11 2 13 4.4 C#CCOc1nc(-c2ccnc(-c3noc(O)n3)c2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL366652 128541 None 0 Human Binding pIC50 = 6.5 6.5 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 615 11 2 13 4.4 C#CCOc1nc(-c2ccnc(-c3noc(O)n3)c2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
10529715 209608 None 0 Pig Binding pIC50 = 4.5 4.5 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 510 12 1 6 4.7 CCCCN(CCCC)CC(=O)N1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL9228 209608 None 0 Pig Binding pIC50 = 4.5 4.5 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 510 12 1 6 4.7 CCCCN(CCCC)CC(=O)N1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
44384852 60260 None 0 Human Binding pIC50 = 6.5 6.5 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 544 9 1 8 5.5 C#CCOc1nc(-c2ccncc2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL174094 60260 None 0 Human Binding pIC50 = 6.5 6.5 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 544 9 1 8 5.5 C#CCOc1nc(-c2ccncc2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL67074 206072 None 0 Rat Binding pIC50 = 6.5 6.5 - 0
Tested for its ability to inhibit the binding of [125I]ET1 to the Endothelin B receptor in rat cerebellum membranes.Tested for its ability to inhibit the binding of [125I]ET1 to the Endothelin B receptor in rat cerebellum membranes.
ChEMBL 646 8 2 13 5.8 COC(=O)C1=C(C)N=C(C)/C(=C(/O)OC(=O)C2=C(C)N=C(C)/C(=C(/O)OC)[C@@H]2c2cccc([N+](=O)[O-])c2)[C@@H]1c1cccc([N+](=O)[O-])c1 10.1016/S0960-894X(01)81025-8
44386162 60429 None 0 Human Binding pIC50 = 5.5 5.5 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 575 11 1 9 6.2 CC/C=C/COc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL175005 60429 None 0 Human Binding pIC50 = 5.5 5.5 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 575 11 1 9 6.2 CC/C=C/COc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
44383754 59903 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 452 5 1 5 5.4 Cc1ccc(/C=C/c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00133-9
CHEMBL172987 59903 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 452 5 1 5 5.4 Cc1ccc(/C=C/c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00133-9
44383742 168608 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 452 5 1 5 5.4 Cc1ccc(/C=C/c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00133-9
CHEMBL435346 168608 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 452 5 1 5 5.4 Cc1ccc(/C=C/c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00133-9
44339662 9854 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 527 13 1 7 4.6 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1nc(C)c(C)o1 10.1021/jm980217s
CHEMBL114074 9854 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 527 13 1 7 4.6 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1nc(C)c(C)o1 10.1021/jm980217s
44385523 61084 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 666 13 2 9 5.9 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C2CC2)nc1OCCNS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(02)01083-1
CHEMBL176418 61084 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 666 13 2 9 5.9 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C2CC2)nc1OCCNS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(02)01083-1
17885918 106029 None 0 Rat Binding pIC50 = 8.5 8.5 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 458 6 1 6 5.9 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccsc2)nn1CC1CCCCC1 10.1016/s0960-894x(00)00513-8
CHEMBL313044 106029 None 0 Rat Binding pIC50 = 8.5 8.5 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 458 6 1 6 5.9 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccsc2)nn1CC1CCCCC1 10.1016/s0960-894x(00)00513-8
44320431 107012 None 0 Rat Binding pIC50 = 8.5 8.5 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 526 9 2 7 4.9 O=C(O)COC1CCCCC1Cn1nc(-c2ccccc2)c(Cc2cc3c(cc2Cl)OCO3)c1C(=O)O 10.1016/s0960-894x(00)00513-8
CHEMBL314973 107012 None 0 Rat Binding pIC50 = 8.5 8.5 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 526 9 2 7 4.9 O=C(O)COC1CCCCC1Cn1nc(-c2ccccc2)c(Cc2cc3c(cc2Cl)OCO3)c1C(=O)O 10.1016/s0960-894x(00)00513-8
10723203 11454 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 678 14 2 7 6.8 CCc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCOC(C)C)cc1)c1ccccc1C 10.1021/jm990171i
CHEMBL1180350 11454 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 678 14 2 7 6.8 CCc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCOC(C)C)cc1)c1ccccc1C 10.1021/jm990171i
CHEMBL123206 11454 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 678 14 2 7 6.8 CCc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCOC(C)C)cc1)c1ccccc1C 10.1021/jm990171i
9961347 11966 None 1 Human Binding pIC50 = 8.5 8.5 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 664 13 2 7 6.6 Cc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCOC(C)C)cc1)c1ccccc1C 10.1021/jm990171i
CHEMBL1182945 11966 None 1 Human Binding pIC50 = 8.5 8.5 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 664 13 2 7 6.6 Cc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCOC(C)C)cc1)c1ccccc1C 10.1021/jm990171i
CHEMBL273642 11966 None 1 Human Binding pIC50 = 8.5 8.5 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 664 13 2 7 6.6 Cc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCOC(C)C)cc1)c1ccccc1C 10.1021/jm990171i
44320212 107056 None 0 Rat Binding pIC50 = 8.5 8.5 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 520 9 2 7 4.7 O=C(O)COc1ccccc1Cn1nc(-c2ccccc2)c(Cc2cc3c(cc2Cl)OCO3)c1C(=O)O 10.1016/s0960-894x(00)00513-8
CHEMBL315280 107056 None 0 Rat Binding pIC50 = 8.5 8.5 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 520 9 2 7 4.7 O=C(O)COc1ccccc1Cn1nc(-c2ccccc2)c(Cc2cc3c(cc2Cl)OCO3)c1C(=O)O 10.1016/s0960-894x(00)00513-8
10768904 12134 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 544 10 2 6 5.2 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(CC(C)C)c2ccccc2)cc1 10.1021/jm990171i
CHEMBL1184117 12134 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 544 10 2 6 5.2 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(CC(C)C)c2ccccc2)cc1 10.1021/jm990171i
CHEMBL333034 12134 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 544 10 2 6 5.2 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(CC(C)C)c2ccccc2)cc1 10.1021/jm990171i
10555208 12409 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 578 9 2 6 5.5 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)c2ccccc2C)cc1 10.1021/jm990171i
CHEMBL1185774 12409 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 578 9 2 6 5.5 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)c2ccccc2C)cc1 10.1021/jm990171i
CHEMBL432227 12409 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 578 9 2 6 5.5 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)c2ccccc2C)cc1 10.1021/jm990171i
17885921 106857 None 0 Rat Binding pIC50 = 8.5 8.5 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 453 6 1 6 5.2 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccn2)nn1CC1CCCCC1 10.1016/s0960-894x(00)00513-8
CHEMBL314454 106857 None 0 Rat Binding pIC50 = 8.5 8.5 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 453 6 1 6 5.2 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccn2)nn1CC1CCCCC1 10.1016/s0960-894x(00)00513-8
155511294 169672 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 469 6 1 8 2.5 Cc1ccc(=O)n([C@@H](C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)n1 10.1016/j.bmcl.2016.06.014
CHEMBL4435789 169672 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 469 6 1 8 2.5 Cc1ccc(=O)n([C@@H](C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)n1 10.1016/j.bmcl.2016.06.014
9985589 168346 None 0 Human Binding pIC50 = 8.4 8.4 - 1
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 576 9 1 8 5.0 CCN(c1ccc2c(c1)oc1c(-c3ccc(OC)cc3)c(C(=O)O)c(=O)n(Cc3ccccc3OC)c12)S(C)(=O)=O 10.1016/s0960-894x(99)00040-2
CHEMBL433700 168346 None 0 Human Binding pIC50 = 8.4 8.4 - 1
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 576 9 1 8 5.0 CCN(c1ccc2c(c1)oc1c(-c3ccc(OC)cc3)c(C(=O)O)c(=O)n(Cc3ccccc3OC)c12)S(C)(=O)=O 10.1016/s0960-894x(99)00040-2
44315008 102886 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Binding affinity rowards Endothelin B receptor in human girardi heart cell membranesBinding affinity rowards Endothelin B receptor in human girardi heart cell membranes
ChEMBL 665 13 5 5 4.7 CCSCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
CHEMBL305524 102886 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Binding affinity rowards Endothelin B receptor in human girardi heart cell membranesBinding affinity rowards Endothelin B receptor in human girardi heart cell membranes
ChEMBL 665 13 5 5 4.7 CCSCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
10792636 168618 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 544 10 2 6 5.4 CCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(CC)cccc2CC)cc1 10.1021/jm990170q
CHEMBL435385 168618 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 544 10 2 6 5.4 CCOc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(CC)cccc2CC)cc1 10.1021/jm990170q
10769177 112975 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 558 11 2 6 5.2 CCc1cccc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CCOC)cc1 10.1021/jm990170q
CHEMBL331066 112975 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 558 11 2 6 5.2 CCc1cccc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CCOC)cc1 10.1021/jm990170q
11006532 12247 None 0 Human Binding pIC50 = 8.4 8.4 - 0
In vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptorIn vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptor
ChEMBL 601 10 1 9 6.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(-c3cccs3)cn2)cc1 10.1021/jm0102304
CHEMBL1184515 12247 None 0 Human Binding pIC50 = 8.4 8.4 - 0
In vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptorIn vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptor
ChEMBL 601 10 1 9 6.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(-c3cccs3)cn2)cc1 10.1021/jm0102304
CHEMBL367445 12247 None 0 Human Binding pIC50 = 8.4 8.4 - 0
In vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptorIn vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptor
ChEMBL 601 10 1 9 6.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(-c3cccs3)cn2)cc1 10.1021/jm0102304
10119177 117529 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
ChEMBL 528 12 1 6 4.8 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm010237l
CHEMBL339904 117529 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
ChEMBL 528 12 1 6 4.8 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1 10.1021/jm010237l
44327890 141499 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL 985 26 9 8 5.5 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)c1ccccc1)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL384052 141499 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL 985 26 9 8 5.5 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)c1ccccc1)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL146155 211234 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]ET1 from Endothelin B receptor of rat cerebellumDisplacement of [125I]ET1 from Endothelin B receptor of rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)81215-4
44333913 5103 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B receptor
ChEMBL 431 6 1 5 4.8 CCCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(02)00663-7
CHEMBL105591 5103 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B receptor
ChEMBL 431 6 1 5 4.8 CCCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(02)00663-7
44371410 49435 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 439 5 1 5 5.5 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3C)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(99)00040-2
CHEMBL156453 49435 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 439 5 1 5 5.5 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3C)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(99)00040-2
11827657 19388 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
ChEMBL 540 13 1 7 4.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(OC)c1 10.1021/jm010237l
CHEMBL129220 19388 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
ChEMBL 540 13 1 7 4.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(OC)c1 10.1021/jm010237l
44279126 100781 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB receptor
ChEMBL 466 3 2 3 5.5 O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(-c3ccc(Cl)cc3Cl)cc21 10.1016/0960-894X(95)00230-Q
CHEMBL29265 100781 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB receptor
ChEMBL 466 3 2 3 5.5 O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(-c3ccc(Cl)cc3Cl)cc21 10.1016/0960-894X(95)00230-Q
44279128 106968 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB receptor
ChEMBL 428 4 2 4 4.2 COc1ccc(-c2ccc3c(c2)C(=O)c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@H]32)cc1 10.1016/0960-894X(95)00230-Q
CHEMBL31469 106968 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB receptor
ChEMBL 428 4 2 4 4.2 COc1ccc(-c2ccc3c(c2)C(=O)c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@H]32)cc1 10.1016/0960-894X(95)00230-Q
44279349 168250 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB receptor
ChEMBL 448 3 2 3 5.3 O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(-c3cccc4ccccc34)cc21 10.1016/0960-894X(95)00230-Q
CHEMBL433039 168250 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB receptor
ChEMBL 448 3 2 3 5.3 O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(-c3cccc4ccccc34)cc21 10.1016/0960-894X(95)00230-Q
44298393 202287 None 0 Pig Binding pIC50 = 6.5 6.5 - 0
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptor
ChEMBL 432 6 1 6 5.2 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2C)c1 10.1016/s0960-894x(00)00366-8
CHEMBL59425 202287 None 0 Pig Binding pIC50 = 6.5 6.5 - 0
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptor
ChEMBL 432 6 1 6 5.2 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2C)c1 10.1016/s0960-894x(00)00366-8
44309996 206217 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptor
ChEMBL 483 5 1 8 5.2 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccc4nsnc4c3)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(97)10151-2
CHEMBL67971 206217 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptor
ChEMBL 483 5 1 8 5.2 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccc4nsnc4c3)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(97)10151-2
9870830 209172 None 29 Human Binding pIC50 = 6.5 6.5 -66 2
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptor
ChEMBL 506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1016/s0960-894x(97)10151-2
CHEMBL8981 209172 None 29 Human Binding pIC50 = 6.5 6.5 -66 2
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptor
ChEMBL 506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1016/s0960-894x(97)10151-2
44387128 168692 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 558 12 2 10 3.8 CNCC(=O)OCCOc1nc(C)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/S0960-894X(97)00400-9
CHEMBL435895 168692 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 558 12 2 10 3.8 CNCC(=O)OCCOc1nc(C)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/S0960-894X(97)00400-9
44371571 119553 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 425 5 1 5 5.2 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(99)00040-2
CHEMBL345380 119553 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 425 5 1 5 5.2 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(99)00040-2
10767505 5302 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 494 6 1 8 3.2 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm9606507
CHEMBL10661 5302 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 494 6 1 8 3.2 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm9606507
10601191 112867 None 0 Rat Binding pIC50 = 5.5 5.5 - 0
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.
ChEMBL 492 11 3 6 5.7 Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1-c1cc(C(=O)O)[nH]n1 10.1021/jm9707131
CHEMBL330679 112867 None 0 Rat Binding pIC50 = 5.5 5.5 - 0
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.
ChEMBL 492 11 3 6 5.7 Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1-c1cc(C(=O)O)[nH]n1 10.1021/jm9707131
CHEMBL293874 213351 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Binding activity against Endothelin B receptor 0f Porcine cerebellum membranesBinding activity against Endothelin B receptor 0f Porcine cerebellum membranes
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@H](C(C)C)NC(=O)CN(C)C(=O)[C@H](CC(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00089a028
22616255 207991 None 6 Human Binding pIC50 = 4.5 4.5 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 297 4 1 6 2.0 Cc1noc(NS(=O)(=O)c2ccc([N+](=O)[O-])cc2)c1C 10.1016/0960-894X(96)00441-6
CHEMBL80945 207991 None 6 Human Binding pIC50 = 4.5 4.5 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 297 4 1 6 2.0 Cc1noc(NS(=O)(=O)c2ccc([N+](=O)[O-])cc2)c1C 10.1016/0960-894X(96)00441-6
345351 9361 None 3 Human Binding pIC50 = 4.5 4.5 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 386 4 1 5 3.8 O=C1OC(O)(c2ccccc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2 10.1021/jm9606507
CHEMBL11131 9361 None 3 Human Binding pIC50 = 4.5 4.5 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 386 4 1 5 3.8 O=C1OC(O)(c2ccccc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2 10.1021/jm9606507
44298419 162093 None 0 Pig Binding pIC50 = 4.5 4.5 - 0
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptor
ChEMBL 420 3 1 4 3.7 Cc1onc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1I 10.1016/s0960-894x(00)00366-8
CHEMBL415942 162093 None 0 Pig Binding pIC50 = 4.5 4.5 - 0
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptor
ChEMBL 420 3 1 4 3.7 Cc1onc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1I 10.1016/s0960-894x(00)00366-8
44386370 60435 None 0 Pig Binding pIC50 = 4.5 4.5 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 531 10 4 6 4.8 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)Nc2ccccc2)nc1C(=O)O 10.1021/jm950592+
CHEMBL175066 60435 None 0 Pig Binding pIC50 = 4.5 4.5 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 531 10 4 6 4.8 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)Nc2ccccc2)nc1C(=O)O 10.1021/jm950592+
CHEMBL342615 214134 None 0 Pig Binding pIC50 = 4.5 4.5 - 0
Inhibitory effect against porcine Endothelin B receptorInhibitory effect against porcine Endothelin B receptor
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CS(=O)(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
10347080 85261 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
ChEMBL 535 7 2 8 3.0 COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(N)=O)ccc12 10.1016/s0960-894x(01)00660-6
CHEMBL22562 85261 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
ChEMBL 535 7 2 8 3.0 COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(N)=O)ccc12 10.1016/s0960-894x(01)00660-6
10576379 101325 None 0 Human Binding pIC50 = 4.5 4.5 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 471 6 2 7 3.9 COc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1021/jm9608366
CHEMBL296291 101325 None 0 Human Binding pIC50 = 4.5 4.5 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 471 6 2 7 3.9 COc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1021/jm9608366
10790376 167005 None 0 Pig Binding pIC50 = 5.5 5.5 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 466 6 1 6 3.3 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N2CCCCC2)cc1 10.1021/jm9505369
CHEMBL428644 167005 None 0 Pig Binding pIC50 = 5.5 5.5 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 466 6 1 6 3.3 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N2CCCCC2)cc1 10.1021/jm9505369
11827489 117050 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Binding affinity against human endothelin B receptor in CHO cellsBinding affinity against human endothelin B receptor in CHO cells
ChEMBL 524 12 1 4 5.6 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CC)c(F)c1 10.1021/jm010237l
CHEMBL338754 117050 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Binding affinity against human endothelin B receptor in CHO cellsBinding affinity against human endothelin B receptor in CHO cells
ChEMBL 524 12 1 4 5.6 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CC)c(F)c1 10.1021/jm010237l
9916121 81698 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 571 10 1 8 4.1 CCCS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1 10.1021/jm3009103
CHEMBL2163693 81698 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 571 10 1 8 4.1 CCCS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1 10.1021/jm3009103
10792319 209692 None 0 Pig Binding pIC50 = 6.5 6.5 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 530 10 1 6 5.1 CCCCN(C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1)c1ccccc1 10.1021/jm9505369
CHEMBL9283 209692 None 0 Pig Binding pIC50 = 6.5 6.5 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 530 10 1 6 5.1 CCCCN(C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1)c1ccccc1 10.1021/jm9505369
44265869 97315 None 0 Pig Binding pIC50 = 6.5 6.5 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 466 7 2 6 3.3 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC2CCCC2)cc1 10.1021/jm9505369
CHEMBL268864 97315 None 0 Pig Binding pIC50 = 6.5 6.5 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 466 7 2 6 3.3 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC2CCCC2)cc1 10.1021/jm9505369
23445457 129092 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B receptor
ChEMBL 470 6 1 6 5.1 Cc1cc(C)c(OCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00132-7
CHEMBL367024 129092 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B receptor
ChEMBL 470 6 1 6 5.1 Cc1cc(C)c(OCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00132-7
10962637 10081 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Ability to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptorAbility to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptor
ChEMBL 549 10 2 9 4.3 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(CO)cn2)cc1 10.1021/jm000538f
CHEMBL115372 10081 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Ability to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptorAbility to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptor
ChEMBL 549 10 2 9 4.3 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(CO)cn2)cc1 10.1021/jm000538f
CHEMBL1627023 10081 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Ability to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptorAbility to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptor
ChEMBL 549 10 2 9 4.3 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(CO)cn2)cc1 10.1021/jm000538f
10531506 12120 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 592 9 2 6 5.8 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)c2cc(C)ccc2C)cc1 10.1021/jm990171i
CHEMBL1184076 12120 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 592 9 2 6 5.8 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)c2cc(C)ccc2C)cc1 10.1021/jm990171i
CHEMBL331548 12120 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 592 9 2 6 5.8 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)c2cc(C)ccc2C)cc1 10.1021/jm990171i
CHEMBL2304013 211928 None 0 Pig Binding pIC50 = 7.5 7.5 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](C(C)(C)C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc2c(Br)[nH]c3ccccc23)NC1=O 10.1021/jm9600914
44320474 107124 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 440 8 1 5 5.7 CCC(CC)Cn1nc(-c2ccccc2)c(Cc2cc3c(cc2Cl)OCO3)c1C(=O)O 10.1016/s0960-894x(00)00513-8
CHEMBL315752 107124 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 440 8 1 5 5.7 CCC(CC)Cn1nc(-c2ccccc2)c(Cc2cc3c(cc2Cl)OCO3)c1C(=O)O 10.1016/s0960-894x(00)00513-8
104865 706 None 60 Human Binding pIC50 = 6.5 6.5 -6 4
Ability to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptorAbility to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm0102304
104865.0 706 None 60 Human Binding pIC50 = 6.5 6.5 -6 4
Ability to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptorAbility to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm0102304
3494 706 None 60 Human Binding pIC50 = 6.5 6.5 -6 4
Ability to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptorAbility to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm0102304
392 706 None 60 Human Binding pIC50 = 6.5 6.5 -6 4
Ability to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptorAbility to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm0102304
CHEMBL957 706 None 60 Human Binding pIC50 = 6.5 6.5 -6 4
Ability to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptorAbility to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm0102304
DB00559 706 None 60 Human Binding pIC50 = 6.5 6.5 -6 4
Ability to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptorAbility to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm0102304
44298330 101603 None 0 Pig Binding pIC50 = 6.5 6.5 - 0
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptor
ChEMBL 518 10 1 8 5.4 COC(=O)CCCc1onc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Sc1cccc(OC)c1 10.1016/s0960-894x(00)00366-8
CHEMBL298340 101603 None 0 Pig Binding pIC50 = 6.5 6.5 - 0
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptor
ChEMBL 518 10 1 8 5.4 COC(=O)CCCc1onc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Sc1cccc(OC)c1 10.1016/s0960-894x(00)00366-8
44458650 84937 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
ChEMBL 521 7 2 8 2.7 COc1ccccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(N)=O)ccc12 10.1016/s0960-894x(01)00660-6
CHEMBL22367 84937 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
ChEMBL 521 7 2 8 2.7 COc1ccccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(N)=O)ccc12 10.1016/s0960-894x(01)00660-6
155544917 173518 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 540 13 2 10 3.4 CCCNS(=O)(=O)Nc1ncnc(OCCOc2cc(OC)ccc2Cl)c1-c1ncc(SC)cn1 10.1016/j.bmcl.2016.06.014
CHEMBL4528516 173518 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 540 13 2 10 3.4 CCCNS(=O)(=O)Nc1ncnc(OCCOc2cc(OC)ccc2Cl)c1-c1ncc(SC)cn1 10.1016/j.bmcl.2016.06.014
11732155 205123 None 0 Pig Binding pIC50 = 4.5 4.5 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 402 4 1 5 4.4 COc1ccccc1C1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccccc21 10.1021/jm010382z
CHEMBL61460 205123 None 0 Pig Binding pIC50 = 4.5 4.5 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 402 4 1 5 4.4 COc1ccccc1C1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccccc21 10.1021/jm010382z
10672060 9262 None 0 Pig Binding pIC50 = 4.5 4.5 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 470 10 1 6 3.4 CCCN(C)C(=O)CN1C[C@H](c2ccc(OC)c(OC)c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL110794 9262 None 0 Pig Binding pIC50 = 4.5 4.5 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 470 10 1 6 3.4 CCCN(C)C(=O)CN1C[C@H](c2ccc(OC)c(OC)c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
19385674 98642 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) receptor expressed in CHO cells
ChEMBL 715 13 1 7 8.3 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)O)c1cc(Br)c(OC)c(OC)c1Br 10.1016/0960-894X(95)00186-W
CHEMBL276819 98642 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) receptor expressed in CHO cells
ChEMBL 715 13 1 7 8.3 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)O)c1cc(Br)c(OC)c(OC)c1Br 10.1016/0960-894X(95)00186-W
19385674 98642 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Inhibitory concentration against endothelin receptor type BInhibitory concentration against endothelin receptor type B
ChEMBL 715 13 1 7 8.3 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)O)c1cc(Br)c(OC)c(OC)c1Br 10.1021/jm058225d
CHEMBL276819 98642 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Inhibitory concentration against endothelin receptor type BInhibitory concentration against endothelin receptor type B
ChEMBL 715 13 1 7 8.3 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)O)c1cc(Br)c(OC)c(OC)c1Br 10.1021/jm058225d
52943105 18486 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 529 9 2 7 4.7 CCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL1272190 18486 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 529 9 2 7 4.7 CCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2017.04.049
52943105 18486 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
ChEMBL 529 9 2 7 4.7 CCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2010.08.074
CHEMBL1272190 18486 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
ChEMBL 529 9 2 7 4.7 CCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2010.08.074
10744973 209734 None 0 Pig Binding pIC50 = 6.5 6.5 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 538 14 1 6 5.5 CCCCCN(CCCCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL9313 209734 None 0 Pig Binding pIC50 = 6.5 6.5 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 538 14 1 6 5.5 CCCCCN(CCCCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
155517241 170261 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 522 14 2 11 2.9 CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1Oc1ccccc1OC 10.1016/j.bmcl.2016.06.014
CHEMBL4444355 170261 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 522 14 2 11 2.9 CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1Oc1ccccc1OC 10.1016/j.bmcl.2016.06.014
44265870 210030 None 0 Pig Binding pIC50 = 6.5 6.5 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 524 12 1 6 5.1 CCCCN(CCCC)C(=O)C(C)N1CC(c2ccc3c(c2)OCO3)C(C(=O)O)C1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL9488 210030 None 0 Pig Binding pIC50 = 6.5 6.5 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 524 12 1 6 5.1 CCCCN(CCCC)C(=O)C(C)N1CC(c2ccc3c(c2)OCO3)C(C(=O)O)C1c1ccc(OC)cc1 10.1021/jm9505369
44384715 60382 None 0 Human Binding pIC50 = 5.5 5.5 - 1
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 559 9 1 9 5.2 CC#CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL174607 60382 None 0 Human Binding pIC50 = 5.5 5.5 - 1
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 559 9 1 9 5.2 CC#CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
10305334 129115 None 0 Human Binding pIC50 = 7.5 7.5 - 1
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 680 12 2 11 6.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccncc2)nc1OCC#CCOC(=O)Nc1ccccc1 10.1016/s0960-894x(02)01084-3
CHEMBL367036 129115 None 0 Human Binding pIC50 = 7.5 7.5 - 1
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 680 12 2 11 6.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccncc2)nc1OCC#CCOC(=O)Nc1ccccc1 10.1016/s0960-894x(02)01084-3
10671928 7278 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 467 5 1 7 4.4 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2nccc3ccccc23)cc1 10.1021/jm9606507
CHEMBL10860 7278 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 467 5 1 7 4.4 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2nccc3ccccc23)cc1 10.1021/jm9606507
44295089 14638 None 0 Pig Binding pIC50 = 5.5 5.5 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 476 8 1 7 5.4 COc1ccc(C(=O)/C(Cc2ccc(SC)cc2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL1205088 14638 None 0 Pig Binding pIC50 = 5.5 5.5 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 476 8 1 7 5.4 COc1ccc(C(=O)/C(Cc2ccc(SC)cc2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL51030 14638 None 0 Pig Binding pIC50 = 5.5 5.5 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 476 8 1 7 5.4 COc1ccc(C(=O)/C(Cc2ccc(SC)cc2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
15340613 106900 None 0 Rat Binding pIC50 = 5.5 5.5 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 414 6 1 5 4.2 COc1cccc(Cn2[nH]c(-c3ccccc3)c(Cc3ccc4c(c3)OCO4)c2=O)c1 10.1016/s0960-894x(00)00232-8
CHEMBL3144732 106900 None 0 Rat Binding pIC50 = 5.5 5.5 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 414 6 1 5 4.2 COc1cccc(Cn2[nH]c(-c3ccccc3)c(Cc3ccc4c(c3)OCO4)c2=O)c1 10.1016/s0960-894x(00)00232-8
10837666 169991 None 0 Pig Binding pIC50 = 4.5 4.5 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 460 8 1 4 4.6 CCCN(C)C(=O)CN1C[C@H](c2cccc3ccccc23)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL444061 169991 None 0 Pig Binding pIC50 = 4.5 4.5 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 460 8 1 4 4.6 CCCN(C)C(=O)CN1C[C@H](c2cccc3ccccc23)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
9870959 8919 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)
ChEMBL 509 13 1 6 4.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1ccccn1 10.1021/jm980217s
CHEMBL109778 8919 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)
ChEMBL 509 13 1 6 4.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1ccccn1 10.1021/jm980217s
71451529 81724 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 632 14 2 12 3.4 CCCNS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC 10.1021/jm3009103
CHEMBL2163719 81724 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 632 14 2 12 3.4 CCCNS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC 10.1021/jm3009103
18184228 61373 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 604 13 2 9 4.6 CCS(=O)(=O)NCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
CHEMBL176749 61373 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 604 13 2 9 4.6 CCS(=O)(=O)NCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
44384651 128566 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 498 6 2 8 4.0 Cc1noc(NS(=O)(=O)c2sccc2/C=C/c2cc3c(cc2CO)OCO3)c1Br 10.1016/S0960-894X(97)00133-9
CHEMBL366680 128566 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 498 6 2 8 4.0 Cc1noc(NS(=O)(=O)c2sccc2/C=C/c2cc3c(cc2CO)OCO3)c1Br 10.1016/S0960-894X(97)00133-9
10696210 99602 None 0 Human Binding pIC50 = 4.5 4.5 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 483 6 2 9 3.7 CC(=O)c1cc2c(cc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl)OCO2 10.1021/jm9608366
CHEMBL283535 99602 None 0 Human Binding pIC50 = 4.5 4.5 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 483 6 2 9 3.7 CC(=O)c1cc2c(cc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl)OCO2 10.1021/jm9608366
44291884 173001 None 0 Human Binding pIC50 = 4.5 4.5 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 483 6 2 9 3.7 CC(=O)c1c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)ccc2c1OCO2 10.1021/jm9700068
CHEMBL45160 173001 None 0 Human Binding pIC50 = 4.5 4.5 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 483 6 2 9 3.7 CC(=O)c1c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)ccc2c1OCO2 10.1021/jm9700068
11795139 166632 None 0 Pig Binding pIC50 = 5.5 5.5 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 398 6 2 6 1.8 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(N)=O)cc1 10.1021/jm9505369
CHEMBL427935 166632 None 0 Pig Binding pIC50 = 5.5 5.5 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 398 6 2 6 1.8 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(N)=O)cc1 10.1021/jm9505369
23445516 106684 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 468 7 1 5 5.9 Cc1noc(NS(=O)(=O)c2sccc2-c2ccc(CCC(C)C)cc2)c1Br 10.1016/S0960-894X(96)00496-9
CHEMBL314307 106684 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 468 7 1 5 5.9 Cc1noc(NS(=O)(=O)c2sccc2-c2ccc(CCC(C)C)cc2)c1Br 10.1016/S0960-894X(96)00496-9
44384757 166243 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 482 5 1 7 4.8 Cc1cc2c(cc1/C=C/c1sccc1S(=O)(=O)Nc1onc(C)c1Br)OCO2 10.1016/S0960-894X(97)00133-9
CHEMBL426218 166243 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 482 5 1 7 4.8 Cc1cc2c(cc1/C=C/c1sccc1S(=O)(=O)Nc1onc(C)c1Br)OCO2 10.1016/S0960-894X(97)00133-9
CHEMBL216082 211776 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL2370255 212278 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
9830495 131217 None 0 Human Binding pIC50 = 7.5 7.5 - 1
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 618 14 2 9 5.0 CCS(=O)(=O)NCCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
CHEMBL368617 131217 None 0 Human Binding pIC50 = 7.5 7.5 - 1
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 618 14 2 9 5.0 CCS(=O)(=O)NCCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
CHEMBL94907 218404 None 0 Rat Binding pIC50 = 6.5 6.5 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00015a003
11505449 171587 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 616 12 3 9 2.6 O=C(O)CCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL4463633 171587 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 616 12 3 9 2.6 O=C(O)CCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1 10.1016/j.bmcl.2016.06.014
44309814 103061 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptor
ChEMBL 487 8 1 7 6.2 CCCOc1ccc2c(c1)c(-c1ccc(OC)cc1)c(C(=O)O)n2Cc1cc2nsnc2cc1C 10.1016/s0960-894x(97)10151-2
CHEMBL306863 103061 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptor
ChEMBL 487 8 1 7 6.2 CCCOc1ccc2c(c1)c(-c1ccc(OC)cc1)c(C(=O)O)n2Cc1cc2nsnc2cc1C 10.1016/s0960-894x(97)10151-2
9909467 207969 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Binding affinity against human ETB receptor in transfected COS 7 cell membrane preparationBinding affinity against human ETB receptor in transfected COS 7 cell membrane preparation
ChEMBL 409 4 1 5 3.8 Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL80782 207969 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Binding affinity against human ETB receptor in transfected COS 7 cell membrane preparationBinding affinity against human ETB receptor in transfected COS 7 cell membrane preparation
ChEMBL 409 4 1 5 3.8 Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL86814 218382 None 0 Rat Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]ET1 from Endothelin B receptor of rat cerebellumDisplacement of [125I]ET1 from Endothelin B receptor of rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)81215-4
44213279 106904 None 0 Rat Binding pIC50 = 5.5 5.5 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 456 6 1 5 4.2 COc1cccc(Cn2[nH]c(C(F)(F)C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2=O)c1 10.1016/s0960-894x(00)00232-8
CHEMBL3144737 106904 None 0 Rat Binding pIC50 = 5.5 5.5 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 456 6 1 5 4.2 COc1cccc(Cn2[nH]c(C(F)(F)C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2=O)c1 10.1016/s0960-894x(00)00232-8
CHEMBL86814 218382 None 0 Rat Binding pIC50 = 5.5 5.5 - 0
Inhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar membranesInhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar membranes
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00095a029
44266549 162461 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 415 4 1 6 4.5 O=C(O)c1c(-c2ccc3c(c2)OCO3)c2ccccc2n1Cc1ccc2c(c1)OCO2 10.1016/0960-894X(96)00170-9
CHEMBL416518 162461 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 415 4 1 6 4.5 O=C(O)c1c(-c2ccc3c(c2)OCO3)c2ccccc2n1Cc1ccc2c(c1)OCO2 10.1016/0960-894X(96)00170-9
44316458 207899 None 1 Human Binding pIC50 = 4.5 4.5 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 408 3 1 4 3.6 Cc1noc(NS(=O)(=O)c2cc(Br)ccc2Br)c1C 10.1016/0960-894X(96)00441-6
CHEMBL80317 207899 None 1 Human Binding pIC50 = 4.5 4.5 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 408 3 1 4 3.6 Cc1noc(NS(=O)(=O)c2cc(Br)ccc2Br)c1C 10.1016/0960-894X(96)00441-6
44277034 106899 None 0 Rat Binding pIC50 = 4.5 4.5 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 406 5 1 5 3.6 COc1ccccc1Cn1[nH]c(C(F)(F)F)c(Cc2ccc3c(c2)OCO3)c1=O 10.1016/s0960-894x(00)00232-8
CHEMBL3144729 106899 None 0 Rat Binding pIC50 = 4.5 4.5 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 406 5 1 5 3.6 COc1ccccc1Cn1[nH]c(C(F)(F)F)c(Cc2ccc3c(c2)OCO3)c1=O 10.1016/s0960-894x(00)00232-8
10576910 108595 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 486 13 1 5 5.1 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC=C(C)C 10.1021/jm980217s
CHEMBL320124 108595 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 486 13 1 5 5.1 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC=C(C)C 10.1021/jm980217s
44384826 59996 None 0 Human Binding pIC50 = 5.5 5.5 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 561 10 1 9 5.8 C/C=C/COc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL173366 59996 None 0 Human Binding pIC50 = 5.5 5.5 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 561 10 1 9 5.8 C/C=C/COc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
22998456 59814 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B receptor
ChEMBL 514 8 1 8 4.9 CCCc1cc2c(cc1OCc1sccc1S(=O)(=O)Nc1onc(C)c1Br)OCO2 10.1016/S0960-894X(97)00132-7
CHEMBL172666 59814 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B receptor
ChEMBL 514 8 1 8 4.9 CCCc1cc2c(cc1OCc1sccc1S(=O)(=O)Nc1onc(C)c1Br)OCO2 10.1016/S0960-894X(97)00132-7
10694547 209533 None 0 Pig Binding pIC50 = 5.5 5.5 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 443 10 1 7 2.9 COCCOCCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL9183 209533 None 0 Pig Binding pIC50 = 5.5 5.5 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 443 10 1 7 2.9 COCCOCCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
10507467 8502 None 0 Pig Binding pIC50 = 7.5 7.5 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 580 12 1 7 4.5 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)Cc1ccccc1 10.1021/jm970101g
CHEMBL109408 8502 None 0 Pig Binding pIC50 = 7.5 7.5 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 580 12 1 7 4.5 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)Cc1ccccc1 10.1021/jm970101g
44314660 104420 None 0 Pig Binding pIC50 = 7.5 7.5 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 633 13 5 4 4.7 CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1CCCCC1C)C(=O)O 10.1021/jm9600914
CHEMBL310111 104420 None 0 Pig Binding pIC50 = 7.5 7.5 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 633 13 5 4 4.7 CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1CCCCC1C)C(=O)O 10.1021/jm9600914
22467235 96578 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
ChEMBL 533 7 2 7 3.8 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(C(N)=O)ccc23)cc1 10.1016/s0960-894x(01)00660-6
CHEMBL262784 96578 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
ChEMBL 533 7 2 7 3.8 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(C(N)=O)ccc23)cc1 10.1016/s0960-894x(01)00660-6
10050696 96831 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 476 7 1 6 5.3 COc1cccc(Cn2nc(-c3ccccc3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)c1 10.1016/s0960-894x(00)00513-8
CHEMBL26474 96831 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 476 7 1 6 5.3 COc1cccc(Cn2nc(-c3ccccc3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)c1 10.1016/s0960-894x(00)00513-8
10050696 96831 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 476 7 1 6 5.3 COc1cccc(Cn2nc(-c3ccccc3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)c1 10.1016/s0960-894x(00)00232-8
CHEMBL26474 96831 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 476 7 1 6 5.3 COc1cccc(Cn2nc(-c3ccccc3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)c1 10.1016/s0960-894x(00)00232-8
73669992 117695 None 0 Rat Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]ET-1 from rat ETB receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETB receptor after 1 hr by Lowry method
ChEMBL 387 9 1 4 5.4 N#CCCC(Oc1cc(OCc2ccccc2)ccc1C(=O)O)c1ccccc1 10.1016/j.bmc.2015.01.003
CHEMBL3400998 117695 None 0 Rat Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]ET-1 from rat ETB receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETB receptor after 1 hr by Lowry method
ChEMBL 387 9 1 4 5.4 N#CCCC(Oc1cc(OCc2ccccc2)ccc1C(=O)O)c1ccccc1 10.1016/j.bmc.2015.01.003
23670447 3029 None 2 Pig Binding pIC50 = 6.5 6.5 - 2
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 528 10 0 9 0.1 COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+] 10.1016/s0960-894x(98)00301-1
999 3029 None 2 Pig Binding pIC50 = 6.5 6.5 - 2
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 528 10 0 9 0.1 COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+] 10.1016/s0960-894x(98)00301-1
CHEMBL1204799 3029 None 2 Pig Binding pIC50 = 6.5 6.5 - 2
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 528 10 0 9 0.1 COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+] 10.1016/s0960-894x(98)00301-1
CHEMBL25438 3029 None 2 Pig Binding pIC50 = 6.5 6.5 - 2
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 528 10 0 9 0.1 COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+] 10.1016/s0960-894x(98)00301-1
10311570 14636 None 0 Pig Binding pIC50 = 6.5 6.5 - 1
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 520 10 1 9 4.7 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL1205068 14636 None 0 Pig Binding pIC50 = 6.5 6.5 - 1
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 520 10 1 9 4.7 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL48907 14636 None 0 Pig Binding pIC50 = 6.5 6.5 - 1
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 520 10 1 9 4.7 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
44295206 14799 None 0 Pig Binding pIC50 = 6.5 6.5 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 580 12 1 11 4.7 COc1cc(C/C(C(=O)c2cc(OC)c(OC)c(OC)c2)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC 10.1016/s0960-894x(98)00301-1
CHEMBL1206728 14799 None 0 Pig Binding pIC50 = 6.5 6.5 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 580 12 1 11 4.7 COc1cc(C/C(C(=O)c2cc(OC)c(OC)c(OC)c2)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC 10.1016/s0960-894x(98)00301-1
CHEMBL301577 14799 None 0 Pig Binding pIC50 = 6.5 6.5 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 580 12 1 11 4.7 COc1cc(C/C(C(=O)c2cc(OC)c(OC)c(OC)c2)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC 10.1016/s0960-894x(98)00301-1
9871348 206485 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptor
ChEMBL 520 8 1 10 4.1 COc1ccc(C2(O)OC(=O)C(c3ccc4nsnc4c3)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1016/s0960-894x(97)10151-2
CHEMBL69741 206485 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptor
ChEMBL 520 8 1 10 4.1 COc1ccc(C2(O)OC(=O)C(c3ccc4nsnc4c3)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1016/s0960-894x(97)10151-2
18617366 167939 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 394 3 1 4 3.3 Cc1noc(NS(=O)(=O)c2ccc(Br)cc2)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL430822 167939 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 394 3 1 4 3.3 Cc1noc(NS(=O)(=O)c2ccc(Br)cc2)c1Br 10.1016/0960-894X(96)00441-6
11102609 168673 None 0 Pig Binding pIC50 = 5.5 5.5 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 462 6 1 6 5.2 COc1ccc([C@@H]2c3cc(OC(C)C)ccc3O[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1021/jm010382z
CHEMBL435773 168673 None 0 Pig Binding pIC50 = 5.5 5.5 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 462 6 1 6 5.2 COc1ccc([C@@H]2c3cc(OC(C)C)ccc3O[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1021/jm010382z
10790183 208703 None 0 Pig Binding pIC50 = 5.5 5.5 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 461 8 1 6 4.3 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CCOc2ccccc2)cc1 10.1021/jm9505369
CHEMBL8677 208703 None 0 Pig Binding pIC50 = 5.5 5.5 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 461 8 1 6 4.3 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CCOc2ccccc2)cc1 10.1021/jm9505369
10673715 9553 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 528 14 1 5 5.4 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCCCC(F)(F)F 10.1021/jm980217s
CHEMBL112314 9553 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 528 14 1 5 5.4 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCCCC(F)(F)F 10.1021/jm980217s
10789715 113161 None 0 Pig Binding pIC50 = 4.5 4.5 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 450 8 1 5 4.2 CCCN(C)C(=O)CN1C[C@H](c2cccc3occc23)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL331375 113161 None 0 Pig Binding pIC50 = 4.5 4.5 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 450 8 1 5 4.2 CCCN(C)C(=O)CN1C[C@H](c2cccc3occc23)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL2369711 212113 None 0 Rat Binding pIC50 = 4.5 4.5 - 0
Inhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellumInhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(95)00152-J
10697633 60354 None 0 Pig Binding pIC50 = 4.5 4.5 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 536 10 5 5 4.4 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2)nc1C(=O)O 10.1021/jm950592+
CHEMBL174448 60354 None 0 Pig Binding pIC50 = 4.5 4.5 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 536 10 5 5 4.4 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2)nc1C(=O)O 10.1021/jm950592+
10415348 61108 None 0 Pig Binding pIC50 = 4.5 4.5 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 557 9 3 6 4.8 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCc3ccccc32)nc1C(=O)O 10.1021/jm950592+
CHEMBL176514 61108 None 0 Pig Binding pIC50 = 4.5 4.5 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 557 9 3 6 4.8 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCc3ccccc32)nc1C(=O)O 10.1021/jm950592+
10697633 60354 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Inhibitory activity was evaluated against human Endothelin B receptorInhibitory activity was evaluated against human Endothelin B receptor
ChEMBL 536 10 5 5 4.4 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2)nc1C(=O)O 10.1021/jm9505932
CHEMBL174448 60354 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Inhibitory activity was evaluated against human Endothelin B receptorInhibitory activity was evaluated against human Endothelin B receptor
ChEMBL 536 10 5 5 4.4 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2)nc1C(=O)O 10.1021/jm9505932
71456862 81714 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 651 12 1 12 4.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
CHEMBL2163709 81714 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 651 12 1 12 4.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
10274552 73538 None 0 Human Binding pIC50 = 4.5 4.5 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 434 6 1 8 3.6 Cc1cc2c(cc1CC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1C)OCO2 10.1021/jm9700068
CHEMBL20168 73538 None 0 Human Binding pIC50 = 4.5 4.5 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 434 6 1 8 3.6 Cc1cc2c(cc1CC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1C)OCO2 10.1021/jm9700068
9807200 85379 None 0 Human Binding pIC50 = 6.5 6.5 -346 2
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cells
ChEMBL 536 7 2 8 3.6 COc1cc(C)ccc1S(=O)(=O)NC(=O)[C@@H](c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(=O)O)ccc12 10.1007/s00044-004-0021-y
CHEMBL2261359 85379 None 0 Human Binding pIC50 = 6.5 6.5 -346 2
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cells
ChEMBL 536 7 2 8 3.6 COc1cc(C)ccc1S(=O)(=O)NC(=O)[C@@H](c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(=O)O)ccc12 10.1007/s00044-004-0021-y
71458720 81715 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 665 13 1 12 4.7 COc1ccccc1Oc1c(NS(=O)(=O)Cc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
CHEMBL2163710 81715 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 665 13 1 12 4.7 COc1ccccc1Oc1c(NS(=O)(=O)Cc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
23445533 60432 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 454 6 1 5 5.0 Cc1ccc(CCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00133-9
CHEMBL175045 60432 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 454 6 1 5 5.0 Cc1ccc(CCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00133-9
10896412 205262 None 0 Pig Binding pIC50 = 7.5 7.5 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 504 9 1 7 5.6 CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc(OC)cc1OC)O2 10.1021/jm010382z
CHEMBL62277 205262 None 0 Pig Binding pIC50 = 7.5 7.5 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 504 9 1 7 5.6 CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc(OC)cc1OC)O2 10.1021/jm010382z
CHEMBL327350 213749 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]ET1 from Endothelin B receptor of rat cerebellumDisplacement of [125I]ET1 from Endothelin B receptor of rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)81215-4
44327585 161877 None 0 Rat Binding pIC50 = 6.5 6.5 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL 992 26 9 8 5.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C1CCCCC1)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL414082 161877 None 0 Rat Binding pIC50 = 6.5 6.5 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL 992 26 9 8 5.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C1CCCCC1)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
44368824 96880 None 0 Rat Binding pIC50 = 6.5 6.5 - 0
Binding affinity against endothelin receptor in rat cerebellar membrane (ET-B) from adult blue laurie ratBinding affinity against endothelin receptor in rat cerebellar membrane (ET-B) from adult blue laurie rat
ChEMBL 1595 31 19 20 0.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)NCCCCC(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)80156-6
77282142 96880 None 0 Rat Binding pIC50 = 6.5 6.5 - 0
Binding affinity against endothelin receptor in rat cerebellar membrane (ET-B) from adult blue laurie ratBinding affinity against endothelin receptor in rat cerebellar membrane (ET-B) from adult blue laurie rat
ChEMBL 1595 31 19 20 0.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)NCCCCC(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)80156-6
CHEMBL265164 96880 None 0 Rat Binding pIC50 = 6.5 6.5 - 0
Binding affinity against endothelin receptor in rat cerebellar membrane (ET-B) from adult blue laurie ratBinding affinity against endothelin receptor in rat cerebellar membrane (ET-B) from adult blue laurie rat
ChEMBL 1595 31 19 20 0.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)NCCCCC(=O)N[C@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)80156-6
10982740 205841 None 0 Pig Binding pIC50 = 6.5 6.5 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 422 5 1 5 5.4 CC(C)Oc1ccc2c(c1)C(C1CCCC1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
CHEMBL65353 205841 None 0 Pig Binding pIC50 = 6.5 6.5 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 422 5 1 5 5.4 CC(C)Oc1ccc2c(c1)C(C1CCCC1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
44371429 48914 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 455 6 1 6 5.2 COc1cccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2ccccc23)c1 10.1016/s0960-894x(99)00040-2
CHEMBL155973 48914 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 455 6 1 6 5.2 COc1cccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2ccccc23)c1 10.1016/s0960-894x(99)00040-2
11762291 100690 None 0 Pig Binding pIC50 = 5.5 5.5 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 460 6 1 6 5.2 COc1ccccc1C1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL292041 100690 None 0 Pig Binding pIC50 = 5.5 5.5 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 460 6 1 6 5.2 COc1ccccc1C1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
9807178 205449 None 0 Pig Binding pIC50 = 5.5 5.5 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 384 5 1 6 3.8 COC1=C(C(=O)O)[C@@H](c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL63121 205449 None 0 Pig Binding pIC50 = 5.5 5.5 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 384 5 1 6 3.8 COC1=C(C(=O)O)[C@@H](c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
10648006 161760 None 0 Human Binding pIC50 = 5.5 5.5 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 468 6 1 6 4.7 Cc1ccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1021/jm9700068
CHEMBL413093 161760 None 0 Human Binding pIC50 = 5.5 5.5 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 468 6 1 6 4.7 Cc1ccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1021/jm9700068
CHEMBL438194 216214 None 13 Rat Binding pIC50 = 5.5 5.5 - 0
Inhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar membranesInhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar membranes
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(-c2ccccc2)cc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00095a029
9848132 210036 None 0 Pig Binding pIC50 = 5.5 5.5 - 2
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranes
ChEMBL 483 6 1 8 2.8 Cc1cc(C)c(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)n1 10.1016/S0960-894X(96)00617-8
CHEMBL94918 210036 None 0 Pig Binding pIC50 = 5.5 5.5 - 2
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranes
ChEMBL 483 6 1 8 2.8 Cc1cc(C)c(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)n1 10.1016/S0960-894X(96)00617-8
44368417 44663 None 0 Pig Binding pIC50 = 4.5 4.5 - 0
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 504 12 2 6 4.9 COc1ccc(CN(Cc2cc(OC)c(OC)c(OC)c2)C(Cc2c[nH]c3ccccc23)C(=O)O)cc1 10.1016/s0960-894x(01)00009-9
CHEMBL152065 44663 None 0 Pig Binding pIC50 = 4.5 4.5 - 0
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 504 12 2 6 4.9 COc1ccc(CN(Cc2cc(OC)c(OC)c(OC)c2)C(Cc2c[nH]c3ccccc23)C(=O)O)cc1 10.1016/s0960-894x(01)00009-9
18617302 104472 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 334 3 1 4 2.7 Cc1noc(NS(=O)(=O)c2ccccc2F)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL310361 104472 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 334 3 1 4 2.7 Cc1noc(NS(=O)(=O)c2ccccc2F)c1Br 10.1016/0960-894X(96)00441-6
44298394 163130 None 0 Pig Binding pIC50 = 4.5 4.5 - 0
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptor
ChEMBL 340 4 1 5 3.8 CSc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)noc1C 10.1016/s0960-894x(00)00366-8
CHEMBL417595 163130 None 0 Pig Binding pIC50 = 4.5 4.5 - 0
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptor
ChEMBL 340 4 1 5 3.8 CSc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)noc1C 10.1016/s0960-894x(00)00366-8
10575356 9711 None 0 Pig Binding pIC50 = 4.5 4.5 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 446 8 1 4 3.7 CCCN(C)C(=O)CN1C[C@H](c2ccc(F)c(F)c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL113184 9711 None 0 Pig Binding pIC50 = 4.5 4.5 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 446 8 1 4 3.7 CCCN(C)C(=O)CN1C[C@H](c2ccc(F)c(F)c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
10298764 9856 None 0 Pig Binding pIC50 = 4.5 4.5 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 468 8 1 6 3.2 CCCN(C)C(=O)CN1C[C@H](c2ccc3c(c2)OCCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL114084 9856 None 0 Pig Binding pIC50 = 4.5 4.5 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 468 8 1 6 3.2 CCCN(C)C(=O)CN1C[C@H](c2ccc3c(c2)OCCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
10647182 109778 None 0 Pig Binding pIC50 = 4.5 4.5 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 449 8 2 4 3.9 CCCN(C)C(=O)CN1C[C@H](c2ccc3cc[nH]c3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL322935 109778 None 0 Pig Binding pIC50 = 4.5 4.5 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 449 8 2 4 3.9 CCCN(C)C(=O)CN1C[C@H](c2ccc3cc[nH]c3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
10765567 111417 None 0 Pig Binding pIC50 = 4.5 4.5 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 440 9 1 5 3.4 CCCN(C)C(=O)CN1C[C@H](c2cccc(OC)c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL326951 111417 None 0 Pig Binding pIC50 = 4.5 4.5 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 440 9 1 5 3.4 CCCN(C)C(=O)CN1C[C@H](c2cccc(OC)c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
10415822 129887 None 0 Pig Binding pIC50 = 4.5 4.5 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 579 9 3 7 4.7 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCOC23CCCCC3)nc1C(=O)O 10.1021/jm950592+
CHEMBL367551 129887 None 0 Pig Binding pIC50 = 4.5 4.5 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 579 9 3 7 4.7 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCOC23CCCCC3)nc1C(=O)O 10.1021/jm950592+
44384610 128538 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 743 16 2 14 4.9 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2cc(OC)c(OC)c(OC)c2)nc1OCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
CHEMBL366627 128538 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 743 16 2 14 4.9 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2cc(OC)c(OC)c(OC)c2)nc1OCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
10813822 97023 None 0 Pig Binding pIC50 = 5.5 5.5 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 460 5 2 5 4.5 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2C(=O)Nc2ccccc2)cc1 10.1021/jm9505369
CHEMBL266336 97023 None 0 Pig Binding pIC50 = 5.5 5.5 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 460 5 2 5 4.5 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2C(=O)Nc2ccccc2)cc1 10.1021/jm9505369
22998447 209133 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 414 5 1 6 4.4 Cc1noc(NS(=O)(=O)c2sccc2Oc2ccccc2)c1Br 10.1016/S0960-894X(96)00496-9
CHEMBL89457 209133 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 414 5 1 6 4.4 Cc1noc(NS(=O)(=O)c2sccc2Oc2ccccc2)c1Br 10.1016/S0960-894X(96)00496-9
10226215 101487 None 0 Human Binding pIC50 = 4.5 4.5 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 455 5 2 8 3.8 Cc1cc2c(cc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl)OCO2 10.1021/jm9608366
CHEMBL297473 101487 None 0 Human Binding pIC50 = 4.5 4.5 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 455 5 2 8 3.8 Cc1cc2c(cc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl)OCO2 10.1021/jm9608366
10648715 109725 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 488 14 1 5 5.1 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCCC(C)C 10.1021/jm980217s
CHEMBL322547 109725 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 488 14 1 5 5.1 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCCC(C)C 10.1021/jm980217s
10598270 96997 None 0 Pig Binding pIC50 = 5.5 5.5 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 421 6 1 5 4.1 CCCC#CCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL266144 96997 None 0 Pig Binding pIC50 = 5.5 5.5 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 421 6 1 5 4.1 CCCC#CCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
10302092 111400 None 0 Pig Binding pIC50 = 7.4 7.4 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 532 12 1 7 3.7 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)CCC 10.1021/jm970101g
CHEMBL326861 111400 None 0 Pig Binding pIC50 = 7.4 7.4 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 532 12 1 7 3.7 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)CCC 10.1021/jm970101g
CHEMBL327350 213749 None 0 Rat Binding pIC50 = 7.4 7.4 - 0
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00070a001
10907399 205414 None 0 Pig Binding pIC50 = 5.4 5.4 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 516 11 1 6 6.8 CCCCOc1ccc(C2Oc3ccc(OCCCC)cc3C(c3ccc4c(c3)OCO4)=C2C(=O)O)cc1 10.1021/jm010382z
CHEMBL62976 205414 None 0 Pig Binding pIC50 = 5.4 5.4 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 516 11 1 6 6.8 CCCCOc1ccc(C2Oc3ccc(OCCCC)cc3C(c3ccc4c(c3)OCO4)=C2C(=O)O)cc1 10.1021/jm010382z
10577405 9654 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 502 14 1 5 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1C(C)(C)CCCC 10.1021/jm980217s
CHEMBL112777 9654 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 502 14 1 5 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1C(C)(C)CCCC 10.1021/jm980217s
10767280 108724 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 486 14 1 5 5.1 C=C(C)CCC[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC 10.1021/jm980217s
CHEMBL320763 108724 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 486 14 1 5 5.1 C=C(C)CCC[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC 10.1021/jm980217s
44277367 106894 None 0 Rat Binding pIC50 = 4.4 4.4 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 392 4 2 5 3.3 O=c1c(Cc2ccc3c(c2)OCO3)c(C(F)(F)F)[nH]n1Cc1cccc(O)c1 10.1016/s0960-894x(00)00232-8
CHEMBL3144606 106894 None 0 Rat Binding pIC50 = 4.4 4.4 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 392 4 2 5 3.3 O=c1c(Cc2ccc3c(c2)OCO3)c(C(F)(F)F)[nH]n1Cc1cccc(O)c1 10.1016/s0960-894x(00)00232-8
10168195 61407 None 0 Human Binding pIC50 = 6.4 6.4 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 631 11 2 13 5.0 C#CCOc1nc(-c2ccnc(-c3noc(S)n3)c2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL176999 61407 None 0 Human Binding pIC50 = 6.4 6.4 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 631 11 2 13 5.0 C#CCOc1nc(-c2ccnc(-c3noc(S)n3)c2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
18184179 129090 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 654 13 2 12 4.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2ccncc2)nc1OCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
CHEMBL367017 129090 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 654 13 2 12 4.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2ccncc2)nc1OCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
CHEMBL421190 215729 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Binding affinity measured in CHO cells stably transfected with the human endothelin B receptorBinding affinity measured in CHO cells stably transfected with the human endothelin B receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL94525 218401 None 0 Rat Binding pIC50 = 5.4 5.4 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00015a003
18617322 207918 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 350 3 1 4 3.2 Cc1noc(NS(=O)(=O)c2ccccc2Cl)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL80438 207918 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 350 3 1 4 3.2 Cc1noc(NS(=O)(=O)c2ccccc2Cl)c1Br 10.1016/0960-894X(96)00441-6
44385593 129542 None 0 Pig Binding pIC50 = 4.4 4.4 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 530 10 5 5 4.5 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)Nc2ccccc2)nc1C(=O)O 10.1021/jm950592+
CHEMBL367208 129542 None 0 Pig Binding pIC50 = 4.4 4.4 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 530 10 5 5 4.5 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)Nc2ccccc2)nc1C(=O)O 10.1021/jm950592+
10839533 101500 None 0 Human Binding pIC50 = 4.4 4.4 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 513 5 2 9 2.9 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)NC(=O)c2ccc3c(c2)OCO3)c1Br 10.1021/jm9700068
CHEMBL297599 101500 None 0 Human Binding pIC50 = 4.4 4.4 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 513 5 2 9 2.9 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)NC(=O)c2ccc3c(c2)OCO3)c1Br 10.1021/jm9700068
10742446 209470 None 0 Pig Binding pIC50 = 5.4 5.4 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 456 9 2 7 2.0 COCCNC(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL9147 209470 None 0 Pig Binding pIC50 = 5.4 5.4 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 456 9 2 7 2.0 COCCNC(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
71460535 81716 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 693 15 1 12 5.1 COc1ccccc1Oc1c(NS(=O)(=O)CCCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
CHEMBL2163711 81716 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 693 15 1 12 5.1 COc1ccccc1Oc1c(NS(=O)(=O)CCCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
10624915 208691 None 0 Pig Binding pIC50 = 5.4 5.4 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 490 6 2 6 4.5 COc1ccc(NC(=O)N2C[C@@H](c3ccc4c(c3)OCO4)[C@H](C(=O)O)[C@H]2c2ccc(OC)cc2)cc1 10.1021/jm9505369
CHEMBL8671 208691 None 0 Pig Binding pIC50 = 5.4 5.4 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 490 6 2 6 4.5 COc1ccc(NC(=O)N2C[C@@H](c3ccc4c(c3)OCO4)[C@H](C(=O)O)[C@H]2c2ccc(OC)cc2)cc1 10.1021/jm9505369
9938571 9599 None 0 Human Binding pIC50 = 7.4 7.4 - 1
Ability to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptorAbility to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptor
ChEMBL 597 9 1 8 5.6 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm000538f
CHEMBL112531 9599 None 0 Human Binding pIC50 = 7.4 7.4 - 1
Ability to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptorAbility to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptor
ChEMBL 597 9 1 8 5.6 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm000538f
CHEMBL369489 9599 None 0 Human Binding pIC50 = 7.4 7.4 - 1
Ability to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptorAbility to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptor
ChEMBL 597 9 1 8 5.6 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm000538f
9938571 9599 None 0 Human Binding pIC50 = 7.4 7.4 - 1
In vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptorIn vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptor
ChEMBL 597 9 1 8 5.6 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm0102304
CHEMBL112531 9599 None 0 Human Binding pIC50 = 7.4 7.4 - 1
In vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptorIn vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptor
ChEMBL 597 9 1 8 5.6 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm0102304
CHEMBL369489 9599 None 0 Human Binding pIC50 = 7.4 7.4 - 1
In vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptorIn vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptor
ChEMBL 597 9 1 8 5.6 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm0102304
9807691 100118 None 0 Human Binding pIC50 = 6.4 6.4 - 1
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 553 10 1 10 5.3 COc1cc2c(Sc3cc(OC)c(OC)c(OC)c3)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OC 10.1016/0960-894X(96)00232-6
CHEMBL287169 100118 None 0 Human Binding pIC50 = 6.4 6.4 - 1
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 553 10 1 10 5.3 COc1cc2c(Sc3cc(OC)c(OC)c(OC)c3)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OC 10.1016/0960-894X(96)00232-6
18617344 207736 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 361 4 1 6 2.5 Cc1noc(NS(=O)(=O)c2ccc([N+](=O)[O-])cc2)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL79080 207736 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 361 4 1 6 2.5 Cc1noc(NS(=O)(=O)c2ccc([N+](=O)[O-])cc2)c1Br 10.1016/0960-894X(96)00441-6
18617395 207730 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 361 4 1 6 2.5 Cc1noc(NS(=O)(=O)c2cccc([N+](=O)[O-])c2)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL79030 207730 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 361 4 1 6 2.5 Cc1noc(NS(=O)(=O)c2cccc([N+](=O)[O-])c2)c1Br 10.1016/0960-894X(96)00441-6
10789279 209023 None 0 Pig Binding pIC50 = 5.4 5.4 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 441 10 1 6 4.1 CCCCOCCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL8878 209023 None 0 Pig Binding pIC50 = 5.4 5.4 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 441 10 1 6 4.1 CCCCOCCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
44327347 96816 None 0 Rat Binding pIC50 = 6.4 6.4 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL 1102 26 9 8 7.1 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C1c2ccccc2CCc2ccccc21)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL264579 96816 None 0 Rat Binding pIC50 = 6.4 6.4 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL 1102 26 9 8 7.1 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C1c2ccccc2CCc2ccccc21)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
10765171 7897 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 432 7 1 6 4.1 COc1ccc(C2(O)OC(=O)C(c3ccc(OC)c(OC)c3)=C2Cc2ccccc2)cc1 10.1021/jm9606507
CHEMBL10901 7897 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 432 7 1 6 4.1 COc1ccc(C2(O)OC(=O)C(c3ccc(OC)c(OC)c3)=C2Cc2ccccc2)cc1 10.1021/jm9606507
10503921 101531 None 0 Human Binding pIC50 = 5.4 5.4 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 454 6 1 8 4.0 Cc1cc2c(cc1CC(=O)c1sccc1S(=O)(=O)Nc1noc(C)c1Cl)OCO2 10.1021/jm9700068
CHEMBL297783 101531 None 0 Human Binding pIC50 = 5.4 5.4 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 454 6 1 8 4.0 Cc1cc2c(cc1CC(=O)c1sccc1S(=O)(=O)Nc1noc(C)c1Cl)OCO2 10.1021/jm9700068
18617318 105669 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 394 3 1 4 3.3 Cc1noc(NS(=O)(=O)c2ccccc2Br)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL312266 105669 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 394 3 1 4 3.3 Cc1noc(NS(=O)(=O)c2ccccc2Br)c1Br 10.1016/0960-894X(96)00441-6
44277245 106903 None 0 Rat Binding pIC50 = 4.4 4.4 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 392 6 1 4 3.9 COc1ccc(Cc2c(C(F)(F)F)[nH]n(Cc3cccc(OC)c3)c2=O)cc1 10.1016/s0960-894x(00)00232-8
CHEMBL3144736 106903 None 0 Rat Binding pIC50 = 4.4 4.4 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 392 6 1 4 3.9 COc1ccc(Cc2c(C(F)(F)F)[nH]n(Cc3cccc(OC)c3)c2=O)cc1 10.1016/s0960-894x(00)00232-8
16004692 2454 None 59 Human Binding pIC50 = 6.4 6.4 - 1
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 10.1016/j.bmcl.2016.06.014
16004692.0 2454 None 59 Human Binding pIC50 = 6.4 6.4 - 1
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 10.1016/j.bmcl.2016.06.014
4809 2454 None 59 Human Binding pIC50 = 6.4 6.4 - 1
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 10.1016/j.bmcl.2016.06.014
7352 2454 None 59 Human Binding pIC50 = 6.4 6.4 - 1
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 10.1016/j.bmcl.2016.06.014
CHEMBL2103873 2454 None 59 Human Binding pIC50 = 6.4 6.4 - 1
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 10.1016/j.bmcl.2016.06.014
DB08932 2454 None 59 Human Binding pIC50 = 6.4 6.4 - 1
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 10.1016/j.bmcl.2016.06.014
16004692 2454 None 59 Human Binding pIC50 = 6.4 6.4 - 1
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 10.1021/jm3009103
16004692.0 2454 None 59 Human Binding pIC50 = 6.4 6.4 - 1
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 10.1021/jm3009103
4809 2454 None 59 Human Binding pIC50 = 6.4 6.4 - 1
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 10.1021/jm3009103
7352 2454 None 59 Human Binding pIC50 = 6.4 6.4 - 1
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 10.1021/jm3009103
CHEMBL2103873 2454 None 59 Human Binding pIC50 = 6.4 6.4 - 1
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 10.1021/jm3009103
DB08932 2454 None 59 Human Binding pIC50 = 6.4 6.4 - 1
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 10.1021/jm3009103
9915510 85189 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
ChEMBL 549 8 2 8 3.4 CCOc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(N)=O)ccc12 10.1016/s0960-894x(01)00660-6
CHEMBL22513 85189 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
ChEMBL 549 8 2 8 3.4 CCOc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(N)=O)ccc12 10.1016/s0960-894x(01)00660-6
9915510 85189 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cells
ChEMBL 549 8 2 8 3.4 CCOc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(N)=O)ccc12 10.1007/s00044-004-0021-y
CHEMBL22513 85189 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cells
ChEMBL 549 8 2 8 3.4 CCOc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(N)=O)ccc12 10.1007/s00044-004-0021-y
9873255 59653 None 0 Human Binding pIC50 = 6.4 6.4 - 2
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 591 14 2 10 3.8 CCS(=O)(=O)NCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
CHEMBL172071 59653 None 0 Human Binding pIC50 = 6.4 6.4 - 2
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 591 14 2 10 3.8 CCS(=O)(=O)NCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
10719598 209448 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Radioligand binding selectivity to human Endothelin B receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin B receptor in chinese hamster ovary cells
ChEMBL 482 10 1 6 3.9 CCCN(CCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL9139 209448 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Radioligand binding selectivity to human Endothelin B receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin B receptor in chinese hamster ovary cells
ChEMBL 482 10 1 6 3.9 CCCN(CCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
44339655 9108 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)
ChEMBL 530 14 1 6 5.3 C/C=C\C(C)(C)C[C@H]1[C@H](C(=O)O)[C@@H](c2cc(OC)c3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC 10.1021/jm980217s
CHEMBL109926 9108 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)
ChEMBL 530 14 1 6 5.3 C/C=C\C(C)(C)C[C@H]1[C@H](C(=O)O)[C@@H](c2cc(OC)c3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC 10.1021/jm980217s
23445254 209613 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 412 5 1 5 4.2 Cc1noc(NS(=O)(=O)c2sccc2Cc2ccccc2)c1Br 10.1016/S0960-894X(96)00496-9
CHEMBL92318 209613 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 412 5 1 5 4.2 Cc1noc(NS(=O)(=O)c2sccc2Cc2ccccc2)c1Br 10.1016/S0960-894X(96)00496-9
10599230 209453 None 0 Pig Binding pIC50 = 6.4 6.4 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 440 8 2 6 2.8 CCCNC(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL9141 209453 None 0 Pig Binding pIC50 = 6.4 6.4 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 440 8 2 6 2.8 CCCNC(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
44314904 103202 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Binding affinity towards Endothelin B receptor in human girardi heart cell membranesBinding affinity towards Endothelin B receptor in human girardi heart cell membranes
ChEMBL 585 12 5 5 3.6 CSCCC(NC(=O)[C@@H](Cc1c(C)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)O 10.1021/jm9600914
CHEMBL307936 103202 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Binding affinity towards Endothelin B receptor in human girardi heart cell membranesBinding affinity towards Endothelin B receptor in human girardi heart cell membranes
ChEMBL 585 12 5 5 3.6 CSCCC(NC(=O)[C@@H](Cc1c(C)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)O 10.1021/jm9600914
10529868 164286 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 516 8 2 6 4.8 CCc1cccc(C)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm990170q
CHEMBL421073 164286 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 516 8 2 6 4.8 CCc1cccc(C)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm990170q
9917706 129807 None 0 Human Binding pIC50 = 8.4 8.4 - 2
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 659 15 2 11 5.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(C2CC2)nc1OCCCNS(=O)(=O)c1cccs1 10.1016/j.bmcl.2016.06.014
CHEMBL367444 129807 None 0 Human Binding pIC50 = 8.4 8.4 - 2
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 659 15 2 11 5.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(C2CC2)nc1OCCCNS(=O)(=O)c1cccs1 10.1016/j.bmcl.2016.06.014
44320777 208663 None 0 Rat Binding pIC50 = 8.4 8.4 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 550 10 2 8 4.7 COc1ccc(Cn2nc(-c3ccccc3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)c(OCC(=O)O)c1 10.1016/s0960-894x(00)00513-8
CHEMBL86505 208663 None 0 Rat Binding pIC50 = 8.4 8.4 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 550 10 2 8 4.7 COc1ccc(Cn2nc(-c3ccccc3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)c(OCC(=O)O)c1 10.1016/s0960-894x(00)00513-8
9897092 59956 None 0 Human Binding pIC50 = 8.4 8.4 - 1
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 779 17 2 13 6.0 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2cc(OC)c(OC)c(OC)c2)nc1OCCNS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(02)01083-1
CHEMBL173201 59956 None 0 Human Binding pIC50 = 8.4 8.4 - 1
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 779 17 2 13 6.0 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2cc(OC)c(OC)c(OC)c2)nc1OCCNS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(02)01083-1
9810400 98660 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 710 14 2 12 5.6 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
CHEMBL276949 98660 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 710 14 2 12 5.6 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
9917706 129807 None 0 Human Binding pIC50 = 8.4 8.4 - 2
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 659 15 2 11 5.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(C2CC2)nc1OCCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
CHEMBL367444 129807 None 0 Human Binding pIC50 = 8.4 8.4 - 2
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 659 15 2 11 5.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(C2CC2)nc1OCCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
10209779 163526 None 0 Pig Binding pIC50 = 8.4 8.4 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 560 14 1 7 4.5 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm970101g
CHEMBL419749 163526 None 0 Pig Binding pIC50 = 8.4 8.4 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 560 14 1 7 4.5 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm970101g
44314659 207578 None 0 Pig Binding pIC50 = 8.4 8.4 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 631 12 5 4 4.5 C=CCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
CHEMBL77853 207578 None 0 Pig Binding pIC50 = 8.4 8.4 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 631 12 5 4 4.5 C=CCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
9894460 209167 None 11 Human Binding pIC50 = 8.4 8.4 -41 3
Ability to displace endothelin ([125I]ET1) from human Endothelin B receptorAbility to displace endothelin ([125I]ET1) from human Endothelin B receptor
ChEMBL 539 10 2 7 4.8 CCCc1cc(C(=O)O)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2 10.1021/jm970101g
CHEMBL313871 209167 None 11 Human Binding pIC50 = 8.4 8.4 -41 3
Ability to displace endothelin ([125I]ET1) from human Endothelin B receptorAbility to displace endothelin ([125I]ET1) from human Endothelin B receptor
ChEMBL 539 10 2 7 4.8 CCCc1cc(C(=O)O)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2 10.1021/jm970101g
CHEMBL8978 209167 None 11 Human Binding pIC50 = 8.4 8.4 -41 3
Ability to displace endothelin ([125I]ET1) from human Endothelin B receptorAbility to displace endothelin ([125I]ET1) from human Endothelin B receptor
ChEMBL 539 10 2 7 4.8 CCCc1cc(C(=O)O)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2 10.1021/jm970101g
10303555 163476 None 0 Pig Binding pIC50 = 8.4 8.4 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 574 15 1 7 4.9 CCCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm970101g
CHEMBL419383 163476 None 0 Pig Binding pIC50 = 8.4 8.4 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 574 15 1 7 4.9 CCCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm970101g
1009 194 None 25 Human Binding pIC50 = 8.4 8.4 676 2
Affinity Biochemical interaction (Inhibition of 125I labeled ET-3 binding) EUB0000350a EDNRBAffinity Biochemical interaction (Inhibition of 125I labeled ET-3 binding) EUB0000350a EDNRB
ChEMBL 558 11 2 6 5.8 CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2 10.6019/CHEMBL5210307
5310991 194 None 25 Human Binding pIC50 = 8.4 8.4 676 2
Affinity Biochemical interaction (Inhibition of 125I labeled ET-3 binding) EUB0000350a EDNRBAffinity Biochemical interaction (Inhibition of 125I labeled ET-3 binding) EUB0000350a EDNRB
ChEMBL 558 11 2 6 5.8 CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2 10.6019/CHEMBL5210307
CHEMBL332794 194 None 25 Human Binding pIC50 = 8.4 8.4 676 2
Affinity Biochemical interaction (Inhibition of 125I labeled ET-3 binding) EUB0000350a EDNRBAffinity Biochemical interaction (Inhibition of 125I labeled ET-3 binding) EUB0000350a EDNRB
ChEMBL 558 11 2 6 5.8 CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2 10.6019/CHEMBL5210307
44315009 103261 None 0 Pig Binding pIC50 = 8.4 8.4 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 665 13 5 5 4.7 CSCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
CHEMBL308403 103261 None 0 Pig Binding pIC50 = 8.4 8.4 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 665 13 5 5 4.7 CSCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
1009 194 None 25 Human Binding pIC50 = 8.4 8.4 676 2
Inhibition of 125I labeled ET-3 binding to EDNRBInhibition of 125I labeled ET-3 binding to EDNRB
ChEMBL 558 11 2 6 5.8 CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2 10.6019/CHEMBL4507261
5310991 194 None 25 Human Binding pIC50 = 8.4 8.4 676 2
Inhibition of 125I labeled ET-3 binding to EDNRBInhibition of 125I labeled ET-3 binding to EDNRB
ChEMBL 558 11 2 6 5.8 CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2 10.6019/CHEMBL4507261
CHEMBL332794 194 None 25 Human Binding pIC50 = 8.4 8.4 676 2
Inhibition of 125I labeled ET-3 binding to EDNRBInhibition of 125I labeled ET-3 binding to EDNRB
ChEMBL 558 11 2 6 5.8 CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2 10.6019/CHEMBL4507261
44314675 98181 None 0 Pig Binding pIC50 = 8.3 8.3 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 603 13 5 4 5.0 CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)CC)C(=O)O 10.1021/jm9600914
CHEMBL273583 98181 None 0 Pig Binding pIC50 = 8.3 8.3 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 603 13 5 4 5.0 CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)CC)C(=O)O 10.1021/jm9600914
44314676 102979 None 0 Pig Binding pIC50 = 8.3 8.3 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 589 12 5 4 4.6 CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)C)C(=O)O 10.1021/jm9600914
CHEMBL306171 102979 None 0 Pig Binding pIC50 = 8.3 8.3 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 589 12 5 4 4.6 CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)C)C(=O)O 10.1021/jm9600914
17885919 208868 None 0 Rat Binding pIC50 = 8.3 8.3 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 526 9 2 8 4.8 O=C(O)COc1ccccc1Cn1nc(-c2cccs2)c(Cc2cc3c(cc2Cl)OCO3)c1C(=O)O 10.1016/s0960-894x(00)00513-8
CHEMBL87801 208868 None 0 Rat Binding pIC50 = 8.3 8.3 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 526 9 2 8 4.8 O=C(O)COc1ccccc1Cn1nc(-c2cccs2)c(Cc2cc3c(cc2Cl)OCO3)c1C(=O)O 10.1016/s0960-894x(00)00513-8
44320171 107013 None 0 Rat Binding pIC50 = 8.3 8.3 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 504 6 1 5 6.4 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1CC12CC3CC(CC(C3)C1)C2 10.1016/s0960-894x(00)00513-8
CHEMBL314974 107013 None 0 Rat Binding pIC50 = 8.3 8.3 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 504 6 1 5 6.4 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1CC12CC3CC(CC(C3)C1)C2 10.1016/s0960-894x(00)00513-8
10252787 99320 None 0 Rat Binding pIC50 = 7.4 7.4 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 442 7 1 6 4.6 COc1cccc(Cn2nc(-c3ccccc3)c(Cc3ccc4c(c3)OCO4)c2C(=O)O)c1 10.1016/s0960-894x(00)00232-8
CHEMBL281865 99320 None 0 Rat Binding pIC50 = 7.4 7.4 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 442 7 1 6 4.6 COc1cccc(Cn2nc(-c3ccccc3)c(Cc3ccc4c(c3)OCO4)c2C(=O)O)c1 10.1016/s0960-894x(00)00232-8
CHEMBL1790519 211352 None 0 Rat Binding pIC50 = 7.4 7.4 - 0
Inhibition of binding to Endothelin B receptor of rat cerebellar membranes.Inhibition of binding to Endothelin B receptor of rat cerebellar membranes.
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N(C)[C@@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@H](C)CC 10.1021/jm970161m
10648937 209765 None 0 Pig Binding pIC50 = 7.4 7.4 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 496 11 1 6 4.3 CCCCN(CCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL9334 209765 None 0 Pig Binding pIC50 = 7.4 7.4 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 496 11 1 6 4.3 CCCCN(CCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
44327466 96504 None 0 Rat Binding pIC50 = 6.4 6.4 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL 966 25 9 8 5.2 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C(C)(C)C)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL262229 96504 None 0 Rat Binding pIC50 = 6.4 6.4 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL 966 25 9 8 5.2 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C(C)(C)C)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
11103152 163335 None 0 Pig Binding pIC50 = 6.4 6.4 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 504 9 1 7 5.6 CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc(OC)c(OC)c1)O2 10.1021/jm010382z
CHEMBL418473 163335 None 0 Pig Binding pIC50 = 6.4 6.4 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 504 9 1 7 5.6 CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc(OC)c(OC)c1)O2 10.1021/jm010382z
10364227 205257 None 0 Pig Binding pIC50 = 6.4 6.4 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 410 7 1 5 5.4 CCCCC1=C(C(=O)O)[C@@H](c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL62264 205257 None 0 Pig Binding pIC50 = 6.4 6.4 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 410 7 1 5 5.4 CCCCC1=C(C(=O)O)[C@@H](c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
11059349 205967 None 0 Pig Binding pIC50 = 6.4 6.4 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 446 6 1 6 4.8 CCOc1ccc2c(c1)C(c1ccc(OC)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
CHEMBL66264 205967 None 0 Pig Binding pIC50 = 6.4 6.4 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 446 6 1 6 4.8 CCOc1ccc2c(c1)C(c1ccc(OC)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
44298279 196591 None 0 Pig Binding pIC50 = 6.4 6.4 - 0
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptor
ChEMBL 502 10 1 7 5.8 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCC(C)=O)c1 10.1016/s0960-894x(00)00366-8
CHEMBL54274 196591 None 0 Pig Binding pIC50 = 6.4 6.4 - 0
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptor
ChEMBL 502 10 1 7 5.8 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCC(C)=O)c1 10.1016/s0960-894x(00)00366-8
10239569 14794 None 0 Pig Binding pIC50 = 6.4 6.4 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 534 9 1 10 4.4 COc1cc(C/C(C(=O)c2ccc3c(c2)OCO3)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC 10.1016/s0960-894x(98)00301-1
CHEMBL1206715 14794 None 0 Pig Binding pIC50 = 6.4 6.4 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 534 9 1 10 4.4 COc1cc(C/C(C(=O)c2ccc3c(c2)OCO3)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC 10.1016/s0960-894x(98)00301-1
CHEMBL299328 14794 None 0 Pig Binding pIC50 = 6.4 6.4 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 534 9 1 10 4.4 COc1cc(C/C(C(=O)c2ccc3c(c2)OCO3)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC 10.1016/s0960-894x(98)00301-1
10364227 205257 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibitory concentration against Endothelin B receptorInhibitory concentration against Endothelin B receptor
ChEMBL 410 7 1 5 5.4 CCCCC1=C(C(=O)O)[C@@H](c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm031041j
CHEMBL62264 205257 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibitory concentration against Endothelin B receptorInhibitory concentration against Endothelin B receptor
ChEMBL 410 7 1 5 5.4 CCCCC1=C(C(=O)O)[C@@H](c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm031041j
18617355 207412 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 330 3 1 4 2.9 Cc1ccc(S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/0960-894X(96)00441-6
CHEMBL76438 207412 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 330 3 1 4 2.9 Cc1ccc(S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/0960-894X(96)00441-6
11026419 205640 None 0 Pig Binding pIC50 = 5.4 5.4 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 432 5 1 6 4.5 COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3c(OC)cccc32)cc1 10.1021/jm010382z
CHEMBL64266 205640 None 0 Pig Binding pIC50 = 5.4 5.4 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 432 5 1 6 4.5 COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3c(OC)cccc32)cc1 10.1021/jm010382z
CHEMBL2370070 212238 None 0 Rat Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]ET1 from Endothelin B receptor of rat cerebellumDisplacement of [125I]ET1 from Endothelin B receptor of rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCN)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)81215-4
CHEMBL315047 213645 None 0 Rat Binding pIC50 = 5.4 5.4 - 0
Inhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar membranesInhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar membranes
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00095a029
10718385 209269 None 0 Pig Binding pIC50 = 5.4 5.4 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 450 7 1 6 2.4 C#CCN(C)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL9040 209269 None 0 Pig Binding pIC50 = 5.4 5.4 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 450 7 1 6 2.4 C#CCN(C)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
10550844 97362 None 0 Pig Binding pIC50 = 4.4 4.4 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 435 5 1 6 3.7 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2C(=O)c2ccco2)cc1 10.1021/jm9505369
CHEMBL269140 97362 None 0 Pig Binding pIC50 = 4.4 4.4 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 435 5 1 6 3.7 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2C(=O)c2ccco2)cc1 10.1021/jm9505369
10553316 97129 None 0 Pig Binding pIC50 = 6.4 6.4 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 496 11 1 6 4.3 CCCCCCN(C)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL267279 97129 None 0 Pig Binding pIC50 = 6.4 6.4 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 496 11 1 6 4.3 CCCCCCN(C)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
10205245 72233 None 0 Human Binding pIC50 = 4.4 4.4 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 466 5 2 9 3.4 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2C#N)OCO3)c1Cl 10.1021/jm9608366
CHEMBL19808 72233 None 0 Human Binding pIC50 = 4.4 4.4 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 466 5 2 9 3.4 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2C#N)OCO3)c1Cl 10.1021/jm9608366
44291575 179541 None 0 Human Binding pIC50 = 4.4 4.4 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 466 5 2 9 3.4 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc3c(c2C#N)OCO3)c1Cl 10.1021/jm9700068
CHEMBL47404 179541 None 0 Human Binding pIC50 = 4.4 4.4 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 466 5 2 9 3.4 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc3c(c2C#N)OCO3)c1Cl 10.1021/jm9700068
137642741 158331 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 553 9 2 9 4.2 CCOc1ccc2c(c1)c(=O)c(Cc1cccc(-c3nnn[nH]3)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL4088349 158331 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 553 9 2 9 4.2 CCOc1ccc2c(c1)c(=O)c(Cc1cccc(-c3nnn[nH]3)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2017.04.049
10005597 119882 None 0 Human Binding pIC50 = 7.4 7.4 - 1
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 485 7 1 7 5.2 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3cc(OC)ccc3OC)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(99)00040-2
CHEMBL348407 119882 None 0 Human Binding pIC50 = 7.4 7.4 - 1
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 485 7 1 7 5.2 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3cc(OC)ccc3OC)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(99)00040-2
10531650 168364 None 0 Pig Binding pIC50 = 7.4 7.4 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 600 11 1 7 5.0 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)c1ccc(Cl)cc1 10.1021/jm970101g
CHEMBL433842 168364 None 0 Pig Binding pIC50 = 7.4 7.4 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 600 11 1 7 5.0 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)c1ccc(Cl)cc1 10.1021/jm970101g
9852318 9616 None 8 Pig Binding pIC50 = 7.4 7.4 - 2
Displacement of 125I-ET1 from pig ETB receptor transfected in grivet COS7 cellsDisplacement of 125I-ET1 from pig ETB receptor transfected in grivet COS7 cells
ChEMBL 613 11 2 9 4.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL112624 9616 None 8 Pig Binding pIC50 = 7.4 7.4 - 2
Displacement of 125I-ET1 from pig ETB receptor transfected in grivet COS7 cellsDisplacement of 125I-ET1 from pig ETB receptor transfected in grivet COS7 cells
ChEMBL 613 11 2 9 4.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL1627022 9616 None 8 Pig Binding pIC50 = 7.4 7.4 - 2
Displacement of 125I-ET1 from pig ETB receptor transfected in grivet COS7 cellsDisplacement of 125I-ET1 from pig ETB receptor transfected in grivet COS7 cells
ChEMBL 613 11 2 9 4.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1016/j.bmcl.2016.06.014
10578320 97363 None 0 Pig Binding pIC50 = 7.4 7.4 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 538 12 1 6 5.2 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(CCC(C)C)CCC(C)C)cc1 10.1021/jm9505369
CHEMBL269141 97363 None 0 Pig Binding pIC50 = 7.4 7.4 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 538 12 1 6 5.2 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(CCC(C)C)CCC(C)C)cc1 10.1021/jm9505369
10917653 205835 None 0 Pig Binding pIC50 = 6.4 6.4 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 468 11 1 6 6.1 CCCCCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL65292 205835 None 0 Pig Binding pIC50 = 6.4 6.4 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 468 11 1 6 6.1 CCCCCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
9821701 4614 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B receptor
ChEMBL 389 4 1 5 3.8 COc1ccc([C@@H]2c3ncccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1016/s0960-894x(02)00663-7
CHEMBL102825 4614 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B receptor
ChEMBL 389 4 1 5 3.8 COc1ccc([C@@H]2c3ncccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1016/s0960-894x(02)00663-7
10767586 9771 None 0 Pig Binding pIC50 = 5.4 5.4 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 496 13 1 5 5.0 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc(OC)cc2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL113529 9771 None 0 Pig Binding pIC50 = 5.4 5.4 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 496 13 1 5 5.0 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc(OC)cc2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
10602183 9241 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 525 13 1 7 3.6 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCn1ccccc1=O 10.1021/jm980217s
CHEMBL110695 9241 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 525 13 1 7 3.6 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCn1ccccc1=O 10.1021/jm980217s
44383537 59267 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Tested for binding affinity towards human Endothelin B receptorTested for binding affinity towards human Endothelin B receptor
ChEMBL 388 4 2 5 3.4 C/C=C/C=C/C=C/C(=O)O[C@@H]1C=C2COC(O)[C@]2(O)[C@@]2(C)CCCC(C)(C)C12 10.1016/s0960-894x(00)00136-0
CHEMBL170335 59267 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Tested for binding affinity towards human Endothelin B receptorTested for binding affinity towards human Endothelin B receptor
ChEMBL 388 4 2 5 3.4 C/C=C/C=C/C=C/C(=O)O[C@@H]1C=C2COC(O)[C@]2(O)[C@@]2(C)CCCC(C)(C)C12 10.1016/s0960-894x(00)00136-0
23445430 61086 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 438 5 1 5 5.1 Cc1ccc(/C=C/c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(97)00133-9
CHEMBL176422 61086 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 438 5 1 5 5.1 Cc1ccc(/C=C/c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(97)00133-9
44384652 61305 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 582 8 1 9 5.2 Cc1noc(NS(=O)(=O)c2sccc2/C=C/c2cc3c(cc2COC2CCOCC2)OCO3)c1Br 10.1016/S0960-894X(97)00133-9
CHEMBL176675 61305 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 582 8 1 9 5.2 Cc1noc(NS(=O)(=O)c2sccc2/C=C/c2cc3c(cc2COC2CCOCC2)OCO3)c1Br 10.1016/S0960-894X(97)00133-9
155519384 170521 None 0 Human Binding pIC50 = 7.4 7.4 - 1
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 674 12 1 13 4.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)c1ccccn1 10.1016/j.bmcl.2016.06.014
CHEMBL4448273 170521 None 0 Human Binding pIC50 = 7.4 7.4 - 1
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 674 12 1 13 4.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)c1ccccn1 10.1016/j.bmcl.2016.06.014
71458719 81709 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 647 15 1 13 4.7 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(SC)cn1 10.1021/jm3009103
CHEMBL2163704 81709 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 647 15 1 13 4.7 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(SC)cn1 10.1021/jm3009103
10146640 210013 None 0 Human Binding pIC50 = 7.4 7.4 - 1
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 689 12 2 13 4.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccccn1 10.1016/s0960-894x(02)01084-3
CHEMBL94786 210013 None 0 Human Binding pIC50 = 7.4 7.4 - 1
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 689 12 2 13 4.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccccn1 10.1016/s0960-894x(02)01084-3
10366278 172567 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B receptor
ChEMBL 446 6 2 6 4.6 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1016/s0960-894x(02)00663-7
CHEMBL448165 172567 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B receptor
ChEMBL 446 6 2 6 4.6 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1016/s0960-894x(02)00663-7
44278215 99612 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 491 5 1 9 4.7 O=C(O)c1c(Sc2ccc3c(c2)OCO3)c2cc3c(cc2n1Cc1ccc2c(c1)OCO2)OCO3 10.1016/0960-894X(96)00232-6
CHEMBL283598 99612 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 491 5 1 9 4.7 O=C(O)c1c(Sc2ccc3c(c2)OCO3)c2cc3c(cc2n1Cc1ccc2c(c1)OCO2)OCO3 10.1016/0960-894X(96)00232-6
18995986 99635 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 537 8 1 10 5.0 COc1ccc(Sc2c(C(=O)O)n(Cc3cc(OC)c4c(c3)OCO4)c3cc4c(cc23)OCO4)cc1OC 10.1016/0960-894X(96)00232-6
CHEMBL283858 99635 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 537 8 1 10 5.0 COc1ccc(Sc2c(C(=O)O)n(Cc3cc(OC)c4c(c3)OCO4)c3cc4c(cc23)OCO4)cc1OC 10.1016/0960-894X(96)00232-6
44270522 45820 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) receptor expressed in CHO cells
ChEMBL 744 15 1 10 8.2 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)NS(=O)(=O)c1ccc(CC(C)C)s1)c1ccc2c(c1)OCO2 10.1016/0960-894X(95)00186-W
CHEMBL15310 45820 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) receptor expressed in CHO cells
ChEMBL 744 15 1 10 8.2 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)NS(=O)(=O)c1ccc(CC(C)C)s1)c1ccc2c(c1)OCO2 10.1016/0960-894X(95)00186-W
44284183 139662 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 518 9 2 7 5.7 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(OCC(C)C)c1 10.1016/j.bmcl.2004.01.008
CHEMBL37973 139662 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 518 9 2 7 5.7 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(OCC(C)C)c1 10.1016/j.bmcl.2004.01.008
44386069 59755 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 704 13 2 11 5.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCNS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(02)01083-1
CHEMBL172441 59755 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 704 13 2 11 5.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCNS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(02)01083-1
44291495 11237 None 0 Human Binding pIC50 = 5.4 5.4 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 455 6 2 9 3.6 Cc1noc(NS(=O)(=O)c2ccsc2/C(Cc2ccc3c(c2)OCO3)=N\O)c1Cl 10.1021/jm9700068
CHEMBL1178832 11237 None 0 Human Binding pIC50 = 5.4 5.4 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 455 6 2 9 3.6 Cc1noc(NS(=O)(=O)c2ccsc2/C(Cc2ccc3c(c2)OCO3)=N\O)c1Cl 10.1021/jm9700068
CHEMBL45351 11237 None 0 Human Binding pIC50 = 5.4 5.4 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 455 6 2 9 3.6 Cc1noc(NS(=O)(=O)c2ccsc2/C(Cc2ccc3c(c2)OCO3)=N\O)c1Cl 10.1021/jm9700068
44213923 108337 None 0 Pig Binding pIC50 = 5.4 5.4 - 0
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranes
ChEMBL 563 8 1 8 4.1 COc1ccc(C2=NN(C(C(=O)NS(=O)(=O)c3ccc(C(C)C)cc3)c3ccc4c(c3)OCO4)C(=O)CC2)cc1 10.1016/S0960-894X(96)00617-8
CHEMBL319743 108337 None 0 Pig Binding pIC50 = 5.4 5.4 - 0
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranes
ChEMBL 563 8 1 8 4.1 COc1ccc(C2=NN(C(C(=O)NS(=O)(=O)c3ccc(C(C)C)cc3)c3ccc4c(c3)OCO4)C(=O)CC2)cc1 10.1016/S0960-894X(96)00617-8
11799440 209434 None 0 Pig Binding pIC50 = 5.4 5.4 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 496 11 1 6 4.3 CCCN(CCC)C(=O)CCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL9132 209434 None 0 Pig Binding pIC50 = 5.4 5.4 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 496 11 1 6 4.3 CCCN(CCC)C(=O)CCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
10506868 63277 None 0 Pig Binding pIC50 = 4.4 4.4 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 550 10 5 5 4.7 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCCC2)nc1C(=O)O 10.1021/jm950592+
CHEMBL179138 63277 None 0 Pig Binding pIC50 = 4.4 4.4 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 550 10 5 5 4.7 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCCC2)nc1C(=O)O 10.1021/jm950592+
10553384 109724 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)
ChEMBL 498 13 1 7 3.6 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCn1cccn1 10.1021/jm980217s
CHEMBL322537 109724 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)
ChEMBL 498 13 1 7 3.6 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCn1cccn1 10.1021/jm980217s
76308472 85388 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cells
ChEMBL 517 6 1 8 3.7 COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C#N)ccc12 10.1007/s00044-004-0021-y
CHEMBL2261600 85388 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cells
ChEMBL 517 6 1 8 3.7 COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C#N)ccc12 10.1007/s00044-004-0021-y
71451527 81711 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 641 15 1 12 4.8 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(C2CC2)cn1 10.1021/jm3009103
CHEMBL2163706 81711 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 641 15 1 12 4.8 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(C2CC2)cn1 10.1021/jm3009103
23445313 165732 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B receptor
ChEMBL 470 6 1 6 5.1 Cc1cc(C)c(OCc2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00132-7
CHEMBL424371 165732 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B receptor
ChEMBL 470 6 1 6 5.1 Cc1cc(C)c(OCc2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00132-7
23445421 59950 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 454 6 1 5 5.0 Cc1ccc(CCc2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00133-9
CHEMBL173189 59950 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 454 6 1 5 5.0 Cc1ccc(CCc2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00133-9
11005242 205353 None 0 Pig Binding pIC50 = 7.4 7.4 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 474 8 1 6 5.6 CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc(OC)cc1)O2 10.1021/jm010382z
CHEMBL62719 205353 None 0 Pig Binding pIC50 = 7.4 7.4 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 474 8 1 6 5.6 CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc(OC)cc1)O2 10.1021/jm010382z
44212539 206551 None 0 Human Binding pIC50 = 7.4 7.4 - 1
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta cell membranes
ChEMBL 671 12 2 12 5.9 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCOC(=O)Nc1ccccn1 10.1016/j.bmcl.2016.06.014
CHEMBL70203 206551 None 0 Human Binding pIC50 = 7.4 7.4 - 1
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta cell membranes
ChEMBL 671 12 2 12 5.9 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCOC(=O)Nc1ccccn1 10.1016/j.bmcl.2016.06.014
44284288 100189 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 559 9 2 7 4.9 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(C)C(=O)N(C)C)c1 10.1016/j.bmcl.2004.01.008
CHEMBL287683 100189 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 559 9 2 7 4.9 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(C)C(=O)N(C)C)c1 10.1016/j.bmcl.2004.01.008
44284266 137019 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 531 8 2 7 4.6 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CN(C)C(C)=O)c1 10.1016/j.bmcl.2004.01.008
CHEMBL37427 137019 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 531 8 2 7 4.6 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CN(C)C(C)=O)c1 10.1016/j.bmcl.2004.01.008
44212539 206551 None 0 Human Binding pIC50 = 7.4 7.4 - 1
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 671 12 2 12 5.9 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
CHEMBL70203 206551 None 0 Human Binding pIC50 = 7.4 7.4 - 1
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 671 12 2 12 5.9 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
44371449 49392 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 485 7 1 7 5.2 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2ccccc23)c(OC)c1 10.1016/s0960-894x(99)00040-2
CHEMBL156404 49392 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 485 7 1 7 5.2 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2ccccc23)c(OC)c1 10.1016/s0960-894x(99)00040-2
44298278 194779 None 0 Pig Binding pIC50 = 6.4 6.4 - 0
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptor
ChEMBL 462 8 2 7 4.5 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCO)c1 10.1016/s0960-894x(00)00366-8
CHEMBL53168 194779 None 0 Pig Binding pIC50 = 6.4 6.4 - 0
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptor
ChEMBL 462 8 2 7 4.5 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCO)c1 10.1016/s0960-894x(00)00366-8
44371670 141750 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Binding affinity in Chinese hamster ovary (CHO) cells stably transfected with human endothelin B (ETB) receptorBinding affinity in Chinese hamster ovary (CHO) cells stably transfected with human endothelin B (ETB) receptor
ChEMBL 1082 23 11 10 3.7 CC(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)C1c2ccccc2CCc2ccccc21 10.1016/0960-894X(95)00084-7
CHEMBL385405 141750 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Binding affinity in Chinese hamster ovary (CHO) cells stably transfected with human endothelin B (ETB) receptorBinding affinity in Chinese hamster ovary (CHO) cells stably transfected with human endothelin B (ETB) receptor
ChEMBL 1082 23 11 10 3.7 CC(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)C1c2ccccc2CCc2ccccc21 10.1016/0960-894X(95)00084-7
CHEMBL432091 216093 None 0 Rat Binding pIC50 = 4.4 4.4 - 0
Inhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar membranesInhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar membranes
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00095a029
CHEMBL432091 216093 None 0 Rat Binding pIC50 = 4.4 4.4 - 0
Inhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellumInhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(95)00152-J
10792785 166819 None 0 Pig Binding pIC50 = 4.4 4.4 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 551 10 3 6 5.0 CCOC(=O)c1nc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)oc1C 10.1021/jm950592+
CHEMBL428298 166819 None 0 Pig Binding pIC50 = 4.4 4.4 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 551 10 3 6 5.0 CCOC(=O)c1nc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)oc1C 10.1021/jm950592+
23445221 205553 None 0 Human Binding pIC50 = 4.4 4.4 - 0
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB receptor
ChEMBL 470 5 1 7 4.4 Cc1ccc(OC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00367-3
CHEMBL63937 205553 None 0 Human Binding pIC50 = 4.4 4.4 - 0
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB receptor
ChEMBL 470 5 1 7 4.4 Cc1ccc(OC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00367-3
10529742 8194 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 511 13 1 6 4.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1cccn1C 10.1021/jm980217s
CHEMBL109206 8194 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 511 13 1 6 4.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1cccn1C 10.1021/jm980217s
10672494 179659 None 0 Human Binding pIC50 = 5.4 5.4 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 483 6 2 6 5.0 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc(C(C)C)cc2)c1Br 10.1021/jm9608366
CHEMBL47417 179659 None 0 Human Binding pIC50 = 5.4 5.4 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 483 6 2 6 5.0 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc(C(C)C)cc2)c1Br 10.1021/jm9608366
23445354 209093 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 426 5 1 5 4.8 CCc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(96)00496-9
CHEMBL89203 209093 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 426 5 1 5 4.8 CCc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(96)00496-9
52944276 18436 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
ChEMBL 559 11 3 8 4.1 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCCCO)ccc31)OCO2 10.1016/j.bmcl.2010.08.074
CHEMBL1271807 18436 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
ChEMBL 559 11 3 8 4.1 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCCCO)ccc31)OCO2 10.1016/j.bmcl.2010.08.074
10674642 113433 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 574 10 3 7 4.7 CCc1cc(C(=O)O)cc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm990170q
CHEMBL331758 113433 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 574 10 3 7 4.7 CCc1cc(C(=O)O)cc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm990170q
44320291 105994 None 0 Rat Binding pIC50 = 7.4 7.4 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 548 7 2 8 4.8 O=C(O)c1cc2c(c(Cn3nc(-c4ccccc4)c(Cc4cc5c(cc4Cl)OCO5)c3C(=O)O)c1)OCOC2 10.1016/s0960-894x(00)00513-8
CHEMBL312854 105994 None 0 Rat Binding pIC50 = 7.4 7.4 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 548 7 2 8 4.8 O=C(O)c1cc2c(c(Cn3nc(-c4ccccc4)c(Cc4cc5c(cc4Cl)OCO5)c3C(=O)O)c1)OCOC2 10.1016/s0960-894x(00)00513-8
10281573 59995 None 0 Human Binding pIC50 = 7.4 7.4 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 574 9 2 9 4.8 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ccncc2)nc1OCC#CCO 10.1016/s0960-894x(02)01084-3
CHEMBL173358 59995 None 0 Human Binding pIC50 = 7.4 7.4 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 574 9 2 9 4.8 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ccncc2)nc1OCC#CCO 10.1016/s0960-894x(02)01084-3
9939960 175679 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta cell membranes
ChEMBL 704 13 2 11 5.2 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)cc(C(=O)N2CCN(C)CC2)cc1OCCOC(=O)Nc1ccccn1 10.1016/j.bmcl.2016.06.014
CHEMBL4579445 175679 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta cell membranes
ChEMBL 704 13 2 11 5.2 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)cc(C(=O)N2CCN(C)CC2)cc1OCCOC(=O)Nc1ccccn1 10.1016/j.bmcl.2016.06.014
44320444 208901 None 0 Rat Binding pIC50 = 6.4 6.4 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 481 7 2 8 4.0 O=C(O)c1cc(Cn2nc(-c3ccccc3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)on1 10.1016/s0960-894x(00)00513-8
CHEMBL88019 208901 None 0 Rat Binding pIC50 = 6.4 6.4 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 481 7 2 8 4.0 O=C(O)c1cc(Cn2nc(-c3ccccc3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)on1 10.1016/s0960-894x(00)00513-8
44309897 207089 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptor
ChEMBL 469 5 1 7 4.9 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccc4c(c3)OCO4)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(97)10151-2
CHEMBL73506 207089 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptor
ChEMBL 469 5 1 7 4.9 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccc4c(c3)OCO4)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(97)10151-2
9936145 19034 None 2 Human Binding pIC50 = 5.4 5.4 - 1
Binding affinity against human endothelin B receptor in CHO cellsBinding affinity against human endothelin B receptor in CHO cells
ChEMBL 510 11 1 4 5.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(C)c(F)c1 10.1021/jm010237l
CHEMBL128818 19034 None 2 Human Binding pIC50 = 5.4 5.4 - 1
Binding affinity against human endothelin B receptor in CHO cellsBinding affinity against human endothelin B receptor in CHO cells
ChEMBL 510 11 1 4 5.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(C)c(F)c1 10.1021/jm010237l
44327890 141499 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Binding affinity measured in CHO cells stably transfected with the human endothelin B receptorBinding affinity measured in CHO cells stably transfected with the human endothelin B receptor
ChEMBL 985 26 9 8 5.5 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)c1ccccc1)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL384052 141499 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Binding affinity measured in CHO cells stably transfected with the human endothelin B receptorBinding affinity measured in CHO cells stably transfected with the human endothelin B receptor
ChEMBL 985 26 9 8 5.5 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)c1ccccc1)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
44266537 4329 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 507 8 1 6 6.4 COc1ccc(Cn2c(C(=O)O)c(-c3ccc4c(c3)OCO4)c3cc(OCc4ccccc4)ccc32)cc1 10.1016/0960-894X(96)00170-9
CHEMBL10092 4329 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 507 8 1 6 6.4 COc1ccc(Cn2c(C(=O)O)c(-c3ccc4c(c3)OCO4)c3cc(OCc4ccccc4)ccc32)cc1 10.1016/0960-894X(96)00170-9
71462320 82035 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Antagonist activity at ETB receptor (unknown origin)Antagonist activity at ETB receptor (unknown origin)
ChEMBL 570 11 2 8 3.9 Cc1ccc(-c2c(NS(=O)(=O)NCc3ccccc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL2165332 82035 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Antagonist activity at ETB receptor (unknown origin)Antagonist activity at ETB receptor (unknown origin)
ChEMBL 570 11 2 8 3.9 Cc1ccc(-c2c(NS(=O)(=O)NCc3ccccc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1016/j.bmcl.2016.06.014
71462320 82035 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 570 11 2 8 3.9 Cc1ccc(-c2c(NS(=O)(=O)NCc3ccccc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm3009103
CHEMBL2165332 82035 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 570 11 2 8 3.9 Cc1ccc(-c2c(NS(=O)(=O)NCc3ccccc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm3009103
10674176 162795 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 548 11 1 9 5.0 CCOc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc(OCC)c1OCC 10.1021/jm9606507
CHEMBL417067 162795 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 548 11 1 9 5.0 CCOc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc(OCC)c1OCC 10.1021/jm9606507
18184256 129551 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 662 13 2 13 3.0 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
CHEMBL367275 129551 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 662 13 2 13 3.0 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
10740439 172851 None 0 Human Binding pIC50 = 4.4 4.4 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 412 5 2 7 3.5 Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)nc1 10.1021/jm9608366
CHEMBL45087 172851 None 0 Human Binding pIC50 = 4.4 4.4 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 412 5 2 7 3.5 Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)nc1 10.1021/jm9608366
23445379 130167 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B receptor
ChEMBL 456 6 1 6 4.8 Cc1ccc(OCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00132-7
CHEMBL367776 130167 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B receptor
ChEMBL 456 6 1 6 4.8 Cc1ccc(OCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00132-7
44284184 140087 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 490 8 2 7 5.0 CCOc1cc(OC)ccc1[C@@H]1c2nc(NC(C)C)ccc2[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O 10.1016/j.bmcl.2004.01.008
CHEMBL38000 140087 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 490 8 2 7 5.0 CCOc1cc(OC)ccc1[C@@H]1c2nc(NC(C)C)ccc2[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O 10.1016/j.bmcl.2004.01.008
44458399 99046 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
ChEMBL 520 7 2 7 4.2 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(CO)ccc23)cc1 10.1016/s0960-894x(01)00660-6
CHEMBL279947 99046 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
ChEMBL 520 7 2 7 4.2 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(CO)ccc23)cc1 10.1016/s0960-894x(01)00660-6
CHEMBL313382 213572 None 0 Rat Binding pIC50 = 6.4 6.4 - 0
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00070a001
CHEMBL87243 218383 None 0 Rat Binding pIC50 = 6.4 6.4 - 0
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00070a001
10288713 102098 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membranesInhibition of [125I]ET1 binding to porcine kidney inner medulla membranes
ChEMBL 473 7 1 7 4.6 CCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)c(=O)n2Cc1ccccc1OC 10.1016/S0960-894X(97)00319-3
CHEMBL301840 102098 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membranesInhibition of [125I]ET1 binding to porcine kidney inner medulla membranes
ChEMBL 473 7 1 7 4.6 CCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)c(=O)n2Cc1ccccc1OC 10.1016/S0960-894X(97)00319-3
10160887 100202 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 447 5 1 7 5.0 O=C(O)c1c(Sc2ccc3c(c2)OCO3)c2ccccc2n1Cc1ccc2c(c1)OCO2 10.1016/0960-894X(96)00232-6
CHEMBL28779 100202 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 447 5 1 7 5.0 O=C(O)c1c(Sc2ccc3c(c2)OCO3)c2ccccc2n1Cc1ccc2c(c1)OCO2 10.1016/0960-894X(96)00232-6
10600668 5160 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 476 7 1 8 3.8 COc1cc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc(OC)c1OC 10.1021/jm9606507
CHEMBL10589 5160 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 476 7 1 8 3.8 COc1cc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc(OC)c1OC 10.1021/jm9606507
10840410 206518 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.
ChEMBL 550 10 2 10 3.3 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCC(=O)O)c2)cc1 10.1021/jm980504w
CHEMBL70017 206518 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.
ChEMBL 550 10 2 10 3.3 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCC(=O)O)c2)cc1 10.1021/jm980504w
44327237 210388 None 0 Pig Binding pIC50 = 5.4 5.4 - 0
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranes
ChEMBL 511 8 1 8 3.5 CCCc1cc(C)c(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)n1 10.1016/S0960-894X(96)00617-8
CHEMBL96847 210388 None 0 Pig Binding pIC50 = 5.4 5.4 - 0
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranes
ChEMBL 511 8 1 8 3.5 CCCc1cc(C)c(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)n1 10.1016/S0960-894X(96)00617-8
18617327 207714 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 330 3 1 4 2.9 Cc1ccccc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL78929 207714 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 330 3 1 4 2.9 Cc1ccccc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/0960-894X(96)00441-6
44439108 167210 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]ET1 from human ETB receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETB receptor expressed in CHO cells
ChEMBL 1267 53 3 22 5.7 CC(=O)CC(=O)CCc1ccc(NC(=O)CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCCC(=O)N(C)Cc2cc(-c3ncco3)ccc2-c2ccccc2S(=O)(=O)Nc2ccno2)cc1 10.1016/j.bmcl.2006.10.009
CHEMBL429019 167210 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]ET1 from human ETB receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETB receptor expressed in CHO cells
ChEMBL 1267 53 3 22 5.7 CC(=O)CC(=O)CCc1ccc(NC(=O)CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCCC(=O)N(C)Cc2cc(-c3ncco3)ccc2-c2ccccc2S(=O)(=O)Nc2ccno2)cc1 10.1016/j.bmcl.2006.10.009
22010352 117690 None 0 Rat Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]ET-1 from rat ETB receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETB receptor after 1 hr by Lowry method
ChEMBL 404 10 1 4 5.5 CC(=O)c1ccc(OCc2ccccc2)cc1OC(CCC(=O)O)c1ccccc1 10.1016/j.bmc.2015.01.003
CHEMBL3400984 117690 None 0 Rat Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]ET-1 from rat ETB receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETB receptor after 1 hr by Lowry method
ChEMBL 404 10 1 4 5.5 CC(=O)c1ccc(OCc2ccccc2)cc1OC(CCC(=O)O)c1ccccc1 10.1016/j.bmc.2015.01.003
44339655 9108 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 530 14 1 6 5.3 C/C=C\C(C)(C)C[C@H]1[C@H](C(=O)O)[C@@H](c2cc(OC)c3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC 10.1021/jm980217s
CHEMBL109926 9108 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 530 14 1 6 5.3 C/C=C\C(C)(C)C[C@H]1[C@H](C(=O)O)[C@@H](c2cc(OC)c3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC 10.1021/jm980217s
11742628 98288 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 416 5 1 6 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1 10.1021/jm9606507
CHEMBL274383 98288 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 416 5 1 6 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1 10.1021/jm9606507
9845967 11097 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Binding affinity for human endothelin B receptor expressed in CHO-K1 cells.Binding affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 416 7 1 5 4.4 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1016/S0960-894X(97)00002-4
CHEMBL10801 11097 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Binding affinity for human endothelin B receptor expressed in CHO-K1 cells.Binding affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 416 7 1 5 4.4 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1016/S0960-894X(97)00002-4
CHEMBL1178000 11097 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Binding affinity for human endothelin B receptor expressed in CHO-K1 cells.Binding affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 416 7 1 5 4.4 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1016/S0960-894X(97)00002-4
CHEMBL51530 11097 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Binding affinity for human endothelin B receptor expressed in CHO-K1 cells.Binding affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 416 7 1 5 4.4 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1016/S0960-894X(97)00002-4
9845967 11097 None 0 Pig Binding pIC50 = 5.3 5.3 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 416 7 1 5 4.4 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL10801 11097 None 0 Pig Binding pIC50 = 5.3 5.3 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 416 7 1 5 4.4 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL1178000 11097 None 0 Pig Binding pIC50 = 5.3 5.3 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 416 7 1 5 4.4 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL51530 11097 None 0 Pig Binding pIC50 = 5.3 5.3 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 416 7 1 5 4.4 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1016/s0960-894x(98)00301-1
71455064 81727 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 694 14 1 12 4.5 COc1ccccc1Oc1c(NS(=O)(=O)N(C)Cc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
CHEMBL2163721 81727 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 694 14 1 12 4.5 COc1ccccc1Oc1c(NS(=O)(=O)N(C)Cc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
71460621 82032 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 602 13 2 10 3.7 COc1cccc(Oc2c(NS(=O)(=O)NCc3ccccc3)ncnc2OCCOc2ncc(Br)cn2)c1 10.1021/jm3009103
CHEMBL2165329 82032 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 602 13 2 10 3.7 COc1cccc(Oc2c(NS(=O)(=O)NCc3ccccc3)ncnc2OCCOc2ncc(Br)cn2)c1 10.1021/jm3009103
10527706 97054 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Radioligand binding selectivity to human Endothelin B receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin B receptor in chinese hamster ovary cells
ChEMBL 454 8 1 6 3.1 CCCN(C)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL266594 97054 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Radioligand binding selectivity to human Endothelin B receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin B receptor in chinese hamster ovary cells
ChEMBL 454 8 1 6 3.1 CCCN(C)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
44386002 60316 None 0 Human Binding pIC50 = 5.3 5.3 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 503 9 1 9 3.9 C#CCOc1nc(-c2ccncc2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL174326 60316 None 0 Human Binding pIC50 = 5.3 5.3 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 503 9 1 9 3.9 C#CCOc1nc(-c2ccncc2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
11015826 205989 None 0 Pig Binding pIC50 = 7.3 7.3 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 450 6 1 5 6.1 CC(C)Oc1ccc2c(c1)C(CC1CCCCC1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
CHEMBL66426 205989 None 0 Pig Binding pIC50 = 7.3 7.3 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 450 6 1 5 6.1 CC(C)Oc1ccc2c(c1)C(CC1CCCCC1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
10626646 16453 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 558 11 2 6 5.8 CCCc1cccc(CCC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm990170q
CHEMBL123305 16453 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 558 11 2 6 5.8 CCCc1cccc(CCC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm990170q
10240093 81718 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 603 12 1 12 3.5 CCS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC 10.1021/jm3009103
CHEMBL2163713 81718 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 603 12 1 12 3.5 CCS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC 10.1021/jm3009103
44295224 14637 None 0 Pig Binding pIC50 = 6.3 6.3 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 532 9 1 9 4.6 COc1cc(C/C(C(=O)c2ccc3c(c2)CCO3)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC 10.1016/s0960-894x(98)00301-1
CHEMBL1205077 14637 None 0 Pig Binding pIC50 = 6.3 6.3 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 532 9 1 9 4.6 COc1cc(C/C(C(=O)c2ccc3c(c2)CCO3)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC 10.1016/s0960-894x(98)00301-1
CHEMBL49675 14637 None 0 Pig Binding pIC50 = 6.3 6.3 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 532 9 1 9 4.6 COc1cc(C/C(C(=O)c2ccc3c(c2)CCO3)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC 10.1016/s0960-894x(98)00301-1
CHEMBL316092 213654 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00070a001
15453209 207589 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Binding affinity against human ETB receptor in transfected COS 7 cell membrane preparationBinding affinity against human ETB receptor in transfected COS 7 cell membrane preparation
ChEMBL 358 3 1 4 3.5 Cc1cc(C)c(S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/0960-894X(96)00441-6
CHEMBL77962 207589 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Binding affinity against human ETB receptor in transfected COS 7 cell membrane preparationBinding affinity against human ETB receptor in transfected COS 7 cell membrane preparation
ChEMBL 358 3 1 4 3.5 Cc1cc(C)c(S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/0960-894X(96)00441-6
71451526 81706 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 635 14 1 12 4.6 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Cl)cn1 10.1021/jm3009103
CHEMBL2163701 81706 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 635 14 1 12 4.6 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Cl)cn1 10.1021/jm3009103
67952994 82037 None 15 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 634 11 2 8 4.4 O=S(=O)(NCc1ccccc1)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1 10.1021/jm3009103
CHEMBL2165334 82037 None 15 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 634 11 2 8 4.4 O=S(=O)(NCc1ccccc1)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1 10.1021/jm3009103
10145418 81703 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Antagonist activity at ETB receptor (unknown origin)Antagonist activity at ETB receptor (unknown origin)
ChEMBL 601 14 1 12 4.0 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncccn1 10.1016/j.bmcl.2016.06.014
CHEMBL2163698 81703 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Antagonist activity at ETB receptor (unknown origin)Antagonist activity at ETB receptor (unknown origin)
ChEMBL 601 14 1 12 4.0 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncccn1 10.1016/j.bmcl.2016.06.014
10145418 81703 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 601 14 1 12 4.0 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncccn1 10.1021/jm3009103
CHEMBL2163698 81703 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 601 14 1 12 4.0 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncccn1 10.1021/jm3009103
44386163 60400 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 577 14 2 10 3.4 CCCS(=O)(=O)NCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
CHEMBL174781 60400 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 577 14 2 10 3.4 CCCS(=O)(=O)NCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
71453356 81696 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 554 13 2 10 2.9 CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1Oc1cccc(OC)c1 10.1021/jm3009103
CHEMBL2163691 81696 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 554 13 2 10 2.9 CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1Oc1cccc(OC)c1 10.1021/jm3009103
44439106 153696 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]ET1 from human ETB receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETB receptor expressed in CHO cells
ChEMBL 1005 37 2 17 5.8 CC(=O)CC(=O)CCc1ccc(NC(=O)CCOCCOCCOCCOCCOCCOCCOCCC(=O)N(C)Cc2cc(-c3ncco3)ccc2-c2ccccc2S(=O)(=O)Nc2ccno2)cc1 10.1016/j.bmcl.2006.10.009
CHEMBL398070 153696 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]ET1 from human ETB receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETB receptor expressed in CHO cells
ChEMBL 1005 37 2 17 5.8 CC(=O)CC(=O)CCc1ccc(NC(=O)CCOCCOCCOCCOCCOCCOCCOCCC(=O)N(C)Cc2cc(-c3ncco3)ccc2-c2ccccc2S(=O)(=O)Nc2ccno2)cc1 10.1016/j.bmcl.2006.10.009
10579100 166436 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 578 10 2 6 5.4 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(Cc2ccccc2)c2ccccc2)cc1 10.1021/jm990171i
CHEMBL122614 166436 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 578 10 2 6 5.4 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(Cc2ccccc2)c2ccccc2)cc1 10.1021/jm990171i
CHEMBL427303 166436 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 578 10 2 6 5.4 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(Cc2ccccc2)c2ccccc2)cc1 10.1021/jm990171i
10006086 121126 None 0 Pig Binding pIC50 = 6.3 6.3 - 0
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 498 9 2 5 4.6 COc1ccc(CN(C(=O)/C=C/c2ccc3c(c2)OCO3)C(Cc2c[nH]c3ccccc23)C(=O)O)cc1 10.1016/s0960-894x(01)00009-9
CHEMBL356916 121126 None 0 Pig Binding pIC50 = 6.3 6.3 - 0
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 498 9 2 5 4.6 COc1ccc(CN(C(=O)/C=C/c2ccc3c(c2)OCO3)C(Cc2c[nH]c3ccccc23)C(=O)O)cc1 10.1016/s0960-894x(01)00009-9
11059249 102673 None 0 Pig Binding pIC50 = 6.3 6.3 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 440 10 1 6 5.3 CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OCCCC)cc21 10.1021/jm010382z
CHEMBL304202 102673 None 0 Pig Binding pIC50 = 6.3 6.3 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 440 10 1 6 5.3 CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OCCCC)cc21 10.1021/jm010382z
11733231 205302 None 0 Pig Binding pIC50 = 6.3 6.3 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 460 6 1 6 5.2 COc1cccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)c1 10.1021/jm010382z
CHEMBL62465 205302 None 0 Pig Binding pIC50 = 6.3 6.3 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 460 6 1 6 5.2 COc1cccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)c1 10.1021/jm010382z
CHEMBL431433 216086 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00015a003
18617340 105459 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 422 4 1 4 3.9 CCc1ccc(Br)c(S(=O)(=O)Nc2onc(C)c2Br)c1 10.1016/0960-894X(96)00441-6
CHEMBL311742 105459 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 422 4 1 4 3.9 CCc1ccc(Br)c(S(=O)(=O)Nc2onc(C)c2Br)c1 10.1016/0960-894X(96)00441-6
44279439 107434 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB receptor
ChEMBL 534 3 2 3 6.2 O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(-c3ccc(C(F)(F)F)cc3C(F)(F)F)cc21 10.1016/0960-894X(95)00230-Q
CHEMBL31781 107434 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB receptor
ChEMBL 534 3 2 3 6.2 O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(-c3ccc(C(F)(F)F)cc3C(F)(F)F)cc21 10.1016/0960-894X(95)00230-Q
CHEMBL303204 213377 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Binding activity against Endothelin B receptor 0f Porcine cerebellum membranesBinding activity against Endothelin B receptor 0f Porcine cerebellum membranes
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H](C)N(C)C(=O)[C@H](CC(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00089a028
44317005 207484 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 320 3 1 4 3.4 Cc1noc(NS(=O)(=O)c2cc(Cl)cc(Cl)c2)c1C 10.1016/0960-894X(96)00441-6
CHEMBL76949 207484 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 320 3 1 4 3.4 Cc1noc(NS(=O)(=O)c2cc(Cl)cc(Cl)c2)c1C 10.1016/0960-894X(96)00441-6
10116355 8268 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 474 14 1 5 4.9 CCCCC[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC 10.1021/jm980217s
CHEMBL109248 8268 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 474 14 1 5 4.9 CCCCC[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC 10.1021/jm980217s
11799503 9755 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 498 13 1 6 4.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1ccco1 10.1021/jm980217s
CHEMBL113472 9755 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 498 13 1 6 4.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1ccco1 10.1021/jm980217s
10095637 49981 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) receptor expressed in CHO cells
ChEMBL 457 9 1 5 5.8 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)ccc1OC(C(=O)O)c1ccccc1 10.1016/0960-894X(95)00186-W
CHEMBL15689 49981 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) receptor expressed in CHO cells
ChEMBL 457 9 1 5 5.8 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)ccc1OC(C(=O)O)c1ccccc1 10.1016/0960-894X(95)00186-W
44459247 88057 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
ChEMBL 575 8 1 7 4.9 CCn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c2ccc(C(=O)N(C)C)cc21 10.1016/s0960-894x(01)00660-6
CHEMBL23444 88057 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
ChEMBL 575 8 1 7 4.9 CCn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c2ccc(C(=O)N(C)C)cc21 10.1016/s0960-894x(01)00660-6
10649546 108670 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 516 13 1 6 4.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC1CCCCO1 10.1021/jm980217s
CHEMBL320569 108670 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 516 13 1 6 4.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC1CCCCO1 10.1021/jm980217s
44284405 100410 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 532 10 2 7 5.4 COCC(C)Cc1cc(OC)ccc1[C@@H]1c2nc(NC(C)C)ccc2[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O 10.1016/j.bmcl.2004.01.008
CHEMBL289634 100410 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 532 10 2 7 5.4 COCC(C)Cc1cc(OC)ccc1[C@@H]1c2nc(NC(C)C)ccc2[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O 10.1016/j.bmcl.2004.01.008
9870830 209172 None 29 Human Binding pIC50 = 6.3 6.3 -66 2
Binding affinity for human endothelin B receptor expressed in CHO-K1 cells.Binding affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1016/S0960-894X(97)00002-4
CHEMBL8981 209172 None 29 Human Binding pIC50 = 6.3 6.3 -66 2
Binding affinity for human endothelin B receptor expressed in CHO-K1 cells.Binding affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1016/S0960-894X(97)00002-4
10971938 205434 None 0 Pig Binding pIC50 = 6.3 6.3 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 424 7 1 5 5.6 CC(C)CCC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL63058 205434 None 0 Pig Binding pIC50 = 6.3 6.3 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 424 7 1 5 5.6 CC(C)CCC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
44295156 14633 None 0 Pig Binding pIC50 = 6.3 6.3 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 520 10 1 9 4.7 COc1ccccc1C(=O)/C(Cc1cc(OC)c(OC)c(OC)c1)=C(\C(=O)O)c1ccc2nsnc2c1 10.1016/s0960-894x(98)00301-1
CHEMBL1205062 14633 None 0 Pig Binding pIC50 = 6.3 6.3 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 520 10 1 9 4.7 COc1ccccc1C(=O)/C(Cc1cc(OC)c(OC)c(OC)c1)=C(\C(=O)O)c1ccc2nsnc2c1 10.1016/s0960-894x(98)00301-1
CHEMBL48411 14633 None 0 Pig Binding pIC50 = 6.3 6.3 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 520 10 1 9 4.7 COc1ccccc1C(=O)/C(Cc1cc(OC)c(OC)c(OC)c1)=C(\C(=O)O)c1ccc2nsnc2c1 10.1016/s0960-894x(98)00301-1
44284199 100164 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 552 9 2 7 6.2 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(OCc2ccccc2)c1 10.1016/j.bmcl.2004.01.008
CHEMBL287517 100164 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 552 9 2 7 6.2 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(OCc2ccccc2)c1 10.1016/j.bmcl.2004.01.008
10961277 101071 None 0 Pig Binding pIC50 = 5.3 5.3 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 446 5 2 6 4.9 CC(C)Oc1ccc2c(c1)C(c1ccc(O)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
CHEMBL294496 101071 None 0 Pig Binding pIC50 = 5.3 5.3 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 446 5 2 6 4.9 CC(C)Oc1ccc2c(c1)C(c1ccc(O)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
10788494 170726 None 0 Human Binding pIC50 = 5.3 5.3 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 424 6 1 6 4.5 Cc1ccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1 10.1021/jm9700068
CHEMBL445101 170726 None 0 Human Binding pIC50 = 5.3 5.3 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 424 6 1 6 4.5 Cc1ccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1 10.1021/jm9700068
CHEMBL133257 211174 None 0 Pig Binding pIC50 = 5.3 5.3 - 0
Inhibitory effect against porcine Endothelin B receptorInhibitory effect against porcine Endothelin B receptor
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C2CCCC2)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
44339840 9290 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 486 13 1 5 5.1 C/C=C(\C)CC[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC 10.1021/jm980217s
CHEMBL110904 9290 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 486 13 1 5 5.1 C/C=C(\C)CC[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC 10.1021/jm980217s
10816110 108622 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 532 13 1 7 4.2 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC1OC(C)C(C)O1 10.1021/jm980217s
CHEMBL320254 108622 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 532 13 1 7 4.2 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC1OC(C)C(C)O1 10.1021/jm980217s
10530156 9559 None 0 Pig Binding pIC50 = 4.3 4.3 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 526 14 1 6 5.0 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc(OC)cc2OC)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL112347 9559 None 0 Pig Binding pIC50 = 4.3 4.3 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 526 14 1 6 5.0 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc(OC)cc2OC)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
10579210 168694 None 0 Pig Binding pIC50 = 4.3 4.3 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 585 10 4 6 5.4 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCc3ccccc32)nc1C(=O)O 10.1021/jm950592+
CHEMBL435901 168694 None 0 Pig Binding pIC50 = 4.3 4.3 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 585 10 4 6 5.4 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCc3ccccc32)nc1C(=O)O 10.1021/jm950592+
10673969 62125 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Inhibitory activity was evaluated against human Endothelin B receptorInhibitory activity was evaluated against human Endothelin B receptor
ChEMBL 538 10 3 7 5.0 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)OC(=O)NC2CCCCC2)nc1C(=O)O 10.1021/jm9505932
CHEMBL177546 62125 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Inhibitory activity was evaluated against human Endothelin B receptorInhibitory activity was evaluated against human Endothelin B receptor
ChEMBL 538 10 3 7 5.0 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)OC(=O)NC2CCCCC2)nc1C(=O)O 10.1021/jm9505932
22998414 205474 None 0 Human Binding pIC50 = 4.3 4.3 - 0
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB receptor
ChEMBL 422 5 1 9 3.1 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Oc2ccc3c(c2)OCO3)c1C 10.1016/S0960-894X(97)00367-3
CHEMBL63290 205474 None 0 Human Binding pIC50 = 4.3 4.3 - 0
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB receptor
ChEMBL 422 5 1 9 3.1 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Oc2ccc3c(c2)OCO3)c1C 10.1016/S0960-894X(97)00367-3
10231591 131428 None 0 Human Binding pIC50 = 7.3 7.3 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 569 10 2 11 2.8 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCO 10.1016/s0960-894x(02)01084-3
CHEMBL368828 131428 None 0 Human Binding pIC50 = 7.3 7.3 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 569 10 2 11 2.8 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCO 10.1016/s0960-894x(02)01084-3
44311232 206565 None 0 Human Binding pIC50 = 7.3 7.3 - 1
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 658 13 2 13 5.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ncccn2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
CHEMBL70293 206565 None 0 Human Binding pIC50 = 7.3 7.3 - 1
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 658 13 2 13 5.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ncccn2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
18995989 100609 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 583 9 1 9 6.6 COc1cc2c(Sc3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OCc1ccccc1 10.1016/0960-894X(96)00232-6
CHEMBL29147 100609 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 583 9 1 9 6.6 COc1cc2c(Sc3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OCc1ccccc1 10.1016/0960-894X(96)00232-6
10426645 163170 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 328 4 1 4 3.8 Cc1noc(NS(=O)(=O)c2cccc(-c3ccccc3)c2)c1C 10.1016/0960-894X(96)00441-6
CHEMBL417651 163170 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 328 4 1 4 3.8 Cc1noc(NS(=O)(=O)c2cccc(-c3ccccc3)c2)c1C 10.1016/0960-894X(96)00441-6
11728313 163370 None 0 Pig Binding pIC50 = 5.3 5.3 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 368 6 1 5 4.2 CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccccc21 10.1021/jm010382z
CHEMBL418667 163370 None 0 Pig Binding pIC50 = 5.3 5.3 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 368 6 1 5 4.2 CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccccc21 10.1021/jm010382z
44368396 44606 None 0 Pig Binding pIC50 = 4.3 4.3 - 0
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 506 8 2 5 4.9 COc1ccc(C(=O)N(Cc2cc3c(cc2Cl)OCO3)C(Cc2c[nH]c3ccccc23)C(=O)O)cc1 10.1016/s0960-894x(01)00009-9
CHEMBL152017 44606 None 0 Pig Binding pIC50 = 4.3 4.3 - 0
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 506 8 2 5 4.9 COc1ccc(C(=O)N(Cc2cc3c(cc2Cl)OCO3)C(Cc2c[nH]c3ccccc23)C(=O)O)cc1 10.1016/s0960-894x(01)00009-9
10357554 97617 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Binding affinity against human ETB receptor in transfected COS 7 cell membrane preparationBinding affinity against human ETB receptor in transfected COS 7 cell membrane preparation
ChEMBL 302 3 1 4 3.2 Cc1noc(NS(=O)(=O)c2cccc3ccccc23)c1C 10.1016/0960-894X(96)00441-6
CHEMBL27065 97617 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Binding affinity against human ETB receptor in transfected COS 7 cell membrane preparationBinding affinity against human ETB receptor in transfected COS 7 cell membrane preparation
ChEMBL 302 3 1 4 3.2 Cc1noc(NS(=O)(=O)c2cccc3ccccc23)c1C 10.1016/0960-894X(96)00441-6
44316973 208063 None 1 Human Binding pIC50 = 4.3 4.3 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 330 3 1 4 2.9 Cc1noc(NS(=O)(=O)c2cccc(Br)c2)c1C 10.1016/0960-894X(96)00441-6
CHEMBL81593 208063 None 1 Human Binding pIC50 = 4.3 4.3 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 330 3 1 4 2.9 Cc1noc(NS(=O)(=O)c2cccc(Br)c2)c1C 10.1016/0960-894X(96)00441-6
44439114 161724 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]ET1 from human ETB receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETB receptor expressed in CHO cells
ChEMBL 993 32 2 15 7.3 CC(=O)CC(=O)CCc1ccc(NC(=O)CCOCCOCCOCCOCCOc2ccc(CCC(=O)N(C)Cc3cc(-c4ncco4)ccc3-c3ccccc3S(=O)(=O)Nc3ccno3)cc2)cc1 10.1016/j.bmcl.2006.10.009
CHEMBL413001 161724 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]ET1 from human ETB receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETB receptor expressed in CHO cells
ChEMBL 993 32 2 15 7.3 CC(=O)CC(=O)CCc1ccc(NC(=O)CCOCCOCCOCCOCCOc2ccc(CCC(=O)N(C)Cc3cc(-c4ncco4)ccc3-c3ccccc3S(=O)(=O)Nc3ccno3)cc2)cc1 10.1016/j.bmcl.2006.10.009
10812400 98432 None 0 Pig Binding pIC50 = 5.3 5.3 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 427 9 1 6 3.7 CCCOCCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL275306 98432 None 0 Pig Binding pIC50 = 5.3 5.3 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 427 9 1 6 3.7 CCCOCCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
10816667 11448 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 558 9 2 6 5.6 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(CC(C)(C)C)c2ccccc2)cc1 10.1021/jm990171i
CHEMBL1180341 11448 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 558 9 2 6 5.6 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(CC(C)(C)C)c2ccccc2)cc1 10.1021/jm990171i
CHEMBL122933 11448 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 558 9 2 6 5.6 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(CC(C)(C)C)c2ccccc2)cc1 10.1021/jm990171i
10768903 12138 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 544 11 2 6 5.3 CCCCC(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1 10.1021/jm990171i
CHEMBL1184133 12138 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 544 11 2 6 5.3 CCCCC(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1 10.1021/jm990171i
CHEMBL334076 12138 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 544 11 2 6 5.3 CCCCC(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1 10.1021/jm990171i
44314579 102972 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Binding affinity towards Endothelin B receptor in human girardi heart cell membranesBinding affinity towards Endothelin B receptor in human girardi heart cell membranes
ChEMBL 580 12 5 5 3.8 CCCCC(NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)C)C(=O)O 10.1021/jm9600914
CHEMBL306123 102972 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Binding affinity towards Endothelin B receptor in human girardi heart cell membranesBinding affinity towards Endothelin B receptor in human girardi heart cell membranes
ChEMBL 580 12 5 5 3.8 CCCCC(NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)C)C(=O)O 10.1021/jm9600914
44314722 155841 None 0 Pig Binding pIC50 = 8.3 8.3 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 597 14 5 4 4.9 CCCCC(NC(=O)[C@@H](Cc1c(CC)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
CHEMBL405724 155841 None 0 Pig Binding pIC50 = 8.3 8.3 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 597 14 5 4 4.9 CCCCC(NC(=O)[C@@H](Cc1c(CC)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
44283421 100211 None 0 Pig Binding pIC50 = 8.3 8.3 - 0
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranesInhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranes
ChEMBL 597 14 5 4 4.9 CCCC[C@H](NC(=O)[C@@H](Cc1c(CC)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1016/0960-894X(95)00237-N
CHEMBL287888 100211 None 0 Pig Binding pIC50 = 8.3 8.3 - 0
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranesInhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranes
ChEMBL 597 14 5 4 4.9 CCCC[C@H](NC(=O)[C@@H](Cc1c(CC)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1016/0960-894X(95)00237-N
9809919 206867 None 0 Human Binding pIC50 = 8.3 8.3 - 2
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 665 13 2 13 4.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
CHEMBL72037 206867 None 0 Human Binding pIC50 = 8.3 8.3 - 2
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 665 13 2 13 4.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
10209320 9287 None 0 Pig Binding pIC50 = 8.3 8.3 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 546 12 1 7 4.0 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)CC(C)C 10.1021/jm970101g
CHEMBL110899 9287 None 0 Pig Binding pIC50 = 8.3 8.3 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 546 12 1 7 4.0 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)CC(C)C 10.1021/jm970101g
10579303 9433 None 0 Pig Binding pIC50 = 8.3 8.3 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 590 16 1 8 4.5 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCOC)cc1 10.1021/jm970101g
CHEMBL111712 9433 None 0 Pig Binding pIC50 = 8.3 8.3 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 590 16 1 8 4.5 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCOC)cc1 10.1021/jm970101g
44314864 103091 None 0 Pig Binding pIC50 = 8.3 8.3 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 566 11 5 5 3.4 CCCC(NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)C)C(=O)O 10.1021/jm9600914
CHEMBL307077 103091 None 0 Pig Binding pIC50 = 8.3 8.3 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 566 11 5 5 3.4 CCCC(NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)C)C(=O)O 10.1021/jm9600914
44314751 161449 None 0 Pig Binding pIC50 = 8.3 8.3 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 603 13 5 4 5.0 CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
CHEMBL412602 161449 None 0 Pig Binding pIC50 = 8.3 8.3 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 603 13 5 4 5.0 CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
44283349 100380 None 0 Pig Binding pIC50 = 8.3 8.3 - 0
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranesInhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranes
ChEMBL 603 13 5 4 5.0 CCCC[C@H](NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1016/0960-894X(95)00237-N
CHEMBL289410 100380 None 0 Pig Binding pIC50 = 8.3 8.3 - 0
Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranesInhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranes
ChEMBL 603 13 5 4 5.0 CCCC[C@H](NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1016/0960-894X(95)00237-N
44284437 100038 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 520 9 4 8 3.5 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(O)CO)c1 10.1016/j.bmcl.2004.01.008
CHEMBL286621 100038 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 520 9 4 8 3.5 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(O)CO)c1 10.1016/j.bmcl.2004.01.008
10506430 113854 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 532 9 2 7 4.5 CCc1cccc(OC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm990170q
CHEMBL332387 113854 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 532 9 2 7 4.5 CCc1cccc(OC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm990170q
CHEMBL313984 213582 None 0 Rat Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]ET1 from Endothelin B receptor of rat cerebellumDisplacement of [125I]ET1 from Endothelin B receptor of rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)81215-4
10188517 61786 None 0 Human Binding pIC50 = 7.3 7.3 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 582 9 2 10 3.6 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(N2CCOCC2)nc1OCC#CCO 10.1016/s0960-894x(02)01084-3
CHEMBL177203 61786 None 0 Human Binding pIC50 = 7.3 7.3 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 582 9 2 10 3.6 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(N2CCOCC2)nc1OCC#CCO 10.1016/s0960-894x(02)01084-3
9850566 4195 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 551 8 1 8 6.1 COc1cc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OCc1ccccc1 10.1016/0960-894X(96)00170-9
CHEMBL10016 4195 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 551 8 1 8 6.1 COc1cc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OCc1ccccc1 10.1016/0960-894X(96)00170-9
44298305 194697 None 0 Pig Binding pIC50 = 6.3 6.3 - 0
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptor
ChEMBL 504 10 2 7 5.3 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCC(=O)O)c1 10.1016/s0960-894x(00)00366-8
CHEMBL53097 194697 None 0 Pig Binding pIC50 = 6.3 6.3 - 0
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptor
ChEMBL 504 10 2 7 5.3 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCC(=O)O)c1 10.1016/s0960-894x(00)00366-8
44298277 197243 None 0 Pig Binding pIC50 = 6.3 6.3 - 0
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptor
ChEMBL 474 9 1 7 5.1 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCC=O)c1 10.1016/s0960-894x(00)00366-8
CHEMBL54773 197243 None 0 Pig Binding pIC50 = 6.3 6.3 - 0
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptor
ChEMBL 474 9 1 7 5.1 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCC=O)c1 10.1016/s0960-894x(00)00366-8
44298988 100773 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membranesInhibition of [125I]ET1 binding to porcine kidney inner medulla membranes
ChEMBL 459 8 1 6 4.8 CCOc1ccc2c(c1)c(-c1ccc(OC)cc1)c(C(=O)O)c(=O)n2Cc1ccccc1OC 10.1016/S0960-894X(97)00319-3
CHEMBL292580 100773 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membranesInhibition of [125I]ET1 binding to porcine kidney inner medulla membranes
ChEMBL 459 8 1 6 4.8 CCOc1ccc2c(c1)c(-c1ccc(OC)cc1)c(C(=O)O)c(=O)n2Cc1ccccc1OC 10.1016/S0960-894X(97)00319-3
CHEMBL329609 213777 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)[C@@H](C)CC 10.1021/jm00015a003
10649266 9634 None 0 Pig Binding pIC50 = 5.3 5.3 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 506 12 1 5 5.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3ccoc3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL112685 9634 None 0 Pig Binding pIC50 = 5.3 5.3 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 506 12 1 5 5.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3ccoc3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
22010244 209259 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.
ChEMBL 407 9 1 5 5.5 Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1C#N 10.1021/jm9707131
CHEMBL90320 209259 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.
ChEMBL 407 9 1 5 5.5 Cc1ccccc1C(CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1C#N 10.1021/jm9707131
10649585 109829 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 518 14 1 7 3.9 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCCC1OCCO1 10.1021/jm980217s
CHEMBL323175 109829 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 518 14 1 7 3.9 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCCC1OCCO1 10.1021/jm980217s
44383592 59922 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Tested for binding affinity towards rabbit Endothelin B receptorTested for binding affinity towards rabbit Endothelin B receptor
ChEMBL 386 4 1 5 3.6 C/C=C/C=C/C=C/C(=O)O[C@@H]1C=C2COC(=O)[C@]2(O)[C@@]2(C)CCCC(C)(C)C12 10.1016/s0960-894x(00)00136-0
CHEMBL173059 59922 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Tested for binding affinity towards rabbit Endothelin B receptorTested for binding affinity towards rabbit Endothelin B receptor
ChEMBL 386 4 1 5 3.6 C/C=C/C=C/C=C/C(=O)O[C@@H]1C=C2COC(=O)[C@]2(O)[C@@]2(C)CCCC(C)(C)C12 10.1016/s0960-894x(00)00136-0
44265853 208860 None 0 Pig Binding pIC50 = 5.3 5.3 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 454 4 1 6 2.7 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2C(=O)N2CCOCC2)cc1 10.1021/jm9505369
CHEMBL8776 208860 None 0 Pig Binding pIC50 = 5.3 5.3 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 454 4 1 6 2.7 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2C(=O)N2CCOCC2)cc1 10.1021/jm9505369
21979593 82036 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 590 11 2 8 4.3 O=S(=O)(NCc1ccccc1)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Cl)cc1 10.1021/jm3009103
CHEMBL2165333 82036 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 590 11 2 8 4.3 O=S(=O)(NCc1ccccc1)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Cl)cc1 10.1021/jm3009103
71455139 82034 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 556 11 2 8 3.6 O=S(=O)(NCc1ccccc1)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccccc1 10.1021/jm3009103
CHEMBL2165331 82034 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 556 11 2 8 3.6 O=S(=O)(NCc1ccccc1)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccccc1 10.1021/jm3009103
10391487 9663 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
ChEMBL 506 12 1 5 5.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3occc3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm010237l
CHEMBL112832 9663 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
ChEMBL 506 12 1 5 5.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3occc3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm010237l
CHEMBL319660 213679 None 0 Rat Binding pIC50 = 7.3 7.3 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00015a003
44284115 100249 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 518 9 3 7 4.8 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(C)CO)c1 10.1016/j.bmcl.2004.01.008
CHEMBL288247 100249 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 518 9 3 7 4.8 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(C)CO)c1 10.1016/j.bmcl.2004.01.008
10391487 9663 None 0 Pig Binding pIC50 = 5.3 5.3 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 506 12 1 5 5.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3occc3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL112832 9663 None 0 Pig Binding pIC50 = 5.3 5.3 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 506 12 1 5 5.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3occc3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
44266903 14592 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cells
ChEMBL 536 11 1 9 4.4 COc1ccc(C(=O)/C(Cc2ccc(OC)c(OC)c2OC)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1 10.1021/jm9606507
CHEMBL10862 14592 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cells
ChEMBL 536 11 1 9 4.4 COc1ccc(C(=O)/C(Cc2ccc(OC)c(OC)c2OC)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1 10.1021/jm9606507
CHEMBL1204672 14592 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cells
ChEMBL 536 11 1 9 4.4 COc1ccc(C(=O)/C(Cc2ccc(OC)c(OC)c2OC)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1 10.1021/jm9606507
44387124 130959 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibitory concentration against Endothelin B receptorInhibitory concentration against Endothelin B receptor
ChEMBL 524 13 1 6 5.1 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](CC(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm031041j
CHEMBL368558 130959 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibitory concentration against Endothelin B receptorInhibitory concentration against Endothelin B receptor
ChEMBL 524 13 1 6 5.1 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](CC(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm031041j
159594 522 None 36 Human Binding pIC50 = 6.3 6.3 -4073 3
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm010237l
159594.0 522 None 36 Human Binding pIC50 = 6.3 6.3 -4073 3
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm010237l
3487 522 None 36 Human Binding pIC50 = 6.3 6.3 -4073 3
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm010237l
CHEMBL9194 522 None 36 Human Binding pIC50 = 6.3 6.3 -4073 3
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm010237l
DB06199 522 None 36 Human Binding pIC50 = 6.3 6.3 -4073 3
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm010237l
9914310 209101 None 9 Pig Binding pIC50 = 6.3 6.3 - 2
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 510 12 1 6 4.7 CCCCN(CCCC)C(=O)CN1CC(c2ccc3c(c2)OCO3)C(C(=O)O)C1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL8923 209101 None 9 Pig Binding pIC50 = 6.3 6.3 - 2
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 510 12 1 6 4.7 CCCCN(CCCC)C(=O)CN1CC(c2ccc3c(c2)OCO3)C(C(=O)O)C1c1ccc(OC)cc1 10.1021/jm9505369
21041273 173852 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 538 12 2 9 2.8 CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(OC)cn2)c1-c1ccc(Br)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL4536769 173852 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 538 12 2 9 2.8 CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(OC)cn2)c1-c1ccc(Br)cc1 10.1016/j.bmcl.2016.06.014
10575845 11233 None 0 Human Binding pIC50 = 4.3 4.3 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 457 7 2 8 3.8 COc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(OC)c1 10.1021/jm9608366
CHEMBL1178807 11233 None 0 Human Binding pIC50 = 4.3 4.3 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 457 7 2 8 3.8 COc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(OC)c1 10.1021/jm9608366
CHEMBL43788 11233 None 0 Human Binding pIC50 = 4.3 4.3 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 457 7 2 8 3.8 COc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(OC)c1 10.1021/jm9608366
CHEMBL97470 218415 None 0 Rat Binding pIC50 = 7.3 7.3 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
11732669 205575 None 0 Pig Binding pIC50 = 6.3 6.3 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 426 9 1 6 5.0 CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OCCC)cc21 10.1021/jm010382z
CHEMBL64039 205575 None 0 Pig Binding pIC50 = 6.3 6.3 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 426 9 1 6 5.0 CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OCCC)cc21 10.1021/jm010382z
44298343 101848 None 0 Pig Binding pIC50 = 6.3 6.3 - 0
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptor
ChEMBL 485 9 1 7 5.8 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCC#N)c1 10.1016/s0960-894x(00)00366-8
CHEMBL300066 101848 None 0 Pig Binding pIC50 = 6.3 6.3 - 0
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptor
ChEMBL 485 9 1 7 5.8 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCC#N)c1 10.1016/s0960-894x(00)00366-8
159594 522 None 36 Pig Binding pIC50 = 6.3 6.3 - 3
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm960077r
159594.0 522 None 36 Pig Binding pIC50 = 6.3 6.3 - 3
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm960077r
3487 522 None 36 Pig Binding pIC50 = 6.3 6.3 - 3
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm960077r
CHEMBL9194 522 None 36 Pig Binding pIC50 = 6.3 6.3 - 3
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm960077r
DB06199 522 None 36 Pig Binding pIC50 = 6.3 6.3 - 3
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm960077r
44371420 50925 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 485 7 1 7 5.2 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3cccc(OC)c3OC)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(99)00040-2
CHEMBL157763 50925 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 485 7 1 7 5.2 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3cccc(OC)c3OC)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(99)00040-2
9888574 104231 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 422 4 1 4 3.9 CCc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL309692 104231 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 422 4 1 4 3.9 CCc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/0960-894X(96)00441-6
10429404 104934 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 372 5 1 4 3.7 CCc1ccc(CC)c(S(=O)(=O)Nc2onc(C)c2Br)c1 10.1016/0960-894X(96)00441-6
CHEMBL311138 104934 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 372 5 1 4 3.7 CCc1ccc(CC)c(S(=O)(=O)Nc2onc(C)c2Br)c1 10.1016/0960-894X(96)00441-6
10670372 97300 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 432 7 1 6 4.1 COc1ccc(C2(O)OC(=O)C(c3cc(OC)cc(OC)c3)=C2Cc2ccccc2)cc1 10.1021/jm9606507
CHEMBL268754 97300 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 432 7 1 6 4.1 COc1ccc(C2(O)OC(=O)C(c3cc(OC)cc(OC)c3)=C2Cc2ccccc2)cc1 10.1021/jm9606507
44327423 210000 None 0 Pig Binding pIC50 = 5.3 5.3 - 0
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranes
ChEMBL 483 6 1 8 2.8 Cc1cc(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)nc1C 10.1016/S0960-894X(96)00617-8
CHEMBL94720 210000 None 0 Pig Binding pIC50 = 5.3 5.3 - 0
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranes
ChEMBL 483 6 1 8 2.8 Cc1cc(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)nc1C 10.1016/S0960-894X(96)00617-8
10915215 100857 None 0 Pig Binding pIC50 = 4.3 4.3 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 354 4 1 5 3.8 CC(C)Oc1ccc2c(c1)C=C(C(=O)O)[C@@H](c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
CHEMBL293161 100857 None 0 Pig Binding pIC50 = 4.3 4.3 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 354 4 1 5 3.8 CC(C)Oc1ccc2c(c1)C=C(C(=O)O)[C@@H](c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
44305079 102146 None 0 Pig Binding pIC50 = 4.3 4.3 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 354 4 1 5 3.8 CC(C)Oc1ccc2c(c1)C=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
CHEMBL302189 102146 None 0 Pig Binding pIC50 = 4.3 4.3 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 354 4 1 5 3.8 CC(C)Oc1ccc2c(c1)C=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
21041249 81693 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 648 11 1 8 4.7 CN(Cc1ccccc1)S(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1 10.1021/jm3009103
CHEMBL2163688 81693 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 648 11 1 8 4.7 CN(Cc1ccccc1)S(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1 10.1021/jm3009103
44384656 130163 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 468 5 1 7 4.5 Cc1noc(NS(=O)(=O)c2ccsc2/C=C/c2ccc3c(c2)OCO3)c1Br 10.1016/S0960-894X(97)00133-9
CHEMBL367763 130163 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 468 5 1 7 4.5 Cc1noc(NS(=O)(=O)c2ccsc2/C=C/c2ccc3c(c2)OCO3)c1Br 10.1016/S0960-894X(97)00133-9
21979601 82031 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Antagonist activity at ETB receptor (unknown origin)Antagonist activity at ETB receptor (unknown origin)
ChEMBL 602 13 2 10 3.7 COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)ncnc1OCCOc1ncc(Br)cn1 10.1016/j.bmcl.2016.06.014
CHEMBL2165328 82031 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Antagonist activity at ETB receptor (unknown origin)Antagonist activity at ETB receptor (unknown origin)
ChEMBL 602 13 2 10 3.7 COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)ncnc1OCCOc1ncc(Br)cn1 10.1016/j.bmcl.2016.06.014
21979601 82031 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 602 13 2 10 3.7 COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)ncnc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
CHEMBL2165328 82031 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 602 13 2 10 3.7 COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)ncnc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
10647372 209575 None 0 Pig Binding pIC50 = 5.3 5.3 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 454 8 1 6 3.1 CCN(CC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL9212 209575 None 0 Pig Binding pIC50 = 5.3 5.3 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 454 8 1 6 3.1 CCN(CC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL2304016 211931 None 0 Pig Binding pIC50 = 7.3 7.3 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](C(C)(C)C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc2c(Cl)[nH]c3ccccc23)NC1=O 10.1021/jm9600914
44333889 5085 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B receptor
ChEMBL 463 7 1 6 5.3 CCCSc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(02)00663-7
CHEMBL105494 5085 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B receptor
ChEMBL 463 7 1 6 5.3 CCCSc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(02)00663-7
44334084 109709 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B receptor
ChEMBL 461 7 2 6 3.8 COc1ccc([C@@H]2c3nc(CCC(=O)O)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1016/s0960-894x(02)00663-7
CHEMBL322434 109709 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B receptor
ChEMBL 461 7 2 6 3.8 COc1ccc([C@@H]2c3nc(CCC(=O)O)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1016/s0960-894x(02)00663-7
18617333 105583 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 424 4 1 5 3.3 COc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL312187 105583 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 424 4 1 5 3.3 COc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/0960-894X(96)00441-6
44309488 206467 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptor
ChEMBL 471 7 1 8 5.1 CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2nonc2c1 10.1016/s0960-894x(97)10151-2
CHEMBL69664 206467 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptorInhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptor
ChEMBL 471 7 1 8 5.1 CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2nonc2c1 10.1016/s0960-894x(97)10151-2
10814655 210059 None 0 Pig Binding pIC50 = 6.3 6.3 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 482 10 1 6 3.9 CCCCN(CC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL9502 210059 None 0 Pig Binding pIC50 = 6.3 6.3 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 482 10 1 6 3.9 CCCCN(CC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
44385127 61388 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Tested for the inhibitory activity of cloned human ETB receptor by using I-ET-1 as radioligand in a competitive radioligand assayTested for the inhibitory activity of cloned human ETB receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 482 5 1 7 4.8 Cc1cc2c(cc1/C=C/c1ccsc1S(=O)(=O)Nc1onc(C)c1Br)OCO2 10.1016/S0960-894X(97)00133-9
CHEMBL176854 61388 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Tested for the inhibitory activity of cloned human ETB receptor by using I-ET-1 as radioligand in a competitive radioligand assayTested for the inhibitory activity of cloned human ETB receptor by using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 482 5 1 7 4.8 Cc1cc2c(cc1/C=C/c1ccsc1S(=O)(=O)Nc1onc(C)c1Br)OCO2 10.1016/S0960-894X(97)00133-9
44284115 100249 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 518 9 3 7 4.8 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(C)CO)c1 10.1016/j.bmcl.2004.01.008
CHEMBL288247 100249 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 518 9 3 7 4.8 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(C)CO)c1 10.1016/j.bmcl.2004.01.008
11826173 205278 None 0 Pig Binding pIC50 = 6.3 6.3 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 432 5 1 6 4.5 COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC)cc32)cc1 10.1021/jm010382z
CHEMBL62363 205278 None 0 Pig Binding pIC50 = 6.3 6.3 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 432 5 1 6 4.5 COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC)cc32)cc1 10.1021/jm010382z
44298956 198136 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membranesInhibition of [125I]ET1 binding to porcine kidney inner medulla membranes
ChEMBL 489 9 1 7 4.8 CCOc1ccc2c(c1)c(-c1ccc(OC)cc1OC)c(C(=O)O)c(=O)n2Cc1ccccc1OC 10.1016/S0960-894X(97)00319-3
CHEMBL55666 198136 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membranesInhibition of [125I]ET1 binding to porcine kidney inner medulla membranes
ChEMBL 489 9 1 7 4.8 CCOc1ccc2c(c1)c(-c1ccc(OC)cc1OC)c(C(=O)O)c(=O)n2Cc1ccccc1OC 10.1016/S0960-894X(97)00319-3
44270602 98912 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) receptor expressed in CHO cells
ChEMBL 688 13 1 10 7.0 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)NS(=O)(=O)c1cccs1)c1ccc2c(c1)OCO2 10.1016/0960-894X(95)00186-W
CHEMBL278930 98912 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) receptor expressed in CHO cells
ChEMBL 688 13 1 10 7.0 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)NS(=O)(=O)c1cccs1)c1ccc2c(c1)OCO2 10.1016/0960-894X(95)00186-W
10553165 9742 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 492 7 1 6 5.4 O=C1OC(O)(c2ccc(OCc3ccccc3)cc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2 10.1021/jm9606507
CHEMBL11341 9742 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 492 7 1 6 5.4 O=C1OC(O)(c2ccc(OCc3ccccc3)cc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2 10.1021/jm9606507
44276946 106902 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 440 5 1 5 4.2 COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3cc(Cl)c4c(c3)OCO4)c2=O)c1 10.1016/s0960-894x(00)00232-8
CHEMBL3144735 106902 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 440 5 1 5 4.2 COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3cc(Cl)c4c(c3)OCO4)c2=O)c1 10.1016/s0960-894x(00)00232-8
10650062 60464 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Inhibitory activity was evaluated against human Endothelin B receptorInhibitory activity was evaluated against human Endothelin B receptor
ChEMBL 537 10 4 6 4.8 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)OC(=O)NC2CCCCC2)nc1C(=O)O 10.1021/jm9505932
CHEMBL175228 60464 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Inhibitory activity was evaluated against human Endothelin B receptorInhibitory activity was evaluated against human Endothelin B receptor
ChEMBL 537 10 4 6 4.8 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)OC(=O)NC2CCCCC2)nc1C(=O)O 10.1021/jm9505932
18184206 60352 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 600 13 2 11 3.2 CCS(=O)(=O)NCCOc1nc(-c2ccncc2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
CHEMBL174413 60352 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 600 13 2 11 3.2 CCS(=O)(=O)NCCOc1nc(-c2ccncc2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
155564169 175437 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 545 11 1 12 2.0 COc1ccc(Cl)c(Oc2c(NS(C)(=O)=O)ncnc2OCCOc2ncc(S(C)(=O)=O)cn2)c1 10.1016/j.bmcl.2016.06.014
CHEMBL4574034 175437 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 545 11 1 12 2.0 COc1ccc(Cl)c(Oc2c(NS(C)(=O)=O)ncnc2OCCOc2ncc(S(C)(=O)=O)cn2)c1 10.1016/j.bmcl.2016.06.014
42630655 18414 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 557 11 2 7 5.5 CCCCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL1271586 18414 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 557 11 2 7 5.5 CCCCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2017.04.049
42630655 18414 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
ChEMBL 557 11 2 7 5.5 CCCCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2010.08.074
CHEMBL1271586 18414 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
ChEMBL 557 11 2 7 5.5 CCCCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2010.08.074
17869231 14632 None 0 Pig Binding pIC50 = 6.3 6.3 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 548 11 1 9 5.5 COc1cc(C/C(C(=O)c2ccc(OC(C)C)cc2)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC 10.1016/s0960-894x(98)00301-1
CHEMBL1205061 14632 None 0 Pig Binding pIC50 = 6.3 6.3 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 548 11 1 9 5.5 COc1cc(C/C(C(=O)c2ccc(OC(C)C)cc2)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC 10.1016/s0960-894x(98)00301-1
CHEMBL48315 14632 None 0 Pig Binding pIC50 = 6.3 6.3 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 548 11 1 9 5.5 COc1cc(C/C(C(=O)c2ccc(OC(C)C)cc2)=C(/C(=O)O)c2ccc3nsnc3c2)cc(OC)c1OC 10.1016/s0960-894x(98)00301-1
44327412 210040 None 0 Pig Binding pIC50 = 6.3 6.3 - 0
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranes
ChEMBL 497 5 1 8 3.0 Cc1cc(C)c(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c2ccc3c(c2)OCO3)n1 10.1016/S0960-894X(96)00617-8
CHEMBL94929 210040 None 0 Pig Binding pIC50 = 6.3 6.3 - 0
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranes
ChEMBL 497 5 1 8 3.0 Cc1cc(C)c(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c2ccc3c(c2)OCO3)n1 10.1016/S0960-894X(96)00617-8
44367767 43762 None 0 Pig Binding pIC50 = 5.3 5.3 - 0
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 469 9 2 6 4.5 COc1ccc(CN(Cc2cc3c(cc2Cl)OCO3)C(Cc2ccc(O)cc2)C(=O)O)cc1 10.1016/s0960-894x(01)00009-9
CHEMBL151064 43762 None 0 Pig Binding pIC50 = 5.3 5.3 - 0
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 469 9 2 6 4.5 COc1ccc(CN(Cc2cc3c(cc2Cl)OCO3)C(Cc2ccc(O)cc2)C(=O)O)cc1 10.1016/s0960-894x(01)00009-9
10814746 181700 None 0 Human Binding pIC50 = 5.3 5.3 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 484 6 1 8 3.8 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Cc2ccc3c(c2)OCO3)c1Br 10.1021/jm9700068
CHEMBL47706 181700 None 0 Human Binding pIC50 = 5.3 5.3 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 484 6 1 8 3.8 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Cc2ccc3c(c2)OCO3)c1Br 10.1021/jm9700068
44368481 121584 None 0 Pig Binding pIC50 = 4.3 4.3 - 0
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 435 9 2 7 2.8 CCOC(=O)CN(Cc1cc2c(cc1Cl)OCO2)C(Cc1ccc(O)cc1)C(=O)O 10.1016/s0960-894x(01)00009-9
CHEMBL358444 121584 None 0 Pig Binding pIC50 = 4.3 4.3 - 0
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 435 9 2 7 2.8 CCOC(=O)CN(Cc1cc2c(cc1Cl)OCO2)C(Cc1ccc(O)cc1)C(=O)O 10.1016/s0960-894x(01)00009-9
9840391 104595 None 4 Human Binding pIC50 = 4.3 4.3 - 1
Binding affinity against human ETB receptor in transfected COS 7 cell membrane preparationBinding affinity against human ETB receptor in transfected COS 7 cell membrane preparation
ChEMBL 328 4 1 4 3.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2)c1C 10.1016/0960-894X(96)00441-6
CHEMBL310427 104595 None 4 Human Binding pIC50 = 4.3 4.3 - 1
Binding affinity against human ETB receptor in transfected COS 7 cell membrane preparationBinding affinity against human ETB receptor in transfected COS 7 cell membrane preparation
ChEMBL 328 4 1 4 3.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2)c1C 10.1016/0960-894X(96)00441-6
10721386 60395 None 0 Pig Binding pIC50 = 4.3 4.3 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 550 11 5 5 4.8 CCn1cc(C[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2)c2nc(C(=O)O)c(C)[nH]2)c2ccccc21 10.1021/jm950592+
CHEMBL174686 60395 None 0 Pig Binding pIC50 = 4.3 4.3 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 550 11 5 5 4.8 CCn1cc(C[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2)c2nc(C(=O)O)c(C)[nH]2)c2ccccc21 10.1021/jm950592+
44386535 131433 None 0 Pig Binding pIC50 = 4.3 4.3 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 549 10 4 6 4.9 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)Nc2cccc(F)c2)nc1C(=O)O 10.1021/jm950592+
CHEMBL368853 131433 None 0 Pig Binding pIC50 = 4.3 4.3 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 549 10 4 6 4.9 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)Nc2cccc(F)c2)nc1C(=O)O 10.1021/jm950592+
CHEMBL414165 215575 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Inhibitory effect against Human Endothelin B receptorInhibitory effect against Human Endothelin B receptor
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](c2cccs2)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
71451528 81720 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Antagonist activity at ETB receptor (unknown origin)Antagonist activity at ETB receptor (unknown origin)
ChEMBL 631 14 1 12 4.3 CCCCS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC 10.1016/j.bmcl.2016.06.014
CHEMBL2163715 81720 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Antagonist activity at ETB receptor (unknown origin)Antagonist activity at ETB receptor (unknown origin)
ChEMBL 631 14 1 12 4.3 CCCCS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC 10.1016/j.bmcl.2016.06.014
71451528 81720 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 631 14 1 12 4.3 CCCCS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC 10.1021/jm3009103
CHEMBL2163715 81720 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 631 14 1 12 4.3 CCCCS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC 10.1021/jm3009103
71462248 81734 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 676 17 2 12 3.8 COCCOc1nc(NS(=O)(=O)NCc2ccccc2)c(Oc2ccccc2OC)c(OCCOc2ncc(Br)cn2)n1 10.1021/jm3009103
CHEMBL2163728 81734 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 676 17 2 12 3.8 COCCOc1nc(NS(=O)(=O)NCc2ccccc2)c(Oc2ccccc2OC)c(OCCOc2ncc(Br)cn2)n1 10.1021/jm3009103
21041307 175073 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 482 10 2 9 2.6 CNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL4566095 175073 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 482 10 2 9 2.6 CNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL265116 213094 None 0 Rat Binding pIC50 = 7.3 7.3 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00015a003
44298324 198325 None 0 Pig Binding pIC50 = 6.3 6.3 - 0
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptor
ChEMBL 448 7 2 7 4.4 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CO)c1 10.1016/s0960-894x(00)00366-8
CHEMBL55876 198325 None 0 Pig Binding pIC50 = 6.3 6.3 - 0
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptor
ChEMBL 448 7 2 7 4.4 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CO)c1 10.1016/s0960-894x(00)00366-8
9869444 97299 None 0 Human Binding pIC50 = 5.3 5.3 - 1
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 473 7 1 7 5.3 CCCOc1ccc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2c1 10.1016/0960-894X(96)00170-9
CHEMBL268751 97299 None 0 Human Binding pIC50 = 5.3 5.3 - 1
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 473 7 1 7 5.3 CCCOc1ccc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2c1 10.1016/0960-894X(96)00170-9
10769045 131285 None 0 Pig Binding pIC50 = 4.3 4.3 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 551 10 4 6 5.0 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2(C)CCCCC2)nc1C(=O)O 10.1021/jm950592+
CHEMBL368641 131285 None 0 Pig Binding pIC50 = 4.3 4.3 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 551 10 4 6 5.0 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2(C)CCCCC2)nc1C(=O)O 10.1021/jm950592+
71455065 81730 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 679 14 2 11 4.8 COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)nc(-c2ccncc2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
CHEMBL2163724 81730 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 679 14 2 11 4.8 COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)nc(-c2ccncc2)nc1OCCOc1ncc(Br)cn1 10.1021/jm3009103
137655285 159069 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 568 10 3 10 3.1 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(-c4nnn[nH]4)c3)c(=O)c3cc(OCCN)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL4096211 159069 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 568 10 3 10 3.1 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(-c4nnn[nH]4)c3)c(=O)c3cc(OCCN)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
23445219 112538 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 428 5 1 6 4.3 COc1cccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c1 10.1016/S0960-894X(96)00496-9
CHEMBL329861 112538 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 428 5 1 6 4.3 COc1cccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c1 10.1016/S0960-894X(96)00496-9
10129267 81719 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 617 13 1 12 3.9 CCCS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC 10.1021/jm3009103
CHEMBL2163714 81719 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 617 13 1 12 3.9 CCCS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC 10.1021/jm3009103
44384723 130955 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 563 13 2 10 3.0 CCS(=O)(=O)NCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
CHEMBL368528 130955 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 563 13 2 10 3.0 CCS(=O)(=O)NCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
58688008 175406 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 496 11 2 9 3.0 CCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL4573273 175406 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 496 11 2 9 3.0 CCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2016.06.014
155563100 175380 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 619 13 2 10 4.6 COc1cnc(OCCOc2nc(-c3ccncc3)nc(NS(=O)(=O)NCc3ccccc3)c2-c2ccc(Cl)cc2)nc1 10.1016/j.bmcl.2016.06.014
CHEMBL4572734 175380 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 619 13 2 10 4.6 COc1cnc(OCCOc2nc(-c3ccncc3)nc(NS(=O)(=O)NCc3ccccc3)c2-c2ccc(Cl)cc2)nc1 10.1016/j.bmcl.2016.06.014
9829478 175429 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 567 10 1 8 4.9 Cc1ccc(-c2c(NS(=O)(=O)/C=C/c3ccccc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL4573806 175429 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 567 10 1 8 4.9 Cc1ccc(-c2c(NS(=O)(=O)/C=C/c3ccccc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1016/j.bmcl.2016.06.014
10281929 9395 None 0 Pig Binding pIC50 = 7.2 7.2 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 588 16 1 7 5.3 CCCCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm970101g
CHEMBL111517 9395 None 0 Pig Binding pIC50 = 7.2 7.2 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 588 16 1 7 5.3 CCCCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm970101g
10816152 16340 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 534 9 2 8 3.9 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(OC)cccc2OC)cc1 10.1021/jm990170q
CHEMBL122832 16340 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 534 9 2 8 3.9 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(OC)cccc2OC)cc1 10.1021/jm990170q
9826741 100812 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B receptor
ChEMBL 486 5 1 9 3.6 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Oc2ccc3c(c2)OCO3)c1Br 10.1016/S0960-894X(97)00132-7
CHEMBL292802 100812 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B receptor
ChEMBL 486 5 1 9 3.6 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Oc2ccc3c(c2)OCO3)c1Br 10.1016/S0960-894X(97)00132-7
44327734 210559 None 0 Pig Binding pIC50 = 5.2 5.2 - 0
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranes
ChEMBL 561 8 1 9 3.9 COc1ccc(-c2ccc(=O)n(C(C(=O)NS(=O)(=O)c3ccc(C(C)C)cc3)c3ccc4c(c3)OCO4)n2)cc1 10.1016/S0960-894X(96)00617-8
CHEMBL97851 210559 None 0 Pig Binding pIC50 = 5.2 5.2 - 0
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranes
ChEMBL 561 8 1 9 3.9 COc1ccc(-c2ccc(=O)n(C(C(=O)NS(=O)(=O)c3ccc(C(C)C)cc3)c3ccc4c(c3)OCO4)n2)cc1 10.1016/S0960-894X(96)00617-8
10265127 96889 None 1 Human Binding pIC50 = 4.2 4.2 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 270 3 1 4 2.2 Cc1noc(NS(=O)(=O)c2ccc(F)cc2)c1C 10.1016/0960-894X(96)00441-6
CHEMBL26522 96889 None 1 Human Binding pIC50 = 4.2 4.2 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 270 3 1 4 2.2 Cc1noc(NS(=O)(=O)c2ccc(F)cc2)c1C 10.1016/0960-894X(96)00441-6
10076527 14621 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
ChEMBL 485 7 2 6 4.3 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3ccccc31)OCO2 10.1016/j.bmcl.2010.08.074
CHEMBL1204990 14621 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
ChEMBL 485 7 2 6 4.3 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3ccccc31)OCO2 10.1016/j.bmcl.2010.08.074
22467237 85377 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cells
ChEMBL 549 8 3 8 2.3 Cn1cc(C(C(=O)NS(=O)(=O)c2ccc(CC(=O)O)cc2)c2ccc3c(c2)OCO3)c2ccc(C(N)=O)cc21 10.1007/s00044-004-0021-y
CHEMBL2261357 85377 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cells
ChEMBL 549 8 3 8 2.3 Cn1cc(C(C(=O)NS(=O)(=O)c2ccc(CC(=O)O)cc2)c2ccc3c(c2)OCO3)c2ccc(C(N)=O)cc21 10.1007/s00044-004-0021-y
9826741 100812 None 0 Human Binding pIC50 = 5.2 5.2 - 0
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB receptor
ChEMBL 486 5 1 9 3.6 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Oc2ccc3c(c2)OCO3)c1Br 10.1016/S0960-894X(97)00367-3
CHEMBL292802 100812 None 0 Human Binding pIC50 = 5.2 5.2 - 0
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB receptor
ChEMBL 486 5 1 9 3.6 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Oc2ccc3c(c2)OCO3)c1Br 10.1016/S0960-894X(97)00367-3
10599230 209453 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Radioligand binding selectivity to human Endothelin B receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin B receptor in chinese hamster ovary cells
ChEMBL 440 8 2 6 2.8 CCCNC(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL9141 209453 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Radioligand binding selectivity to human Endothelin B receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin B receptor in chinese hamster ovary cells
ChEMBL 440 8 2 6 2.8 CCCNC(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
11113541 205726 None 0 Pig Binding pIC50 = 7.2 7.2 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 476 7 1 7 5.2 COc1ccc(OC2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
CHEMBL64632 205726 None 0 Pig Binding pIC50 = 7.2 7.2 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 476 7 1 7 5.2 COc1ccc(OC2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
11015023 102775 None 0 Pig Binding pIC50 = 5.2 5.2 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 406 3 1 4 5.1 O=C(O)C1=C(c2ccc(Cl)cc2)c2ccccc2OC1c1ccc2c(c1)OCO2 10.1021/jm010382z
CHEMBL304875 102775 None 0 Pig Binding pIC50 = 5.2 5.2 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 406 3 1 4 5.1 O=C(O)C1=C(c2ccc(Cl)cc2)c2ccccc2OC1c1ccc2c(c1)OCO2 10.1021/jm010382z
11826259 205363 None 0 Pig Binding pIC50 = 5.2 5.2 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 437 8 1 7 4.5 CC(C)Oc1ccc2c(c1)C(OCCCC#N)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
CHEMBL62759 205363 None 0 Pig Binding pIC50 = 5.2 5.2 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 437 8 1 7 4.5 CC(C)Oc1ccc2c(c1)C(OCCCC#N)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
44316527 207938 None 0 Human Binding pIC50 = 4.2 4.2 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 280 3 1 4 2.7 Cc1ccc(C)c(S(=O)(=O)Nc2onc(C)c2C)c1 10.1016/0960-894X(96)00441-6
CHEMBL80532 207938 None 0 Human Binding pIC50 = 4.2 4.2 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 280 3 1 4 2.7 Cc1ccc(C)c(S(=O)(=O)Nc2onc(C)c2C)c1 10.1016/0960-894X(96)00441-6
10211772 56539 None 0 Human Binding pIC50 = 6.2 6.2 - 1
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 660 11 2 12 4.2 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccccc1 10.1016/s0960-894x(02)01084-3
CHEMBL163638 56539 None 0 Human Binding pIC50 = 6.2 6.2 - 1
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 660 11 2 12 4.2 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccccc1 10.1016/s0960-894x(02)01084-3
10815167 101247 None 0 Human Binding pIC50 = 5.2 5.2 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 497 7 2 6 5.4 CCC(C)c1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1021/jm9608366
CHEMBL295697 101247 None 0 Human Binding pIC50 = 5.2 5.2 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 497 7 2 6 5.4 CCC(C)c1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1021/jm9608366
CHEMBL2304015 211930 None 0 Pig Binding pIC50 = 7.2 7.2 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL None None None Cc1[nH]c2ccccc2c1C[C@@H]1NC(=O)[C@@H](C2CC2)NC(=O)[C@H](C2CCCC2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC1=O 10.1021/jm9600914
CHEMBL405599 215028 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Binding affinity measured in CHO cells stably transfected with the human endothelin B receptorBinding affinity measured in CHO cells stably transfected with the human endothelin B receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
44328019 155794 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL 1000 26 9 8 5.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL405178 155794 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL 1000 26 9 8 5.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
44327347 96816 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Binding affinity measured in CHO cells stably transfected with the human endothelin B receptorBinding affinity measured in CHO cells stably transfected with the human endothelin B receptor
ChEMBL 1102 26 9 8 7.1 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C1c2ccccc2CCc2ccccc21)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL264579 96816 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Binding affinity measured in CHO cells stably transfected with the human endothelin B receptorBinding affinity measured in CHO cells stably transfected with the human endothelin B receptor
ChEMBL 1102 26 9 8 7.1 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C1c2ccccc2CCc2ccccc21)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
10961510 205293 None 0 Pig Binding pIC50 = 5.2 5.2 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 458 7 1 4 6.6 COc1ccc(C2=C(C(=O)O)C(c3ccc(C(C)C)cc3)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
CHEMBL62425 205293 None 0 Pig Binding pIC50 = 5.2 5.2 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 458 7 1 4 6.6 COc1ccc(C2=C(C(=O)O)C(c3ccc(C(C)C)cc3)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
10696788 176019 None 0 Human Binding pIC50 = 5.2 5.2 - 0
In vitro inhibitory activity against human Endothelin B receptor using radioligand binding assay.In vitro inhibitory activity against human Endothelin B receptor using radioligand binding assay.
ChEMBL 501 5 2 9 3.9 Cc1noc(NS(=O)(=O)c2ccsc2NC(=O)Oc2ccc3c(c2)OCO3)c1Br 10.1021/jm9700068
CHEMBL45872 176019 None 0 Human Binding pIC50 = 5.2 5.2 - 0
In vitro inhibitory activity against human Endothelin B receptor using radioligand binding assay.In vitro inhibitory activity against human Endothelin B receptor using radioligand binding assay.
ChEMBL 501 5 2 9 3.9 Cc1noc(NS(=O)(=O)c2ccsc2NC(=O)Oc2ccc3c(c2)OCO3)c1Br 10.1021/jm9700068
44316526 207879 None 1 Human Binding pIC50 = 4.2 4.2 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 344 3 1 4 3.2 Cc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1C 10.1016/0960-894X(96)00441-6
CHEMBL80180 207879 None 1 Human Binding pIC50 = 4.2 4.2 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 344 3 1 4 3.2 Cc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1C 10.1016/0960-894X(96)00441-6
23445506 112621 None 0 Human Binding pIC50 = 4.2 4.2 - 0
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 428 5 1 6 4.3 COc1ccccc1-c1ccsc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/S0960-894X(96)00496-9
CHEMBL330003 112621 None 0 Human Binding pIC50 = 4.2 4.2 - 0
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 428 5 1 6 4.3 COc1ccccc1-c1ccsc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/S0960-894X(96)00496-9
23445227 120889 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B receptor
ChEMBL 472 6 1 8 3.9 Cc1noc(NS(=O)(=O)c2ccsc2COc2ccc3c(c2)OCO3)c1Br 10.1016/S0960-894X(97)00132-7
CHEMBL355800 120889 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B receptor
ChEMBL 472 6 1 8 3.9 Cc1noc(NS(=O)(=O)c2ccsc2COc2ccc3c(c2)OCO3)c1Br 10.1016/S0960-894X(97)00132-7
10719598 209448 None 0 Pig Binding pIC50 = 6.2 6.2 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 482 10 1 6 3.9 CCCN(CCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL9139 209448 None 0 Pig Binding pIC50 = 6.2 6.2 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 482 10 1 6 3.9 CCCN(CCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
44284437 100038 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 520 9 4 8 3.5 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(O)CO)c1 10.1016/j.bmcl.2004.01.008
CHEMBL286621 100038 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 520 9 4 8 3.5 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(O)CO)c1 10.1016/j.bmcl.2004.01.008
10722389 12129 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 606 10 2 6 6.0 CCc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1C 10.1021/jm990171i
CHEMBL1184099 12129 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 606 10 2 6 6.0 CCc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1C 10.1021/jm990171i
CHEMBL332424 12129 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 606 10 2 6 6.0 CCc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1C 10.1021/jm990171i
44314661 103080 None 0 Pig Binding pIC50 = 8.2 8.2 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 603 14 5 4 5.1 CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(CCCC)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
CHEMBL306977 103080 None 0 Pig Binding pIC50 = 8.2 8.2 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 603 14 5 4 5.1 CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(CCCC)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
44314645 172775 None 0 Pig Binding pIC50 = 8.2 8.2 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 601 13 5 4 4.7 CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(CC1CC1)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
CHEMBL449962 172775 None 0 Pig Binding pIC50 = 8.2 8.2 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 601 13 5 4 4.7 CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(CC1CC1)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
10507211 110427 None 0 Pig Binding pIC50 = 8.2 8.2 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 566 13 1 7 3.9 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)CCCCl 10.1021/jm970101g
CHEMBL324214 110427 None 0 Pig Binding pIC50 = 8.2 8.2 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 566 13 1 7 3.9 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)CCCCl 10.1021/jm970101g
44320783 106749 None 0 Rat Binding pIC50 = 8.2 8.2 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 453 6 1 6 5.2 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2cccnc2)nn1CC1CCCCC1 10.1016/s0960-894x(00)00513-8
CHEMBL314357 106749 None 0 Rat Binding pIC50 = 8.2 8.2 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 453 6 1 6 5.2 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2cccnc2)nn1CC1CCCCC1 10.1016/s0960-894x(00)00513-8
1009 194 None 25 Human Binding pIC50 = 8.2 8.2 676 2
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 558 11 2 6 5.8 CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2 10.1021/jm990170q
5310991 194 None 25 Human Binding pIC50 = 8.2 8.2 676 2
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 558 11 2 6 5.8 CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2 10.1021/jm990170q
CHEMBL332794 194 None 25 Human Binding pIC50 = 8.2 8.2 676 2
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 558 11 2 6 5.8 CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2 10.1021/jm990170q
10841576 11447 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 620 11 2 6 6.3 CCc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1CC 10.1021/jm990171i
CHEMBL1180336 11447 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 620 11 2 6 6.3 CCc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1CC 10.1021/jm990171i
CHEMBL122673 11447 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 620 11 2 6 6.3 CCc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1CC 10.1021/jm990171i
10650477 114313 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 558 10 2 6 5.8 CCc1cccc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC(C)C)cc1 10.1021/jm990170q
CHEMBL333009 114313 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 558 10 2 6 5.8 CCc1cccc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC(C)C)cc1 10.1021/jm990170q
10209319 9372 None 0 Pig Binding pIC50 = 7.2 7.2 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 546 13 1 7 4.1 CCCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)CCC 10.1021/jm970101g
CHEMBL111355 9372 None 0 Pig Binding pIC50 = 7.2 7.2 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 546 13 1 7 4.1 CCCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)CCC 10.1021/jm970101g
CHEMBL412460 215451 None 0 Rat Binding pIC50 = 7.2 7.2 - 0
Binding affinity against Endothelin B receptor in rat cerebellar membrane (ET-B) from adult blue laurie ratBinding affinity against Endothelin B receptor in rat cerebellar membrane (ET-B) from adult blue laurie rat
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)80156-6
CHEMBL328942 213775 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Binding affinity against endothelin B receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin B receptor from rabbit renal vascular smooth muscles
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL433349 216098 None 0 Rat Binding pIC50 = 7.2 7.2 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
9896251 98827 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Compound was evaluated for inhibitory activity against human Endothelin B receptor (ETB)Compound was evaluated for inhibitory activity against human Endothelin B receptor (ETB)
ChEMBL 682 12 1 9 7.1 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2 10.1021/jm020138n
CHEMBL278176 98827 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Compound was evaluated for inhibitory activity against human Endothelin B receptor (ETB)Compound was evaluated for inhibitory activity against human Endothelin B receptor (ETB)
ChEMBL 682 12 1 9 7.1 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2 10.1021/jm020138n
44213959 170471 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta cell membranes
ChEMBL 592 11 3 9 5.0 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C(=O)Nc2ccccc2)nc1OCCO 10.1016/j.bmcl.2016.06.014
CHEMBL4447655 170471 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta cell membranes
ChEMBL 592 11 3 9 5.0 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C(=O)Nc2ccccc2)nc1OCCO 10.1016/j.bmcl.2016.06.014
CHEMBL313984 213582 None 0 Rat Binding pIC50 = 7.2 7.2 - 0
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00070a001
CHEMBL1791271 211375 None 1 Rat Binding pIC50 = 7.2 7.2 - 0
Inhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellumInhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)[C@H](C)CC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(95)00152-J
9896251 98827 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) receptor expressed in CHO cells
ChEMBL 682 12 1 9 7.1 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2 10.1016/0960-894X(95)00186-W
CHEMBL278176 98827 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) receptor expressed in CHO cells
ChEMBL 682 12 1 9 7.1 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2 10.1016/0960-894X(95)00186-W
44404967 135489 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Inhibitory concentration against endothelin receptor type BInhibitory concentration against endothelin receptor type B
ChEMBL 680 12 1 8 7.3 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCC2 10.1021/jm058225d
CHEMBL372814 135489 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Inhibitory concentration against endothelin receptor type BInhibitory concentration against endothelin receptor type B
ChEMBL 680 12 1 8 7.3 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCC2 10.1021/jm058225d
44311528 206600 None 0 Human Binding pIC50 = 7.2 7.2 - 1
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 633 12 2 10 6.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C2CC2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
CHEMBL70487 206600 None 0 Human Binding pIC50 = 7.2 7.2 - 1
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 633 12 2 10 6.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C2CC2)nc1OCCOC(=O)Nc1ccccn1 10.1016/S0960-894X(97)00400-9
10650546 12124 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 562 7 2 6 5.2 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC2c3ccccc3-c3ccccc32)cc1 10.1021/jm990171i
CHEMBL1184091 12124 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 562 7 2 6 5.2 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC2c3ccccc3-c3ccccc32)cc1 10.1021/jm990171i
CHEMBL332144 12124 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 562 7 2 6 5.2 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC2c3ccccc3-c3ccccc32)cc1 10.1021/jm990171i
44327656 141876 None 0 Rat Binding pIC50 = 6.2 6.2 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL 977 25 9 8 4.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C(F)(F)F)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL386181 141876 None 0 Rat Binding pIC50 = 6.2 6.2 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL 977 25 9 8 4.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C(F)(F)F)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
10918533 102898 None 0 Pig Binding pIC50 = 6.2 6.2 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 536 8 1 6 6.8 CC(C)Oc1ccc2c(c1)C(c1ccc(OCc3ccccc3)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
CHEMBL305577 102898 None 0 Pig Binding pIC50 = 6.2 6.2 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 536 8 1 6 6.8 CC(C)Oc1ccc2c(c1)C(c1ccc(OCc3ccccc3)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
10674095 113577 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 544 9 1 6 5.1 CCc1cccc(CC)c1N(C)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm990170q
CHEMBL332093 113577 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 544 9 1 6 5.1 CCc1cccc(CC)c1N(C)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm990170q
8260 531 None 42 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta cell membranes
ChEMBL 479 8 1 9 3.9 COc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cn1)C)c1ccncc1 10.1016/j.bmcl.2016.06.014
9912992 531 None 42 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta cell membranes
ChEMBL 479 8 1 9 3.9 COc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cn1)C)c1ccncc1 10.1016/j.bmcl.2016.06.014
CHEMBL3989834 531 None 42 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta cell membranes
ChEMBL 479 8 1 9 3.9 COc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cn1)C)c1ccncc1 10.1016/j.bmcl.2016.06.014
10578853 103647 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.
ChEMBL 564 10 1 11 3.4 COC(=O)COc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc(OC)c1OC 10.1021/jm980504w
CHEMBL308646 103647 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.
ChEMBL 564 10 1 11 3.4 COC(=O)COc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc(OC)c1OC 10.1021/jm980504w
CHEMBL1793926 211389 None 0 Rat Binding pIC50 = 6.2 6.2 - 0
Inhibition of binding to Endothelin B receptor of rat cerebellar membranes.Inhibition of binding to Endothelin B receptor of rat cerebellar membranes.
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm970161m
CHEMBL318020 213668 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00015a003
10504689 9443 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 474 6 1 8 3.6 COC(=O)c1cccc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)c1 10.1021/jm9606507
CHEMBL11176 9443 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 474 6 1 8 3.6 COC(=O)c1cccc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)c1 10.1021/jm9606507
10895198 101008 None 0 Pig Binding pIC50 = 5.2 5.2 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 426 9 1 6 5.0 CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2cccc(OCCC)c21 10.1021/jm010382z
CHEMBL294123 101008 None 0 Pig Binding pIC50 = 5.2 5.2 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 426 9 1 6 5.0 CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2cccc(OCCC)c21 10.1021/jm010382z
10814318 9154 None 0 Human Binding pIC50 = 4.2 4.2 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 472 14 1 5 4.7 C=CCCC[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC 10.1021/jm980217s
CHEMBL110064 9154 None 0 Human Binding pIC50 = 4.2 4.2 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 472 14 1 5 4.7 C=CCCC[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC 10.1021/jm980217s
44439102 90333 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [125I]ET1 from human ETB receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETB receptor expressed in CHO cells
ChEMBL 508 8 1 7 5.2 CN(Cc1cc(-c2ncco2)ccc1-c1ccccc1S(=O)(=O)Nc1ccno1)C(=O)CC(C)(C)C 10.1016/j.bmcl.2006.10.009
CHEMBL238539 90333 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [125I]ET1 from human ETB receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETB receptor expressed in CHO cells
ChEMBL 508 8 1 7 5.2 CN(Cc1cc(-c2ncco2)ccc1-c1ccccc1S(=O)(=O)Nc1ccno1)C(=O)CC(C)(C)C 10.1016/j.bmcl.2006.10.009
10305181 60469 None 0 Human Binding pIC50 = 6.2 6.2 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 666 11 2 12 4.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)NC1CCCCC1 10.1016/s0960-894x(02)01084-3
CHEMBL175278 60469 None 0 Human Binding pIC50 = 6.2 6.2 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 666 11 2 12 4.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)NC1CCCCC1 10.1016/s0960-894x(02)01084-3
23445498 209158 None 0 Human Binding pIC50 = 4.2 4.2 - 0
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 426 4 1 5 4.9 Cc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(96)00496-9
CHEMBL89688 209158 None 0 Human Binding pIC50 = 4.2 4.2 - 0
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 426 4 1 5 4.9 Cc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(96)00496-9
44284041 100357 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 520 9 3 8 4.4 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(OC(C)CO)c1 10.1016/j.bmcl.2004.01.008
CHEMBL289216 100357 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 520 9 3 8 4.4 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(OC(C)CO)c1 10.1016/j.bmcl.2004.01.008
11801523 8258 None 0 Pig Binding pIC50 = 6.2 6.2 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 588 16 1 7 5.3 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCC)cc1 10.1021/jm970101g
CHEMBL109242 8258 None 0 Pig Binding pIC50 = 6.2 6.2 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 588 16 1 7 5.3 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCCC)cc1 10.1021/jm970101g
15453170 104957 None 3 Human Binding pIC50 = 6.2 6.2 - 0
Binding affinity against human ETB receptor in transfected COS 7 cell membrane preparationBinding affinity against human ETB receptor in transfected COS 7 cell membrane preparation
ChEMBL 328 4 1 4 3.8 Cc1noc(NS(=O)(=O)c2ccc(-c3ccccc3)cc2)c1C 10.1016/0960-894X(96)00441-6
CHEMBL311258 104957 None 3 Human Binding pIC50 = 6.2 6.2 - 0
Binding affinity against human ETB receptor in transfected COS 7 cell membrane preparationBinding affinity against human ETB receptor in transfected COS 7 cell membrane preparation
ChEMBL 328 4 1 4 3.8 Cc1noc(NS(=O)(=O)c2ccc(-c3ccccc3)cc2)c1C 10.1016/0960-894X(96)00441-6
10916597 205773 None 0 Pig Binding pIC50 = 6.2 6.2 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 410 7 1 5 5.4 CCCCC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL64832 205773 None 0 Pig Binding pIC50 = 6.2 6.2 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 410 7 1 5 5.4 CCCCC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL2370254 212277 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
44291583 101445 None 0 Human Binding pIC50 = 4.2 4.2 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 500 8 3 9 2.9 COc1cc(OC)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(N)=O)c1 10.1021/jm9608366
CHEMBL297215 101445 None 0 Human Binding pIC50 = 4.2 4.2 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 500 8 3 9 2.9 COc1cc(OC)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(N)=O)c1 10.1021/jm9608366
CHEMBL336033 214033 None 0 Human Binding pIC50 = 4.2 4.2 - 0
Inhibitory effect against Human Endothelin B receptorInhibitory effect against Human Endothelin B receptor
ChEMBL None None None CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm00021a021
23445285 112440 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 454 7 1 5 5.6 CCCCc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(96)00496-9
CHEMBL329560 112440 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 454 7 1 5 5.6 CCCCc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(96)00496-9
58688006 171219 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 524 13 2 9 3.8 CCCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL4458005 171219 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 524 13 2 9 3.8 CCCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2016.06.014
10165809 131867 None 0 Human Binding pIC50 = 6.2 6.2 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 541 9 2 11 2.0 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCO 10.1016/s0960-894x(02)01084-3
CHEMBL369362 131867 None 0 Human Binding pIC50 = 6.2 6.2 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 541 9 2 11 2.0 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCO 10.1016/s0960-894x(02)01084-3
137637038 156031 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 581 11 2 9 5.0 CCCCOc1ccc2c(c1)c(=O)c(Cc1cccc(-c3nnn[nH]3)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL4061110 156031 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 581 11 2 9 5.0 CCCCOc1ccc2c(c1)c(=O)c(Cc1cccc(-c3nnn[nH]3)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2017.04.049
10577255 175523 None 0 Human Binding pIC50 = 5.2 5.2 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 497 8 2 6 5.2 CCCCc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1021/jm9608366
CHEMBL45760 175523 None 0 Human Binding pIC50 = 5.2 5.2 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 497 8 2 6 5.2 CCCCc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1021/jm9608366
10576378 101177 None 0 Human Binding pIC50 = 4.2 4.2 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 471 6 2 7 3.9 COc1ccccc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Br 10.1021/jm9608366
CHEMBL295207 101177 None 0 Human Binding pIC50 = 4.2 4.2 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 471 6 2 7 3.9 COc1ccccc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Br 10.1021/jm9608366
10623888 163253 None 0 Pig Binding pIC50 = 5.2 5.2 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 461 8 1 6 3.4 CCCCS(=O)(=O)N1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL417971 163253 None 0 Pig Binding pIC50 = 5.2 5.2 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 461 8 1 6 3.4 CCCCS(=O)(=O)N1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
10230835 110289 None 0 Pig Binding pIC50 = 7.2 7.2 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 546 12 1 7 4.0 CCCS(=O)(=O)N(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)CC(C)C 10.1021/jm970101g
CHEMBL323789 110289 None 0 Pig Binding pIC50 = 7.2 7.2 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 546 12 1 7 4.0 CCCS(=O)(=O)N(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)CC(C)C 10.1021/jm970101g
10344914 100191 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 476 7 3 7 4.1 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CO)c1 10.1016/j.bmcl.2004.01.008
CHEMBL287711 100191 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 476 7 3 7 4.1 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CO)c1 10.1016/j.bmcl.2004.01.008
9936145 19034 None 2 Human Binding pIC50 = 5.2 5.2 - 1
Binding affinity against human endothelin B receptor in CHO cellsBinding affinity against human endothelin B receptor in CHO cells
ChEMBL 510 11 1 4 5.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(C)c(F)c1 10.1021/jm010237l
CHEMBL128818 19034 None 2 Human Binding pIC50 = 5.2 5.2 - 1
Binding affinity against human endothelin B receptor in CHO cellsBinding affinity against human endothelin B receptor in CHO cells
ChEMBL 510 11 1 4 5.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(C)c(F)c1 10.1021/jm010237l
10577829 9669 None 0 Human Binding pIC50 = 4.2 4.2 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 518 13 1 7 3.9 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC1OCCCO1 10.1021/jm980217s
CHEMBL112877 9669 None 0 Human Binding pIC50 = 4.2 4.2 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 518 13 1 7 3.9 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC1OCCCO1 10.1021/jm980217s
10278777 168235 None 0 Human Binding pIC50 = 4.2 4.2 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 502 14 1 5 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC 10.1021/jm980217s
CHEMBL432974 168235 None 0 Human Binding pIC50 = 4.2 4.2 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 502 14 1 5 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC 10.1021/jm980217s
44322947 209159 None 0 Human Binding pIC50 = 4.2 4.2 - 0
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 428 5 1 6 4.3 COc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(96)00496-9
CHEMBL89689 209159 None 0 Human Binding pIC50 = 4.2 4.2 - 0
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 428 5 1 6 4.3 COc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(96)00496-9
11798998 209293 None 0 Pig Binding pIC50 = 6.2 6.2 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 482 10 1 6 3.9 CCCCCN(C)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL9050 209293 None 0 Pig Binding pIC50 = 6.2 6.2 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 482 10 1 6 3.9 CCCCCN(C)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
21041284 171040 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 568 13 2 9 3.9 CCCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Br)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL4455360 171040 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 568 13 2 9 3.9 CCCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Br)cc1 10.1016/j.bmcl.2016.06.014
44334065 167925 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B receptor
ChEMBL 429 5 1 5 4.7 COc1ccc([C@@H]2c3nc(C4CC4)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1016/s0960-894x(02)00663-7
CHEMBL430695 167925 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B receptor
ChEMBL 429 5 1 5 4.7 COc1ccc([C@@H]2c3nc(C4CC4)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1016/s0960-894x(02)00663-7
44334146 168103 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B receptor
ChEMBL 446 7 2 6 4.6 CCCNc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(02)00663-7
CHEMBL432012 168103 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B receptor
ChEMBL 446 7 2 6 4.6 CCCNc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(02)00663-7
44311285 102354 None 0 Human Binding pIC50 = 7.2 7.2 - 1
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 635 13 2 10 6.4 CCCc1nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c(Oc2ccccc2OC)c(OCCOC(=O)Nc2ccccn2)n1 10.1016/S0960-894X(97)00400-9
CHEMBL303428 102354 None 0 Human Binding pIC50 = 7.2 7.2 - 1
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 635 13 2 10 6.4 CCCc1nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c(Oc2ccccc2OC)c(OCCOC(=O)Nc2ccccn2)n1 10.1016/S0960-894X(97)00400-9
159594 522 None 36 Human Binding pIC50 = 7.2 7.2 -4073 3
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm990171i
159594.0 522 None 36 Human Binding pIC50 = 7.2 7.2 -4073 3
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm990171i
3487 522 None 36 Human Binding pIC50 = 7.2 7.2 -4073 3
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm990171i
CHEMBL9194 522 None 36 Human Binding pIC50 = 7.2 7.2 -4073 3
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm990171i
DB06199 522 None 36 Human Binding pIC50 = 7.2 7.2 -4073 3
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm990171i
44327881 161769 None 0 Rat Binding pIC50 = 6.2 6.2 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL 1044 26 9 8 6.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C12CC3CC(CC(C3)C1)C2)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
CHEMBL413179 161769 None 0 Rat Binding pIC50 = 6.2 6.2 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL 1044 26 9 8 6.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C12CC3CC(CC(C3)C1)C2)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
10597575 6898 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 408 5 1 6 4.2 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2CC2CCCC2)cc1 10.1021/jm9606507
CHEMBL10843 6898 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 408 5 1 6 4.2 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2CC2CCCC2)cc1 10.1021/jm9606507
10576377 12011 None 0 Human Binding pIC50 = 4.2 4.2 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 471 6 2 7 3.9 COc1cccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c1 10.1021/jm9608366
CHEMBL1183291 12011 None 0 Human Binding pIC50 = 4.2 4.2 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 471 6 2 7 3.9 COc1cccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c1 10.1021/jm9608366
CHEMBL288967 12011 None 0 Human Binding pIC50 = 4.2 4.2 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 471 6 2 7 3.9 COc1cccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c1 10.1021/jm9608366
10503525 5869 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 446 6 1 7 3.8 COc1ccc(C2(O)OC(=O)C(c3cc(OC)c4c(c3)OCO4)=C2Cc2ccccc2)cc1 10.1021/jm9606507
CHEMBL10794 5869 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 446 6 1 7 3.8 COc1ccc(C2(O)OC(=O)C(c3cc(OC)c4c(c3)OCO4)=C2Cc2ccccc2)cc1 10.1021/jm9606507
44368414 121351 None 0 Pig Binding pIC50 = 5.2 5.2 - 0
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 459 9 1 5 4.2 COc1ccc(CN(C(=O)/C=C/c2ccc3c(c2)OCO3)C(Cc2ccccc2)C(=O)O)cc1 10.1016/s0960-894x(01)00009-9
CHEMBL357978 121351 None 0 Pig Binding pIC50 = 5.2 5.2 - 0
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 459 9 1 5 4.2 COc1ccc(CN(C(=O)/C=C/c2ccc3c(c2)OCO3)C(Cc2ccccc2)C(=O)O)cc1 10.1016/s0960-894x(01)00009-9
44371396 49532 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 471 6 1 6 5.9 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3SC)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(99)00040-2
CHEMBL156532 49532 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 471 6 1 6 5.9 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3SC)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(99)00040-2
10992620 205808 None 0 Pig Binding pIC50 = 5.2 5.2 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 384 5 1 6 3.8 COC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL65070 205808 None 0 Pig Binding pIC50 = 5.2 5.2 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 384 5 1 6 3.8 COC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
10766067 9740 None 0 Pig Binding pIC50 = 5.2 5.2 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 452 8 1 5 3.3 CCCN(C)C(=O)CN1C[C@H](c2ccc3c(c2)OCC3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL113379 9740 None 0 Pig Binding pIC50 = 5.2 5.2 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 452 8 1 5 3.3 CCCN(C)C(=O)CN1C[C@H](c2ccc3c(c2)OCC3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
44213924 209955 None 0 Pig Binding pIC50 = 5.2 5.2 - 0
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranes
ChEMBL 567 7 1 7 4.8 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)N2N=C(c3ccc(Cl)cc3)CCC2=O)cc1 10.1016/S0960-894X(96)00617-8
CHEMBL94426 209955 None 0 Pig Binding pIC50 = 5.2 5.2 - 0
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranes
ChEMBL 567 7 1 7 4.8 CC(C)c1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)N2N=C(c3ccc(Cl)cc3)CCC2=O)cc1 10.1016/S0960-894X(96)00617-8
10289311 110498 None 0 Human Binding pIC50 = 4.2 4.2 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 514 13 1 5 5.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)C=C(C)C 10.1021/jm980217s
CHEMBL324586 110498 None 0 Human Binding pIC50 = 4.2 4.2 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 514 13 1 5 5.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)C=C(C)C 10.1021/jm980217s
23445388 208982 None 0 Human Binding pIC50 = 4.2 4.2 - 0
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 398 4 1 5 4.3 Cc1noc(NS(=O)(=O)c2sccc2-c2ccccc2)c1Br 10.1016/S0960-894X(96)00496-9
CHEMBL88506 208982 None 0 Human Binding pIC50 = 4.2 4.2 - 0
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 398 4 1 5 4.3 Cc1noc(NS(=O)(=O)c2sccc2-c2ccccc2)c1Br 10.1016/S0960-894X(96)00496-9
44333598 109246 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B receptor
ChEMBL 447 7 1 6 4.6 CCCOc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(02)00663-7
CHEMBL321520 109246 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B receptor
ChEMBL 447 7 1 6 4.6 CCCOc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(02)00663-7
22009947 85378 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cells
ChEMBL 536 7 2 8 3.6 COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(=O)O)ccc12 10.1007/s00044-004-0021-y
CHEMBL2261358 85378 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cells
ChEMBL 536 7 2 8 3.6 COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(=O)O)ccc12 10.1007/s00044-004-0021-y
CHEMBL413825 215547 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Binding affinity in Chinese hamster ovary (CHO) cells stably transfected with human endothelin B (ETB) receptorBinding affinity in Chinese hamster ovary (CHO) cells stably transfected with human endothelin B (ETB) receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(N)=O)NC(=O)CNC(=O)[C@H](CC(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H]2CCCN2C1=O 10.1016/0960-894X(95)00084-7
10602726 165881 None 0 Pig Binding pIC50 = 4.2 4.2 - 0
Inhibition of Endothelin-3 (ET-3) binding to Endothelin B receptor binding sites in porcine cerebellar membranes.Inhibition of Endothelin-3 (ET-3) binding to Endothelin B receptor binding sites in porcine cerebellar membranes.
ChEMBL 549 10 4 5 5.1 CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(C2CC2)o1 10.1021/jm950591h
CHEMBL424764 165881 None 0 Pig Binding pIC50 = 4.2 4.2 - 0
Inhibition of Endothelin-3 (ET-3) binding to Endothelin B receptor binding sites in porcine cerebellar membranes.Inhibition of Endothelin-3 (ET-3) binding to Endothelin B receptor binding sites in porcine cerebellar membranes.
ChEMBL 549 10 4 5 5.1 CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(C2CC2)o1 10.1021/jm950591h
10506524 61200 None 0 Pig Binding pIC50 = 4.2 4.2 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 536 9 4 5 4.2 CNC(=O)c1nc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)oc1C 10.1021/jm950592+
CHEMBL176565 61200 None 0 Pig Binding pIC50 = 4.2 4.2 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 536 9 4 5 4.2 CNC(=O)c1nc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)oc1C 10.1021/jm950592+
9806559 9152 None 0 Human Binding pIC50 = 4.2 4.2 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 515 13 1 6 3.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCN1CCCC1=O 10.1021/jm980217s
CHEMBL110053 9152 None 0 Human Binding pIC50 = 4.2 4.2 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 515 13 1 6 3.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCN1CCCC1=O 10.1021/jm980217s
71456864 81723 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 618 13 2 12 3.0 CCNS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC 10.1021/jm3009103
CHEMBL2163718 81723 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 618 13 2 12 3.0 CCNS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC 10.1021/jm3009103
10233400 128753 None 0 Human Binding pIC50 = 6.2 6.2 - 1
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 661 11 2 13 3.6 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccncc1 10.1016/s0960-894x(02)01084-3
CHEMBL366885 128753 None 0 Human Binding pIC50 = 6.2 6.2 - 1
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 661 11 2 13 3.6 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccncc1 10.1016/s0960-894x(02)01084-3
10651146 108920 None 0 Pig Binding pIC50 = 7.2 7.2 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 596 12 1 8 4.4 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)c1ccc(OC)cc1 10.1021/jm970101g
CHEMBL321035 108920 None 0 Pig Binding pIC50 = 7.2 7.2 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 596 12 1 8 4.4 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)c1ccc(OC)cc1 10.1021/jm970101g
10415067 45379 None 0 Pig Binding pIC50 = 6.2 6.2 - 0
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 546 8 2 6 5.0 O=C(O)C(Cc1c[nH]c2ccccc12)N(Cc1cc2c(cc1Cl)OCO2)C(=O)/C=C/c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00009-9
CHEMBL152713 45379 None 0 Pig Binding pIC50 = 6.2 6.2 - 0
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 546 8 2 6 5.0 O=C(O)C(Cc1c[nH]c2ccccc12)N(Cc1cc2c(cc1Cl)OCO2)C(=O)/C=C/c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00009-9
44371531 164960 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 467 6 1 5 6.3 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3C(C)C)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(99)00040-2
CHEMBL422002 164960 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 467 6 1 5 6.3 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3C(C)C)c3c2oc2ccccc23)cc1 10.1016/s0960-894x(99)00040-2
10433234 207905 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 436 5 1 4 4.3 CCCc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL80342 207905 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 436 5 1 4 4.3 CCCc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL2369714 212115 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
Inhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellumInhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(95)00152-J
44368482 44698 None 0 Pig Binding pIC50 = 4.2 4.2 - 0
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 523 8 2 7 4.2 O=C(O)C(Cc1ccc(O)cc1)N(Cc1cc2c(cc1Cl)OCO2)C(=O)/C=C/c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00009-9
CHEMBL152091 44698 None 0 Pig Binding pIC50 = 4.2 4.2 - 0
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 523 8 2 7 4.2 O=C(O)C(Cc1ccc(O)cc1)N(Cc1cc2c(cc1Cl)OCO2)C(=O)/C=C/c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00009-9
44386143 130760 None 0 Pig Binding pIC50 = 4.2 4.2 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 571 9 3 6 5.2 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCc3ccccc32)nc1C(=O)O 10.1021/jm950592+
CHEMBL368360 130760 None 0 Pig Binding pIC50 = 4.2 4.2 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 571 9 3 6 5.2 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCc3ccccc32)nc1C(=O)O 10.1021/jm950592+
44385490 131876 None 0 Pig Binding pIC50 = 4.2 4.2 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 532 10 4 7 4.2 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)Nc2ccccn2)nc1C(=O)O 10.1021/jm950592+
CHEMBL369386 131876 None 0 Pig Binding pIC50 = 4.2 4.2 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 532 10 4 7 4.2 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)Nc2ccccn2)nc1C(=O)O 10.1021/jm950592+
23445544 61395 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 438 5 1 5 5.1 Cc1ccc(/C=C/c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(97)00133-9
CHEMBL176912 61395 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 438 5 1 5 5.1 Cc1ccc(/C=C/c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(97)00133-9
44266640 98170 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 459 4 1 8 4.2 O=C(O)c1c(-c2ccc3c(c2)OCO3)c2cc3c(cc2n1Cc1ccc2c(c1)OCO2)OCO3 10.1016/0960-894X(96)00170-9
CHEMBL273529 98170 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 459 4 1 8 4.2 O=C(O)c1c(-c2ccc3c(c2)OCO3)c2cc3c(cc2n1Cc1ccc2c(c1)OCO2)OCO3 10.1016/0960-894X(96)00170-9
44368416 44706 None 0 Pig Binding pIC50 = 5.2 5.2 - 0
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 540 8 2 6 5.6 O=C(O)C(Cc1c[nH]c2ccccc12)N(Cc1cc2c(cc1Cl)OCO2)Cc1cc2c(cc1Cl)OCO2 10.1016/s0960-894x(01)00009-9
CHEMBL152098 44706 None 0 Pig Binding pIC50 = 5.2 5.2 - 0
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 540 8 2 6 5.6 O=C(O)C(Cc1c[nH]c2ccccc12)N(Cc1cc2c(cc1Cl)OCO2)Cc1cc2c(cc1Cl)OCO2 10.1016/s0960-894x(01)00009-9
18996000 99406 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 491 9 1 7 6.1 CCCOc1ccc2c(Sc3cccc(OC)c3)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2c1 10.1016/0960-894X(96)00232-6
CHEMBL282398 99406 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 491 9 1 7 6.1 CCCOc1ccc2c(Sc3cccc(OC)c3)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2c1 10.1016/0960-894X(96)00232-6
18617354 207935 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 384 3 1 4 3.9 Cc1noc(NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL80507 207935 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 384 3 1 4 3.9 Cc1noc(NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1Br 10.1016/0960-894X(96)00441-6
10648135 9344 None 0 Human Binding pIC50 = 4.2 4.2 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 472 13 1 5 4.7 C/C=C/CC[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC 10.1021/jm980217s
CHEMBL111218 9344 None 0 Human Binding pIC50 = 4.2 4.2 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 472 13 1 5 4.7 C/C=C/CC[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC 10.1021/jm980217s
44386621 61297 None 0 Pig Binding pIC50 = 4.2 4.2 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 549 10 4 6 4.5 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CC3CCC2C3)nc1C(=O)O 10.1021/jm950592+
CHEMBL176653 61297 None 0 Pig Binding pIC50 = 4.2 4.2 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 549 10 4 6 4.5 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CC3CCC2C3)nc1C(=O)O 10.1021/jm950592+
10768346 131611 None 0 Pig Binding pIC50 = 4.2 4.2 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 522 10 5 5 4.0 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCC2)nc1C(=O)O 10.1021/jm950592+
CHEMBL369202 131611 None 0 Pig Binding pIC50 = 4.2 4.2 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 522 10 5 5 4.0 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCC2)nc1C(=O)O 10.1021/jm950592+
10527774 183794 None 0 Human Binding pIC50 = 4.2 4.2 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 455 5 2 6 4.2 Cc1cccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c1 10.1021/jm9608366
CHEMBL48031 183794 None 0 Human Binding pIC50 = 4.2 4.2 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 455 5 2 6 4.2 Cc1cccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c1 10.1021/jm9608366
10718688 183732 None 0 Human Binding pIC50 = 4.2 4.2 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 457 5 3 7 3.6 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cccc(O)c2)c1Br 10.1021/jm9608366
CHEMBL48024 183732 None 0 Human Binding pIC50 = 4.2 4.2 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 457 5 3 7 3.6 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cccc(O)c2)c1Br 10.1021/jm9608366
10548486 174220 None 0 Human Binding pIC50 = 4.2 4.2 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 391 5 2 6 3.7 Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1021/jm9608366
CHEMBL45456 174220 None 0 Human Binding pIC50 = 4.2 4.2 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 391 5 2 6 3.7 Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1021/jm9608366
42630531 18495 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
ChEMBL 543 9 2 7 5.1 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OC(C)C)ccc31)OCO2 10.1016/j.bmcl.2010.08.074
CHEMBL1272299 18495 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
ChEMBL 543 9 2 7 5.1 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OC(C)C)ccc31)OCO2 10.1016/j.bmcl.2010.08.074
10650638 9186 None 0 Pig Binding pIC50 = 7.2 7.2 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 566 13 1 6 4.8 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(F)c(F)c1 10.1021/jm970101g
CHEMBL110305 9186 None 0 Pig Binding pIC50 = 7.2 7.2 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 566 13 1 6 4.8 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(F)c(F)c1 10.1021/jm970101g
18738878 194963 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
ChEMBL 547 8 2 7 4.2 CCn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c2ccc(C(N)=O)cc21 10.1016/s0960-894x(01)00660-6
CHEMBL539420 194963 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
ChEMBL 547 8 2 7 4.2 CCn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c2ccc(C(N)=O)cc21 10.1016/s0960-894x(01)00660-6
44266851 14591 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cells
ChEMBL 550 11 1 9 4.7 COc1ccc(C(=O)/C(Cc2ccc(OC)c(OC)c2OC)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1C 10.1021/jm9606507
CHEMBL10847 14591 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cells
ChEMBL 550 11 1 9 4.7 COc1ccc(C(=O)/C(Cc2ccc(OC)c(OC)c2OC)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1C 10.1021/jm9606507
CHEMBL1204671 14591 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cells
ChEMBL 550 11 1 9 4.7 COc1ccc(C(=O)/C(Cc2ccc(OC)c(OC)c2OC)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1C 10.1021/jm9606507
44371450 48878 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 485 7 1 7 5.2 COc1ccc(OC)c(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2ccccc23)c1 10.1016/s0960-894x(99)00040-2
CHEMBL155937 48878 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 485 7 1 7 5.2 COc1ccc(OC)c(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2ccccc23)c1 10.1016/s0960-894x(99)00040-2
CHEMBL2370253 212276 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
10151203 100854 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membranesInhibition of [125I]ET1 binding to porcine kidney inner medulla membranes
ChEMBL 429 5 1 6 4.2 COc1ccc(Cn2c(=O)c(C(=O)O)c(-c3ccc4c(c3)OCO4)c3ccccc32)cc1 10.1016/S0960-894X(97)00319-3
CHEMBL293151 100854 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membranesInhibition of [125I]ET1 binding to porcine kidney inner medulla membranes
ChEMBL 429 5 1 6 4.2 COc1ccc(Cn2c(=O)c(C(=O)O)c(-c3ccc4c(c3)OCO4)c3ccccc32)cc1 10.1016/S0960-894X(97)00319-3
76312118 85381 None 0 Human Binding pIC50 = 6.2 6.2 -691 2
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cells
ChEMBL 522 7 2 8 3.4 COc1cc(C)ccc1S(=O)(=O)NC(=O)[C@@H](c1ccc2c(c1)OCO2)c1cn(C)c2cc(CO)ccc12 10.1007/s00044-004-0021-y
CHEMBL2261361 85381 None 0 Human Binding pIC50 = 6.2 6.2 -691 2
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cells
ChEMBL 522 7 2 8 3.4 COc1cc(C)ccc1S(=O)(=O)NC(=O)[C@@H](c1ccc2c(c1)OCO2)c1cn(C)c2cc(CO)ccc12 10.1007/s00044-004-0021-y
23445412 102317 None 0 Human Binding pIC50 = 4.2 4.2 - 0
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB receptor
ChEMBL 426 5 1 7 4.3 Cc1ccc(OC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1 10.1016/S0960-894X(97)00367-3
CHEMBL303203 102317 None 0 Human Binding pIC50 = 4.2 4.2 - 0
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB receptor
ChEMBL 426 5 1 7 4.3 Cc1ccc(OC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1 10.1016/S0960-894X(97)00367-3
21041297 169710 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 510 12 2 9 3.4 CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL4436531 169710 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 510 12 2 9 3.4 CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2016.06.014
1011 3352 None 26 Human Binding pIC50 = 7.2 7.2 - 0
Antagonist activity at human ETB receptor expressed in CHO cells in presence of ET1Antagonist activity at human ETB receptor expressed in CHO cells in presence of ET1
ChEMBL 609 12 3 10 4.8 OC[C@H](COc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ccc(cc1)OC)O 10.1016/j.bmcl.2016.06.014
5312146 3352 None 26 Human Binding pIC50 = 7.2 7.2 - 0
Antagonist activity at human ETB receptor expressed in CHO cells in presence of ET1Antagonist activity at human ETB receptor expressed in CHO cells in presence of ET1
ChEMBL 609 12 3 10 4.8 OC[C@H](COc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ccc(cc1)OC)O 10.1016/j.bmcl.2016.06.014
CHEMBL1628620 3352 None 26 Human Binding pIC50 = 7.2 7.2 - 0
Antagonist activity at human ETB receptor expressed in CHO cells in presence of ET1Antagonist activity at human ETB receptor expressed in CHO cells in presence of ET1
ChEMBL 609 12 3 10 4.8 OC[C@H](COc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ccc(cc1)OC)O 10.1016/j.bmcl.2016.06.014
11015645 205645 None 0 Pig Binding pIC50 = 7.2 7.2 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 438 9 1 5 6.1 CCCCCCC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL64282 205645 None 0 Pig Binding pIC50 = 7.2 7.2 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 438 9 1 5 6.1 CCCCCCC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
18738879 90267 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cells
ChEMBL 548 8 2 7 4.8 CCn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c2ccc(C(=O)O)cc21 10.1007/s00044-004-0021-y
CHEMBL23833 90267 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cells
ChEMBL 548 8 2 7 4.8 CCn1cc(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)c2ccc(C(=O)O)cc21 10.1007/s00044-004-0021-y
18995996 99256 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 569 10 1 8 6.9 COc1cccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc(OC)c(OCc4ccccc4)cc23)c1 10.1016/0960-894X(96)00232-6
CHEMBL281451 99256 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 569 10 1 8 6.9 COc1cccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc(OC)c(OCc4ccccc4)cc23)c1 10.1016/0960-894X(96)00232-6
10971076 205321 None 0 Pig Binding pIC50 = 5.2 5.2 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 386 3 1 4 4.7 Cc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccccc32)cc1 10.1021/jm010382z
CHEMBL62585 205321 None 0 Pig Binding pIC50 = 5.2 5.2 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 386 3 1 4 4.7 Cc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccccc32)cc1 10.1021/jm010382z
10627378 60443 None 0 Pig Binding pIC50 = 4.2 4.2 - 0
Inhibition of Endothelin-3 (ET-3) binding to Endothelin B receptor binding sites in porcine cerebellar membranes.Inhibition of Endothelin-3 (ET-3) binding to Endothelin B receptor binding sites in porcine cerebellar membranes.
ChEMBL 598 11 5 4 5.6 CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(Cc2ccccc2)[nH]1 10.1021/jm950591h
CHEMBL175103 60443 None 0 Pig Binding pIC50 = 4.2 4.2 - 0
Inhibition of Endothelin-3 (ET-3) binding to Endothelin B receptor binding sites in porcine cerebellar membranes.Inhibition of Endothelin-3 (ET-3) binding to Endothelin B receptor binding sites in porcine cerebellar membranes.
ChEMBL 598 11 5 4 5.6 CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(Cc2ccccc2)[nH]1 10.1021/jm950591h
10815168 168254 None 0 Human Binding pIC50 = 5.2 5.2 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 497 5 2 6 5.2 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc(C(C)(C)C)cc2)c1Br 10.1021/jm9608366
CHEMBL433074 168254 None 0 Human Binding pIC50 = 5.2 5.2 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 497 5 2 6 5.2 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc(C(C)(C)C)cc2)c1Br 10.1021/jm9608366
137647152 157742 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 581 10 2 9 4.8 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(-c4nnn[nH]4)c3)c(=O)c3cc(OCC(C)C)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL4081426 157742 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 581 10 2 9 4.8 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(-c4nnn[nH]4)c3)c(=O)c3cc(OCC(C)C)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
10745942 9313 None 0 Pig Binding pIC50 = 8.2 8.2 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 588 13 1 8 4.3 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc2c(c1)OCCO2 10.1021/jm970101g
CHEMBL111010 9313 None 0 Pig Binding pIC50 = 8.2 8.2 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 588 13 1 8 4.3 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc2c(c1)OCCO2 10.1021/jm970101g
11050177 10261 None 0 Human Binding pIC50 = 8.2 8.2 - 0
In vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptorIn vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptor
ChEMBL 585 10 1 9 6.1 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(-c3ccco3)cn2)cc1 10.1021/jm0102304
CHEMBL116108 10261 None 0 Human Binding pIC50 = 8.2 8.2 - 0
In vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptorIn vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptor
ChEMBL 585 10 1 9 6.1 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(-c3ccco3)cn2)cc1 10.1021/jm0102304
CHEMBL175501 10261 None 0 Human Binding pIC50 = 8.2 8.2 - 0
In vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptorIn vitro for specific binding of [125I]ET1 to GHcell expressed in Endothelin B receptor
ChEMBL 585 10 1 9 6.1 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(-c3ccco3)cn2)cc1 10.1021/jm0102304
9853680 98701 None 0 Human Binding pIC50 = 8.2 8.2 - 1
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 771 17 2 14 5.7 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2cc(OC)c(OC)c(OC)c2)nc1OCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
CHEMBL277275 98701 None 0 Human Binding pIC50 = 8.2 8.2 - 1
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 771 17 2 14 5.7 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2cc(OC)c(OC)c(OC)c2)nc1OCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
44314580 207595 None 0 Pig Binding pIC50 = 8.2 8.2 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 608 13 5 5 4.5 CCCCC(NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)C(C)C)C(=O)O 10.1021/jm9600914
CHEMBL78023 207595 None 0 Pig Binding pIC50 = 8.2 8.2 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 608 13 5 5 4.5 CCCCC(NC(=O)[C@@H](Cc1c(C#N)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(C)C(C)C)C(=O)O 10.1021/jm9600914
10697520 12121 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 530 10 2 6 4.9 CCCC(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1 10.1021/jm990171i
CHEMBL1184086 12121 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 530 10 2 6 4.9 CCCC(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1 10.1021/jm990171i
CHEMBL331936 12121 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 530 10 2 6 4.9 CCCC(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1 10.1021/jm990171i
44314658 207626 None 0 Pig Binding pIC50 = 8.1 8.1 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 589 13 5 4 4.7 CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(CCC)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
CHEMBL78230 207626 None 0 Pig Binding pIC50 = 8.1 8.1 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 589 13 5 4 4.7 CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(CCC)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O 10.1021/jm9600914
CHEMBL1788127 213575 None 5 Rat Binding pIC50 = 7.2 7.2 - 0
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00070a001
CHEMBL313760 213575 None 5 Rat Binding pIC50 = 7.2 7.2 - 0
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00070a001
19432649 206946 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 487 9 2 8 4.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCO 10.1016/S0960-894X(97)00400-9
CHEMBL72473 206946 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 487 9 2 8 4.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCO 10.1016/S0960-894X(97)00400-9
44311321 206643 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 607 11 2 10 5.7 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCOC(=O)Nc1cccnc1 10.1016/S0960-894X(97)00400-9
CHEMBL70788 206643 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 607 11 2 10 5.7 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCOC(=O)Nc1cccnc1 10.1016/S0960-894X(97)00400-9
18617284 207666 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 350 3 1 4 3.2 Cc1noc(NS(=O)(=O)c2ccc(Cl)cc2)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL78552 207666 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 350 3 1 4 3.2 Cc1noc(NS(=O)(=O)c2ccc(Cl)cc2)c1Br 10.1016/0960-894X(96)00441-6
44339714 111371 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 500 14 1 5 5.4 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC/C=C(/C)CC 10.1021/jm980217s
CHEMBL326685 111371 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 500 14 1 5 5.4 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC/C=C(/C)CC 10.1021/jm980217s
10138169 99415 None 0 Human Binding pIC50 = 5.2 5.2 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 440 6 1 8 3.7 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Cc2ccc3c(c2)OCO3)c1Cl 10.1021/jm9700068
CHEMBL282470 99415 None 0 Human Binding pIC50 = 5.2 5.2 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 440 6 1 8 3.7 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Cc2ccc3c(c2)OCO3)c1Cl 10.1021/jm9700068
CHEMBL85341 218378 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
Inhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar membranesInhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar membranes
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00095a029
44266567 98286 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 461 5 1 8 4.5 COc1cc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(-c3ccc4c(c3)OCO4)c2cc1OC 10.1016/0960-894X(96)00170-9
CHEMBL274368 98286 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 461 5 1 8 4.5 COc1cc2c(-c3ccc4c(c3)OCO4)c(C(=O)O)n(-c3ccc4c(c3)OCO4)c2cc1OC 10.1016/0960-894X(96)00170-9
44383536 120461 None 0 Human Binding pIC50 = 4.2 4.2 - 0
Tested for binding affinity towards rabbit Endothelin B receptorTested for binding affinity towards rabbit Endothelin B receptor
ChEMBL 362 3 2 5 2.9 C/C=C/C=C/C(=O)O[C@@H]1C=C2COC(O)[C@]2(O)[C@@]2(C)CCCC(C)(C)C12 10.1016/s0960-894x(00)00136-0
CHEMBL353502 120461 None 0 Human Binding pIC50 = 4.2 4.2 - 0
Tested for binding affinity towards rabbit Endothelin B receptorTested for binding affinity towards rabbit Endothelin B receptor
ChEMBL 362 3 2 5 2.9 C/C=C/C=C/C(=O)O[C@@H]1C=C2COC(O)[C@]2(O)[C@@]2(C)CCCC(C)(C)C12 10.1016/s0960-894x(00)00136-0
11133491 102224 None 0 Pig Binding pIC50 = 6.2 6.2 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 416 3 1 6 4.2 O=C(O)C1=C(c2ccc3c(c2)OCO3)c2ccccc2OC1c1ccc2c(c1)OCO2 10.1021/jm010382z
CHEMBL302659 102224 None 0 Pig Binding pIC50 = 6.2 6.2 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 416 3 1 6 4.2 O=C(O)C1=C(c2ccc3c(c2)OCO3)c2ccccc2OC1c1ccc2c(c1)OCO2 10.1021/jm010382z
11122785 205433 None 0 Pig Binding pIC50 = 6.2 6.2 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 426 8 1 6 4.6 COCCCC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL63057 205433 None 0 Pig Binding pIC50 = 6.2 6.2 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 426 8 1 6 4.6 COCCCC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
10184817 9576 None 0 Human Binding pIC50 = 4.2 4.2 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 488 14 1 5 5.1 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)CCC 10.1021/jm980217s
CHEMBL112417 9576 None 0 Human Binding pIC50 = 4.2 4.2 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 488 14 1 5 5.1 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)CCC 10.1021/jm980217s
21041370 82033 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 636 13 2 10 4.4 COc1ccc(Cl)c(Oc2c(NS(=O)(=O)NCc3ccccc3)ncnc2OCCOc2ncc(Br)cn2)c1 10.1021/jm3009103
CHEMBL2165330 82033 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 636 13 2 10 4.4 COc1ccc(Cl)c(Oc2c(NS(=O)(=O)NCc3ccccc3)ncnc2OCCOc2ncc(Br)cn2)c1 10.1021/jm3009103
52949155 18418 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 557 10 2 7 5.4 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCC(C)C)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL1271640 18418 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 557 10 2 7 5.4 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCC(C)C)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
11070564 205858 None 0 Pig Binding pIC50 = 7.1 7.1 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 460 7 1 6 5.2 CCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc(OC)cc1)O2 10.1021/jm010382z
CHEMBL65494 205858 None 0 Pig Binding pIC50 = 7.1 7.1 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 460 7 1 6 5.2 CCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc(OC)cc1)O2 10.1021/jm010382z
11058202 205281 None 0 Pig Binding pIC50 = 5.1 5.1 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 388 4 1 5 4.4 CC(C)Oc1ccc2c(c1)C(Cl)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
CHEMBL62374 205281 None 0 Pig Binding pIC50 = 5.1 5.1 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 388 4 1 5 4.4 CC(C)Oc1ccc2c(c1)C(Cl)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
10696818 9652 None 0 Human Binding pIC50 = 4.1 4.1 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 502 15 1 5 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC(CC)CC 10.1021/jm980217s
CHEMBL112770 9652 None 0 Human Binding pIC50 = 4.1 4.1 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 502 15 1 5 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC(CC)CC 10.1021/jm980217s
10814222 9554 None 0 Pig Binding pIC50 = 4.1 4.1 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 470 10 1 6 3.4 CCCN(C)C(=O)CN1C[C@H](c2ccc(OC)cc2OC)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL112325 9554 None 0 Pig Binding pIC50 = 4.1 4.1 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 470 10 1 6 3.4 CCCN(C)C(=O)CN1C[C@H](c2ccc(OC)cc2OC)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
44291775 101221 None 0 Human Binding pIC50 = 6.1 6.1 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 506 6 1 10 4.1 CC#N.Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Cc2cc3c(cc2C#N)OCO3)c1Cl 10.1021/jm9700068
CHEMBL295557 101221 None 0 Human Binding pIC50 = 6.1 6.1 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 506 6 1 10 4.1 CC#N.Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Cc2cc3c(cc2C#N)OCO3)c1Cl 10.1021/jm9700068
23445538 60091 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B receptor
ChEMBL 456 6 1 6 4.8 Cc1ccc(OCc2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00132-7
CHEMBL173805 60091 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B receptor
ChEMBL 456 6 1 6 4.8 Cc1ccc(OCc2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1 10.1016/S0960-894X(97)00132-7
9808602 109265 None 0 Pig Binding pIC50 = 7.1 7.1 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 590 15 1 8 4.5 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(OC)c1 10.1021/jm970101g
CHEMBL321673 109265 None 0 Pig Binding pIC50 = 7.1 7.1 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 590 15 1 8 4.5 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(OC)c1 10.1021/jm970101g
CHEMBL330144 213786 None 0 Rat Binding pIC50 = 6.1 6.1 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)C(C)C 10.1021/jm00015a003
CHEMBL97431 218414 None 0 Rat Binding pIC50 = 6.1 6.1 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00015a003
10993320 205438 None 0 Pig Binding pIC50 = 6.1 6.1 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 412 6 1 6 4.6 CC(C)OC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL63067 205438 None 0 Pig Binding pIC50 = 6.1 6.1 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 412 6 1 6 4.6 CC(C)OC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
44383592 59922 None 0 Human Binding pIC50 = 4.1 4.1 - 0
Tested for binding affinity towards human Endothelin B receptorTested for binding affinity towards human Endothelin B receptor
ChEMBL 386 4 1 5 3.6 C/C=C/C=C/C=C/C(=O)O[C@@H]1C=C2COC(=O)[C@]2(O)[C@@]2(C)CCCC(C)(C)C12 10.1016/s0960-894x(00)00136-0
CHEMBL173059 59922 None 0 Human Binding pIC50 = 4.1 4.1 - 0
Tested for binding affinity towards human Endothelin B receptorTested for binding affinity towards human Endothelin B receptor
ChEMBL 386 4 1 5 3.6 C/C=C/C=C/C=C/C(=O)O[C@@H]1C=C2COC(=O)[C@]2(O)[C@@]2(C)CCCC(C)(C)C12 10.1016/s0960-894x(00)00136-0
10625269 14462 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 502 7 2 6 4.5 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2ccc(C)cc2C)cc1 10.1021/jm990170q
CHEMBL120106 14462 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 502 7 2 6 4.5 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2ccc(C)cc2C)cc1 10.1021/jm990170q
CHEMBL411797 215417 None 0 Rat Binding pIC50 = 6.1 6.1 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
15289331 99618 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 433 6 1 6 5.3 COc1cccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3ccccc23)c1 10.1016/0960-894X(96)00232-6
CHEMBL283648 99618 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 433 6 1 6 5.3 COc1cccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3ccccc23)c1 10.1016/0960-894X(96)00232-6
18617381 105737 None 0 Human Binding pIC50 = 4.1 4.1 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 300 3 1 4 3.1 Cc1noc(NS(=O)(=O)c2cccc(Cl)c2C)c1C 10.1016/0960-894X(96)00441-6
CHEMBL312551 105737 None 0 Human Binding pIC50 = 4.1 4.1 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 300 3 1 4 3.1 Cc1noc(NS(=O)(=O)c2cccc(Cl)c2C)c1C 10.1016/0960-894X(96)00441-6
10504542 179669 None 0 Human Binding pIC50 = 5.1 5.1 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 469 6 2 6 4.4 CCc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1021/jm9608366
CHEMBL47418 179669 None 0 Human Binding pIC50 = 5.1 5.1 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 469 6 2 6 4.4 CCc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1021/jm9608366
22998396 100868 None 0 Human Binding pIC50 = 4.1 4.1 - 0
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 398 4 1 5 4.3 Cc1noc(NS(=O)(=O)c2ccsc2-c2ccccc2)c1Br 10.1016/S0960-894X(96)00496-9
CHEMBL293232 100868 None 0 Human Binding pIC50 = 4.1 4.1 - 0
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 398 4 1 5 4.3 Cc1noc(NS(=O)(=O)c2ccsc2-c2ccccc2)c1Br 10.1016/S0960-894X(96)00496-9
10604167 12421 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 640 10 2 6 6.4 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)(c2ccccc2)c2ccccc2)cc1 10.1021/jm990171i
CHEMBL1185826 12421 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 640 10 2 6 6.4 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)(c2ccccc2)c2ccccc2)cc1 10.1021/jm990171i
CHEMBL434986 12421 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 640 10 2 6 6.4 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)(c2ccccc2)c2ccccc2)cc1 10.1021/jm990171i
10185233 60082 None 0 Human Binding pIC50 = 6.1 6.1 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 497 8 2 8 3.8 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)ncnc1OCC#CCO 10.1016/s0960-894x(02)01084-3
CHEMBL173721 60082 None 0 Human Binding pIC50 = 6.1 6.1 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 497 8 2 8 3.8 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)ncnc1OCC#CCO 10.1016/s0960-894x(02)01084-3
44385576 131445 None 0 Human Binding pIC50 = 6.1 6.1 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 539 10 1 10 3.4 C#CCOc1nc(N2CCOCC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL368929 131445 None 0 Human Binding pIC50 = 6.1 6.1 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 539 10 1 10 3.4 C#CCOc1nc(N2CCOCC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
11113473 205827 None 0 Pig Binding pIC50 = 6.1 6.1 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 472 6 1 5 6.3 CC(C)Oc1ccc2c(c1)C(c1ccc(C(C)C)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
CHEMBL65201 205827 None 0 Pig Binding pIC50 = 6.1 6.1 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 472 6 1 5 6.3 CC(C)Oc1ccc2c(c1)C(c1ccc(C(C)C)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
11798762 209081 None 0 Pig Binding pIC50 = 6.1 6.1 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 475 9 1 7 3.1 CCCS(=O)(=O)CCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL8911 209081 None 0 Pig Binding pIC50 = 6.1 6.1 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 475 9 1 7 3.1 CCCS(=O)(=O)CCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL405709 215036 None 0 Rat Binding pIC50 = 5.1 5.1 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00015a003
10792782 131432 None 0 Pig Binding pIC50 = 4.1 4.1 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 551 10 4 6 5.0 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCCC2)nc1C(=O)O 10.1021/jm950592+
CHEMBL368847 131432 None 0 Pig Binding pIC50 = 4.1 4.1 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 551 10 4 6 5.0 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCCC2)nc1C(=O)O 10.1021/jm950592+
137638953 156939 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 579 10 2 9 4.6 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(-c4nnn[nH]4)c3)c(=O)c3cc(OCC4CC4)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL4071505 156939 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 579 10 2 9 4.6 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(-c4nnn[nH]4)c3)c(=O)c3cc(OCC4CC4)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
11798109 12363 None 0 Human Binding pIC50 = 5.1 5.1 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 457 7 2 7 4.2 COc1cccc(NCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)c1 10.1021/jm9608366
CHEMBL1185459 12363 None 0 Human Binding pIC50 = 5.1 5.1 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 457 7 2 7 4.2 COc1cccc(NCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)c1 10.1021/jm9608366
CHEMBL416086 12363 None 0 Human Binding pIC50 = 5.1 5.1 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 457 7 2 7 4.2 COc1cccc(NCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)c1 10.1021/jm9608366
44314610 102911 None 0 Pig Binding pIC50 = 7.1 7.1 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 671 12 6 5 3.9 CC(C)CC(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)N[C@H](Cc1c(Br)[nH]c2ccccc12)C(=O)NC(Cc1c[nH]cn1)C(=O)O 10.1021/jm9600914
CHEMBL305650 102911 None 0 Pig Binding pIC50 = 7.1 7.1 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 671 12 6 5 3.9 CC(C)CC(NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)N[C@H](Cc1c(Br)[nH]c2ccccc12)C(=O)NC(Cc1c[nH]cn1)C(=O)O 10.1021/jm9600914
71451525 81702 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 629 12 1 12 5.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCOc1ncccn1 10.1021/jm3009103
CHEMBL2163697 81702 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 629 12 1 12 5.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCOc1ncccn1 10.1021/jm3009103
18995999 98565 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 477 6 1 8 5.0 COc1cccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc4c(cc23)OCO4)c1 10.1016/0960-894X(96)00232-6
CHEMBL27617 98565 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 477 6 1 8 5.0 COc1cccc(Sc2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc4c(cc23)OCO4)c1 10.1016/0960-894X(96)00232-6
10719367 98283 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 476 7 1 8 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)cc(OC)c2)cc1 10.1021/jm9606507
CHEMBL274359 98283 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 476 7 1 8 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)cc(OC)c2)cc1 10.1021/jm9606507
11826847 205377 None 0 Pig Binding pIC50 = 6.1 6.1 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 474 8 1 6 5.6 CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccccc1OC)O2 10.1021/jm010382z
CHEMBL62814 205377 None 0 Pig Binding pIC50 = 6.1 6.1 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 474 8 1 6 5.6 CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccccc1OC)O2 10.1021/jm010382z
CHEMBL405677 215034 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Binding affinity in Chinese hamster ovary (CHO) cells stably transfected with human endothelin B (ETB) receptorBinding affinity in Chinese hamster ovary (CHO) cells stably transfected with human endothelin B (ETB) receptor
ChEMBL None None None CC(=O)[C@@H](Cc1c[nH]c2ccccc12)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(95)00084-7
11103224 205110 None 0 Pig Binding pIC50 = 5.1 5.1 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 510 14 1 6 7.3 CCCCCCCCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL61406 205110 None 0 Pig Binding pIC50 = 5.1 5.1 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 510 14 1 6 7.3 CCCCCCCCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
44384177 120357 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B receptor
ChEMBL 506 6 1 8 4.6 Cc1noc(NS(=O)(=O)c2ccsc2COc2cc3c(cc2Cl)OCO3)c1Br 10.1016/S0960-894X(97)00132-7
CHEMBL352657 120357 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B receptor
ChEMBL 506 6 1 8 4.6 Cc1noc(NS(=O)(=O)c2ccsc2COc2cc3c(cc2Cl)OCO3)c1Br 10.1016/S0960-894X(97)00132-7
10721344 7542 None 0 Pig Binding pIC50 = 7.1 7.1 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 548 13 1 8 3.0 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)CCOC 10.1021/jm970101g
CHEMBL108748 7542 None 0 Pig Binding pIC50 = 7.1 7.1 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 548 13 1 8 3.0 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)CCOC 10.1021/jm970101g
10144334 130732 None 0 Human Binding pIC50 = 7.1 7.1 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 561 10 2 10 4.0 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccncc2)nc1OCC#CCO 10.1016/s0960-894x(02)01084-3
CHEMBL368211 130732 None 0 Human Binding pIC50 = 7.1 7.1 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 561 10 2 10 4.0 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccncc2)nc1OCC#CCO 10.1016/s0960-894x(02)01084-3
11113542 205668 None 0 Pig Binding pIC50 = 6.1 6.1 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 476 8 1 6 5.5 COc1ccc(C2=C(C(=O)O)C(c3ccc(OC)cc3OC)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
CHEMBL64398 205668 None 0 Pig Binding pIC50 = 6.1 6.1 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 476 8 1 6 5.5 COc1ccc(C2=C(C(=O)O)C(c3ccc(OC)cc3OC)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
44311288 206642 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 592 11 1 10 5.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCOC(=O)c1cccnc1 10.1016/S0960-894X(97)00400-9
CHEMBL70781 206642 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptorReceptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
ChEMBL 592 11 1 10 5.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCOC(=O)c1cccnc1 10.1016/S0960-894X(97)00400-9
10918390 19328 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
ChEMBL 522 12 1 5 5.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CC)cc1 10.1021/jm010237l
CHEMBL129060 19328 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
ChEMBL 522 12 1 5 5.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CC)cc1 10.1021/jm010237l
44327714 210398 None 0 Pig Binding pIC50 = 5.1 5.1 - 0
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranes
ChEMBL 575 8 1 9 4.2 COc1ccc(-c2cc(C)c(=O)n(C(C(=O)NS(=O)(=O)c3ccc(C(C)C)cc3)c3ccc4c(c3)OCO4)n2)cc1 10.1016/S0960-894X(96)00617-8
CHEMBL96935 210398 None 0 Pig Binding pIC50 = 5.1 5.1 - 0
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranes
ChEMBL 575 8 1 9 4.2 COc1ccc(-c2cc(C)c(=O)n(C(C(=O)NS(=O)(=O)c3ccc(C(C)C)cc3)c3ccc4c(c3)OCO4)n2)cc1 10.1016/S0960-894X(96)00617-8
10743478 109324 None 0 Pig Binding pIC50 = 4.1 4.1 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 484 12 1 4 5.1 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc(F)cc2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL321852 109324 None 0 Pig Binding pIC50 = 4.1 4.1 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 484 12 1 4 5.1 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc(F)cc2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
10029171 98819 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
ChEMBL 505 6 2 7 3.0 Cc1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(C(N)=O)ccc23)cc1 10.1016/s0960-894x(01)00660-6
CHEMBL278109 98819 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
ChEMBL 505 6 2 7 3.0 Cc1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(C(N)=O)ccc23)cc1 10.1016/s0960-894x(01)00660-6
10503334 173448 None 0 Human Binding pIC50 = 4.1 4.1 - 0
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB receptor
ChEMBL 441 5 2 6 3.9 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccccc2)c1Br 10.1016/S0960-894X(97)00367-3
CHEMBL45269 173448 None 0 Human Binding pIC50 = 4.1 4.1 - 0
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB receptor
ChEMBL 441 5 2 6 3.9 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccccc2)c1Br 10.1016/S0960-894X(97)00367-3
10503334 173448 None 0 Human Binding pIC50 = 4.1 4.1 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 441 5 2 6 3.9 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccccc2)c1Br 10.1021/jm9608366
CHEMBL45269 173448 None 0 Human Binding pIC50 = 4.1 4.1 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 441 5 2 6 3.9 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccccc2)c1Br 10.1021/jm9608366
11080933 205870 None 0 Pig Binding pIC50 = 7.1 7.1 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 454 10 1 6 5.7 CCCCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL65599 205870 None 0 Pig Binding pIC50 = 7.1 7.1 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 454 10 1 6 5.7 CCCCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
44284041 100357 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 520 9 3 8 4.4 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(OC(C)CO)c1 10.1016/j.bmcl.2004.01.008
CHEMBL289216 100357 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 520 9 3 8 4.4 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(OC(C)CO)c1 10.1016/j.bmcl.2004.01.008
9870830 209172 None 29 Human Binding pIC50 = 6.1 6.1 -66 2
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1021/jm9606507
CHEMBL8981 209172 None 29 Human Binding pIC50 = 6.1 6.1 -66 2
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1021/jm9606507
11122784 163017 None 0 Pig Binding pIC50 = 6.1 6.1 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 426 8 1 6 4.9 CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
CHEMBL417413 163017 None 0 Pig Binding pIC50 = 6.1 6.1 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 426 8 1 6 4.9 CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21 10.1021/jm010382z
9870830 209172 None 29 Mouse Binding pIC50 = 6.1 6.1 - 2
Displacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomesDisplacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomes
ChEMBL 506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1016/j.bmc.2009.08.058
CHEMBL8981 209172 None 29 Mouse Binding pIC50 = 6.1 6.1 - 2
Displacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomesDisplacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomes
ChEMBL 506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1016/j.bmc.2009.08.058
CHEMBL2369713 212114 None 0 Rat Binding pIC50 = 6.1 6.1 - 0
Inhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellumInhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(95)00152-J
9870830 209172 None 29 Human Binding pIC50 = 6.1 6.1 -66 2
Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.
ChEMBL 506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1021/jm980504w
CHEMBL8981 209172 None 29 Human Binding pIC50 = 6.1 6.1 -66 2
Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.
ChEMBL 506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1021/jm980504w
21041324 81695 None 5 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 542 11 2 8 3.5 CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Cl)cc1 10.1021/jm3009103
CHEMBL2163690 81695 None 5 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 542 11 2 8 3.5 CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Cl)cc1 10.1021/jm3009103
10918216 205300 None 0 Pig Binding pIC50 = 6.1 6.1 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 508 7 1 6 6.0 COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OCc4ccccc4)cc32)cc1 10.1021/jm010382z
CHEMBL62450 205300 None 0 Pig Binding pIC50 = 6.1 6.1 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 508 7 1 6 6.0 COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OCc4ccccc4)cc32)cc1 10.1021/jm010382z
15453177 207979 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 392 4 1 4 4.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL80857 207979 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 392 4 1 4 4.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2)c1Br 10.1016/0960-894X(96)00441-6
14041110 100068 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB receptor
ChEMBL 322 2 2 3 2.5 O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccccc21 10.1016/0960-894X(95)00230-Q
CHEMBL286808 100068 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB receptor
ChEMBL 322 2 2 3 2.5 O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccccc21 10.1016/0960-894X(95)00230-Q
10626245 131230 None 0 Human Binding pIC50 = 4.1 4.1 - 0
Inhibitory activity was evaluated against human Endothelin B receptorInhibitory activity was evaluated against human Endothelin B receptor
ChEMBL 539 10 2 8 5.5 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)OC(=O)OC2CCCCC2)nc1C(=O)O 10.1021/jm9505932
CHEMBL368629 131230 None 0 Human Binding pIC50 = 4.1 4.1 - 0
Inhibitory activity was evaluated against human Endothelin B receptorInhibitory activity was evaluated against human Endothelin B receptor
ChEMBL 539 10 2 8 5.5 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)OC(=O)OC2CCCCC2)nc1C(=O)O 10.1021/jm9505932
10647172 209224 None 0 Pig Binding pIC50 = 5.1 5.1 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 449 6 1 5 4.6 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2Cc2ccc(F)cc2)cc1 10.1021/jm9505369
CHEMBL9012 209224 None 0 Pig Binding pIC50 = 5.1 5.1 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 449 6 1 5 4.6 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2Cc2ccc(F)cc2)cc1 10.1021/jm9505369
9803428 102259 None 0 Human Binding pIC50 = 5.1 5.1 - 0
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB receptor
ChEMBL 442 5 1 9 3.4 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Oc2ccc3c(c2)OCO3)c1Cl 10.1016/S0960-894X(97)00367-3
CHEMBL302872 102259 None 0 Human Binding pIC50 = 5.1 5.1 - 0
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB receptor
ChEMBL 442 5 1 9 3.4 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Oc2ccc3c(c2)OCO3)c1Cl 10.1016/S0960-894X(97)00367-3
10793053 11462 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 564 9 2 6 5.2 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)c2ccccc2)cc1 10.1021/jm990171i
CHEMBL1180363 11462 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 564 9 2 6 5.2 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)c2ccccc2)cc1 10.1021/jm990171i
CHEMBL123994 11462 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptorBinding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B receptor
ChEMBL 564 9 2 6 5.2 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)c2ccccc2)cc1 10.1021/jm990171i
9852318 9616 None 8 Human Binding pIC50 = 8.1 8.1 -2691 2
Ability to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptorAbility to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptor
ChEMBL 613 11 2 9 4.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm000538f
CHEMBL112624 9616 None 8 Human Binding pIC50 = 8.1 8.1 -2691 2
Ability to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptorAbility to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptor
ChEMBL 613 11 2 9 4.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm000538f
CHEMBL1627022 9616 None 8 Human Binding pIC50 = 8.1 8.1 -2691 2
Ability to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptorAbility to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptor
ChEMBL 613 11 2 9 4.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm000538f
44334150 4536 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B receptor
ChEMBL 445 6 1 5 5.0 COc1ccc([C@@H]2c3nc(CC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1016/s0960-894x(02)00663-7
CHEMBL102314 4536 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B receptor
ChEMBL 445 6 1 5 5.0 COc1ccc([C@@H]2c3nc(CC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1016/s0960-894x(02)00663-7
44371773 48607 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 562 8 1 8 4.6 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2cc(N(C)S(C)(=O)=O)ccc23)cc1 10.1016/s0960-894x(99)00040-2
CHEMBL155708 48607 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Ability to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranesAbility to displace [125I]endothelin-1 from endothelin B receptor in porcine kidney membranes
ChEMBL 562 8 1 8 4.6 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2cc(N(C)S(C)(=O)=O)ccc23)cc1 10.1016/s0960-894x(99)00040-2
44320590 106617 None 0 Rat Binding pIC50 = 8.1 8.1 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 556 10 2 9 4.8 COc1ccc(Cn2nc(-c3cccs3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)c(OCC(=O)O)c1 10.1016/s0960-894x(00)00513-8
CHEMBL314206 106617 None 0 Rat Binding pIC50 = 8.1 8.1 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 556 10 2 9 4.8 COc1ccc(Cn2nc(-c3cccs3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)c(OCC(=O)O)c1 10.1016/s0960-894x(00)00513-8
CHEMBL384728 214794 None 0 Rat Binding pIC50 = 7.1 7.1 - 0
Binding affinity against endothelin B receptor rat cerebellar membranes.Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
11733450 205878 None 0 Pig Binding pIC50 = 7.1 7.1 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 474 6 1 7 5.0 CCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
CHEMBL65658 205878 None 0 Pig Binding pIC50 = 7.1 7.1 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 474 6 1 7 5.0 CCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
CHEMBL2369736 212123 None 0 Rat Binding pIC50 = 7.1 7.1 - 0
Inhibition of binding to Endothelin B receptor of rat cerebellar membranes.Inhibition of binding to Endothelin B receptor of rat cerebellar membranes.
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N(C)[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm970161m
44270524 98260 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) receptor expressed in CHO cells
ChEMBL 682 13 1 9 6.9 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)NS(=O)(=O)c1ccccc1)c1ccc2c(c1)OCO2 10.1016/0960-894X(95)00186-W
CHEMBL274243 98260 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) receptor expressed in CHO cells
ChEMBL 682 13 1 9 6.9 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)NS(=O)(=O)c1ccccc1)c1ccc2c(c1)OCO2 10.1016/0960-894X(95)00186-W
44368428 44590 None 0 Pig Binding pIC50 = 5.1 5.1 - 0
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 521 9 2 5 5.5 O=C(O)C(Cc1ccc(O)cc1)N(Cc1ccccc1-c1ccccc1)C(=O)/C=C/c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00009-9
CHEMBL152001 44590 None 0 Pig Binding pIC50 = 5.1 5.1 - 0
Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin B receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
ChEMBL 521 9 2 5 5.5 O=C(O)C(Cc1ccc(O)cc1)N(Cc1ccccc1-c1ccccc1)C(=O)/C=C/c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00009-9
10505771 163451 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
ChEMBL 506 12 1 4 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCC3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm010237l
CHEMBL419211 163451 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
ChEMBL 506 12 1 4 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCC3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm010237l
10299975 110310 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 488 14 1 5 5.1 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC(C)CC 10.1021/jm980217s
CHEMBL323791 110310 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 488 14 1 5 5.1 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC(C)CC 10.1021/jm980217s
10505771 163451 None 0 Pig Binding pIC50 = 5.1 5.1 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 506 12 1 4 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCC3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL419211 163451 None 0 Pig Binding pIC50 = 5.1 5.1 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 506 12 1 4 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCC3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
56678451 63346 None 0 Rat Binding pIC50 = 5.1 5.1 - 0
Inhibition of binding to Endothelin B receptor of rat cerebellar membranes.Inhibition of binding to Endothelin B receptor of rat cerebellar membranes.
ChEMBL 937 25 8 8 4.5 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C(c1ccccc1)c1ccccc1)N(C)C(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm970161m
CHEMBL1793927 63346 None 0 Rat Binding pIC50 = 5.1 5.1 - 0
Inhibition of binding to Endothelin B receptor of rat cerebellar membranes.Inhibition of binding to Endothelin B receptor of rat cerebellar membranes.
ChEMBL 937 25 8 8 4.5 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C(c1ccccc1)c1ccccc1)N(C)C(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm970161m
3795752 105258 None 0 Human Binding pIC50 = 4.1 4.1 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 320 3 1 4 3.4 Cc1noc(NS(=O)(=O)c2cc(Cl)ccc2Cl)c1C 10.1016/0960-894X(96)00441-6
CHEMBL311455 105258 None 0 Human Binding pIC50 = 4.1 4.1 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 320 3 1 4 3.4 Cc1noc(NS(=O)(=O)c2cc(Cl)ccc2Cl)c1C 10.1016/0960-894X(96)00441-6
10769025 60290 None 0 Pig Binding pIC50 = 4.1 4.1 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 550 10 5 5 4.6 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCC(C)CC2)nc1C(=O)O 10.1021/jm950592+
CHEMBL174171 60290 None 0 Pig Binding pIC50 = 4.1 4.1 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 550 10 5 5 4.6 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCC(C)CC2)nc1C(=O)O 10.1021/jm950592+
137649592 157502 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 567 10 2 9 4.6 CCCOc1ccc2c(c1)c(=O)c(Cc1cccc(-c3nnn[nH]3)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL4078537 157502 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 567 10 2 9 4.6 CCCOc1ccc2c(c1)c(=O)c(Cc1cccc(-c3nnn[nH]3)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2017.04.049
10838921 208804 None 0 Pig Binding pIC50 = 6.1 6.1 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 494 7 1 6 4.1 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(C)C2CCCCC2)cc1 10.1021/jm9505369
CHEMBL8736 208804 None 0 Pig Binding pIC50 = 6.1 6.1 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 494 7 1 6 4.1 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(C)C2CCCCC2)cc1 10.1021/jm9505369
10744040 113633 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 502 7 2 6 4.5 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2cccc(C)c2C)cc1 10.1021/jm990170q
CHEMBL332231 113633 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 502 7 2 6 4.5 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2cccc(C)c2C)cc1 10.1021/jm990170q
9874379 60466 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 653 14 2 10 5.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(C2CC2)nc1OCCNS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(02)01083-1
CHEMBL175268 60466 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 653 14 2 10 5.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(C2CC2)nc1OCCNS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(02)01083-1
44320419 107130 None 0 Rat Binding pIC50 = 6.1 6.1 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 496 7 2 6 5.1 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1CC1CCC(C(=O)O)CC1 10.1016/s0960-894x(00)00513-8
CHEMBL315805 107130 None 0 Rat Binding pIC50 = 6.1 6.1 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 496 7 2 6 5.1 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1CC1CCC(C(=O)O)CC1 10.1016/s0960-894x(00)00513-8
21041267 82040 None 15 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 558 9 2 8 2.8 CNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1 10.1021/jm3009103
CHEMBL2165337 82040 None 15 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 558 9 2 8 2.8 CNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1 10.1021/jm3009103
10983992 19468 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
ChEMBL 506 12 1 4 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CC)cc1 10.1021/jm010237l
CHEMBL129740 19468 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
ChEMBL 506 12 1 4 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CC)cc1 10.1021/jm010237l
23445468 11236 None 0 Human Binding pIC50 = 4.1 4.1 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 459 5 3 9 2.4 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc(O)nn2)c1Br 10.1021/jm9608366
CHEMBL1178818 11236 None 0 Human Binding pIC50 = 4.1 4.1 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 459 5 3 9 2.4 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc(O)nn2)c1Br 10.1021/jm9608366
CHEMBL44615 11236 None 0 Human Binding pIC50 = 4.1 4.1 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 459 5 3 9 2.4 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc(O)nn2)c1Br 10.1021/jm9608366
10275056 112572 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 440 6 1 5 5.2 CCCc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(96)00496-9
CHEMBL329890 112572 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 440 6 1 5 5.2 CCCc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(96)00496-9
10577388 15586 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 502 7 2 6 4.5 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2cc(C)ccc2C)cc1 10.1021/jm990170q
CHEMBL122111 15586 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 502 7 2 6 4.5 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2cc(C)ccc2C)cc1 10.1021/jm990170q
10602620 16598 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 544 10 2 6 5.4 CCCc1cccc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm990170q
CHEMBL123997 16598 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 544 10 2 6 5.4 CCCc1cccc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm990170q
21041278 171880 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 554 12 2 9 3.5 CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Br)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL4467748 171880 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 554 12 2 9 3.5 CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Br)cc1 10.1016/j.bmcl.2016.06.014
17869279 14885 None 0 Pig Binding pIC50 = 6.1 6.1 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 460 8 1 7 4.7 COc1ccc(C(=O)/C(Cc2ccccc2OC)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL1207701 14885 None 0 Pig Binding pIC50 = 6.1 6.1 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 460 8 1 7 4.7 COc1ccc(C(=O)/C(Cc2ccccc2OC)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
CHEMBL431160 14885 None 0 Pig Binding pIC50 = 6.1 6.1 - 0
In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptorIn vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
ChEMBL 460 8 1 7 4.7 COc1ccc(C(=O)/C(Cc2ccccc2OC)=C(\C(=O)O)c2ccc3nsnc3c2)cc1 10.1016/s0960-894x(98)00301-1
10576428 14593 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cells
ChEMBL 473 8 2 6 4.3 COc1ccc(C(=O)/C(Cc2ccc(NC(C)=O)cc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1021/jm9606507
CHEMBL10905 14593 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cells
ChEMBL 473 8 2 6 4.3 COc1ccc(C(=O)/C(Cc2ccc(NC(C)=O)cc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1021/jm9606507
CHEMBL1204673 14593 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cellsInhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors expressed in CHO-K1 cells
ChEMBL 473 8 2 6 4.3 COc1ccc(C(=O)/C(Cc2ccc(NC(C)=O)cc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1 10.1021/jm9606507
44385586 61682 None 0 Human Binding pIC50 = 6.1 6.1 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 531 10 1 9 4.7 C#CCOc1nc(-c2ccncc2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL177143 61682 None 0 Human Binding pIC50 = 6.1 6.1 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 531 10 1 9 4.7 C#CCOc1nc(-c2ccncc2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
10137382 182290 None 0 Human Binding pIC50 = 5.1 5.1 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 427 5 3 7 3.8 Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(O)c1 10.1021/jm9608366
CHEMBL47827 182290 None 0 Human Binding pIC50 = 5.1 5.1 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 427 5 3 7 3.8 Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(O)c1 10.1021/jm9608366
44385792 60371 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 617 13 2 11 4.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(C2CC2)nc1OCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
CHEMBL174547 60371 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 617 13 2 11 4.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(C2CC2)nc1OCCNS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)01083-1
10097589 208739 None 0 Rat Binding pIC50 = 6.1 6.1 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 502 7 2 7 5.2 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2cccs2)nn1CC1CCC(C(=O)O)CC1 10.1016/s0960-894x(00)00513-8
CHEMBL86965 208739 None 0 Rat Binding pIC50 = 6.1 6.1 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 502 7 2 7 5.2 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2cccs2)nn1CC1CCC(C(=O)O)CC1 10.1016/s0960-894x(00)00513-8
10717923 98747 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B receptor
ChEMBL 439 5 2 6 4.7 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1 10.1016/S0960-894X(97)00132-7
CHEMBL277595 98747 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B receptor
ChEMBL 439 5 2 6 4.7 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1 10.1016/S0960-894X(97)00132-7
11799625 113862 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 502 7 2 6 4.5 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2ccc(C)c(C)c2)cc1 10.1021/jm990170q
CHEMBL332431 113862 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Binding affinity towards human Endothelin B receptor (hET -B)Binding affinity towards human Endothelin B receptor (hET -B)
ChEMBL 502 7 2 6 4.5 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2ccc(C)c(C)c2)cc1 10.1021/jm990170q
71462322 82041 None 12 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 572 10 2 8 3.2 CCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1 10.1021/jm3009103
CHEMBL2165338 82041 None 12 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 572 10 2 8 3.2 CCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1 10.1021/jm3009103
CHEMBL1791280 211379 None 0 Rat Binding pIC50 = 5.1 5.1 - 0
Inhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellumInhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(95)00152-J
44387111 166277 None 0 Pig Binding pIC50 = 5.1 5.1 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 548 10 5 5 4.2 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CC3CCC2C3)nc1C(=O)O 10.1021/jm950592+
CHEMBL426413 166277 None 0 Pig Binding pIC50 = 5.1 5.1 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 548 10 5 5 4.2 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CC3CCC2C3)nc1C(=O)O 10.1021/jm950592+
10281606 129740 None 0 Human Binding pIC50 = 6.1 6.1 - 1
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 575 9 2 10 4.2 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCC#CCO 10.1016/s0960-894x(02)01084-3
CHEMBL367382 129740 None 0 Human Binding pIC50 = 6.1 6.1 - 1
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 575 9 2 10 4.2 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCC#CCO 10.1016/s0960-894x(02)01084-3
10765750 163254 None 0 Pig Binding pIC50 = 6.1 6.1 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 445 8 1 6 3.0 CC[S+]([O-])CCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL417972 163254 None 0 Pig Binding pIC50 = 6.1 6.1 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 445 8 1 6 3.0 CC[S+]([O-])CCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
44265906 97322 None 0 Pig Binding pIC50 = 5.1 5.1 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 441 9 1 6 3.9 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CCOCC(C)C)cc1 10.1021/jm9505369
CHEMBL268902 97322 None 0 Pig Binding pIC50 = 5.1 5.1 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 441 9 1 6 3.9 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CCOCC(C)C)cc1 10.1021/jm9505369
18184229 59627 None 0 Human Binding pIC50 = 7.1 7.1 - 2
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 605 15 2 10 4.2 CCCS(=O)(=O)NCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
CHEMBL171950 59627 None 0 Human Binding pIC50 = 7.1 7.1 - 2
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 605 15 2 10 4.2 CCCS(=O)(=O)NCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
CHEMBL313056 213570 None 0 Rat Binding pIC50 = 6.1 6.1 - 0
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00070a001
44276947 106907 None 0 Rat Binding pIC50 = 5.1 5.1 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 430 5 1 3 5.2 COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccc(Cl)c(Cl)c3)c2=O)c1 10.1016/s0960-894x(00)00232-8
CHEMBL3144803 106907 None 0 Rat Binding pIC50 = 5.1 5.1 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 430 5 1 3 5.2 COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccc(Cl)c(Cl)c3)c2=O)c1 10.1016/s0960-894x(00)00232-8
44327238 107463 None 0 Pig Binding pIC50 = 5.1 5.1 - 0
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranes
ChEMBL 497 8 1 8 3.1 CCCc1ccc(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)n1 10.1016/S0960-894X(96)00617-8
CHEMBL318017 107463 None 0 Pig Binding pIC50 = 5.1 5.1 - 0
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranes
ChEMBL 497 8 1 8 3.1 CCCc1ccc(=O)n(C(C(=O)NS(=O)(=O)c2ccc(C(C)C)cc2)c2ccc3c(c2)OCO3)n1 10.1016/S0960-894X(96)00617-8
44458597 98845 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
ChEMBL 535 7 3 8 2.3 Cn1cc(C(C(=O)NS(=O)(=O)c2ccccc2C(=O)O)c2ccc3c(c2)OCO3)c2ccc(C(N)=O)cc21 10.1016/s0960-894x(01)00660-6
CHEMBL278349 98845 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
ChEMBL 535 7 3 8 2.3 Cn1cc(C(C(=O)NS(=O)(=O)c2ccccc2C(=O)O)c2ccc3c(c2)OCO3)c2ccc(C(N)=O)cc21 10.1016/s0960-894x(01)00660-6
10817057 9696 None 0 Pig Binding pIC50 = 7.1 7.1 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 580 11 1 7 4.7 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)c1ccc(C)cc1 10.1021/jm970101g
CHEMBL113087 9696 None 0 Pig Binding pIC50 = 7.1 7.1 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 580 11 1 7 4.7 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)c1ccc(C)cc1 10.1021/jm970101g
10994374 205874 None 0 Pig Binding pIC50 = 7.1 7.1 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 474 7 1 6 5.4 COc1ccc(CC2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
CHEMBL65619 205874 None 0 Pig Binding pIC50 = 7.1 7.1 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 474 7 1 6 5.4 COc1ccc(CC2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1 10.1021/jm010382z
44298356 197229 None 0 Pig Binding pIC50 = 7.1 7.1 - 0
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptor
ChEMBL 503 10 2 8 5.7 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCC/C=N/O)c1 10.1016/s0960-894x(00)00366-8
CHEMBL54703 197229 None 0 Pig Binding pIC50 = 7.1 7.1 - 0
Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptorBinding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptor
ChEMBL 503 10 2 8 5.7 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCC/C=N/O)c1 10.1016/s0960-894x(00)00366-8
10791823 9451 None 0 Pig Binding pIC50 = 6.1 6.1 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 510 12 1 6 4.7 CCCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)C(=O)CCC 10.1021/jm970101g
CHEMBL111783 9451 None 0 Pig Binding pIC50 = 6.1 6.1 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 510 12 1 6 4.7 CCCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)C(=O)CCC 10.1021/jm970101g
10601668 98499 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)cc2OC)cc1 10.1021/jm9606507
CHEMBL275701 98499 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)cc2OC)cc1 10.1021/jm9606507
44266594 4202 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 491 8 1 8 4.8 COc1ccc(-c2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc(OC)c(OC)cc23)cc1OC 10.1016/0960-894X(96)00170-9
CHEMBL10019 4202 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 491 8 1 8 4.8 COc1ccc(-c2c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c3cc(OC)c(OC)cc23)cc1OC 10.1016/0960-894X(96)00170-9
44266552 4515 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 473 7 1 7 5.3 CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2c(c1)OCO2 10.1016/0960-894X(96)00170-9
CHEMBL10218 4515 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibitory concentration against Endothelin B receptor expressed in CHO-K1 cellsInhibitory concentration against Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 473 7 1 7 5.3 CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2c(c1)OCO2 10.1016/0960-894X(96)00170-9
9846065 171022 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta cell membranes
ChEMBL 439 7 2 6 3.6 O=S(=O)(Nc1ncnc(OCCO)c1-c1ccc(Cl)cc1)c1ccc(Cl)cc1 10.1016/j.bmcl.2016.06.014
CHEMBL4455096 171022 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of radioligand from ETB receptor in human placenta cell membranesDisplacement of radioligand from ETB receptor in human placenta cell membranes
ChEMBL 439 7 2 6 3.6 O=S(=O)(Nc1ncnc(OCCO)c1-c1ccc(Cl)cc1)c1ccc(Cl)cc1 10.1016/j.bmcl.2016.06.014
10602267 8589 None 0 Human Binding pIC50 = 4.1 4.1 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 529 13 1 6 3.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCN1CCCCC1=O 10.1021/jm980217s
CHEMBL109478 8589 None 0 Human Binding pIC50 = 4.1 4.1 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 529 13 1 6 3.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCN1CCCCC1=O 10.1021/jm980217s
52949197 18431 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 555 10 2 7 5.1 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCC4CC4)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL1271746 18431 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 555 10 2 7 5.1 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCC4CC4)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL2304012 211927 None 0 Pig Binding pIC50 = 7.1 7.1 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](C2CCCC2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc2c(Br)[nH]c3ccccc23)NC1=O 10.1021/jm9600914
44333578 4607 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B receptor
ChEMBL 417 5 1 5 4.4 CCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(02)00663-7
CHEMBL102773 4607 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B receptor
ChEMBL 417 5 1 5 4.4 CCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(02)00663-7
44278003 99322 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 449 8 1 6 5.6 COc1cccc(Sc2c(C(=O)O)n(Cc3ccccc3)c3cc(OC)c(OC)cc23)c1 10.1016/0960-894X(96)00232-6
CHEMBL28188 99322 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Affinity for human endothelin B receptor expressed in CHO-K1 cells.Affinity for human endothelin B receptor expressed in CHO-K1 cells.
ChEMBL 449 8 1 6 5.6 COc1cccc(Sc2c(C(=O)O)n(Cc3ccccc3)c3cc(OC)c(OC)cc23)c1 10.1016/0960-894X(96)00232-6
CHEMBL2304005 211920 None 0 Pig Binding pIC50 = 6.1 6.1 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL None None None Cc1[nH]c2ccccc2c1C[C@@H]1NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](C(C)C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC1=O 10.1021/jm9600914
10625738 169596 None 0 Human Binding pIC50 = 5.1 5.1 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 517 6 2 6 5.5 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc(-c3ccccc3)cc2)c1Br 10.1021/jm9608366
CHEMBL44321 169596 None 0 Human Binding pIC50 = 5.1 5.1 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 517 6 2 6 5.5 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2ccc(-c3ccccc3)cc2)c1Br 10.1021/jm9608366
44385522 59645 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 642 13 2 11 4.2 CCS(=O)(=O)NCCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
CHEMBL172029 59645 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 642 13 2 11 4.2 CCS(=O)(=O)NCCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
44284329 100466 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 504 8 2 7 5.4 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(OC(C)C)c1 10.1016/j.bmcl.2004.01.008
CHEMBL290181 100466 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 504 8 2 7 5.4 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(OC(C)C)c1 10.1016/j.bmcl.2004.01.008
159594 522 None 36 Human Binding pIC50 = 7.1 7.1 -4073 3
Inhibitory activity against human endothelin B receptorInhibitory activity against human endothelin B receptor
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm010237l
159594.0 522 None 36 Human Binding pIC50 = 7.1 7.1 -4073 3
Inhibitory activity against human endothelin B receptorInhibitory activity against human endothelin B receptor
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm010237l
3487 522 None 36 Human Binding pIC50 = 7.1 7.1 -4073 3
Inhibitory activity against human endothelin B receptorInhibitory activity against human endothelin B receptor
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm010237l
CHEMBL9194 522 None 36 Human Binding pIC50 = 7.1 7.1 -4073 3
Inhibitory activity against human endothelin B receptorInhibitory activity against human endothelin B receptor
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm010237l
DB06199 522 None 36 Human Binding pIC50 = 7.1 7.1 -4073 3
Inhibitory activity against human endothelin B receptorInhibitory activity against human endothelin B receptor
ChEMBL 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 10.1021/jm010237l
10576427 5372 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 473 6 2 7 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(NC(C)=O)cc2)cc1 10.1021/jm9606507
CHEMBL10697 5372 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 473 6 2 7 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(NC(C)=O)cc2)cc1 10.1021/jm9606507
11037806 205282 None 0 Pig Binding pIC50 = 6.1 6.1 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 456 10 2 7 4.3 CC(C)Oc1ccc2c(c1)C(OCCCCCO)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
CHEMBL62376 205282 None 0 Pig Binding pIC50 = 6.1 6.1 - 0
Binding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cellsBinding affinity to endothelin B receptor measured by inhibition of [125I]ET-3 binding recombinant pig ET-B receptor expressed in COS-7 cells
ChEMBL 456 10 2 7 4.3 CC(C)Oc1ccc2c(c1)C(OCCCCCO)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2 10.1021/jm010382z
3370402 105847 None 1 Human Binding pIC50 = 4.1 4.1 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 252 3 1 4 2.1 Cc1noc(NS(=O)(=O)c2ccccc2)c1C 10.1016/0960-894X(96)00441-6
CHEMBL312670 105847 None 1 Human Binding pIC50 = 4.1 4.1 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 252 3 1 4 2.1 Cc1noc(NS(=O)(=O)c2ccccc2)c1C 10.1016/0960-894X(96)00441-6
10670664 209776 None 0 Pig Binding pIC50 = 6.1 6.1 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 438 8 2 6 2.6 C=CCNC(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL9342 209776 None 0 Pig Binding pIC50 = 6.1 6.1 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 438 8 2 6 2.6 C=CCNC(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
23445304 131414 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 484 6 1 7 4.4 Cc1cc2c(cc1CCc1sccc1S(=O)(=O)Nc1onc(C)c1Br)OCO2 10.1016/S0960-894X(97)00133-9
CHEMBL368780 131414 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 484 6 1 7 4.4 Cc1cc2c(cc1CCc1sccc1S(=O)(=O)Nc1onc(C)c1Br)OCO2 10.1016/S0960-894X(97)00133-9
44320315 107113 None 0 Rat Binding pIC50 = 7.1 7.1 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 496 7 2 7 5.0 O=C(O)c1cccc(Cn2nc(-c3cccs3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)c1 10.1016/s0960-894x(00)00513-8
CHEMBL315638 107113 None 0 Rat Binding pIC50 = 7.1 7.1 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 496 7 2 7 5.0 O=C(O)c1cccc(Cn2nc(-c3cccs3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)c1 10.1016/s0960-894x(00)00513-8
44279413 100006 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB receptor
ChEMBL 400 2 2 3 3.3 O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(Br)cc21 10.1016/0960-894X(95)00230-Q
CHEMBL286395 100006 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Binding affinity towards cloned human ETB receptorBinding affinity towards cloned human ETB receptor
ChEMBL 400 2 2 3 3.3 O=C1c2ccccc2[C@@H]2[C@H](C(=O)O)[C@H](C(=O)O)[C@@H]2c2ccc(Br)cc21 10.1016/0960-894X(95)00230-Q
9831527 129550 None 0 Human Binding pIC50 = 8.1 8.1 - 1
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 698 14 2 12 4.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCNS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(02)01083-1
CHEMBL367274 129550 None 0 Human Binding pIC50 = 8.1 8.1 - 1
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 698 14 2 12 4.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCNS(=O)(=O)c1ccc(C)cc1 10.1016/s0960-894x(02)01083-1
44334129 108610 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B receptor
ChEMBL 459 8 1 5 5.5 CCCCCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(02)00663-7
CHEMBL320208 108610 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B receptor
ChEMBL 459 8 1 5 5.5 CCCCCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(02)00663-7
10230836 8911 None 0 Pig Binding pIC50 = 8.0 8.0 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 546 13 1 7 4.1 CCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm970101g
CHEMBL109765 8911 None 0 Pig Binding pIC50 = 8.0 8.0 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 546 13 1 7 4.1 CCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm970101g
44284288 100189 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 559 9 2 7 4.9 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(C)C(=O)N(C)C)c1 10.1016/j.bmcl.2004.01.008
CHEMBL287683 100189 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Inhibitory activity against [125I]ET1 binding to human endothelin B receptorInhibitory activity against [125I]ET1 binding to human endothelin B receptor
ChEMBL 559 9 2 7 4.9 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(C)C(=O)N(C)C)c1 10.1016/j.bmcl.2004.01.008
44320375 107201 None 0 Rat Binding pIC50 = 8.0 8.0 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 506 8 1 7 5.3 COc1cc(Cn2nc(-c3ccccc3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)cc(OC)c1 10.1016/s0960-894x(00)00513-8
CHEMBL316187 107201 None 0 Rat Binding pIC50 = 8.0 8.0 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 506 8 1 7 5.3 COc1cc(Cn2nc(-c3ccccc3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)cc(OC)c1 10.1016/s0960-894x(00)00513-8
44320480 106014 None 0 Rat Binding pIC50 = 8.0 8.0 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 442 6 1 6 5.4 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccco2)nn1CC1CCCCC1 10.1016/s0960-894x(00)00513-8
CHEMBL312979 106014 None 0 Rat Binding pIC50 = 8.0 8.0 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 442 6 1 6 5.4 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccco2)nn1CC1CCCCC1 10.1016/s0960-894x(00)00513-8
17885920 208899 None 0 Rat Binding pIC50 = 8 8.0 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 502 7 2 7 5.2 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2cccs2)nn1CC1CCCC(C(=O)O)C1 10.1016/s0960-894x(00)00513-8
CHEMBL88011 208899 None 0 Rat Binding pIC50 = 8 8.0 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 502 7 2 7 5.2 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2cccs2)nn1CC1CCCC(C(=O)O)C1 10.1016/s0960-894x(00)00513-8
155542285 173180 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 522 14 2 11 2.9 CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1Oc1cccc(OC)c1 10.1016/j.bmcl.2016.06.014
CHEMBL4519822 173180 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 522 14 2 11 2.9 CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1Oc1cccc(OC)c1 10.1016/j.bmcl.2016.06.014
44270498 98978 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) receptor expressed in CHO cells
ChEMBL 702 13 1 10 7.2 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)ccc1OC(C(=O)NS(=O)(=O)c1ccc(CC(C)C)s1)c1ccc2c(c1)OCO2 10.1016/0960-894X(95)00186-W
CHEMBL279419 98978 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Inhibition of human endothelin B (ETB) receptor expressed in CHO cellsInhibition of human endothelin B (ETB) receptor expressed in CHO cells
ChEMBL 702 13 1 10 7.2 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)ccc1OC(C(=O)NS(=O)(=O)c1ccc(CC(C)C)s1)c1ccc2c(c1)OCO2 10.1016/0960-894X(95)00186-W
CHEMBL265116 213094 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Binding affinity measured in CHO cells stably transfected with the human endothelin B receptorBinding affinity measured in CHO cells stably transfected with the human endothelin B receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00015a003
10722385 100553 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.
ChEMBL 606 13 1 11 4.6 COC(=O)CCCCOc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc(OC)c1OC 10.1021/jm980504w
CHEMBL291058 100553 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor.
ChEMBL 606 13 1 11 4.6 COC(=O)CCCCOc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc(OC)c1OC 10.1021/jm980504w
9894460 209167 None 11 Pig Binding pIC50 = 6.1 6.1 - 3
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranes
ChEMBL 539 10 2 7 4.8 CCCc1cc(C(=O)O)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2 10.1016/S0960-894X(96)00617-8
CHEMBL313871 209167 None 11 Pig Binding pIC50 = 6.1 6.1 - 3
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranes
ChEMBL 539 10 2 7 4.8 CCCc1cc(C(=O)O)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2 10.1016/S0960-894X(96)00617-8
CHEMBL8978 209167 None 11 Pig Binding pIC50 = 6.1 6.1 - 3
Inhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranesInhibition of specific binding of [125I]ET1 (endothelin 1) to endothelin B receptor of porcine kidney membranes
ChEMBL 539 10 2 7 4.8 CCCc1cc(C(=O)O)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2 10.1016/S0960-894X(96)00617-8
10410546 9414 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 432 7 1 6 4.1 COc1ccc(CC2=C(c3ccc(OC)cc3)C(=O)OC2(O)c2ccc(OC)cc2)cc1 10.1021/jm9606507
CHEMBL11162 9414 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 432 7 1 6 4.1 COc1ccc(CC2=C(c3ccc(OC)cc3)C(=O)OC2(O)c2ccc(OC)cc2)cc1 10.1021/jm9606507
44316993 207397 None 0 Human Binding pIC50 = 4.1 4.1 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 286 3 1 4 2.7 Cc1noc(NS(=O)(=O)c2cccc(Cl)c2)c1C 10.1016/0960-894X(96)00441-6
CHEMBL76360 207397 None 0 Human Binding pIC50 = 4.1 4.1 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 286 3 1 4 2.7 Cc1noc(NS(=O)(=O)c2cccc(Cl)c2)c1C 10.1016/0960-894X(96)00441-6
10627398 130755 None 0 Pig Binding pIC50 = 4.1 4.1 - 0
Inhibition of Endothelin-3 (ET-3) binding to Endothelin B receptor binding sites in porcine cerebellar membranes.Inhibition of Endothelin-3 (ET-3) binding to Endothelin B receptor binding sites in porcine cerebellar membranes.
ChEMBL 599 11 4 5 5.8 CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(Cc2ccccc2)o1 10.1021/jm950591h
CHEMBL368339 130755 None 0 Pig Binding pIC50 = 4.1 4.1 - 0
Inhibition of Endothelin-3 (ET-3) binding to Endothelin B receptor binding sites in porcine cerebellar membranes.Inhibition of Endothelin-3 (ET-3) binding to Endothelin B receptor binding sites in porcine cerebellar membranes.
ChEMBL 599 11 4 5 5.8 CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(Cc2ccccc2)o1 10.1021/jm950591h
9959298 60535 None 0 Human Binding pIC50 = 4.1 4.1 - 0
Inhibitory activity was evaluated against human Endothelin B receptorInhibitory activity was evaluated against human Endothelin B receptor
ChEMBL 552 10 2 7 5.4 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)OC(=O)N(C)C2CCCCC2)nc1C(=O)O 10.1021/jm9505932
CHEMBL175698 60535 None 0 Human Binding pIC50 = 4.1 4.1 - 0
Inhibitory activity was evaluated against human Endothelin B receptorInhibitory activity was evaluated against human Endothelin B receptor
ChEMBL 552 10 2 7 5.4 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)OC(=O)N(C)C2CCCCC2)nc1C(=O)O 10.1021/jm9505932
10764220 209542 None 0 Pig Binding pIC50 = 5.0 5.0 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 413 8 1 6 3.3 CCOCCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL9189 209542 None 0 Pig Binding pIC50 = 5.0 5.0 - 0
Inhibitory activity measured against Endothelin B receptor binding to porcine cerebellumInhibitory activity measured against Endothelin B receptor binding to porcine cerebellum
ChEMBL 413 8 1 6 3.3 CCOCCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 10.1021/jm9505369
44384966 60017 None 0 Human Binding pIC50 = 6.0 6.0 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 545 9 1 9 4.8 C#CCOc1nc(-c2cnccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
CHEMBL173465 60017 None 0 Human Binding pIC50 = 6.0 6.0 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 545 9 1 9 4.8 C#CCOc1nc(-c2cnccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01084-3
22467234 85387 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cells
ChEMBL 534 7 1 8 4.1 COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(C)=O)ccc12 10.1007/s00044-004-0021-y
CHEMBL2261599 85387 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cells
ChEMBL 534 7 1 8 4.1 COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(C)=O)ccc12 10.1007/s00044-004-0021-y
11799541 181375 None 0 Human Binding pIC50 = 5.0 5.0 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 499 8 3 9 3.4 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2CCCO)OCO3)c1Cl 10.1021/jm9608366
CHEMBL47620 181375 None 0 Human Binding pIC50 = 5.0 5.0 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 499 8 3 9 3.4 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Nc2cc3c(cc2CCCO)OCO3)c1Cl 10.1021/jm9608366
CHEMBL289687 213334 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]cn1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00070a001
10695071 101212 None 0 Human Binding pIC50 = 5.0 5.0 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 454 6 1 6 4.3 Cc1ccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1021/jm9700068
CHEMBL295477 101212 None 0 Human Binding pIC50 = 5.0 5.0 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 454 6 1 6 4.3 Cc1ccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1021/jm9700068
CHEMBL289687 213334 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
Inhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellumInhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]cn1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(95)00152-J
10599879 101330 None 0 Human Binding pIC50 = 5.0 5.0 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 455 5 2 6 4.2 Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1021/jm9608366
CHEMBL296326 101330 None 0 Human Binding pIC50 = 5.0 5.0 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 455 5 2 6 4.2 Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1021/jm9608366
25211074 18492 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
ChEMBL 543 10 2 7 5.1 CCCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2010.08.074
CHEMBL1272244 18492 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]ET1 from human ETB receptor expressed in membranesDisplacement of [125I]ET1 from human ETB receptor expressed in membranes
ChEMBL 543 10 2 7 5.1 CCCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2 10.1016/j.bmcl.2010.08.074
9871561 174904 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Antagonist activity at ETB receptor (unknown origin)Antagonist activity at ETB receptor (unknown origin)
ChEMBL 527 10 2 8 4.6 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cc2)nc(C(F)(F)F)nc1OCCO 10.1016/j.bmcl.2016.06.014
CHEMBL4562189 174904 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Antagonist activity at ETB receptor (unknown origin)Antagonist activity at ETB receptor (unknown origin)
ChEMBL 527 10 2 8 4.6 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cc2)nc(C(F)(F)F)nc1OCCO 10.1016/j.bmcl.2016.06.014
10168597 61357 None 0 Human Binding pIC50 = 6.0 6.0 - 1
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 661 11 2 13 3.6 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1cccnc1 10.1016/s0960-894x(02)01084-3
CHEMBL176741 61357 None 0 Human Binding pIC50 = 6.0 6.0 - 1
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 661 11 2 13 3.6 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1cccnc1 10.1016/s0960-894x(02)01084-3
44213278 106905 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 406 5 1 5 3.6 COc1ccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2=O)cc1 10.1016/s0960-894x(00)00232-8
CHEMBL3144799 106905 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
In vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellumIn vitro inhibition of [125-I] labelled ET-1 endothelin binding to Endothelin B receptor in rat cerebellum
ChEMBL 406 5 1 5 3.6 COc1ccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2=O)cc1 10.1016/s0960-894x(00)00232-8
23445404 100965 None 0 Human Binding pIC50 = 5.0 5.0 - 0
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB receptor
ChEMBL 456 5 1 7 4.1 Cc1ccc(OC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(97)00367-3
CHEMBL293877 100965 None 0 Human Binding pIC50 = 5.0 5.0 - 0
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETB receptor
ChEMBL 456 5 1 7 4.1 Cc1ccc(OC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(97)00367-3
10621170 11244 None 0 Human Binding pIC50 = 4.0 4.0 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 402 5 2 8 3.0 Cc1cc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)no1 10.1021/jm9608366
CHEMBL1178890 11244 None 0 Human Binding pIC50 = 4.0 4.0 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 402 5 2 8 3.0 Cc1cc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)no1 10.1021/jm9608366
CHEMBL48120 11244 None 0 Human Binding pIC50 = 4.0 4.0 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 402 5 2 8 3.0 Cc1cc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)no1 10.1021/jm9608366
23445256 60209 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 470 6 1 7 4.1 Cc1noc(NS(=O)(=O)c2ccsc2CCc2ccc3c(c2)OCO3)c1Br 10.1016/S0960-894X(97)00133-9
CHEMBL173982 60209 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 470 6 1 7 4.1 Cc1noc(NS(=O)(=O)c2ccsc2CCc2ccc3c(c2)OCO3)c1Br 10.1016/S0960-894X(97)00133-9
44340049 110387 None 0 Human Binding pIC50 = 4.0 4.0 - 0
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)
ChEMBL 500 13 1 5 5.3 C/C=C\C(C)(C)C[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC 10.1021/jm980217s
CHEMBL323951 110387 None 0 Human Binding pIC50 = 4.0 4.0 - 0
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from chinese hamster ovary cells(CHO)
ChEMBL 500 13 1 5 5.3 C/C=C\C(C)(C)C[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC 10.1021/jm980217s
10383884 207667 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 359 4 2 5 2.9 CNc1ccc(C)cc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL78563 207667 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 359 4 2 5 2.9 CNc1ccc(C)cc1S(=O)(=O)Nc1onc(C)c1Br 10.1016/0960-894X(96)00441-6
10673644 9784 None 0 Pig Binding pIC50 = 6.0 6.0 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 524 12 1 6 4.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL113611 9784 None 0 Pig Binding pIC50 = 6.0 6.0 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 524 12 1 6 4.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
76324075 85874 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]ET-1 from ETB receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hrDisplacement of [125I]ET-1 from ETB receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hr
ChEMBL 340 4 1 6 4.0 Cc1c(C(=O)O)oc2cccc(OCc3ccc4nsnc4c3)c12 10.1007/s00044-013-0542-3
CHEMBL2296899 85874 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]ET-1 from ETB receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hrDisplacement of [125I]ET-1 from ETB receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hr
ChEMBL 340 4 1 6 4.0 Cc1c(C(=O)O)oc2cccc(OCc3ccc4nsnc4c3)c12 10.1007/s00044-013-0542-3
CHEMBL315658 213650 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
Displacement of [125I]ET1 from Endothelin B receptor of rat cerebellumDisplacement of [125I]ET1 from Endothelin B receptor of rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/S0960-894X(01)81215-4
CHEMBL315658 213650 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00070a001
9809270 131408 None 0 Human Binding pIC50 = 6.0 6.0 - 2
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 622 14 2 12 2.3 CCCS(=O)(=O)NCCOc1nc(N2CCOCC2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
CHEMBL368738 131408 None 0 Human Binding pIC50 = 6.0 6.0 - 2
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 622 14 2 12 2.3 CCCS(=O)(=O)NCCOc1nc(N2CCOCC2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC 10.1016/s0960-894x(02)01083-1
137643691 158350 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 569 10 2 7 5.5 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCC4CCC4)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL4088634 158350 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 569 10 2 7 5.5 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCC4CCC4)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
23445272 127817 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 440 6 1 5 4.7 Cc1ccc(CCc2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(97)00133-9
CHEMBL366364 127817 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 440 6 1 5 4.7 Cc1ccc(CCc2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(97)00133-9
44458670 99106 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
ChEMBL 521 7 2 8 2.7 COc1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(C(N)=O)ccc23)cc1 10.1016/s0960-894x(01)00660-6
CHEMBL280379 99106 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
ChEMBL 521 7 2 8 2.7 COc1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(C(N)=O)ccc23)cc1 10.1016/s0960-894x(01)00660-6
10238141 198307 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membranesInhibition of [125I]ET1 binding to porcine kidney inner medulla membranes
ChEMBL 429 5 1 6 4.2 COc1ccccc1Cn1c(=O)c(C(=O)O)c(-c2ccc3c(c2)OCO3)c2ccccc21 10.1016/S0960-894X(97)00319-3
CHEMBL55853 198307 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Inhibition of [125I]ET1 binding to porcine kidney inner medulla membranesInhibition of [125I]ET1 binding to porcine kidney inner medulla membranes
ChEMBL 429 5 1 6 4.2 COc1ccccc1Cn1c(=O)c(C(=O)O)c(-c2ccc3c(c2)OCO3)c2ccccc21 10.1016/S0960-894X(97)00319-3
44333887 108681 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B receptor
ChEMBL 446 7 2 6 3.9 CCNCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(02)00663-7
CHEMBL320631 108681 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Inhibitory activity against I-labeled ET-1 binding to Endothelin B receptorInhibitory activity against I-labeled ET-1 binding to Endothelin B receptor
ChEMBL 446 7 2 6 3.9 CCNCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(02)00663-7
18617403 207731 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 394 3 1 4 3.3 Cc1noc(NS(=O)(=O)c2cccc(Br)c2)c1Br 10.1016/0960-894X(96)00441-6
CHEMBL79031 207731 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL 394 3 1 4 3.3 Cc1noc(NS(=O)(=O)c2cccc(Br)c2)c1Br 10.1016/0960-894X(96)00441-6
10142669 9446 None 0 Pig Binding pIC50 = 7.0 7.0 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 518 11 1 7 3.3 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)CC 10.1021/jm970101g
CHEMBL111769 9446 None 0 Pig Binding pIC50 = 7.0 7.0 - 0
Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
ChEMBL 518 11 1 7 3.3 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)CC 10.1021/jm970101g
104865 706 None 60 Human Binding pIC50 = 7.0 7.0 -6 4
Binding affinity to human ETB receptorBinding affinity to human ETB receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.ejmech.2016.06.006
104865.0 706 None 60 Human Binding pIC50 = 7.0 7.0 -6 4
Binding affinity to human ETB receptorBinding affinity to human ETB receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.ejmech.2016.06.006
3494 706 None 60 Human Binding pIC50 = 7.0 7.0 -6 4
Binding affinity to human ETB receptorBinding affinity to human ETB receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.ejmech.2016.06.006
392 706 None 60 Human Binding pIC50 = 7.0 7.0 -6 4
Binding affinity to human ETB receptorBinding affinity to human ETB receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.ejmech.2016.06.006
CHEMBL957 706 None 60 Human Binding pIC50 = 7.0 7.0 -6 4
Binding affinity to human ETB receptorBinding affinity to human ETB receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.ejmech.2016.06.006
DB00559 706 None 60 Human Binding pIC50 = 7.0 7.0 -6 4
Binding affinity to human ETB receptorBinding affinity to human ETB receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.ejmech.2016.06.006
104865 706 None 60 Rat Binding pIC50 = 7.0 7.0 -123 4
Displacement of [125I]ET-1 from rat ETB receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETB receptor after 1 hr by Lowry method
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.bmc.2015.01.003
104865.0 706 None 60 Rat Binding pIC50 = 7.0 7.0 -123 4
Displacement of [125I]ET-1 from rat ETB receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETB receptor after 1 hr by Lowry method
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.bmc.2015.01.003
3494 706 None 60 Rat Binding pIC50 = 7.0 7.0 -123 4
Displacement of [125I]ET-1 from rat ETB receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETB receptor after 1 hr by Lowry method
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.bmc.2015.01.003
392 706 None 60 Rat Binding pIC50 = 7.0 7.0 -123 4
Displacement of [125I]ET-1 from rat ETB receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETB receptor after 1 hr by Lowry method
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.bmc.2015.01.003
CHEMBL957 706 None 60 Rat Binding pIC50 = 7.0 7.0 -123 4
Displacement of [125I]ET-1 from rat ETB receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETB receptor after 1 hr by Lowry method
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.bmc.2015.01.003
DB00559 706 None 60 Rat Binding pIC50 = 7.0 7.0 -123 4
Displacement of [125I]ET-1 from rat ETB receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETB receptor after 1 hr by Lowry method
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1016/j.bmc.2015.01.003
10790757 97266 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 476 7 1 8 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(OC)c(OC)c2)cc1 10.1021/jm9606507
CHEMBL268480 97266 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cellsBinding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
ChEMBL 476 7 1 8 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(OC)c(OC)c2)cc1 10.1021/jm9606507
11027946 18920 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding affinity against human endothelin B receptor in CHO cellsBinding affinity against human endothelin B receptor in CHO cells
ChEMBL 540 12 1 5 5.4 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CC)c(F)c1 10.1021/jm010237l
CHEMBL128479 18920 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding affinity against human endothelin B receptor in CHO cellsBinding affinity against human endothelin B receptor in CHO cells
ChEMBL 540 12 1 5 5.4 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CC)c(F)c1 10.1021/jm010237l
44387111 166277 None 0 Pig Binding pIC50 = 5.0 5.0 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 548 10 5 5 4.2 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CC3CCC2C3)nc1C(=O)O 10.1021/jm950592+
CHEMBL426413 166277 None 0 Pig Binding pIC50 = 5.0 5.0 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 548 10 5 5 4.2 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CC3CCC2C3)nc1C(=O)O 10.1021/jm950592+
10289348 9315 None 0 Human Binding pIC50 = 4.0 4.0 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 516 16 1 5 5.9 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(CCC)CCC 10.1021/jm980217s
CHEMBL111023 9315 None 0 Human Binding pIC50 = 4.0 4.0 - 0
Binding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissueBinding affinity for endothelin B receptor by measuring its ability to displace [125I]-ET-3 from porcine cerebellar tissue
ChEMBL 516 16 1 5 5.9 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(CCC)CCC 10.1021/jm980217s
71458717 81701 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 433 9 2 10 1.5 COc1ccccc1Oc1c(NS(C)(=O)=O)nc(-c2ncccn2)nc1OCCO 10.1021/jm3009103
CHEMBL2163696 81701 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 433 9 2 10 1.5 COc1ccccc1Oc1c(NS(C)(=O)=O)nc(-c2ncccn2)nc1OCCO 10.1021/jm3009103
44320432 208713 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 442 6 1 7 3.6 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1CC1OCCO1 10.1016/s0960-894x(00)00513-8
CHEMBL86821 208713 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
In vitro binding affinity to endothelin B receptor in rat cerebellumIn vitro binding affinity to endothelin B receptor in rat cerebellum
ChEMBL 442 6 1 7 3.6 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccccc2)nn1CC1OCCO1 10.1016/s0960-894x(00)00513-8
23445523 60041 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B receptor
ChEMBL 472 6 1 8 3.9 Cc1noc(NS(=O)(=O)c2sccc2COc2ccc3c(c2)OCO3)c1Br 10.1016/S0960-894X(97)00132-7
CHEMBL173557 60041 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Inhibition of I-ET-1 binding to human Endothelin B receptorInhibition of I-ET-1 binding to human Endothelin B receptor
ChEMBL 472 6 1 8 3.9 Cc1noc(NS(=O)(=O)c2sccc2COc2ccc3c(c2)OCO3)c1Br 10.1016/S0960-894X(97)00132-7
22998508 209390 None 0 Human Binding pIC50 = 4.0 4.0 - 0
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 412 4 1 5 4.6 Cc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(96)00496-9
CHEMBL91073 209390 None 0 Human Binding pIC50 = 4.0 4.0 - 0
Compound was tested for binding affinity against Endothelin B receptorCompound was tested for binding affinity against Endothelin B receptor
ChEMBL 412 4 1 5 4.6 Cc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)cc1 10.1016/S0960-894X(96)00496-9
10649321 111009 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
ChEMBL 508 12 1 5 4.9 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCC3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm010237l
CHEMBL326191 111009 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
ChEMBL 508 12 1 5 4.9 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCC3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm010237l
CHEMBL328942 213775 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding affinity measured in CHO cells stably transfected with the human endothelin B receptorBinding affinity measured in CHO cells stably transfected with the human endothelin B receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00015a003
10649321 111009 None 0 Pig Binding pIC50 = 6.0 6.0 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 508 12 1 5 4.9 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCC3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
CHEMBL326191 111009 None 0 Pig Binding pIC50 = 6.0 6.0 - 0
Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
ChEMBL 508 12 1 5 4.9 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCC3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm960077r
10602312 59683 None 0 Pig Binding pIC50 = 4.0 4.0 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 531 11 5 5 4.5 Cc1oc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NCc2ccccc2)nc1C(=O)O 10.1021/jm950592+
CHEMBL172178 59683 None 0 Pig Binding pIC50 = 4.0 4.0 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 531 11 5 5 4.5 Cc1oc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NCc2ccccc2)nc1C(=O)O 10.1021/jm950592+
137633242 156571 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 569 10 2 10 3.8 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(-c4nnn[nH]4)c3)c(=O)c3cc(OCOC)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
CHEMBL4067475 156571 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Antagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETB receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
ChEMBL 569 10 2 10 3.8 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(-c4nnn[nH]4)c3)c(=O)c3cc(OCOC)ccc31)OCO2 10.1016/j.bmcl.2017.04.049
10189776 60077 None 0 Human Binding pIC50 = 6.0 6.0 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 651 11 1 10 6.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCC#CCOc1ccccc1 10.1016/s0960-894x(02)01084-3
CHEMBL173689 60077 None 0 Human Binding pIC50 = 6.0 6.0 - 0
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
ChEMBL 651 11 1 10 6.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCC#CCOc1ccccc1 10.1016/s0960-894x(02)01084-3
10766198 162980 None 0 Human Binding pIC50 = 4.0 4.0 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 455 6 2 6 3.5 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)NCc2ccccc2)c1Br 10.1021/jm9608366
CHEMBL417358 162980 None 0 Human Binding pIC50 = 4.0 4.0 - 0
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 455 6 2 6 3.5 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)NCc2ccccc2)c1Br 10.1021/jm9608366
9914310 209101 None 9 Human Binding pIC50 = 7.0 7.0 -1995 2
Radioligand binding selectivity to human Endothelin B receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin B receptor in chinese hamster ovary cells
ChEMBL 510 12 1 6 4.7 CCCCN(CCCC)C(=O)CN1CC(c2ccc3c(c2)OCO3)C(C(=O)O)C1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL8923 209101 None 9 Human Binding pIC50 = 7.0 7.0 -1995 2
Radioligand binding selectivity to human Endothelin B receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin B receptor in chinese hamster ovary cells
ChEMBL 510 12 1 6 4.7 CCCCN(CCCC)C(=O)CN1CC(c2ccc3c(c2)OCO3)C(C(=O)O)C1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL315780 213651 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
Effective concentration against Endothelin B receptor from rat cerebellumEffective concentration against Endothelin B receptor from rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@H](C(=O)O)c1csc2ccccc12)[C@@H](C)CC 10.1021/jm00070a001
11477084 3610 None 36 Human Binding pIC50 = 5.0 5.0 - 2
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C 10.1021/jm9700068
216235 3610 None 36 Human Binding pIC50 = 5.0 5.0 - 2
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C 10.1021/jm9700068
3548 3610 None 36 Human Binding pIC50 = 5.0 5.0 - 2
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C 10.1021/jm9700068
3950 3610 None 36 Human Binding pIC50 = 5.0 5.0 - 2
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C 10.1021/jm9700068
CHEMBL282724 3610 None 36 Human Binding pIC50 = 5.0 5.0 - 2
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C 10.1021/jm9700068
DB06268 3610 None 36 Human Binding pIC50 = 5.0 5.0 - 2
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
ChEMBL 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C 10.1021/jm9700068
10673644 9784 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
ChEMBL 524 12 1 6 4.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm010237l
CHEMBL113611 9784 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding affinity against endothelin B receptor in porcine cerebellar tissueBinding affinity against endothelin B receptor in porcine cerebellar tissue
ChEMBL 524 12 1 6 4.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1 10.1021/jm010237l
16004692 2454 None 59 Human Binding pIC50 = 6.0 6.0 - 1
Antagonist activity at human ETB receptor expressed in CHO cells in presence of ET1Antagonist activity at human ETB receptor expressed in CHO cells in presence of ET1
ChEMBL 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 10.1016/j.bmcl.2016.06.014
16004692.0 2454 None 59 Human Binding pIC50 = 6.0 6.0 - 1
Antagonist activity at human ETB receptor expressed in CHO cells in presence of ET1Antagonist activity at human ETB receptor expressed in CHO cells in presence of ET1
ChEMBL 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 10.1016/j.bmcl.2016.06.014
4809 2454 None 59 Human Binding pIC50 = 6.0 6.0 - 1
Antagonist activity at human ETB receptor expressed in CHO cells in presence of ET1Antagonist activity at human ETB receptor expressed in CHO cells in presence of ET1
ChEMBL 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 10.1016/j.bmcl.2016.06.014
7352 2454 None 59 Human Binding pIC50 = 6.0 6.0 - 1
Antagonist activity at human ETB receptor expressed in CHO cells in presence of ET1Antagonist activity at human ETB receptor expressed in CHO cells in presence of ET1
ChEMBL 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 10.1016/j.bmcl.2016.06.014
CHEMBL2103873 2454 None 59 Human Binding pIC50 = 6.0 6.0 - 1
Antagonist activity at human ETB receptor expressed in CHO cells in presence of ET1Antagonist activity at human ETB receptor expressed in CHO cells in presence of ET1
ChEMBL 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 10.1016/j.bmcl.2016.06.014
DB08932 2454 None 59 Human Binding pIC50 = 6.0 6.0 - 1
Antagonist activity at human ETB receptor expressed in CHO cells in presence of ET1Antagonist activity at human ETB receptor expressed in CHO cells in presence of ET1
ChEMBL 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br 10.1016/j.bmcl.2016.06.014
10070 449 None 43 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 544 8 2 8 2.5 Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N 10.1016/j.bmcl.2016.06.014
25099191 449 None 43 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 544 8 2 8 2.5 Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N 10.1016/j.bmcl.2016.06.014
25099191.0 449 None 43 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 544 8 2 8 2.5 Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N 10.1016/j.bmcl.2016.06.014
CHEMBL2165326 449 None 43 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 544 8 2 8 2.5 Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N 10.1016/j.bmcl.2016.06.014
DB15059 449 None 43 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 544 8 2 8 2.5 Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N 10.1016/j.bmcl.2016.06.014
10070 449 None 43 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 544 8 2 8 2.5 Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N 10.1021/jm3009103
25099191 449 None 43 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 544 8 2 8 2.5 Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N 10.1021/jm3009103
25099191.0 449 None 43 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 544 8 2 8 2.5 Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N 10.1021/jm3009103
CHEMBL2165326 449 None 43 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 544 8 2 8 2.5 Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N 10.1021/jm3009103
DB15059 449 None 43 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
ChEMBL 544 8 2 8 2.5 Brc1ccc(cc1)c1c(OCCOc2ncc(cn2)Br)ncnc1NS(=O)(=O)N 10.1021/jm3009103
44314906 103633 None 0 Pig Binding pIC50 = 7 7.0 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 607 12 6 5 3.4 Cc1[nH]c2ccccc2c1C[C@@H](NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)NC(Cc1c[nH]cn1)C(=O)O 10.1021/jm9600914
CHEMBL308621 103633 None 0 Pig Binding pIC50 = 7 7.0 - 0
Binding affinity towards endothelin B receptor in porcine cerebellum membranesBinding affinity towards endothelin B receptor in porcine cerebellum membranes
ChEMBL 607 12 6 5 3.4 Cc1[nH]c2ccccc2c1C[C@@H](NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)NC(Cc1c[nH]cn1)C(=O)O 10.1021/jm9600914
10697377 61107 None 0 Pig Binding pIC50 = 4 4.0 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 523 10 4 6 4.2 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCC2)nc1C(=O)O 10.1021/jm950592+
CHEMBL176513 61107 None 0 Pig Binding pIC50 = 4 4.0 - 0
Inhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranesInhibitory activity was evaluated against ET- B Binding to Endothelin B receptor from porcine cerebellar membranes
ChEMBL 523 10 4 6 4.2 Cc1oc([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCC2)nc1C(=O)O 10.1021/jm950592+
23445458 60320 None 0 Human Binding pIC50 = 5 5.0 - 0
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 468 5 1 7 4.5 Cc1noc(NS(=O)(=O)c2sccc2/C=C/c2ccc3c(c2)OCO3)c1Br 10.1016/S0960-894X(97)00133-9
CHEMBL174363 60320 None 0 Human Binding pIC50 = 5 5.0 - 0
Inhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assayInhibition of human Endothelin B receptor using I-ET-1 as radioligand in a competitive radioligand assay
ChEMBL 468 5 1 7 4.5 Cc1noc(NS(=O)(=O)c2sccc2/C=C/c2ccc3c(c2)OCO3)c1Br 10.1016/S0960-894X(97)00133-9
44284481 216186 None 0 Rat Binding pKi = 11 11.0 3 5
Compound was evaluated for the binding affinity to Endothelin B receptor in the rat hippocampusCompound was evaluated for the binding affinity to Endothelin B receptor in the rat hippocampus
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00087a001
CHEMBL437472 216186 None 0 Rat Binding pKi = 11 11.0 3 5
Compound was evaluated for the binding affinity to Endothelin B receptor in the rat hippocampusCompound was evaluated for the binding affinity to Endothelin B receptor in the rat hippocampus
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00087a001
131845706 3472 None 5 Rat Binding pKi = 10.9 10.9 11 2
Compound was evaluated for the binding affinity to Endothelin B receptor in the rat hippocampusCompound was evaluated for the binding affinity to Endothelin B receptor in the rat hippocampus
ChEMBL None None None None 10.1021/jm00087a001
71308726 3472 None 5 Rat Binding pKi = 10.9 10.9 11 2
Compound was evaluated for the binding affinity to Endothelin B receptor in the rat hippocampusCompound was evaluated for the binding affinity to Endothelin B receptor in the rat hippocampus
ChEMBL None None None None 10.1021/jm00087a001
995 3472 None 5 Rat Binding pKi = 10.9 10.9 11 2
Compound was evaluated for the binding affinity to Endothelin B receptor in the rat hippocampusCompound was evaluated for the binding affinity to Endothelin B receptor in the rat hippocampus
ChEMBL None None None None 10.1021/jm00087a001
CHEMBL1222310 3472 None 5 Rat Binding pKi = 10.9 10.9 11 2
Compound was evaluated for the binding affinity to Endothelin B receptor in the rat hippocampusCompound was evaluated for the binding affinity to Endothelin B receptor in the rat hippocampus
ChEMBL None None None None 10.1021/jm00087a001
CHEMBL4524099 3472 None 5 Rat Binding pKi = 10.9 10.9 11 2
Compound was evaluated for the binding affinity to Endothelin B receptor in the rat hippocampusCompound was evaluated for the binding affinity to Endothelin B receptor in the rat hippocampus
ChEMBL None None None None 10.1021/jm00087a001
131845706 3472 None 5 Rat Binding pKi = 10.9 10.9 11 2
Compound was evaluated for the binding affinity to Endothelin B receptor in the rat cerebellumCompound was evaluated for the binding affinity to Endothelin B receptor in the rat cerebellum
ChEMBL None None None None 10.1021/jm00087a001
71308726 3472 None 5 Rat Binding pKi = 10.9 10.9 11 2
Compound was evaluated for the binding affinity to Endothelin B receptor in the rat cerebellumCompound was evaluated for the binding affinity to Endothelin B receptor in the rat cerebellum
ChEMBL None None None None 10.1021/jm00087a001
995 3472 None 5 Rat Binding pKi = 10.9 10.9 11 2
Compound was evaluated for the binding affinity to Endothelin B receptor in the rat cerebellumCompound was evaluated for the binding affinity to Endothelin B receptor in the rat cerebellum
ChEMBL None None None None 10.1021/jm00087a001
CHEMBL1222310 3472 None 5 Rat Binding pKi = 10.9 10.9 11 2
Compound was evaluated for the binding affinity to Endothelin B receptor in the rat cerebellumCompound was evaluated for the binding affinity to Endothelin B receptor in the rat cerebellum
ChEMBL None None None None 10.1021/jm00087a001
CHEMBL4524099 3472 None 5 Rat Binding pKi = 10.9 10.9 11 2
Compound was evaluated for the binding affinity to Endothelin B receptor in the rat cerebellumCompound was evaluated for the binding affinity to Endothelin B receptor in the rat cerebellum
ChEMBL None None None None 10.1021/jm00087a001
44284481 216186 None 0 Rat Binding pKi = 10.8 10.8 3 5
Compound was evaluated for the binding affinity to Endothelin B receptor in the rat cerebellumCompound was evaluated for the binding affinity to Endothelin B receptor in the rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00087a001
CHEMBL437472 216186 None 0 Rat Binding pKi = 10.8 10.8 3 5
Compound was evaluated for the binding affinity to Endothelin B receptor in the rat cerebellumCompound was evaluated for the binding affinity to Endothelin B receptor in the rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00087a001
155543936 173338 None 0 Rat Binding pKi = 10.8 10.8 218776 2
Compound was evaluated for the binding affinity to Endothelin B receptor in the rat cerebellumCompound was evaluated for the binding affinity to Endothelin B receptor in the rat cerebellum
ChEMBL 2514 48 34 38 -9.8 CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](CC(N)=O)NC2=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](CC(N)=O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00087a001
CHEMBL4524100 173338 None 0 Rat Binding pKi = 10.8 10.8 218776 2
Compound was evaluated for the binding affinity to Endothelin B receptor in the rat cerebellumCompound was evaluated for the binding affinity to Endothelin B receptor in the rat cerebellum
ChEMBL 2514 48 34 38 -9.8 CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](CC(N)=O)NC2=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](CC(N)=O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00087a001
CHEMBL1790180 211342 None 0 Human Binding pKi = 10.8 10.8 -1 3
Binding affinity to human ETB receptor by radioligand displacement assayBinding affinity to human ETB receptor by radioligand displacement assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CCc3ccc(O)cc3)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H](Cc3ccccc3)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/j.ejmech.2013.01.044
CHEMBL1790180 211342 None 0 Rat Binding pKi = 10.7 10.7 1 3
Compound was evaluated for the binding affinity to Endothelin B receptor in the rat cerebellumCompound was evaluated for the binding affinity to Endothelin B receptor in the rat cerebellum
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CCc3ccc(O)cc3)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H](Cc3ccccc3)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00087a001
155543936 173338 None 0 Rat Binding pKi = 10.6 10.6 218776 2
Compound was evaluated for the binding affinity to Endothelin B receptor in the rat hippocampusCompound was evaluated for the binding affinity to Endothelin B receptor in the rat hippocampus
ChEMBL 2514 48 34 38 -9.8 CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](CC(N)=O)NC2=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](CC(N)=O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00087a001
CHEMBL4524100 173338 None 0 Rat Binding pKi = 10.6 10.6 218776 2
Compound was evaluated for the binding affinity to Endothelin B receptor in the rat hippocampusCompound was evaluated for the binding affinity to Endothelin B receptor in the rat hippocampus
ChEMBL 2514 48 34 38 -9.8 CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](CC(N)=O)NC2=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](CC(N)=O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm00087a001
CHEMBL1790180 211342 None 0 Rat Binding pKi = 10.4 10.4 1 3
Compound was evaluated for the binding affinity to Endothelin B receptor in the rat hippocampusCompound was evaluated for the binding affinity to Endothelin B receptor in the rat hippocampus
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CCc3ccc(O)cc3)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H](Cc3ccccc3)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm00087a001
CHEMBL1790180 211342 None 0 Human Binding pKi = 10.3 10.3 -1 3
Displacement of radiolabeled endothelin-3 from human endothelin ETB receptorDisplacement of radiolabeled endothelin-3 from human endothelin ETB receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CCc3ccc(O)cc3)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H](Cc3ccccc3)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm8007618
44284481 216186 None 0 Human Binding pKi = 10.2 10.2 -4 5
Displacement of [125I]Endothelin-1 from human recombinant ETB receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Endothelin-1 from human recombinant ETB receptor expressed in CHOK1 cells after 2 hrs
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/j.bmcl.2013.01.025
CHEMBL437472 216186 None 0 Human Binding pKi = 10.2 10.2 -4 5
Displacement of [125I]Endothelin-1 from human recombinant ETB receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Endothelin-1 from human recombinant ETB receptor expressed in CHOK1 cells after 2 hrs
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/j.bmcl.2013.01.025
44314783 166544 None 0 Pig Binding pKi = 10.1 10.1 7943 2
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 1576 47 19 18 0.8 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(96)00421-0
77282213 166544 None 0 Pig Binding pKi = 10.1 10.1 7943 2
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 1576 47 19 18 0.8 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(96)00421-0
CHEMBL427778 166544 None 0 Pig Binding pKi = 10.1 10.1 7943 2
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 1576 47 19 18 0.8 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(96)00421-0
44311728 104408 None 0 Human Binding pKi = 9.9 9.9 13 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 653 12 3 7 4.4 C=CS(=O)(=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
CHEMBL310039 104408 None 0 Human Binding pKi = 9.9 9.9 13 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 653 12 3 7 4.4 C=CS(=O)(=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
44311701 168259 None 1 Human Binding pKi = 9.7 9.7 213 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 564 10 3 5 4.9 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccno3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1 10.1016/s0960-894x(98)00387-4
CHEMBL433106 168259 None 1 Human Binding pKi = 9.7 9.7 213 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 564 10 3 5 4.9 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccno3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1 10.1016/s0960-894x(98)00387-4
44311700 102877 None 0 Human Binding pKi = 9.6 9.6 234 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 579 10 3 4 6.0 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccsc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1 10.1016/s0960-894x(98)00387-4
CHEMBL305462 102877 None 0 Human Binding pKi = 9.6 9.6 234 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 579 10 3 4 6.0 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccsc3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1 10.1016/s0960-894x(98)00387-4
44311692 103221 None 0 Human Binding pKi = 9.6 9.6 3 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 667 13 3 7 4.5 C=CCS(=O)(=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
CHEMBL308102 103221 None 0 Human Binding pKi = 9.6 9.6 3 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 667 13 3 7 4.5 C=CCS(=O)(=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
44311803 207012 None 0 Human Binding pKi = 9.6 9.6 26 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 699 15 3 8 4.3 CCOCCS(=O)(=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
CHEMBL72924 207012 None 0 Human Binding pKi = 9.6 9.6 26 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 699 15 3 8 4.3 CCOCCS(=O)(=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
44311804 103073 None 0 Human Binding pKi = 9.6 9.6 12 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 683 14 3 7 5.1 CCCCS(=O)(=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
CHEMBL306950 103073 None 0 Human Binding pKi = 9.6 9.6 12 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 683 14 3 7 5.1 CCCCS(=O)(=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
44311727 206927 None 0 Human Binding pKi = 9.6 9.6 9 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 669 13 3 7 4.7 CCCS(=O)(=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
CHEMBL72348 206927 None 0 Human Binding pKi = 9.6 9.6 9 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 669 13 3 7 4.7 CCCS(=O)(=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
44314820 155811 None 0 Pig Binding pKi = 9.6 9.6 380 2
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 1518 45 18 17 1.0 CC[C@H](C)[C@H](NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(96)00421-0
77282210 155811 None 0 Pig Binding pKi = 9.6 9.6 380 2
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 1518 45 18 17 1.0 CC[C@H](C)[C@H](NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(96)00421-0
CHEMBL405377 155811 None 0 Pig Binding pKi = 9.6 9.6 380 2
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 1518 45 18 17 1.0 CC[C@H](C)[C@H](NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(96)00421-0
44311915 104847 None 0 Human Binding pKi = 9.5 9.5 6 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 703 12 3 7 5.4 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccno3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NS(=O)(=O)c2ccccc2)c1 10.1016/s0960-894x(98)00387-4
CHEMBL310920 104847 None 0 Human Binding pKi = 9.5 9.5 6 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 703 12 3 7 5.4 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccno3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NS(=O)(=O)c2ccccc2)c1 10.1016/s0960-894x(98)00387-4
44311805 207024 None 0 Human Binding pKi = 9.4 9.4 26 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 669 12 3 7 4.7 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccno3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NS(=O)(=O)C(C)C)c1 10.1016/s0960-894x(98)00387-4
CHEMBL73000 207024 None 0 Human Binding pKi = 9.4 9.4 26 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 669 12 3 7 4.7 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccno3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NS(=O)(=O)C(C)C)c1 10.1016/s0960-894x(98)00387-4
44311838 207076 None 0 Human Binding pKi = 9.4 9.4 13 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 655 12 3 7 4.3 CCS(=O)(=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
CHEMBL73373 207076 None 0 Human Binding pKi = 9.4 9.4 13 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 655 12 3 7 4.3 CCS(=O)(=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
44311726 103140 None 0 Human Binding pKi = 9.4 9.4 10 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 667 12 3 7 4.8 C/C=C/S(=O)(=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
CHEMBL307471 103140 None 0 Human Binding pKi = 9.4 9.4 10 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 667 12 3 7 4.8 C/C=C/S(=O)(=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
44311772 103088 None 0 Human Binding pKi = 9.3 9.3 10 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 628 15 2 8 4.1 CCCCS(=O)(=O)NC(=O)C(CCSC)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
CHEMBL307045 103088 None 0 Human Binding pKi = 9.3 9.3 10 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 628 15 2 8 4.1 CCCCS(=O)(=O)NC(=O)C(CCSC)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
44311850 103246 None 0 Human Binding pKi = 9.3 9.3 10 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 717 13 3 7 5.5 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccno3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NS(=O)(=O)Cc2ccccc2)c1 10.1016/s0960-894x(98)00387-4
CHEMBL308269 103246 None 0 Human Binding pKi = 9.3 9.3 10 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 717 13 3 7 5.5 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccno3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NS(=O)(=O)Cc2ccccc2)c1 10.1016/s0960-894x(98)00387-4
44311849 103128 None 0 Human Binding pKi = 9.2 9.2 5 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 694 14 2 7 5.8 CCCCS(=O)(=O)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
CHEMBL307384 103128 None 0 Human Binding pKi = 9.2 9.2 5 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 694 14 2 7 5.8 CCCCS(=O)(=O)NC(=O)C(Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
44311852 103139 None 0 Human Binding pKi = 9.2 9.2 144 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 579 10 3 4 6.0 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3cccs3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1 10.1016/s0960-894x(98)00387-4
CHEMBL307470 103139 None 0 Human Binding pKi = 9.2 9.2 144 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 579 10 3 4 6.0 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3cccs3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1 10.1016/s0960-894x(98)00387-4
44311773 207136 None 0 Human Binding pKi = 9.2 9.2 7 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 582 13 2 7 3.8 CCCCS(=O)(=O)NC(=O)C(CC)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
CHEMBL73835 207136 None 0 Human Binding pKi = 9.2 9.2 7 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 582 13 2 7 3.8 CCCCS(=O)(=O)NC(=O)C(CC)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
44311699 206627 None 0 Human Binding pKi = 9.1 9.1 331 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 563 10 3 4 5.5 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccco3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1 10.1016/s0960-894x(98)00387-4
CHEMBL70686 206627 None 0 Human Binding pKi = 9.1 9.1 331 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 563 10 3 4 5.5 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccco3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1 10.1016/s0960-894x(98)00387-4
44311851 207121 None 0 Human Binding pKi = 9.1 9.1 162 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 564 10 3 5 4.9 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccon3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1 10.1016/s0960-894x(98)00387-4
CHEMBL73697 207121 None 0 Human Binding pKi = 9.1 9.1 162 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 564 10 3 5 4.9 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccon3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1 10.1016/s0960-894x(98)00387-4
44314607 161355 None 0 Pig Binding pKi = 9.0 9.0 1412 2
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 1534 46 19 18 -0.2 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(96)00421-0
77282208 161355 None 0 Pig Binding pKi = 9.0 9.0 1412 2
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 1534 46 19 18 -0.2 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(96)00421-0
CHEMBL412003 161355 None 0 Pig Binding pKi = 9.0 9.0 1412 2
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 1534 46 19 18 -0.2 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(96)00421-0
3887 2072 None 35 Pig Binding pKi = 9 9.0 7 4
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL None None None None 10.1016/0960-894X(96)00421-0
5311192 2072 None 35 Pig Binding pKi = 9 9.0 7 4
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL None None None None 10.1016/0960-894X(96)00421-0
CHEMBL72410 2072 None 35 Pig Binding pKi = 9 9.0 7 4
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL None None None None 10.1016/0960-894X(96)00421-0
44314832 161367 None 0 Pig Binding pKi = 9 9.0 251 2
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 1496 45 18 17 0.5 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(96)00421-0
CHEMBL412065 161367 None 0 Pig Binding pKi = 9 9.0 251 2
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 1496 45 18 17 0.5 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(96)00421-0
3887 2072 None 35 Human Binding pKi = 9 9.0 -7 4
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL None None None None 10.1016/s0960-894x(98)00387-4
5311192 2072 None 35 Human Binding pKi = 9 9.0 -7 4
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL None None None None 10.1016/s0960-894x(98)00387-4
CHEMBL72410 2072 None 35 Human Binding pKi = 9 9.0 -7 4
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL None None None None 10.1016/s0960-894x(98)00387-4
9938533 105469 None 4 Human Binding pKi = 8.9 8.9 1 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 596 13 2 7 4.0 CCCCS(=O)(=O)NC(=O)[C@@H](NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C(C)C 10.1016/s0960-894x(98)00387-4
CHEMBL311854 105469 None 4 Human Binding pKi = 8.9 8.9 1 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 596 13 2 7 4.0 CCCCS(=O)(=O)NC(=O)[C@@H](NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C(C)C 10.1016/s0960-894x(98)00387-4
9938533 105469 None 4 Human Binding pKi = 8.9 8.9 1 2
Compound was tested for the binding affinity against Endothelin B receptorCompound was tested for the binding affinity against Endothelin B receptor
ChEMBL 596 13 2 7 4.0 CCCCS(=O)(=O)NC(=O)[C@@H](NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C(C)C 10.1016/s0960-894x(98)00388-6
CHEMBL311854 105469 None 4 Human Binding pKi = 8.9 8.9 1 2
Compound was tested for the binding affinity against Endothelin B receptorCompound was tested for the binding affinity against Endothelin B receptor
ChEMBL 596 13 2 7 4.0 CCCCS(=O)(=O)NC(=O)[C@@H](NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C(C)C 10.1016/s0960-894x(98)00388-6
46228117 202240 None 0 Mouse Binding pKi = 8.9 8.9 - 1
Displacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomesDisplacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomes
ChEMBL 690 13 1 12 4.7 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCOc3ccc(S(C)(=O)=O)cc3)c2)cc1 10.1016/j.bmc.2009.08.058
CHEMBL593928 202240 None 0 Mouse Binding pKi = 8.9 8.9 - 1
Displacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomesDisplacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomes
ChEMBL 690 13 1 12 4.7 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCOc3ccc(S(C)(=O)=O)cc3)c2)cc1 10.1016/j.bmc.2009.08.058
44311763 206907 None 0 Human Binding pKi = 8.9 8.9 6 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 610 14 2 7 4.4 CCCCS(=O)(=O)NC(=O)C(CC(C)C)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
CHEMBL72217 206907 None 0 Human Binding pKi = 8.9 8.9 6 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 610 14 2 7 4.4 CCCCS(=O)(=O)NC(=O)C(CC(C)C)NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1 10.1016/s0960-894x(98)00387-4
9953358 94853 None 14 Human Binding pKi = 6 6.0 -102 2
Binding affinity against human Endothelin B receptor; orally active in vivo at 30 mg/kg, poBinding affinity against human Endothelin B receptor; orally active in vivo at 30 mg/kg, po
ChEMBL 410 9 1 7 2.9 COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1 10.1021/jm030480f
CHEMBL25344 94853 None 14 Human Binding pKi = 6 6.0 -102 2
Binding affinity against human Endothelin B receptor; orally active in vivo at 30 mg/kg, poBinding affinity against human Endothelin B receptor; orally active in vivo at 30 mg/kg, po
ChEMBL 410 9 1 7 2.9 COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1 10.1021/jm030480f
9953358 94853 None 14 Human Binding pKi = 6 6.0 -102 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 410 9 1 7 2.9 COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1 10.1021/jm960274q
CHEMBL25344 94853 None 14 Human Binding pKi = 6 6.0 -102 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 410 9 1 7 2.9 COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1 10.1021/jm960274q
10599129 102291 None 0 Human Binding pKi = 6 6.0 -5 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 438 9 1 7 3.5 COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2ccc(C)cc2)c2ccc(C)cc2)n1 10.1021/jm960274q
CHEMBL303034 102291 None 0 Human Binding pKi = 6 6.0 -5 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 438 9 1 7 3.5 COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2ccc(C)cc2)c2ccc(C)cc2)n1 10.1021/jm960274q
10737908 41464 None 0 Rat Binding pKi = 4 4.0 -102 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 370 6 1 4 4.6 Cc1cnoc1NS(=O)(=O)c1ccccc1-c1ccc(CC(C)C)cc1 10.1021/jm970872k
CHEMBL149060 41464 None 0 Rat Binding pKi = 4 4.0 -102 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 370 6 1 4 4.6 Cc1cnoc1NS(=O)(=O)c1ccccc1-c1ccc(CC(C)C)cc1 10.1021/jm970872k
10835335 4839 None 0 Human Binding pKi = 4 4.0 -50118 2
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B receptor expressed in CHO Cells.
ChEMBL 409 5 1 6 4.7 Cc1coc(-c2ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)cc2)n1 10.1021/jm000105c
CHEMBL104223 4839 None 0 Human Binding pKi = 4 4.0 -50118 2
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B receptor expressed in CHO Cells.
ChEMBL 409 5 1 6 4.7 Cc1coc(-c2ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)cc2)n1 10.1021/jm000105c
10321341 145524 None 0 Human Binding pKi = 6.0 6.0 -93 2
Inhibition of [125I]ET1 binding to cloned human ET-B receptorInhibition of [125I]ET1 binding to cloned human ET-B receptor
ChEMBL 446 7 1 5 5.2 CCCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1021/jm00037a003
CHEMBL39142 145524 None 0 Human Binding pKi = 6.0 6.0 -93 2
Inhibition of [125I]ET1 binding to cloned human ET-B receptorInhibition of [125I]ET1 binding to cloned human ET-B receptor
ChEMBL 446 7 1 5 5.2 CCCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1021/jm00037a003
11762890 100717 None 0 Human Binding pKi = 6.0 6.0 -14791 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 505 8 2 9 5.3 Cc1cc(NCc2cc(-c3ncco3)ccc2-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)no1 10.1021/jm020289q
CHEMBL29223 100717 None 0 Human Binding pKi = 6.0 6.0 -14791 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 505 8 2 9 5.3 Cc1cc(NCc2cc(-c3ncco3)ccc2-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)no1 10.1021/jm020289q
44314444 161816 None 0 Pig Binding pKi = 8.0 8.0 457 2
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 1470 45 18 17 -0.5 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(96)00421-0
CHEMBL413604 161816 None 0 Pig Binding pKi = 8.0 8.0 457 2
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 1470 45 18 17 -0.5 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(96)00421-0
178103 168054 None 17 Human Binding pKi = 7.0 7.0 -100 2
Ability to displace endothelin ([125I]ET1) from human Endothelin B receptorAbility to displace endothelin ([125I]ET1) from human Endothelin B receptor
ChEMBL 506 10 2 7 4.6 CCCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1OCCO)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1021/jm970101g
CHEMBL431651 168054 None 17 Human Binding pKi = 7.0 7.0 -100 2
Ability to displace endothelin ([125I]ET1) from human Endothelin B receptorAbility to displace endothelin ([125I]ET1) from human Endothelin B receptor
ChEMBL 506 10 2 7 4.6 CCCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1OCCO)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1021/jm970101g
10763862 163312 None 0 Human Binding pKi = 6.0 6.0 -1096 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 406 9 1 5 4.0 CCc1cc(CC)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1 10.1021/jm960274q
CHEMBL418326 163312 None 0 Human Binding pKi = 6.0 6.0 -1096 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 406 9 1 5 4.0 CCc1cc(CC)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1 10.1021/jm960274q
10907333 102137 None 0 Human Binding pKi = 6.0 6.0 -1819 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 508 7 2 7 4.9 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CC(=O)NC(C)(C)C)c1C 10.1021/jm020289q
CHEMBL30215 102137 None 0 Human Binding pKi = 6.0 6.0 -1819 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 508 7 2 7 4.9 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CC(=O)NC(C)(C)C)c1C 10.1021/jm020289q
19934535 107031 None 0 Rat Binding pKi = 5.0 5.0 7 2
Affinity against ET B receptorAffinity against ET B receptor
ChEMBL 468 6 3 4 5.0 CCCN1c2ccccc2C(=O)N(CC(=O)O)c2cc(NC(=O)c3c[nH]c4ccccc34)ccc21 10.1016/0960-894X(95)00019-P
CHEMBL315096 107031 None 0 Rat Binding pKi = 5.0 5.0 7 2
Affinity against ET B receptorAffinity against ET B receptor
ChEMBL 468 6 3 4 5.0 CCCN1c2ccccc2C(=O)N(CC(=O)O)c2cc(NC(=O)c3c[nH]c4ccccc34)ccc21 10.1016/0960-894X(95)00019-P
11812665 99822 None 0 Human Binding pKi = 5.0 5.0 -18197 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 467 8 1 7 5.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2COC(C)C)c1C 10.1021/jm020289q
CHEMBL285118 99822 None 0 Human Binding pKi = 5.0 5.0 -18197 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 467 8 1 7 5.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2COC(C)C)c1C 10.1021/jm020289q
178103 168054 None 17 Human Binding pKi = 7.0 7.0 -100 2
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 from chinese hamster ovary cells(CHO)
ChEMBL 506 10 2 7 4.6 CCCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1OCCO)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1021/jm980217s
CHEMBL431651 168054 None 17 Human Binding pKi = 7.0 7.0 -100 2
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 from chinese hamster ovary cells(CHO)
ChEMBL 506 10 2 7 4.6 CCCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1OCCO)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 10.1021/jm980217s
10553793 4463 None 0 Human Binding pKi = 6.9 6.9 -75 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 512 11 2 6 4.8 Cc1cc(C)nc(OC(C(=O)O)C(OCCc2ccc(C(=O)O)cc2)(c2ccccc2)c2ccccc2)n1 10.1021/jm9910425
CHEMBL101742 4463 None 0 Human Binding pKi = 6.9 6.9 -75 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 512 11 2 6 4.8 Cc1cc(C)nc(OC(C(=O)O)C(OCCc2ccc(C(=O)O)cc2)(c2ccccc2)c2ccccc2)n1 10.1021/jm9910425
10813050 44067 None 0 Rat Binding pKi = 5.9 5.9 -602 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 441 9 2 5 4.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2CNC=O)c1C 10.1021/jm970872k
CHEMBL151440 44067 None 0 Rat Binding pKi = 5.9 5.9 -602 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 441 9 2 5 4.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2CNC=O)c1C 10.1021/jm970872k
9830098 103085 None 0 Human Binding pKi = 5.9 5.9 5 2
Compound was tested for the binding affinity against Endothelin B receptorCompound was tested for the binding affinity against Endothelin B receptor
ChEMBL 596 13 2 7 4.0 CCCCS(=O)(=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C(C)C 10.1016/s0960-894x(98)00388-6
CHEMBL307033 103085 None 0 Human Binding pKi = 5.9 5.9 5 2
Compound was tested for the binding affinity against Endothelin B receptorCompound was tested for the binding affinity against Endothelin B receptor
ChEMBL 596 13 2 7 4.0 CCCCS(=O)(=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C(C)C 10.1016/s0960-894x(98)00388-6
44312023 206922 None 0 Human Binding pKi = 5.9 5.9 22 2
Compound was tested for the binding affinity against Endothelin B receptorCompound was tested for the binding affinity against Endothelin B receptor
ChEMBL 596 13 2 7 4.0 CCCCS(=O)(=O)NC(=O)[C@H](NC(=O)[C@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C(C)C 10.1016/s0960-894x(98)00388-6
CHEMBL72295 206922 None 0 Human Binding pKi = 5.9 5.9 22 2
Compound was tested for the binding affinity against Endothelin B receptorCompound was tested for the binding affinity against Endothelin B receptor
ChEMBL 596 13 2 7 4.0 CCCCS(=O)(=O)NC(=O)[C@H](NC(=O)[C@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C(C)C 10.1016/s0960-894x(98)00388-6
10984658 100905 None 0 Human Binding pKi = 5.9 5.9 - 1
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 570 10 1 7 6.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)CCc2ccccc2)c1C 10.1021/jm020289q
CHEMBL29346 100905 None 0 Human Binding pKi = 5.9 5.9 - 1
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 570 10 1 7 6.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)CCc2ccccc2)c1C 10.1021/jm020289q
10812403 39111 None 0 Rat Binding pKi = 4.9 4.9 -120 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 427 7 2 5 4.1 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2C(N)=O)c1C 10.1021/jm970872k
CHEMBL146904 39111 None 0 Rat Binding pKi = 4.9 4.9 -120 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 427 7 2 5 4.1 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2C(N)=O)c1C 10.1021/jm970872k
10668819 121178 None 0 Rat Binding pKi = 4.9 4.9 -602 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 402 6 1 4 5.1 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2F)c1C 10.1021/jm970872k
CHEMBL357395 121178 None 0 Rat Binding pKi = 4.9 4.9 -602 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 402 6 1 4 5.1 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2F)c1C 10.1021/jm970872k
10742502 121331 None 0 Rat Binding pKi = 4.9 4.9 -134 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 457 9 3 6 4.5 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2NCC(=O)O)c1C 10.1021/jm970872k
CHEMBL357823 121331 None 0 Rat Binding pKi = 4.9 4.9 -134 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 457 9 3 6 4.5 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2NCC(=O)O)c1C 10.1021/jm970872k
19934549 106049 None 0 Rat Binding pKi = 4.9 4.9 3 2
Affinity against ET B receptorAffinity against ET B receptor
ChEMBL 439 6 2 3 5.4 CCCN1c2ccccc2C(=O)N(CC(=O)O)c2cc(Cc3c[nH]c4ccccc34)ccc21 10.1016/0960-894X(95)00019-P
CHEMBL313184 106049 None 0 Rat Binding pKi = 4.9 4.9 3 2
Affinity against ET B receptorAffinity against ET B receptor
ChEMBL 439 6 2 3 5.4 CCCN1c2ccccc2C(=O)N(CC(=O)O)c2cc(Cc3c[nH]c4ccccc34)ccc21 10.1016/0960-894X(95)00019-P
10740953 5318 None 0 Human Binding pKi = 4.9 4.9 -758 2
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B receptor expressed in CHO Cells.
ChEMBL 423 5 1 6 5.0 Cc1nc(-c2ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)cc2)oc1C 10.1021/jm000105c
CHEMBL106749 5318 None 0 Human Binding pKi = 4.9 4.9 -758 2
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B receptor expressed in CHO Cells.
ChEMBL 423 5 1 6 5.0 Cc1nc(-c2ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)cc2)oc1C 10.1021/jm000105c
10740258 109734 None 0 Human Binding pKi = 4.9 4.9 -1096 2
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B receptor expressed in CHO Cells.
ChEMBL 409 5 1 6 4.7 Cc1cnc(-c2ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)cc2)o1 10.1021/jm000105c
CHEMBL322674 109734 None 0 Human Binding pKi = 4.9 4.9 -1096 2
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B receptor expressed in CHO Cells.
ChEMBL 409 5 1 6 4.7 Cc1cnc(-c2ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)cc2)o1 10.1021/jm000105c
9938571 9599 None 0 Human Binding pKi = 6.9 6.9 - 1
Ability to inhibit [125I]-ET-1 binding to human cloned ETB receptors expressed on CHO cellsAbility to inhibit [125I]-ET-1 binding to human cloned ETB receptors expressed on CHO cells
ChEMBL 597 9 1 8 5.6 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm000538f
CHEMBL112531 9599 None 0 Human Binding pKi = 6.9 6.9 - 1
Ability to inhibit [125I]-ET-1 binding to human cloned ETB receptors expressed on CHO cellsAbility to inhibit [125I]-ET-1 binding to human cloned ETB receptors expressed on CHO cells
ChEMBL 597 9 1 8 5.6 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm000538f
CHEMBL369489 9599 None 0 Human Binding pKi = 6.9 6.9 - 1
Ability to inhibit [125I]-ET-1 binding to human cloned ETB receptors expressed on CHO cellsAbility to inhibit [125I]-ET-1 binding to human cloned ETB receptors expressed on CHO cells
ChEMBL 597 9 1 8 5.6 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm000538f
11801906 98581 None 0 Human Binding pKi = 6.9 6.9 1 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 612 13 1 8 6.2 COc1cc(C)nc(OC(C(=O)O)C(OCCc2ccc(OC)c(OC)c2)(c2ccc(Cl)cc2)c2ccc(Cl)cc2)n1 10.1021/jm9910425
CHEMBL276288 98581 None 0 Human Binding pKi = 6.9 6.9 1 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 612 13 1 8 6.2 COc1cc(C)nc(OC(C(=O)O)C(OCCc2ccc(OC)c(OC)c2)(c2ccc(Cl)cc2)c2ccc(Cl)cc2)n1 10.1021/jm9910425
10501931 43887 None 0 Rat Binding pKi = 5.9 5.9 -64 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 414 7 2 5 4.5 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2CO)c1C 10.1021/jm970872k
CHEMBL151160 43887 None 0 Rat Binding pKi = 5.9 5.9 -64 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 414 7 2 5 4.5 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2CO)c1C 10.1021/jm970872k
10719157 102350 None 0 Human Binding pKi = 5.9 5.9 -58 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 470 11 1 9 2.9 COc1cccc(C(OC)(c2cccc(OC)c2)C(Oc2nc(OC)cc(OC)n2)C(=O)O)c1 10.1021/jm960274q
CHEMBL303390 102350 None 0 Human Binding pKi = 5.9 5.9 -58 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 470 11 1 9 2.9 COc1cccc(C(OC)(c2cccc(OC)c2)C(Oc2nc(OC)cc(OC)n2)C(=O)O)c1 10.1021/jm960274q
10552683 205569 None 0 Human Binding pKi = 5.9 5.9 -5 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 478 9 1 7 4.2 COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2ccc(Cl)cc2)c2ccc(Cl)cc2)n1 10.1021/jm960274q
CHEMBL64009 205569 None 0 Human Binding pKi = 5.9 5.9 -5 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 478 9 1 7 4.2 COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2ccc(Cl)cc2)c2ccc(Cl)cc2)n1 10.1021/jm960274q
10670662 205906 None 0 Human Binding pKi = 5.9 5.9 -53 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 438 9 1 7 3.5 COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2cccc(C)c2)c2cccc(C)c2)n1 10.1021/jm960274q
CHEMBL65833 205906 None 0 Human Binding pKi = 5.9 5.9 -53 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 438 9 1 7 3.5 COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2cccc(C)c2)c2cccc(C)c2)n1 10.1021/jm960274q
11103181 99438 None 0 Human Binding pKi = 5.9 5.9 - 1
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 507 7 1 7 4.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN2CCN(C)C2=O)c1C 10.1021/jm020289q
CHEMBL282628 99438 None 0 Human Binding pKi = 5.9 5.9 - 1
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 507 7 1 7 4.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN2CCN(C)C2=O)c1C 10.1021/jm020289q
9915028 9413 None 19 Human Binding pKi = 4.9 4.9 -28183 3
Selectivity interaction (CEREP panel (Eurofins, receptors, ion channels, and other enzymes)) EUB0000348aPTSA EDNRBSelectivity interaction (CEREP panel (Eurofins, receptors, ion channels, and other enzymes)) EUB0000348aPTSA EDNRB
ChEMBL 532 15 1 6 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC 10.6019/CHEMBL5212743
CHEMBL111612 9413 None 19 Human Binding pKi = 4.9 4.9 -28183 3
Selectivity interaction (CEREP panel (Eurofins, receptors, ion channels, and other enzymes)) EUB0000348aPTSA EDNRBSelectivity interaction (CEREP panel (Eurofins, receptors, ion channels, and other enzymes)) EUB0000348aPTSA EDNRB
ChEMBL 532 15 1 6 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC 10.6019/CHEMBL5212743
CHEMBL4761843 9413 None 19 Human Binding pKi = 4.9 4.9 -28183 3
Selectivity interaction (CEREP panel (Eurofins, receptors, ion channels, and other enzymes)) EUB0000348aPTSA EDNRBSelectivity interaction (CEREP panel (Eurofins, receptors, ion channels, and other enzymes)) EUB0000348aPTSA EDNRB
ChEMBL 532 15 1 6 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC 10.6019/CHEMBL5212743
9915028 9413 None 19 Human Binding pKi = 4.9 4.9 -28183 3
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 from chinese hamster ovary cells(CHO)
ChEMBL 532 15 1 6 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC 10.1021/jm980217s
CHEMBL111612 9413 None 19 Human Binding pKi = 4.9 4.9 -28183 3
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 from chinese hamster ovary cells(CHO)
ChEMBL 532 15 1 6 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC 10.1021/jm980217s
CHEMBL4761843 9413 None 19 Human Binding pKi = 4.9 4.9 -28183 3
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 from chinese hamster ovary cells(CHO)
ChEMBL 532 15 1 6 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC 10.1021/jm980217s
9914310 209101 None 9 Human Binding pKi = 6.9 6.9 -1995 2
Inhibitory activity against human Endothelin B receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin B receptor in chinese hamster ovary cells
ChEMBL 510 12 1 6 4.7 CCCCN(CCCC)C(=O)CN1CC(c2ccc3c(c2)OCO3)C(C(=O)O)C1c1ccc(OC)cc1 10.1021/jm9505369
CHEMBL8923 209101 None 9 Human Binding pKi = 6.9 6.9 -1995 2
Inhibitory activity against human Endothelin B receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin B receptor in chinese hamster ovary cells
ChEMBL 510 12 1 6 4.7 CCCCN(CCCC)C(=O)CN1CC(c2ccc3c(c2)OCO3)C(C(=O)O)C1c1ccc(OC)cc1 10.1021/jm9505369
9870830 209172 None 29 Human Binding pKi = 6.9 6.9 -66 2
Inhibitory activity against human Endothelin B receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin B receptor in chinese hamster ovary cells
ChEMBL 506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1021/jm9505369
CHEMBL8981 209172 None 29 Human Binding pKi = 6.9 6.9 -66 2
Inhibitory activity against human Endothelin B receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin B receptor in chinese hamster ovary cells
ChEMBL 506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1 10.1021/jm9505369
23670447 3029 None 2 Human Binding pKi = 6.9 6.9 -114 2
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 from chinese hamster ovary cells(CHO)
ChEMBL 528 10 0 9 0.1 COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+] 10.1021/jm980217s
999 3029 None 2 Human Binding pKi = 6.9 6.9 -114 2
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 from chinese hamster ovary cells(CHO)
ChEMBL 528 10 0 9 0.1 COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+] 10.1021/jm980217s
CHEMBL1204799 3029 None 2 Human Binding pKi = 6.9 6.9 -114 2
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 from chinese hamster ovary cells(CHO)
ChEMBL 528 10 0 9 0.1 COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+] 10.1021/jm980217s
CHEMBL25438 3029 None 2 Human Binding pKi = 6.9 6.9 -114 2
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 from chinese hamster ovary cells(CHO)
ChEMBL 528 10 0 9 0.1 COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+] 10.1021/jm980217s
9849547 184112 None 0 Human Binding pKi = 7.8 7.8 -34 2
Inhibition of [125I]-ET-1 binding to CHO cells expressing human Endothelin B receptor at a concentration of 1 uMInhibition of [125I]-ET-1 binding to CHO cells expressing human Endothelin B receptor at a concentration of 1 uM
ChEMBL 520 10 2 7 4.7 CCCOc1ccc2c(c1)[C@H](c1ccc(OC)cc1OCC(=O)O)[C@@H](C(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
CHEMBL48196 184112 None 0 Human Binding pKi = 7.8 7.8 -34 2
Inhibition of [125I]-ET-1 binding to CHO cells expressing human Endothelin B receptor at a concentration of 1 uMInhibition of [125I]-ET-1 binding to CHO cells expressing human Endothelin B receptor at a concentration of 1 uM
ChEMBL 520 10 2 7 4.7 CCCOc1ccc2c(c1)[C@H](c1ccc(OC)cc1OCC(=O)O)[C@@H](C(=O)O)[C@@H]2c1ccc2c(c1)OCO2 10.1016/s0960-894x(01)00273-6
10768897 107713 None 1 Human Binding pKi = 7.8 7.8 -6 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 544 13 1 8 4.8 COc1cc(C)nc(OC(C(=O)O)C(OCCc2ccc(OC)c(OC)c2)(c2ccccc2)c2ccccc2)n1 10.1021/jm9910425
CHEMBL319031 107713 None 1 Human Binding pKi = 7.8 7.8 -6 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 544 13 1 8 4.8 COc1cc(C)nc(OC(C(=O)O)C(OCCc2ccc(OC)c(OC)c2)(c2ccccc2)c2ccccc2)n1 10.1021/jm9910425
108002 3494 None 22 Human Binding pKi = 7.8 7.8 -56 2
Inhibition of [125I]ET1 binding to cloned human ET-B receptorInhibition of [125I]ET1 binding to cloned human ET-B receptor
ChEMBL 520 10 2 7 4.7 CCCOc1ccc2c(c1)[C@H]([C@@H]([C@H]2c1ccc2c(c1)OCO2)C(=O)O)c1ccc(cc1OCC(=O)O)OC 10.1021/jm00037a003
3528 3494 None 22 Human Binding pKi = 7.8 7.8 -56 2
Inhibition of [125I]ET1 binding to cloned human ET-B receptorInhibition of [125I]ET1 binding to cloned human ET-B receptor
ChEMBL 520 10 2 7 4.7 CCCOc1ccc2c(c1)[C@H]([C@@H]([C@H]2c1ccc2c(c1)OCO2)C(=O)O)c1ccc(cc1OCC(=O)O)OC 10.1021/jm00037a003
CHEMBL8823 3494 None 22 Human Binding pKi = 7.8 7.8 -56 2
Inhibition of [125I]ET1 binding to cloned human ET-B receptorInhibition of [125I]ET1 binding to cloned human ET-B receptor
ChEMBL 520 10 2 7 4.7 CCCOc1ccc2c(c1)[C@H]([C@@H]([C@H]2c1ccc2c(c1)OCO2)C(=O)O)c1ccc(cc1OCC(=O)O)OC 10.1021/jm00037a003
108002 3494 None 22 Human Binding pKi = 7.8 7.8 -56 2
Inhibitory activity against human Endothelin B receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin B receptor in chinese hamster ovary cells
ChEMBL 520 10 2 7 4.7 CCCOc1ccc2c(c1)[C@H]([C@@H]([C@H]2c1ccc2c(c1)OCO2)C(=O)O)c1ccc(cc1OCC(=O)O)OC 10.1021/jm9505369
3528 3494 None 22 Human Binding pKi = 7.8 7.8 -56 2
Inhibitory activity against human Endothelin B receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin B receptor in chinese hamster ovary cells
ChEMBL 520 10 2 7 4.7 CCCOc1ccc2c(c1)[C@H]([C@@H]([C@H]2c1ccc2c(c1)OCO2)C(=O)O)c1ccc(cc1OCC(=O)O)OC 10.1021/jm9505369
CHEMBL8823 3494 None 22 Human Binding pKi = 7.8 7.8 -56 2
Inhibitory activity against human Endothelin B receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin B receptor in chinese hamster ovary cells
ChEMBL 520 10 2 7 4.7 CCCOc1ccc2c(c1)[C@H]([C@@H]([C@H]2c1ccc2c(c1)OCO2)C(=O)O)c1ccc(cc1OCC(=O)O)OC 10.1021/jm9505369
104865 706 None 60 Human Binding pKi = 6.9 6.9 -6 4
Ability to inhibit [125I]-ET-1 binding to human cloned ETB receptors expressed on CHO cellsAbility to inhibit [125I]-ET-1 binding to human cloned ETB receptors expressed on CHO cells
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm000538f
104865.0 706 None 60 Human Binding pKi = 6.9 6.9 -6 4
Ability to inhibit [125I]-ET-1 binding to human cloned ETB receptors expressed on CHO cellsAbility to inhibit [125I]-ET-1 binding to human cloned ETB receptors expressed on CHO cells
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm000538f
3494 706 None 60 Human Binding pKi = 6.9 6.9 -6 4
Ability to inhibit [125I]-ET-1 binding to human cloned ETB receptors expressed on CHO cellsAbility to inhibit [125I]-ET-1 binding to human cloned ETB receptors expressed on CHO cells
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm000538f
392 706 None 60 Human Binding pKi = 6.9 6.9 -6 4
Ability to inhibit [125I]-ET-1 binding to human cloned ETB receptors expressed on CHO cellsAbility to inhibit [125I]-ET-1 binding to human cloned ETB receptors expressed on CHO cells
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm000538f
CHEMBL957 706 None 60 Human Binding pKi = 6.9 6.9 -6 4
Ability to inhibit [125I]-ET-1 binding to human cloned ETB receptors expressed on CHO cellsAbility to inhibit [125I]-ET-1 binding to human cloned ETB receptors expressed on CHO cells
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm000538f
DB00559 706 None 60 Human Binding pKi = 6.9 6.9 -6 4
Ability to inhibit [125I]-ET-1 binding to human cloned ETB receptors expressed on CHO cellsAbility to inhibit [125I]-ET-1 binding to human cloned ETB receptors expressed on CHO cells
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm000538f
10741151 43081 None 0 Rat Binding pKi = 5.9 5.9 -223 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 427 8 2 5 5.4 CCNc1cc(CC(C)C)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm970872k
CHEMBL150474 43081 None 0 Rat Binding pKi = 5.9 5.9 -223 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 427 8 2 5 5.4 CCNc1cc(CC(C)C)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm970872k
10743346 102666 None 0 Human Binding pKi = 5.9 5.9 -4 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 480 11 1 7 4.7 COc1cc(OC)nc(OC(C(=O)O)C(OCCC(C)(C)C)(c2ccccc2)c2ccccc2)n1 10.1021/jm960274q
CHEMBL304173 102666 None 0 Human Binding pKi = 5.9 5.9 -4 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 480 11 1 7 4.7 COc1cc(OC)nc(OC(C(=O)O)C(OCCC(C)(C)C)(c2ccccc2)c2ccccc2)n1 10.1021/jm960274q
10941181 99399 None 0 Human Binding pKi = 5.9 5.9 - 1
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 624 9 1 7 6.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)Cc2ccc(C(F)(F)F)cc2)c1C 10.1021/jm020289q
CHEMBL282336 99399 None 0 Human Binding pKi = 5.9 5.9 - 1
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 624 9 1 7 6.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)Cc2ccc(C(F)(F)F)cc2)c1C 10.1021/jm020289q
11730445 101963 None 0 Human Binding pKi = 5.9 5.9 -4677 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 475 7 1 8 4.7 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2Cn2cccn2)c1C 10.1021/jm020289q
CHEMBL30092 101963 None 0 Human Binding pKi = 5.9 5.9 -4677 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 475 7 1 8 4.7 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2Cn2cccn2)c1C 10.1021/jm020289q
9807200 85379 None 0 Human Binding pKi = 5.8 5.8 -346 2
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cells
ChEMBL 536 7 2 8 3.6 COc1cc(C)ccc1S(=O)(=O)NC(=O)[C@@H](c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(=O)O)ccc12 10.1007/s00044-004-0021-y
CHEMBL2261359 85379 None 0 Human Binding pKi = 5.8 5.8 -346 2
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cells
ChEMBL 536 7 2 8 3.6 COc1cc(C)ccc1S(=O)(=O)NC(=O)[C@@H](c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(=O)O)ccc12 10.1007/s00044-004-0021-y
10918301 101551 None 0 Human Binding pKi = 6.8 6.8 -7585 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 514 8 1 7 6.1 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)c2ccccc2)c1C 10.1021/jm020289q
CHEMBL29793 101551 None 0 Human Binding pKi = 6.8 6.8 -7585 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 514 8 1 7 6.1 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)c2ccccc2)c1C 10.1021/jm020289q
10620185 119715 None 0 Rat Binding pKi = 5.8 5.8 -89 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 386 6 1 5 4.5 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(OC(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL346853 119715 None 0 Rat Binding pKi = 5.8 5.8 -89 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 386 6 1 5 4.5 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(OC(C)C)cc2)c1C 10.1021/jm970872k
10814297 205987 None 0 Human Binding pKi = 5.8 5.8 -17 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 472 10 1 7 4.3 COc1cc(OC)nc(OC(C(=O)O)C(Oc2ccccc2)(c2ccccc2)c2ccccc2)n1 10.1021/jm960274q
CHEMBL66402 205987 None 0 Human Binding pKi = 5.8 5.8 -17 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 472 10 1 7 4.3 COc1cc(OC)nc(OC(C(=O)O)C(Oc2ccccc2)(c2ccccc2)c2ccccc2)n1 10.1021/jm960274q
11124425 99918 None 0 Human Binding pKi = 5.8 5.8 -75857 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 543 7 1 8 5.7 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2Cn2ccc(C(F)(F)F)n2)c1C 10.1021/jm020289q
CHEMBL285832 99918 None 0 Human Binding pKi = 5.8 5.8 -75857 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 543 7 1 8 5.7 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2Cn2ccc(C(F)(F)F)n2)c1C 10.1021/jm020289q
10595347 42495 None 0 Rat Binding pKi = 4.8 4.8 -537 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 370 6 1 4 4.7 CCCc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1021/jm970872k
CHEMBL149953 42495 None 0 Rat Binding pKi = 4.8 4.8 -537 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 370 6 1 4 4.7 CCCc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1021/jm970872k
10691439 44557 None 0 Rat Binding pKi = 4.8 4.8 -245 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 384 4 1 4 5.1 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(C(C)(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL151971 44557 None 0 Rat Binding pKi = 4.8 4.8 -245 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 384 4 1 4 5.1 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(C(C)(C)C)cc2)c1C 10.1021/jm970872k
76312118 85381 None 0 Human Binding pKi = 5.8 5.8 -691 2
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cells
ChEMBL 522 7 2 8 3.4 COc1cc(C)ccc1S(=O)(=O)NC(=O)[C@@H](c1ccc2c(c1)OCO2)c1cn(C)c2cc(CO)ccc12 10.1007/s00044-004-0021-y
CHEMBL2261361 85381 None 0 Human Binding pKi = 5.8 5.8 -691 2
Displacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETB receptor expressed in CHO cells
ChEMBL 522 7 2 8 3.4 COc1cc(C)ccc1S(=O)(=O)NC(=O)[C@@H](c1ccc2c(c1)OCO2)c1cn(C)c2cc(CO)ccc12 10.1007/s00044-004-0021-y
9863132 163405 None 0 Pig Binding pKi = 7.8 7.8 - 1
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 348 6 3 2 3.1 O=C(N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)C1CC1c1ccccc1 10.1016/0960-894X(96)00421-0
CHEMBL418898 163405 None 0 Pig Binding pKi = 7.8 7.8 - 1
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 348 6 3 2 3.1 O=C(N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)C1CC1c1ccccc1 10.1016/0960-894X(96)00421-0
10528863 4622 None 0 Human Binding pKi = 7.8 7.8 -4 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 484 10 2 6 4.8 Cc1cc(C)nc(OC(C(=O)O)C(OCCc2ccc(O)cc2)(c2ccccc2)c2ccccc2)n1 10.1021/jm9910425
CHEMBL102868 4622 None 0 Human Binding pKi = 7.8 7.8 -4 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 484 10 2 6 4.8 Cc1cc(C)nc(OC(C(=O)O)C(OCCc2ccc(O)cc2)(c2ccccc2)c2ccccc2)n1 10.1021/jm9910425
10786696 102842 None 0 Human Binding pKi = 6.8 6.8 -223 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 392 8 1 5 3.8 CCc1cc(C)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1 10.1021/jm960274q
CHEMBL305270 102842 None 0 Human Binding pKi = 6.8 6.8 -223 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 392 8 1 5 3.8 CCc1cc(C)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1 10.1021/jm960274q
10603135 109800 None 0 Human Binding pKi = 6.8 6.8 -1 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 570 14 1 7 6.0 CCc1ccc(C(OCCc2ccc(OC)cc2)(c2ccc(CC)cc2)C(Oc2nc(C)cc(OC)n2)C(=O)O)cc1 10.1021/jm9910425
CHEMBL322996 109800 None 0 Human Binding pKi = 6.8 6.8 -1 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 570 14 1 7 6.0 CCc1ccc(C(OCCc2ccc(OC)cc2)(c2ccc(CC)cc2)C(Oc2nc(C)cc(OC)n2)C(=O)O)cc1 10.1021/jm9910425
10503421 119573 None 0 Rat Binding pKi = 5.8 5.8 -245 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 443 9 3 6 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2NCCO)c1C 10.1021/jm970872k
CHEMBL345542 119573 None 0 Rat Binding pKi = 5.8 5.8 -245 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 443 9 3 6 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2NCCO)c1C 10.1021/jm970872k
9822616 122058 None 0 Human Binding pKi = 4.8 4.8 -17782 2
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B receptor.
ChEMBL 406 5 1 6 4.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncccn3)cc2)c1C 10.1016/s0960-894x(01)00791-0
CHEMBL359273 122058 None 0 Human Binding pKi = 4.8 4.8 -17782 2
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B receptor.
ChEMBL 406 5 1 6 4.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncccn3)cc2)c1C 10.1016/s0960-894x(01)00791-0
46228086 202290 None 0 Mouse Binding pKi = 6.8 6.8 - 1
Displacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomesDisplacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomes
ChEMBL 598 10 1 9 4.6 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCBr)c2)cc1 10.1016/j.bmc.2009.08.058
CHEMBL594265 202290 None 0 Mouse Binding pKi = 6.8 6.8 - 1
Displacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomesDisplacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomes
ChEMBL 598 10 1 9 4.6 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCBr)c2)cc1 10.1016/j.bmc.2009.08.058
10505434 4668 None 0 Human Binding pKi = 6.8 6.8 -7 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 496 11 1 5 5.8 Cc1ccc(CCCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1 10.1021/jm9910425
CHEMBL103190 4668 None 0 Human Binding pKi = 6.8 6.8 -7 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 496 11 1 5 5.8 Cc1ccc(CCCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1 10.1021/jm9910425
10691437 5084 None 0 Rat Binding pKi = 5.8 5.8 -95 4
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 384 6 1 4 5.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL105490 5084 None 0 Rat Binding pKi = 5.8 5.8 -95 4
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 384 6 1 4 5.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
9908909 5311 None 12 Rat Binding pKi = 5.8 5.8 -363 3
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 399 6 2 5 4.5 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2N)c1C 10.1021/jm970872k
CHEMBL106684 5311 None 12 Rat Binding pKi = 5.8 5.8 -363 3
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 399 6 2 5 4.5 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2N)c1C 10.1021/jm970872k
11797288 206074 None 0 Human Binding pKi = 5.8 5.8 -89 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 438 11 1 7 3.7 CCCOC(c1ccccc1)(c1ccccc1)C(Oc1nc(OC)cc(OC)n1)C(=O)O 10.1021/jm960274q
CHEMBL67084 206074 None 0 Human Binding pKi = 5.8 5.8 -89 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 438 11 1 7 3.7 CCCOC(c1ccccc1)(c1ccccc1)C(Oc1nc(OC)cc(OC)n1)C(=O)O 10.1021/jm960274q
10691437 5084 None 0 Human Binding pKi = 5.8 5.8 -95 4
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B receptor expressed in CHO Cells.
ChEMBL 384 6 1 4 5.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm000105c
CHEMBL105490 5084 None 0 Human Binding pKi = 5.8 5.8 -95 4
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B receptor expressed in CHO Cells.
ChEMBL 384 6 1 4 5.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm000105c
11081276 101277 None 0 Human Binding pKi = 5.8 5.8 -2238 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 476 7 1 8 5.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2Cc2ncco2)c1C 10.1021/jm020289q
CHEMBL29598 101277 None 0 Human Binding pKi = 5.8 5.8 -2238 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 476 7 1 8 5.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2Cc2ncco2)c1C 10.1021/jm020289q
10864118 101523 None 0 Human Binding pKi = 5.8 5.8 -4265 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 508 8 1 7 5.2 CC(=O)N(Cc1cc(-c2ncco2)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C)C(C)C 10.1021/jm020289q
CHEMBL29775 101523 None 0 Human Binding pKi = 5.8 5.8 -4265 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 508 8 1 7 5.2 CC(=O)N(Cc1cc(-c2ncco2)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C)C(C)C 10.1021/jm020289q
10667808 119355 None 0 Rat Binding pKi = 4.8 4.8 -338 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 385 6 2 5 4.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(NC(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL343867 119355 None 0 Rat Binding pKi = 4.8 4.8 -338 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 385 6 2 5 4.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(NC(C)C)cc2)c1C 10.1021/jm970872k
12286 948 None 29 Human Binding pKi = 6.8 6.8 -1348 2
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 from chinese hamster ovary cells(CHO)
ChEMBL 577 11 3 13 2.4 Cc1cnc(cc1)S(=O)(=O)Nc1c(c(nc(n1)c1cc(ncc1)c1n[nH]nn1)OCCO)Oc1ccccc1OC 10.1021/jm980217s
6433095 948 None 29 Human Binding pKi = 6.8 6.8 -1348 2
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 from chinese hamster ovary cells(CHO)
ChEMBL 577 11 3 13 2.4 Cc1cnc(cc1)S(=O)(=O)Nc1c(c(nc(n1)c1cc(ncc1)c1n[nH]nn1)OCCO)Oc1ccccc1OC 10.1021/jm980217s
6433095.0 948 None 29 Human Binding pKi = 6.8 6.8 -1348 2
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 from chinese hamster ovary cells(CHO)
ChEMBL 577 11 3 13 2.4 Cc1cnc(cc1)S(=O)(=O)Nc1c(c(nc(n1)c1cc(ncc1)c1n[nH]nn1)OCCO)Oc1ccccc1OC 10.1021/jm980217s
CHEMBL109648 948 None 29 Human Binding pKi = 6.8 6.8 -1348 2
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 from chinese hamster ovary cells(CHO)
ChEMBL 577 11 3 13 2.4 Cc1cnc(cc1)S(=O)(=O)Nc1c(c(nc(n1)c1cc(ncc1)c1n[nH]nn1)OCCO)Oc1ccccc1OC 10.1021/jm980217s
DB06677 948 None 29 Human Binding pKi = 6.8 6.8 -1348 2
Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin B receptor by measuring its ability to displace [125I]-ET-3 from chinese hamster ovary cells(CHO)
ChEMBL 577 11 3 13 2.4 Cc1cnc(cc1)S(=O)(=O)Nc1c(c(nc(n1)c1cc(ncc1)c1n[nH]nn1)OCCO)Oc1ccccc1OC 10.1021/jm980217s
108002 3494 None 22 Human Binding pKi = 7.8 7.8 -56 2
Ability to displace endothelin ([125I]ET1) from human Endothelin B receptorAbility to displace endothelin ([125I]ET1) from human Endothelin B receptor
ChEMBL 520 10 2 7 4.7 CCCOc1ccc2c(c1)[C@H]([C@@H]([C@H]2c1ccc2c(c1)OCO2)C(=O)O)c1ccc(cc1OCC(=O)O)OC 10.1021/jm970101g
3528 3494 None 22 Human Binding pKi = 7.8 7.8 -56 2
Ability to displace endothelin ([125I]ET1) from human Endothelin B receptorAbility to displace endothelin ([125I]ET1) from human Endothelin B receptor
ChEMBL 520 10 2 7 4.7 CCCOc1ccc2c(c1)[C@H]([C@@H]([C@H]2c1ccc2c(c1)OCO2)C(=O)O)c1ccc(cc1OCC(=O)O)OC 10.1021/jm970101g
CHEMBL8823 3494 None 22 Human Binding pKi = 7.8 7.8 -56 2
Ability to displace endothelin ([125I]ET1) from human Endothelin B receptorAbility to displace endothelin ([125I]ET1) from human Endothelin B receptor
ChEMBL 520 10 2 7 4.7 CCCOc1ccc2c(c1)[C@H]([C@@H]([C@H]2c1ccc2c(c1)OCO2)C(=O)O)c1ccc(cc1OCC(=O)O)OC 10.1021/jm970101g
44314884 160846 None 0 Pig Binding pKi = 6.8 6.8 - 1
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 1520 45 19 18 -0.6 CC[C@H](C)[C@H](NC(=O)CNC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(96)00421-0
77282209 160846 None 0 Pig Binding pKi = 6.8 6.8 - 1
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 1520 45 19 18 -0.6 CC[C@H](C)[C@H](NC(=O)CNC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(96)00421-0
CHEMBL411399 160846 None 0 Pig Binding pKi = 6.8 6.8 - 1
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 1520 45 19 18 -0.6 CC[C@H](C)[C@H](NC(=O)CNC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(96)00421-0
10742005 206155 None 0 Human Binding pKi = 5.8 5.8 -162 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 446 9 1 7 3.2 COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2cccc(F)c2)c2cccc(F)c2)n1 10.1021/jm960274q
CHEMBL67536 206155 None 0 Human Binding pKi = 5.8 5.8 -162 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 446 9 1 7 3.2 COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2cccc(F)c2)c2cccc(F)c2)n1 10.1021/jm960274q
13016 670 None 14 Human Binding pKi = 4.7 4.7 -13182 4
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B receptor.
ChEMBL 395 5 1 6 4.4 CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4 10.1016/s0960-894x(01)00791-0
9843631 670 None 14 Human Binding pKi = 4.7 4.7 -13182 4
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B receptor.
ChEMBL 395 5 1 6 4.4 CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4 10.1016/s0960-894x(01)00791-0
CHEMBL24461 670 None 14 Human Binding pKi = 4.7 4.7 -13182 4
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B receptor.
ChEMBL 395 5 1 6 4.4 CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4 10.1016/s0960-894x(01)00791-0
13016 670 None 14 Human Binding pKi = 4.7 4.7 -13182 4
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B receptor expressed in CHO Cells.
ChEMBL 395 5 1 6 4.4 CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4 10.1021/jm000105c
9843631 670 None 14 Human Binding pKi = 4.7 4.7 -13182 4
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B receptor expressed in CHO Cells.
ChEMBL 395 5 1 6 4.4 CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4 10.1021/jm000105c
CHEMBL24461 670 None 14 Human Binding pKi = 4.7 4.7 -13182 4
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B receptor expressed in CHO Cells.
ChEMBL 395 5 1 6 4.4 CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4 10.1021/jm000105c
13016 670 None 14 Human Binding pKi = 4.7 4.7 -13182 4
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 395 5 1 6 4.4 CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4 10.1021/jm020289q
9843631 670 None 14 Human Binding pKi = 4.7 4.7 -13182 4
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 395 5 1 6 4.4 CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4 10.1021/jm020289q
CHEMBL24461 670 None 14 Human Binding pKi = 4.7 4.7 -13182 4
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 395 5 1 6 4.4 CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4 10.1021/jm020289q
9865409 102384 None 0 Human Binding pKi = 7.7 7.7 -199 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from CHO cellsBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from CHO cells
ChEMBL 394 8 1 6 3.2 COc1cc(C)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1 10.1021/jm960274q
CHEMBL303631 102384 None 0 Human Binding pKi = 7.7 7.7 -199 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from CHO cellsBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from CHO cells
ChEMBL 394 8 1 6 3.2 COc1cc(C)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1 10.1021/jm960274q
10691438 44506 None 0 Rat Binding pKi = 5.7 5.7 -51 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 384 7 1 4 5.1 CCCCc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1021/jm970872k
CHEMBL151926 44506 None 0 Rat Binding pKi = 5.7 5.7 -51 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 384 7 1 4 5.1 CCCCc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1021/jm970872k
10718666 121585 None 0 Rat Binding pKi = 5.7 5.7 -3 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 457 9 3 6 4.5 Cc1noc(NS(=O)(=O)c2ccc(NCC(=O)O)cc2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL358461 121585 None 0 Rat Binding pKi = 5.7 5.7 -3 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 457 9 3 6 4.5 Cc1noc(NS(=O)(=O)c2ccc(NCC(=O)O)cc2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
5122650 102986 None 3 Human Binding pKi = 5.7 5.7 -100 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 364 7 1 5 3.2 COC(c1ccccc1)(c1ccccc1)C(Oc1nccc(C)n1)C(=O)O 10.1021/jm960274q
CHEMBL306218 102986 None 3 Human Binding pKi = 5.7 5.7 -100 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 364 7 1 5 3.2 COC(c1ccccc1)(c1ccccc1)C(Oc1nccc(C)n1)C(=O)O 10.1021/jm960274q
13016 670 None 14 Rat Binding pKi = 5.7 5.7 -1348 4
Displacement of [125I]-ET1 from ETB receptor in rat cerebellum after 3 hrs by scintillation counting methodDisplacement of [125I]-ET1 from ETB receptor in rat cerebellum after 3 hrs by scintillation counting method
ChEMBL 395 5 1 6 4.4 CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4 10.1016/j.bmcl.2016.06.014
9843631 670 None 14 Rat Binding pKi = 5.7 5.7 -1348 4
Displacement of [125I]-ET1 from ETB receptor in rat cerebellum after 3 hrs by scintillation counting methodDisplacement of [125I]-ET1 from ETB receptor in rat cerebellum after 3 hrs by scintillation counting method
ChEMBL 395 5 1 6 4.4 CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4 10.1016/j.bmcl.2016.06.014
CHEMBL24461 670 None 14 Rat Binding pKi = 5.7 5.7 -1348 4
Displacement of [125I]-ET1 from ETB receptor in rat cerebellum after 3 hrs by scintillation counting methodDisplacement of [125I]-ET1 from ETB receptor in rat cerebellum after 3 hrs by scintillation counting method
ChEMBL 395 5 1 6 4.4 CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4 10.1016/j.bmcl.2016.06.014
11113812 100850 None 0 Human Binding pKi = 5.7 5.7 -1258 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 497 7 1 6 6.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2/C=C\c2ccccc2)c1C 10.1021/jm020289q
CHEMBL29313 100850 None 0 Human Binding pKi = 5.7 5.7 -1258 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 497 7 1 6 6.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2/C=C\c2ccccc2)c1C 10.1021/jm020289q
11103326 168008 None 0 Human Binding pKi = 5.7 5.7 -12589 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 520 8 1 7 5.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)CC(F)(F)F)c1C 10.1021/jm020289q
CHEMBL431296 168008 None 0 Human Binding pKi = 5.7 5.7 -12589 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 520 8 1 7 5.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)CC(F)(F)F)c1C 10.1021/jm020289q
10620897 41630 None 0 Rat Binding pKi = 4.7 4.7 -14 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 398 6 1 4 5.3 Cc1cccc(-c2ccc(CC(C)C)cc2)c1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm970872k
CHEMBL149171 41630 None 0 Rat Binding pKi = 4.7 4.7 -14 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 398 6 1 4 5.3 Cc1cccc(-c2ccc(CC(C)C)cc2)c1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm970872k
10761688 119919 None 0 Rat Binding pKi = 4.7 4.7 -380 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 370 5 1 4 4.9 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(C(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL348700 119919 None 0 Rat Binding pKi = 4.7 4.7 -380 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 370 5 1 4 4.9 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(C(C)C)cc2)c1C 10.1021/jm970872k
10810897 121557 None 0 Rat Binding pKi = 4.7 4.7 -3801 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 398 6 1 4 5.3 Cc1cc(CC(C)C)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm970872k
CHEMBL358254 121557 None 0 Rat Binding pKi = 4.7 4.7 -3801 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 398 6 1 4 5.3 Cc1cc(CC(C)C)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm970872k
197712 102235 None 37 Human Binding pKi = 6.7 6.7 -194 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 378 7 1 5 3.5 COC(c1ccccc1)(c1ccccc1)C(Oc1nc(C)cc(C)n1)C(=O)O 10.1021/jm960274q
CHEMBL302753 102235 None 37 Human Binding pKi = 6.7 6.7 -194 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 378 7 1 5 3.5 COC(c1ccccc1)(c1ccccc1)C(Oc1nc(C)cc(C)n1)C(=O)O 10.1021/jm960274q
10721484 107417 None 0 Human Binding pKi = 6.7 6.7 1 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 554 13 1 6 6.3 CCc1ccc(C(OCCc2ccc(OC)cc2)(c2ccc(CC)cc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1 10.1021/jm9910425
CHEMBL317716 107417 None 0 Human Binding pKi = 6.7 6.7 1 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 554 13 1 6 6.3 CCc1ccc(C(OCCc2ccc(OC)cc2)(c2ccc(CC)cc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1 10.1021/jm9910425
10793160 98459 None 0 Human Binding pKi = 7.7 7.7 2 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 570 13 1 8 5.6 COc1cc(/C=C/COC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc(OC)c1OC 10.1021/jm9910425
CHEMBL275471 98459 None 0 Human Binding pKi = 7.7 7.7 2 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 570 13 1 8 5.6 COc1cc(/C=C/COC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc(OC)c1OC 10.1021/jm9910425
10432263 102207 None 0 Human Binding pKi = 7.7 7.7 -85 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from CHO cellsBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from CHO cells
ChEMBL 420 8 1 6 3.4 COc1nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)nc2c1CCC2 10.1021/jm960274q
CHEMBL302564 102207 None 0 Human Binding pKi = 7.7 7.7 -85 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from CHO cellsBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from CHO cells
ChEMBL 420 8 1 6 3.4 COc1nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)nc2c1CCC2 10.1021/jm960274q
10549727 164982 None 0 Rat Binding pKi = 5.7 5.7 -125 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 414 7 1 5 5.0 COc1cccc(S(=O)(=O)Nc2onc(C)c2C)c1-c1ccc(CC(C)C)cc1 10.1021/jm970872k
CHEMBL422128 164982 None 0 Rat Binding pKi = 5.7 5.7 -125 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 414 7 1 5 5.0 COc1cccc(S(=O)(=O)Nc2onc(C)c2C)c1-c1ccc(CC(C)C)cc1 10.1021/jm970872k
10762600 168405 None 0 Rat Binding pKi = 5.7 5.7 -154 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 384 6 1 4 5.0 Cc1onc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL434082 168405 None 0 Rat Binding pKi = 5.7 5.7 -154 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 384 6 1 4 5.0 Cc1onc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
10620958 41723 None 0 Rat Binding pKi = 4.7 4.7 -331 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 399 6 1 5 4.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(N(C)C(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL149241 41723 None 0 Rat Binding pKi = 4.7 4.7 -331 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 399 6 1 5 4.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(N(C)C(C)C)cc2)c1C 10.1021/jm970872k
44365561 42284 None 0 Human Binding pKi = 4.7 4.7 -524 2
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B receptor.
ChEMBL 404 5 1 4 5.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ccccc3)cc2)c1C 10.1016/s0960-894x(01)00791-0
CHEMBL149763 42284 None 0 Human Binding pKi = 4.7 4.7 -524 2
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B receptor.
ChEMBL 404 5 1 4 5.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ccccc3)cc2)c1C 10.1016/s0960-894x(01)00791-0
19085510 119619 None 0 Human Binding pKi = 4.7 4.7 -6025 2
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B receptor.
ChEMBL 405 5 1 5 4.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3cccnc3)cc2)c1C 10.1016/s0960-894x(01)00791-0
CHEMBL345951 119619 None 0 Human Binding pKi = 4.7 4.7 -6025 2
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B receptor.
ChEMBL 405 5 1 5 4.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3cccnc3)cc2)c1C 10.1016/s0960-894x(01)00791-0
11794992 4974 None 0 Human Binding pKi = 4.7 4.7 -39810 2
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B receptor expressed in CHO Cells.
ChEMBL 395 5 1 6 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3cocn3)cc2)c1C 10.1021/jm000105c
CHEMBL104848 4974 None 0 Human Binding pKi = 4.7 4.7 -39810 2
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B receptor expressed in CHO Cells.
ChEMBL 395 5 1 6 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3cocn3)cc2)c1C 10.1021/jm000105c
10668636 122038 None 0 Rat Binding pKi = 5.7 5.7 -147 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 399 6 2 5 4.5 Cc1noc(NS(=O)(=O)c2ccc(N)cc2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL359167 122038 None 0 Rat Binding pKi = 5.7 5.7 -147 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 399 6 2 5 4.5 Cc1noc(NS(=O)(=O)c2ccc(N)cc2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
10508342 4732 None 0 Human Binding pKi = 6.7 6.7 1 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 638 13 1 8 6.3 COc1ccc(CCOC(c2ccc(Cl)cc2)(c2ccc(Cl)cc2)C(Oc2nc3c(c(OC)n2)CCC3)C(=O)O)cc1OC 10.1021/jm9910425
CHEMBL103605 4732 None 0 Human Binding pKi = 6.7 6.7 1 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 638 13 1 8 6.3 COc1ccc(CCOC(c2ccc(Cl)cc2)(c2ccc(Cl)cc2)C(Oc2nc3c(c(OC)n2)CCC3)C(=O)O)cc1OC 10.1021/jm9910425
10740469 39316 None 0 Rat Binding pKi = 5.7 5.7 -154 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 413 7 2 5 5.0 CNc1cc(CC(C)C)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm970872k
CHEMBL147081 39316 None 0 Rat Binding pKi = 5.7 5.7 -154 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 413 7 2 5 5.0 CNc1cc(CC(C)C)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm970872k
18660520 39575 None 0 Human Binding pKi = 4.7 4.7 -3548 2
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B receptor.
ChEMBL 406 5 1 6 4.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3cnccn3)cc2)c1C 10.1016/s0960-894x(01)00791-0
CHEMBL147340 39575 None 0 Human Binding pKi = 4.7 4.7 -3548 2
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B receptor.
ChEMBL 406 5 1 6 4.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3cnccn3)cc2)c1C 10.1016/s0960-894x(01)00791-0
11799974 4533 None 0 Human Binding pKi = 7.6 7.6 -12 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 514 12 1 7 4.8 COc1ccc(CCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(OC)n2)C(=O)O)cc1 10.1021/jm9910425
CHEMBL102307 4533 None 0 Human Binding pKi = 7.6 7.6 -12 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 514 12 1 7 4.8 COc1ccc(CCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(OC)n2)C(=O)O)cc1 10.1021/jm9910425
3921421 107355 None 6 Human Binding pKi = 6.6 6.6 -9 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 468 10 1 5 5.1 Cc1cc(C)nc(OC(C(=O)O)C(OCCc2ccccc2)(c2ccccc2)c2ccccc2)n1 10.1021/jm9910425
CHEMBL317233 107355 None 6 Human Binding pKi = 6.6 6.6 -9 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 468 10 1 5 5.1 Cc1cc(C)nc(OC(C(=O)O)C(OCCc2ccccc2)(c2ccccc2)c2ccccc2)n1 10.1021/jm9910425
10670965 42340 None 0 Rat Binding pKi = 5.6 5.6 -851 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 444 9 2 6 4.3 Cc1noc(NS(=O)(=O)c2cccc(OCCO)c2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL149819 42340 None 0 Rat Binding pKi = 5.6 5.6 -851 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 444 9 2 6 4.3 Cc1noc(NS(=O)(=O)c2cccc(OCCO)c2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
11006149 101152 None 0 Human Binding pKi = 5.6 5.6 -380 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 550 8 1 7 6.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C(=O)C(C)(C)C)C(C)C)c1C 10.1021/jm020289q
CHEMBL29502 101152 None 0 Human Binding pKi = 5.6 5.6 -380 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 550 8 1 7 6.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C(=O)C(C)(C)C)C(C)C)c1C 10.1021/jm020289q
10521258 121360 None 0 Rat Binding pKi = 4.6 4.6 -416 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 342 4 1 4 4.1 Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1021/jm970872k
CHEMBL358020 121360 None 0 Rat Binding pKi = 4.6 4.6 -416 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 342 4 1 4 4.1 Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1 10.1021/jm970872k
44311810 104846 None 0 Human Binding pKi = 7.6 7.6 35 2
Compound was tested for the binding affinity against Endothelin B receptorCompound was tested for the binding affinity against Endothelin B receptor
ChEMBL 596 13 2 7 4.0 CCCCS(=O)(=O)NC(=O)[C@H](NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C(C)C 10.1016/s0960-894x(98)00388-6
CHEMBL310919 104846 None 0 Human Binding pKi = 7.6 7.6 35 2
Compound was tested for the binding affinity against Endothelin B receptorCompound was tested for the binding affinity against Endothelin B receptor
ChEMBL 596 13 2 7 4.0 CCCCS(=O)(=O)NC(=O)[C@H](NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C(C)C 10.1016/s0960-894x(98)00388-6
10555112 4739 None 0 Human Binding pKi = 7.6 7.6 -12 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 572 14 2 8 4.6 COc1cc(CCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)ccc1OCC(=O)O 10.1021/jm9910425
CHEMBL103695 4739 None 0 Human Binding pKi = 7.6 7.6 -12 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 572 14 2 8 4.6 COc1cc(CCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)ccc1OCC(=O)O 10.1021/jm9910425
10648996 4355 None 0 Human Binding pKi = 7.6 7.6 -3 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 498 11 1 6 5.1 COc1ccc(CCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1 10.1021/jm9910425
CHEMBL101069 4355 None 0 Human Binding pKi = 7.6 7.6 -3 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 498 11 1 6 5.1 COc1ccc(CCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1 10.1021/jm9910425
9979632 102956 None 0 Human Binding pKi = 7.6 7.6 -41 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from CHO cellsBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from CHO cells
ChEMBL 422 8 1 7 2.8 COc1nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)nc2c1CCO2 10.1021/jm960274q
CHEMBL305980 102956 None 0 Human Binding pKi = 7.6 7.6 -41 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from CHO cellsBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from CHO cells
ChEMBL 422 8 1 7 2.8 COc1nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)nc2c1CCO2 10.1021/jm960274q
45257114 202319 None 0 Mouse Binding pKi = 6.6 6.6 - 1
Displacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting
ChEMBL 538 10 1 9 4.2 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCF)c2)cc1 10.1021/jm101110w
CHEMBL594482 202319 None 0 Mouse Binding pKi = 6.6 6.6 - 1
Displacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting
ChEMBL 538 10 1 9 4.2 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCF)c2)cc1 10.1021/jm101110w
45257114 202319 None 0 Mouse Binding pKi = 6.6 6.6 - 1
Displacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomesDisplacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomes
ChEMBL 538 10 1 9 4.2 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCF)c2)cc1 10.1016/j.bmc.2009.08.058
CHEMBL594482 202319 None 0 Mouse Binding pKi = 6.6 6.6 - 1
Displacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomesDisplacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomes
ChEMBL 538 10 1 9 4.2 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCF)c2)cc1 10.1016/j.bmc.2009.08.058
10501166 41892 None 0 Rat Binding pKi = 4.6 4.6 -47 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 400 6 2 5 4.7 Cc1noc(NS(=O)(=O)c2cc(O)ccc2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL149391 41892 None 0 Rat Binding pKi = 4.6 4.6 -47 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 400 6 2 5 4.7 Cc1noc(NS(=O)(=O)c2cc(O)ccc2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
10407051 100447 None 0 Human Binding pKi = 5.6 5.6 -5 2
Inhibition of [125I]ET1 binding to cloned human ET-B receptorInhibition of [125I]ET1 binding to cloned human ET-B receptor
ChEMBL 374 5 1 3 4.7 COc1ccc([C@H]2c3ccccc3[C@@H](c3ccc(OC)cc3)[C@@H]2C(=O)O)cc1 10.1021/jm00037a003
CHEMBL290026 100447 None 0 Human Binding pKi = 5.6 5.6 -5 2
Inhibition of [125I]ET1 binding to cloned human ET-B receptorInhibition of [125I]ET1 binding to cloned human ET-B receptor
ChEMBL 374 5 1 3 4.7 COc1ccc([C@H]2c3ccccc3[C@@H](c3ccc(OC)cc3)[C@@H]2C(=O)O)cc1 10.1021/jm00037a003
9937336 174783 None 1 Human Binding pKi = 7.6 7.6 -229 2
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 510 9 1 7 4.8 CCCc1nc(C)ccc1O[C@@H](C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2016.06.014
CHEMBL4559129 174783 None 1 Human Binding pKi = 7.6 7.6 -229 2
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 510 9 1 7 4.8 CCCc1nc(C)ccc1O[C@@H](C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2016.06.014
11800649 4611 None 0 Human Binding pKi = 7.6 7.6 -7 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 542 13 1 7 5.5 CCOc1ccc(CCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1OC 10.1021/jm9910425
CHEMBL102797 4611 None 0 Human Binding pKi = 7.6 7.6 -7 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 542 13 1 7 5.5 CCOc1ccc(CCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1OC 10.1021/jm9910425
10693607 102761 None 0 Human Binding pKi = 5.6 5.6 -354 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 424 10 1 7 3.3 CCOC(c1ccccc1)(c1ccccc1)C(Oc1nc(OC)cc(OC)n1)C(=O)O 10.1021/jm960274q
CHEMBL304778 102761 None 0 Human Binding pKi = 5.6 5.6 -354 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 424 10 1 7 3.3 CCOC(c1ccccc1)(c1ccccc1)C(Oc1nc(OC)cc(OC)n1)C(=O)O 10.1021/jm960274q
10836754 206048 None 0 Human Binding pKi = 5.6 5.6 -14 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 438 11 1 7 3.7 CCOc1cc(OCC)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1 10.1021/jm960274q
CHEMBL66893 206048 None 0 Human Binding pKi = 5.6 5.6 -14 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 438 11 1 7 3.7 CCOc1cc(OCC)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1 10.1021/jm960274q
11124545 101428 None 0 Human Binding pKi = 5.6 5.6 -4168 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 557 9 1 8 5.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)Cc2ccccn2)c1C 10.1021/jm020289q
CHEMBL29710 101428 None 0 Human Binding pKi = 5.6 5.6 -4168 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 557 9 1 8 5.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)Cc2ccccn2)c1C 10.1021/jm020289q
44314445 161354 None 0 Pig Binding pKi = 6.6 6.6 - 1
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 1486 45 19 18 -0.8 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](C)NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(96)00421-0
CHEMBL412002 161354 None 0 Pig Binding pKi = 6.6 6.6 - 1
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 1486 45 19 18 -0.8 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](C)NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(96)00421-0
10670204 41547 None 0 Rat Binding pKi = 4.6 4.6 -17 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 428 7 2 5 4.7 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2C(=O)O)c1C 10.1021/jm970872k
CHEMBL149111 41547 None 0 Rat Binding pKi = 4.6 4.6 -17 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 428 7 2 5 4.7 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2C(=O)O)c1C 10.1021/jm970872k
11145758 101799 None 0 Human Binding pKi = 6.6 6.6 - 1
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 520 7 1 7 5.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN2CCC(C)(C)C2=O)c1C 10.1021/jm020289q
CHEMBL29972 101799 None 0 Human Binding pKi = 6.6 6.6 - 1
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 520 7 1 7 5.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN2CCC(C)(C)C2=O)c1C 10.1021/jm020289q
10973218 101023 None 0 Human Binding pKi = 5.6 5.6 -3388 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 506 8 2 7 5.1 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CNCC(F)(F)F)c1C 10.1021/jm020289q
CHEMBL29420 101023 None 0 Human Binding pKi = 5.6 5.6 -3388 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 506 8 2 7 5.1 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CNCC(F)(F)F)c1C 10.1021/jm020289q
10525034 119738 None 0 Rat Binding pKi = 5.6 5.6 -89 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 400 7 1 5 4.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(OCC(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL347125 119738 None 0 Rat Binding pKi = 5.6 5.6 -89 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 400 7 1 5 4.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(OCC(C)C)cc2)c1C 10.1021/jm970872k
11734435 101356 None 0 Human Binding pKi = 5.6 5.6 -6456 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 562 9 1 7 6.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)CC2CCCCC2)c1C 10.1021/jm020289q
CHEMBL29652 101356 None 0 Human Binding pKi = 5.6 5.6 -6456 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 562 9 1 7 6.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)CC2CCCCC2)c1C 10.1021/jm020289q
51003354 58084 None 0 Mouse Binding pKi = 6.5 6.5 - 1
Displacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting
ChEMBL 920 24 1 17 4.5 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCOCCOCCOCCn3cc(CN(C)S(=O)(=O)c4ccc(F)cc4)nn3)c2)cc1 10.1021/jm101110w
CHEMBL1672884 58084 None 0 Mouse Binding pKi = 6.5 6.5 - 1
Displacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting
ChEMBL 920 24 1 17 4.5 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCOCCOCCOCCn3cc(CN(C)S(=O)(=O)c4ccc(F)cc4)nn3)c2)cc1 10.1021/jm101110w
9865409 102384 None 0 Human Binding pKi = 7.5 7.5 -199 2
Binding affinity towards Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 394 8 1 6 3.2 COc1cc(C)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1 10.1021/jm960274q
CHEMBL303631 102384 None 0 Human Binding pKi = 7.5 7.5 -199 2
Binding affinity towards Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 394 8 1 6 3.2 COc1cc(C)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1 10.1021/jm960274q
10741834 44057 None 0 Rat Binding pKi = 5.5 5.5 -85 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 441 8 2 5 5.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2NC(C)C)c1C 10.1021/jm970872k
CHEMBL151422 44057 None 0 Rat Binding pKi = 5.5 5.5 -85 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 441 8 2 5 5.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2NC(C)C)c1C 10.1021/jm970872k
44311873 206928 None 0 Human Binding pKi = 8.5 8.5 2 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 636 13 2 7 5.0 CCCCS(=O)(=O)NC(=O)C(NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C1CCCCC1 10.1016/s0960-894x(98)00387-4
CHEMBL72358 206928 None 0 Human Binding pKi = 8.5 8.5 2 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 636 13 2 7 5.0 CCCCS(=O)(=O)NC(=O)C(NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C1CCCCC1 10.1016/s0960-894x(98)00387-4
44311858 96656 None 0 Human Binding pKi = 8.5 8.5 2 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 598 13 3 8 2.8 CCCCS(=O)(=O)NC(=O)C(NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C(C)O 10.1016/s0960-894x(98)00387-4
CHEMBL263301 96656 None 0 Human Binding pKi = 8.5 8.5 2 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 598 13 3 8 2.8 CCCCS(=O)(=O)NC(=O)C(NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C(C)O 10.1016/s0960-894x(98)00387-4
10840560 4669 None 0 Human Binding pKi = 8.5 8.5 -2 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 558 13 1 8 5.2 COc1cc(CCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc(OC)c1OC 10.1021/jm9910425
CHEMBL103201 4669 None 0 Human Binding pKi = 8.5 8.5 -2 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 558 13 1 8 5.2 COc1cc(CCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc(OC)c1OC 10.1021/jm9910425
44311989 207029 None 0 Human Binding pKi = 8.5 8.5 1 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 610 14 2 7 4.4 CCCCS(=O)(=O)NC(=O)C(NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C(C)CC 10.1016/s0960-894x(98)00387-4
CHEMBL73042 207029 None 0 Human Binding pKi = 8.5 8.5 1 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 610 14 2 7 4.4 CCCCS(=O)(=O)NC(=O)C(NC(=O)[C@@H](Cc1ccc(-c2ccno2)cc1)N(C)C(=O)c1cc(C)cc(C)c1)C(C)CC 10.1016/s0960-894x(98)00387-4
44274960 99617 None 0 Human Binding pKi = 5.5 5.5 -12 2
Binding affinity against human Endothelin B receptor showed weak activityBinding affinity against human Endothelin B receptor showed weak activity
ChEMBL 450 10 1 6 4.9 COc1cc(OC)nc(CC(C(=O)O)C(C)(Oc2ccc(C(C)C)cc2)c2ccccc2)n1 10.1021/jm030480f
CHEMBL283637 99617 None 0 Human Binding pKi = 5.5 5.5 -12 2
Binding affinity against human Endothelin B receptor showed weak activityBinding affinity against human Endothelin B receptor showed weak activity
ChEMBL 450 10 1 6 4.9 COc1cc(OC)nc(CC(C(=O)O)C(C)(Oc2ccc(C(C)C)cc2)c2ccccc2)n1 10.1021/jm030480f
44307412 206116 None 0 Human Binding pKi = 5.5 5.5 -12 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from CHO cellsBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from CHO cells
ChEMBL 466 10 0 8 4.5 COC(=O)C(Oc1nc(OC)cc(OC)n1)C(C)(Oc1ccc(C(C)C)cc1)c1ccccc1 10.1021/jm960274q
CHEMBL67325 206116 None 0 Human Binding pKi = 5.5 5.5 -12 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from CHO cellsBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from CHO cells
ChEMBL 466 10 0 8 4.5 COC(=O)C(Oc1nc(OC)cc(OC)n1)C(C)(Oc1ccc(C(C)C)cc1)c1ccccc1 10.1021/jm960274q
10621777 43088 None 0 Rat Binding pKi = 4.5 4.5 -12 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 415 7 1 6 4.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2)c1[N+](=O)[O-] 10.1021/jm970872k
CHEMBL150481 43088 None 0 Rat Binding pKi = 4.5 4.5 -12 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 415 7 1 6 4.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2)c1[N+](=O)[O-] 10.1021/jm970872k
10548904 119574 None 0 Rat Binding pKi = 4.5 4.5 -380 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 398 7 1 4 5.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CCC(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL345551 119574 None 0 Rat Binding pKi = 4.5 4.5 -380 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 398 7 1 4 5.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CCC(C)C)cc2)c1C 10.1021/jm970872k
44213540 39492 None 0 Human Binding pKi = 4.5 4.5 -831 2
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B receptor.
ChEMBL 421 5 1 5 4.1 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3cccc[n+]3[O-])cc2)c1C 10.1016/s0960-894x(01)00791-0
CHEMBL147238 39492 None 0 Human Binding pKi = 4.5 4.5 -831 2
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B receptor.
ChEMBL 421 5 1 5 4.1 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3cccc[n+]3[O-])cc2)c1C 10.1016/s0960-894x(01)00791-0
11124821 99343 None 0 Human Binding pKi = 6.5 6.5 - 1
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 595 8 1 8 6.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)c2cc3ccccc3n2C)c1C 10.1021/jm020289q
CHEMBL281977 99343 None 0 Human Binding pKi = 6.5 6.5 - 1
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 595 8 1 8 6.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)c2cc3ccccc3n2C)c1C 10.1021/jm020289q
10505357 109459 None 0 Human Binding pKi = 6.5 6.5 -10 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 494 10 1 5 5.9 Cc1ccc(/C=C/COC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1 10.1021/jm9910425
CHEMBL321984 109459 None 0 Human Binding pKi = 6.5 6.5 -10 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 494 10 1 5 5.9 Cc1ccc(/C=C/COC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1 10.1021/jm9910425
10941084 102039 None 0 Human Binding pKi = 6.5 6.5 - 1
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 610 8 1 7 7.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)c2cc(Cl)cc(Cl)c2)c1C 10.1021/jm020289q
CHEMBL30150 102039 None 0 Human Binding pKi = 6.5 6.5 - 1
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 610 8 1 7 7.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)c2cc(Cl)cc(Cl)c2)c1C 10.1021/jm020289q
443289 711 None 39 Rat Binding pKi = 4.5 4.5 -831 3
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL None None None None 10.1021/jm970872k
997 711 None 39 Rat Binding pKi = 4.5 4.5 -831 3
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL None None None None 10.1021/jm970872k
CHEMBL314691 711 None 39 Rat Binding pKi = 4.5 4.5 -831 3
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL None None None None 10.1021/jm970872k
DB12054 711 None 39 Rat Binding pKi = 4.5 4.5 -831 3
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL None None None None 10.1021/jm970872k
10119517 99288 None 0 Human Binding pKi = 5.5 5.5 -169824 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 536 8 1 7 5.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)CC(C)(C)C)c1C 10.1021/jm020289q
CHEMBL281659 99288 None 0 Human Binding pKi = 5.5 5.5 -169824 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 536 8 1 7 5.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)CC(C)(C)C)c1C 10.1021/jm020289q
104865 706 None 60 Human Binding pKi = 6.5 6.5 -6 4
Ability to displace endothelin ([125I]ET1) from human Endothelin B receptorAbility to displace endothelin ([125I]ET1) from human Endothelin B receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm970101g
104865.0 706 None 60 Human Binding pKi = 6.5 6.5 -6 4
Ability to displace endothelin ([125I]ET1) from human Endothelin B receptorAbility to displace endothelin ([125I]ET1) from human Endothelin B receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm970101g
3494 706 None 60 Human Binding pKi = 6.5 6.5 -6 4
Ability to displace endothelin ([125I]ET1) from human Endothelin B receptorAbility to displace endothelin ([125I]ET1) from human Endothelin B receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm970101g
392 706 None 60 Human Binding pKi = 6.5 6.5 -6 4
Ability to displace endothelin ([125I]ET1) from human Endothelin B receptorAbility to displace endothelin ([125I]ET1) from human Endothelin B receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm970101g
CHEMBL957 706 None 60 Human Binding pKi = 6.5 6.5 -6 4
Ability to displace endothelin ([125I]ET1) from human Endothelin B receptorAbility to displace endothelin ([125I]ET1) from human Endothelin B receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm970101g
DB00559 706 None 60 Human Binding pKi = 6.5 6.5 -6 4
Ability to displace endothelin ([125I]ET1) from human Endothelin B receptorAbility to displace endothelin ([125I]ET1) from human Endothelin B receptor
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm970101g
10669224 108522 None 0 Human Binding pKi = 4.5 4.5 -1778 2
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B receptor expressed in CHO Cells.
ChEMBL 409 6 1 6 4.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(Cc3ncco3)cc2)c1C 10.1021/jm000105c
CHEMBL319924 108522 None 0 Human Binding pKi = 4.5 4.5 -1778 2
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B receptor expressed in CHO Cells.
ChEMBL 409 6 1 6 4.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(Cc3ncco3)cc2)c1C 10.1021/jm000105c
44265871 167014 None 0 Human Binding pKi = 6.5 6.5 -53 2
Inhibitory activity against human Endothelin B receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin B receptor in chinese hamster ovary cells
ChEMBL 547 10 2 8 4.6 COc1ccccc1Cc1c(CCCO)nc(-c2ncccn2)nc1NS(=O)(=O)c1ccc(C(C)(C)C)cc1 10.1021/jm9505369
CHEMBL428661 167014 None 0 Human Binding pKi = 6.5 6.5 -53 2
Inhibitory activity against human Endothelin B receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin B receptor in chinese hamster ovary cells
ChEMBL 547 10 2 8 4.6 COc1ccccc1Cc1c(CCCO)nc(-c2ncccn2)nc1NS(=O)(=O)c1ccc(C(C)(C)C)cc1 10.1021/jm9505369
10692125 205521 None 0 Human Binding pKi = 5.5 5.5 -26 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 396 8 2 7 2.3 COc1cc(OC)nc(OC(C(=O)O)C(O)(c2ccccc2)c2ccccc2)n1 10.1021/jm960274q
CHEMBL63648 205521 None 0 Human Binding pKi = 5.5 5.5 -26 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 396 8 2 7 2.3 COc1cc(OC)nc(OC(C(=O)O)C(O)(c2ccccc2)c2ccccc2)n1 10.1021/jm960274q
9848710 169183 None 4 Pig Binding pKi = 7.4 7.4 -1 4
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 497 9 3 3 4.3 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1 10.1016/0960-894X(96)00421-0
CHEMBL439759 169183 None 4 Pig Binding pKi = 7.4 7.4 -1 4
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 497 9 3 3 4.3 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1 10.1016/0960-894X(96)00421-0
9848710 169183 None 4 Human Binding pKi = 7.4 7.4 1 4
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 497 9 3 3 4.3 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1 10.1016/s0960-894x(98)00387-4
CHEMBL439759 169183 None 4 Human Binding pKi = 7.4 7.4 1 4
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 497 9 3 3 4.3 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1 10.1016/s0960-894x(98)00387-4
11082049 99614 None 0 Human Binding pKi = 6.4 6.4 -933 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 534 7 1 7 5.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN2CCCC(C)(C)C2=O)c1C 10.1021/jm020289q
CHEMBL283610 99614 None 0 Human Binding pKi = 6.4 6.4 -933 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 534 7 1 7 5.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN2CCCC(C)(C)C2=O)c1C 10.1021/jm020289q
51003353 58083 None 0 Mouse Binding pKi = 7.4 7.4 - 1
Displacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting
ChEMBL 886 26 1 17 5.5 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCOCCOCCOCCn3cc(CCCCOc4cccnc4F)nn3)c2)cc1 10.1021/jm101110w
CHEMBL1672883 58083 None 0 Mouse Binding pKi = 7.4 7.4 - 1
Displacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting
ChEMBL 886 26 1 17 5.5 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCOCCOCCOCCn3cc(CCCCOc4cccnc4F)nn3)c2)cc1 10.1021/jm101110w
10599293 39036 None 0 Rat Binding pKi = 5.4 5.4 -128 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 441 9 2 5 5.8 CCCNc1cc(CC(C)C)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm970872k
CHEMBL146845 39036 None 0 Rat Binding pKi = 5.4 5.4 -128 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 441 9 2 5 5.8 CCCNc1cc(CC(C)C)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm970872k
9953358 94853 None 14 Human Binding pKi = 6.4 6.4 -102 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from CHO cellsBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from CHO cells
ChEMBL 410 9 1 7 2.9 COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1 10.1021/jm960274q
CHEMBL25344 94853 None 14 Human Binding pKi = 6.4 6.4 -102 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from CHO cellsBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from CHO cells
ChEMBL 410 9 1 7 2.9 COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1 10.1021/jm960274q
177236 1325 None 32 Human Binding pKi = 6.4 6.4 -134 3
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 410 9 1 7 2.9 COC([C@@H](C(=O)O)Oc1nc(OC)cc(n1)OC)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2016.06.014
3508 1325 None 32 Human Binding pKi = 6.4 6.4 -134 3
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 410 9 1 7 2.9 COC([C@@H](C(=O)O)Oc1nc(OC)cc(n1)OC)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2016.06.014
CHEMBL23261 1325 None 32 Human Binding pKi = 6.4 6.4 -134 3
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 410 9 1 7 2.9 COC([C@@H](C(=O)O)Oc1nc(OC)cc(n1)OC)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2016.06.014
DB04883 1325 None 32 Human Binding pKi = 6.4 6.4 -134 3
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
ChEMBL 410 9 1 7 2.9 COC([C@@H](C(=O)O)Oc1nc(OC)cc(n1)OC)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2016.06.014
11082168 99269 None 0 Human Binding pKi = 6.4 6.4 -7585 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 548 8 1 7 5.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)CC(F)(F)F)c1C 10.1021/jm020289q
CHEMBL281549 99269 None 0 Human Binding pKi = 6.4 6.4 -7585 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 548 8 1 7 5.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)CC(F)(F)F)c1C 10.1021/jm020289q
10839202 119300 None 0 Rat Binding pKi = 4.4 4.4 -6 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 503 8 2 5 6.2 Cc1noc(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3)cc2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL343477 119300 None 0 Rat Binding pKi = 4.4 4.4 -6 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 503 8 2 5 6.2 Cc1noc(NS(=O)(=O)c2ccc(NC(=O)c3ccccc3)cc2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
22103537 42086 None 0 Human Binding pKi = 4.4 4.4 -144 2
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B receptor.
ChEMBL 395 5 1 6 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ccno3)cc2)c1C 10.1016/s0960-894x(01)00791-0
CHEMBL149592 42086 None 0 Human Binding pKi = 4.4 4.4 -144 2
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B receptor.
ChEMBL 395 5 1 6 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ccno3)cc2)c1C 10.1016/s0960-894x(01)00791-0
44311698 206568 None 0 Human Binding pKi = 8.4 8.4 524 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 574 10 3 4 5.3 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccccn3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1 10.1016/s0960-894x(98)00387-4
CHEMBL70310 206568 None 0 Human Binding pKi = 8.4 8.4 524 2
Binding affinity to Endothelin B receptorBinding affinity to Endothelin B receptor
ChEMBL 574 10 3 4 5.3 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccc(-c3ccccn3)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)c1 10.1016/s0960-894x(98)00387-4
9893800 107286 None 11 Human Binding pKi = 8.3 8.3 -2 2
Displacement of [125I]ET-3 from human ET-B receptor expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting methodDisplacement of [125I]ET-3 from human ET-B receptor expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting method
ChEMBL 528 12 1 7 5.1 COc1ccc(CCOC(c2ccccc2)(c2ccccc2)[C@H](Oc2nc(C)cc(C)n2)C(=O)O)cc1OC 10.1021/acs.jmedchem.5b01781
CHEMBL316735 107286 None 11 Human Binding pKi = 8.3 8.3 -2 2
Displacement of [125I]ET-3 from human ET-B receptor expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting methodDisplacement of [125I]ET-3 from human ET-B receptor expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting method
ChEMBL 528 12 1 7 5.1 COc1ccc(CCOC(c2ccccc2)(c2ccccc2)[C@H](Oc2nc(C)cc(C)n2)C(=O)O)cc1OC 10.1021/acs.jmedchem.5b01781
9893800 107286 None 11 Human Binding pKi = 8.3 8.3 -2 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 528 12 1 7 5.1 COc1ccc(CCOC(c2ccccc2)(c2ccccc2)[C@H](Oc2nc(C)cc(C)n2)C(=O)O)cc1OC 10.1021/jm9910425
CHEMBL316735 107286 None 11 Human Binding pKi = 8.3 8.3 -2 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 528 12 1 7 5.1 COc1ccc(CCOC(c2ccccc2)(c2ccccc2)[C@H](Oc2nc(C)cc(C)n2)C(=O)O)cc1OC 10.1021/jm9910425
10769887 107548 None 0 Human Binding pKi = 7.4 7.4 -1 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 600 15 1 8 6.0 CCc1ccc(C(OCCc2ccc(OC)c(OC)c2)(c2ccc(CC)cc2)C(Oc2nc(C)cc(OC)n2)C(=O)O)cc1 10.1021/jm9910425
CHEMBL318535 107548 None 0 Human Binding pKi = 7.4 7.4 -1 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 600 15 1 8 6.0 CCc1ccc(C(OCCc2ccc(OC)c(OC)c2)(c2ccc(CC)cc2)C(Oc2nc(C)cc(OC)n2)C(=O)O)cc1 10.1021/jm9910425
10528341 14583 None 0 Rat Binding pKi = 5.4 5.4 -95 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 458 9 2 6 4.4 Cc1noc(NS(=O)(=O)c2cccc(OCC(=O)O)c2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL1204523 14583 None 0 Rat Binding pKi = 5.4 5.4 -95 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 458 9 2 6 4.4 Cc1noc(NS(=O)(=O)c2cccc(OCC(=O)O)c2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL149152 14583 None 0 Rat Binding pKi = 5.4 5.4 -95 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 458 9 2 6 4.4 Cc1noc(NS(=O)(=O)c2cccc(OCC(=O)O)c2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
10972867 99757 None 0 Human Binding pKi = 5.4 5.4 -19952 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 480 7 1 7 4.4 CC(=O)N(C)Cc1cc(-c2ncco2)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm020289q
CHEMBL284656 99757 None 0 Human Binding pKi = 5.4 5.4 -19952 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 480 7 1 7 4.4 CC(=O)N(C)Cc1cc(-c2ncco2)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm020289q
9852318 9616 None 8 Human Binding pKi = 7.4 7.4 -2691 2
Ability to inhibit [125I]-ET-1 binding to human cloned ETB receptors expressed on CHO cellsAbility to inhibit [125I]-ET-1 binding to human cloned ETB receptors expressed on CHO cells
ChEMBL 613 11 2 9 4.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm000538f
CHEMBL112624 9616 None 8 Human Binding pKi = 7.4 7.4 -2691 2
Ability to inhibit [125I]-ET-1 binding to human cloned ETB receptors expressed on CHO cellsAbility to inhibit [125I]-ET-1 binding to human cloned ETB receptors expressed on CHO cells
ChEMBL 613 11 2 9 4.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm000538f
CHEMBL1627022 9616 None 8 Human Binding pKi = 7.4 7.4 -2691 2
Ability to inhibit [125I]-ET-1 binding to human cloned ETB receptors expressed on CHO cellsAbility to inhibit [125I]-ET-1 binding to human cloned ETB receptors expressed on CHO cells
ChEMBL 613 11 2 9 4.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1 10.1021/jm000538f
10715881 121605 None 0 Rat Binding pKi = 5.4 5.4 -37 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 398 5 1 4 5.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL358545 121605 None 0 Rat Binding pKi = 5.4 5.4 -37 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 398 5 1 4 5.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)(C)C)cc2)c1C 10.1021/jm970872k
51003306 58080 None 0 Mouse Binding pKi = 6.4 6.4 - 1
Displacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting
ChEMBL 670 19 1 12 4.2 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCOCCOCCOCCF)c2)cc1 10.1021/jm101110w
CHEMBL1672880 58080 None 0 Mouse Binding pKi = 6.4 6.4 - 1
Displacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting
ChEMBL 670 19 1 12 4.2 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCOCCOCCOCCF)c2)cc1 10.1021/jm101110w
10718053 44127 None 0 Rat Binding pKi = 4.4 4.4 -5 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 442 8 1 6 4.8 CCOC(=O)c1c(C)noc1NS(=O)(=O)c1ccccc1-c1ccc(CC(C)C)cc1 10.1021/jm970872k
CHEMBL151525 44127 None 0 Rat Binding pKi = 4.4 4.4 -5 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 442 8 1 6 4.8 CCOC(=O)c1c(C)noc1NS(=O)(=O)c1ccccc1-c1ccc(CC(C)C)cc1 10.1021/jm970872k
11123603 101851 None 0 Human Binding pKi = 5.4 5.4 -14125 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 475 7 1 8 4.7 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2Cn2ccnc2)c1C 10.1021/jm020289q
CHEMBL30009 101851 None 0 Human Binding pKi = 5.4 5.4 -14125 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 475 7 1 8 4.7 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2Cn2ccnc2)c1C 10.1021/jm020289q
11754273 101027 None 0 Human Binding pKi = 5.4 5.4 -21877 2
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B receptor expressed in CHO Cells.
ChEMBL 466 7 2 7 4.1 CC(=O)NCc1cc(-c2ncco2)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm000105c
CHEMBL29422 101027 None 0 Human Binding pKi = 5.4 5.4 -21877 2
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B receptor expressed in CHO Cells.
ChEMBL 466 7 2 7 4.1 CC(=O)NCc1cc(-c2ncco2)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm000105c
11754273 101027 None 0 Human Binding pKi = 5.4 5.4 -21877 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 466 7 2 7 4.1 CC(=O)NCc1cc(-c2ncco2)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm020289q
CHEMBL29422 101027 None 0 Human Binding pKi = 5.4 5.4 -21877 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 466 7 2 7 4.1 CC(=O)NCc1cc(-c2ncco2)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm020289q
11795351 42863 None 0 Rat Binding pKi = 4.4 4.4 -109 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 401 6 1 4 4.8 CC(C)Cc1ccc(-c2ccccc2S(=O)(=O)Nc2ccc(Cl)nn2)cc1 10.1021/jm970872k
CHEMBL150273 42863 None 0 Rat Binding pKi = 4.4 4.4 -109 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 401 6 1 4 4.8 CC(C)Cc1ccc(-c2ccccc2S(=O)(=O)Nc2ccc(Cl)nn2)cc1 10.1021/jm970872k
11103112 99922 None 0 Human Binding pKi = 5.3 5.3 -4570 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 501 8 1 7 6.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2COc2ccccc2)c1C 10.1021/jm020289q
CHEMBL28586 99922 None 0 Human Binding pKi = 5.3 5.3 -4570 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 501 8 1 7 6.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2COc2ccccc2)c1C 10.1021/jm020289q
44274885 94139 None 0 Human Binding pKi = 5.3 5.3 -29 2
Binding affinity against human Endothelin B receptor showed weak activityBinding affinity against human Endothelin B receptor showed weak activity
ChEMBL 454 10 1 7 4.5 COc1cc(OC)nc(CC(C(=O)O)C(C)(Oc2ccc(SC)cc2)c2ccccc2)n1 10.1021/jm030480f
CHEMBL24906 94139 None 0 Human Binding pKi = 5.3 5.3 -29 2
Binding affinity against human Endothelin B receptor showed weak activityBinding affinity against human Endothelin B receptor showed weak activity
ChEMBL 454 10 1 7 4.5 COc1cc(OC)nc(CC(C(=O)O)C(C)(Oc2ccc(SC)cc2)c2ccccc2)n1 10.1021/jm030480f
44307287 206216 None 0 Human Binding pKi = 5.3 5.3 -29 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from CHO cellsBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from CHO cells
ChEMBL 470 10 0 9 4.1 COC(=O)C(Oc1nc(OC)cc(OC)n1)C(C)(Oc1ccc(SC)cc1)c1ccccc1 10.1021/jm960274q
CHEMBL67957 206216 None 0 Human Binding pKi = 5.3 5.3 -29 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from CHO cellsBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from CHO cells
ChEMBL 470 10 0 9 4.1 COC(=O)C(Oc1nc(OC)cc(OC)n1)C(C)(Oc1ccc(SC)cc1)c1ccccc1 10.1021/jm960274q
11059912 99394 None 0 Human Binding pKi = 5.3 5.3 -23988 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 481 9 1 7 5.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2COCC(C)C)c1C 10.1021/jm020289q
CHEMBL282303 99394 None 0 Human Binding pKi = 5.3 5.3 -23988 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 481 9 1 7 5.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2COCC(C)C)c1C 10.1021/jm020289q
19085508 39597 None 0 Human Binding pKi = 4.3 4.3 -218 2
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B receptor.
ChEMBL 466 7 1 8 4.2 COc1cc(OC)nc(-c2ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)cc2)n1 10.1016/s0960-894x(01)00791-0
CHEMBL147365 39597 None 0 Human Binding pKi = 4.3 4.3 -218 2
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B receptor.
ChEMBL 466 7 1 8 4.2 COc1cc(OC)nc(-c2ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)cc2)n1 10.1016/s0960-894x(01)00791-0
10453858 160196 None 0 Human Binding pKi = 6.3 6.3 -31 2
Inhibition of [125I]ET1 binding to cloned human ET-B receptorInhibition of [125I]ET1 binding to cloned human ET-B receptor
ChEMBL 404 4 2 5 4.1 COc1ccc([C@@H]2c3cc(O)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1021/jm00037a003
CHEMBL41087 160196 None 0 Human Binding pKi = 6.3 6.3 -31 2
Inhibition of [125I]ET1 binding to cloned human ET-B receptorInhibition of [125I]ET1 binding to cloned human ET-B receptor
ChEMBL 404 4 2 5 4.1 COc1ccc([C@@H]2c3cc(O)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1 10.1021/jm00037a003
9955561 102908 None 0 Pig Binding pKi = 8.3 8.3 - 1
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 453 8 2 2 4.8 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccccc2)C(=O)NCCc2c[nH]c3ccccc23)c1 10.1016/0960-894X(96)00421-0
CHEMBL305615 102908 None 0 Pig Binding pKi = 8.3 8.3 - 1
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 453 8 2 2 4.8 Cc1cc(C)cc(C(=O)N(C)[C@H](Cc2ccccc2)C(=O)NCCc2c[nH]c3ccccc23)c1 10.1016/0960-894X(96)00421-0
44314882 157268 None 0 Pig Binding pKi = 8.3 8.3 380 2
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 1562 47 19 18 0.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(96)00421-0
77282212 157268 None 0 Pig Binding pKi = 8.3 8.3 380 2
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 1562 47 19 18 0.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(96)00421-0
CHEMBL407559 157268 None 0 Pig Binding pKi = 8.3 8.3 380 2
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 1562 47 19 18 0.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(96)00421-0
9894460 209167 None 11 Human Binding pKi = 8.3 8.3 -41 3
Inhibitory activity against human Endothelin B receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin B receptor in chinese hamster ovary cells
ChEMBL 539 10 2 7 4.8 CCCc1cc(C(=O)O)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2 10.1021/jm9505369
CHEMBL313871 209167 None 11 Human Binding pKi = 8.3 8.3 -41 3
Inhibitory activity against human Endothelin B receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin B receptor in chinese hamster ovary cells
ChEMBL 539 10 2 7 4.8 CCCc1cc(C(=O)O)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2 10.1021/jm9505369
CHEMBL8978 209167 None 11 Human Binding pKi = 8.3 8.3 -41 3
Inhibitory activity against human Endothelin B receptor in chinese hamster ovary cellsInhibitory activity against human Endothelin B receptor in chinese hamster ovary cells
ChEMBL 539 10 2 7 4.8 CCCc1cc(C(=O)O)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2 10.1021/jm9505369
44314883 155851 None 0 Pig Binding pKi = 8.2 8.2 - 1
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 1520 45 19 18 -0.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(96)00421-0
77282211 155851 None 0 Pig Binding pKi = 8.2 8.2 - 1
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 1520 45 19 18 -0.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(96)00421-0
CHEMBL405796 155851 None 0 Pig Binding pKi = 8.2 8.2 - 1
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 1520 45 19 18 -0.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1016/0960-894X(96)00421-0
10526510 121132 None 0 Rat Binding pKi = 4.3 4.3 -12 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 427 8 1 6 4.2 COc1cc(OC)nc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2)n1 10.1021/jm970872k
CHEMBL356972 121132 None 0 Rat Binding pKi = 4.3 4.3 -12 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 427 8 1 6 4.2 COc1cc(OC)nc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2)n1 10.1021/jm970872k
44314819 155847 None 0 Pig Binding pKi = 5.3 5.3 - 1
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 1520 45 19 18 -0.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(96)00421-0
77282207 155847 None 0 Pig Binding pKi = 5.3 5.3 - 1
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 1520 45 19 18 -0.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(96)00421-0
CHEMBL405753 155847 None 0 Pig Binding pKi = 5.3 5.3 - 1
Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluatedAbility to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated
ChEMBL 1520 45 19 18 -0.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)CCC(=O)O)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1016/0960-894X(96)00421-0
22103743 42850 None 0 Human Binding pKi = 4.3 4.3 -9332 2
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B receptor.
ChEMBL 411 5 1 6 4.9 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3nccs3)cc2)c1C 10.1016/s0960-894x(01)00791-0
CHEMBL150260 42850 None 0 Human Binding pKi = 4.3 4.3 -9332 2
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B receptor.
ChEMBL 411 5 1 6 4.9 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3nccs3)cc2)c1C 10.1016/s0960-894x(01)00791-0
51003352 58082 None 0 Mouse Binding pKi = 5.3 5.3 - 1
Displacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting
ChEMBL 1020 35 1 21 4.7 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCOCCOCCOCCOCc3cn(CCOCCOCCOCCOc4cccnc4F)nn3)c2)cc1 10.1021/jm101110w
CHEMBL1672882 58082 None 0 Mouse Binding pKi = 5.3 5.3 - 1
Displacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting
ChEMBL 1020 35 1 21 4.7 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCOCCOCCOCCOCc3cn(CCOCCOCCOCCOc4cccnc4F)nn3)c2)cc1 10.1021/jm101110w
10647471 42339 None 0 Rat Binding pKi = 5.3 5.3 -125 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 456 7 3 5 4.7 CNC(=O)Nc1cc(CC(C)C)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm970872k
CHEMBL149818 42339 None 0 Rat Binding pKi = 5.3 5.3 -125 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 456 7 3 5 4.7 CNC(=O)Nc1cc(CC(C)C)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm970872k
10597897 41188 None 0 Rat Binding pKi = 4.3 4.3 -724 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 414 7 1 5 5.0 COc1cc(CC(C)C)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm970872k
CHEMBL148853 41188 None 0 Rat Binding pKi = 4.3 4.3 -724 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 414 7 1 5 5.0 COc1cc(CC(C)C)ccc1-c1ccccc1S(=O)(=O)Nc1onc(C)c1C 10.1021/jm970872k
10624645 4334 None 0 Human Binding pKi = 7.3 7.3 -1 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 482 10 1 5 5.4 Cc1ccc(CCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1 10.1021/jm9910425
CHEMBL100954 4334 None 0 Human Binding pKi = 7.3 7.3 -1 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 482 10 1 5 5.4 Cc1ccc(CCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1 10.1021/jm9910425
10929533 100409 None 0 Human Binding pKi = 6.3 6.3 -10964 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 534 9 1 7 5.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C(=O)C(C)C)C2CC2)c1C 10.1021/jm020289q
CHEMBL28963 100409 None 0 Human Binding pKi = 6.3 6.3 -10964 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 534 9 1 7 5.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C(=O)C(C)C)C2CC2)c1C 10.1021/jm020289q
10432263 102207 None 0 Human Binding pKi = 7.3 7.3 -85 2
Binding affinity towards Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 420 8 1 6 3.4 COc1nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)nc2c1CCC2 10.1021/jm960274q
CHEMBL302564 102207 None 0 Human Binding pKi = 7.3 7.3 -85 2
Binding affinity towards Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 420 8 1 6 3.4 COc1nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)nc2c1CCC2 10.1021/jm960274q
10643748 121501 None 0 Rat Binding pKi = 5.3 5.3 -29 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 384 6 1 4 5.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2cccc(CC(C)C)c2)c1C 10.1021/jm970872k
CHEMBL358226 121501 None 0 Rat Binding pKi = 5.3 5.3 -29 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 384 6 1 4 5.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2cccc(CC(C)C)c2)c1C 10.1021/jm970872k
9979632 102956 None 0 Human Binding pKi = 7.2 7.2 -41 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 422 8 1 7 2.8 COc1nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)nc2c1CCO2 10.1021/jm960274q
CHEMBL305980 102956 None 0 Human Binding pKi = 7.2 7.2 -41 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 422 8 1 7 2.8 COc1nc(OC(C(=O)O)C(OC)(c2ccccc2)c2ccccc2)nc2c1CCO2 10.1021/jm960274q
10501299 119918 None 0 Rat Binding pKi = 5.2 5.2 -147 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 402 6 1 5 5.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(SC(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL348685 119918 None 0 Rat Binding pKi = 5.2 5.2 -147 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 402 6 1 5 5.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(SC(C)C)cc2)c1C 10.1021/jm970872k
11813553 99400 None 0 Human Binding pKi = 6.2 6.2 -14454 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 542 8 1 7 5.7 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)c2ccccc2)c1C 10.1021/jm020289q
CHEMBL282359 99400 None 0 Human Binding pKi = 6.2 6.2 -14454 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 542 8 1 7 5.7 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)c2ccccc2)c1C 10.1021/jm020289q
10815239 108614 None 0 Human Binding pKi = 7.2 7.2 -125 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 500 10 1 7 5.0 COc1ccc(OC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1OC 10.1021/jm9910425
CHEMBL320224 108614 None 0 Human Binding pKi = 7.2 7.2 -125 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 500 10 1 7 5.0 COc1ccc(OC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1OC 10.1021/jm9910425
10690608 121123 None 0 Rat Binding pKi = 5.2 5.2 -112 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 371 5 1 5 3.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(N(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL356901 121123 None 0 Rat Binding pKi = 5.2 5.2 -112 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 371 5 1 5 3.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(N(C)C)cc2)c1C 10.1021/jm970872k
19934534 106751 None 0 Rat Binding pKi = 5.2 5.2 5 2
Affinity against ET B receptorAffinity against ET B receptor
ChEMBL 468 6 3 4 5.0 CCCN1c2ccccc2C(=O)N(CC(=O)O)c2cc(NC(=O)c3cc4ccccc4[nH]3)ccc21 10.1016/0960-894X(95)00019-P
CHEMBL314364 106751 None 0 Rat Binding pKi = 5.2 5.2 5 2
Affinity against ET B receptorAffinity against ET B receptor
ChEMBL 468 6 3 4 5.0 CCCN1c2ccccc2C(=O)N(CC(=O)O)c2cc(NC(=O)c3cc4ccccc4[nH]3)ccc21 10.1016/0960-894X(95)00019-P
10837085 102364 None 0 Human Binding pKi = 5.2 5.2 -39 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 446 9 1 7 3.2 COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2ccccc2F)c2ccccc2F)n1 10.1021/jm960274q
CHEMBL303501 102364 None 0 Human Binding pKi = 5.2 5.2 -39 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 446 9 1 7 3.2 COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2ccccc2F)c2ccccc2F)n1 10.1021/jm960274q
19934546 208672 None 0 Rat Binding pKi = 4.2 4.2 -8 2
Affinity against ET B receptorAffinity against ET B receptor
ChEMBL 466 7 1 4 6.0 CCCN1c2ccccc2C(=O)N(CC(=O)O)c2cc(OCc3cccc4ccccc34)ccc21 10.1016/0960-894X(95)00019-P
CHEMBL86581 208672 None 0 Rat Binding pKi = 4.2 4.2 -8 2
Affinity against ET B receptorAffinity against ET B receptor
ChEMBL 466 7 1 4 6.0 CCCN1c2ccccc2C(=O)N(CC(=O)O)c2cc(OCc3cccc4ccccc34)ccc21 10.1016/0960-894X(95)00019-P
10693130 122035 None 0 Rat Binding pKi = 5.2 5.2 -16 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 414 7 1 5 5.0 COc1ccc(S(=O)(=O)Nc2onc(C)c2C)c(-c2ccc(CC(C)C)cc2)c1 10.1021/jm970872k
CHEMBL359152 122035 None 0 Rat Binding pKi = 5.2 5.2 -16 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 414 7 1 5 5.0 COc1ccc(S(=O)(=O)Nc2onc(C)c2C)c(-c2ccc(CC(C)C)cc2)c1 10.1021/jm970872k
11799973 4433 None 0 Human Binding pKi = 7.2 7.2 -31 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 514 11 1 7 5.1 COc1ccc(COC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1OC 10.1021/jm9910425
CHEMBL101587 4433 None 0 Human Binding pKi = 7.2 7.2 -31 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 514 11 1 7 5.1 COc1ccc(COC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1OC 10.1021/jm9910425
18660521 41711 None 0 Human Binding pKi = 5.2 5.2 -2754 2
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B receptor.
ChEMBL 405 5 1 5 4.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ccccn3)cc2)c1C 10.1016/s0960-894x(01)00791-0
CHEMBL149232 41711 None 0 Human Binding pKi = 5.2 5.2 -2754 2
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B receptor.
ChEMBL 405 5 1 5 4.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ccccn3)cc2)c1C 10.1016/s0960-894x(01)00791-0
11731054 98865 None 0 Human Binding pKi = 6.2 6.2 -21379 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 522 7 1 7 5.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)C(C)(C)C)c1C 10.1021/jm020289q
CHEMBL27855 98865 None 0 Human Binding pKi = 6.2 6.2 -21379 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 522 7 1 7 5.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)C(C)(C)C)c1C 10.1021/jm020289q
51002602 58086 None 0 Mouse Binding pKi = 5.2 5.2 - 1
Displacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting
ChEMBL 751 21 1 15 4.0 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCOCCOCCOCCn3cc(CF)nn3)c2)cc1 10.1021/jm101110w
CHEMBL1672886 58086 None 0 Mouse Binding pKi = 5.2 5.2 - 1
Displacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting
ChEMBL 751 21 1 15 4.0 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCOCCOCCOCCn3cc(CF)nn3)c2)cc1 10.1021/jm101110w
9864017 41341 None 0 Human Binding pKi = 4.2 4.2 -194 2
Ability to inhibit ET-1 induced contractions in rabbit carotid artery rings (Endothelin B receptor) was determined in an in vitro functional assay.Ability to inhibit ET-1 induced contractions in rabbit carotid artery rings (Endothelin B receptor) was determined in an in vitro functional assay.
ChEMBL 367 4 2 4 4.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2cc3ccccc3[nH]2)c1C 10.1021/jm970872k
CHEMBL148967 41341 None 0 Human Binding pKi = 4.2 4.2 -194 2
Ability to inhibit ET-1 induced contractions in rabbit carotid artery rings (Endothelin B receptor) was determined in an in vitro functional assay.Ability to inhibit ET-1 induced contractions in rabbit carotid artery rings (Endothelin B receptor) was determined in an in vitro functional assay.
ChEMBL 367 4 2 4 4.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2cc3ccccc3[nH]2)c1C 10.1021/jm970872k
10741144 119833 None 0 Rat Binding pKi = 5.2 5.2 -407 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 427 8 2 5 4.5 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2NC=O)c1C 10.1021/jm970872k
CHEMBL347982 119833 None 0 Rat Binding pKi = 5.2 5.2 -407 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 427 8 2 5 4.5 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2NC=O)c1C 10.1021/jm970872k
6433100 4551 None 6 Human Binding pKi = 8.2 8.2 -2 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 528 12 1 7 5.1 COc1ccc(CCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1OC 10.1021/jm9910425
CHEMBL102405 4551 None 6 Human Binding pKi = 8.2 8.2 -2 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 528 12 1 7 5.1 COc1ccc(CCOC(c2ccccc2)(c2ccccc2)C(Oc2nc(C)cc(C)n2)C(=O)O)cc1OC 10.1021/jm9910425
443289 711 None 39 Rat Binding pKi = 5.2 5.2 -831 3
Affinity against ET B receptorAffinity against ET B receptor
ChEMBL None None None None 10.1016/0960-894X(95)00019-P
997 711 None 39 Rat Binding pKi = 5.2 5.2 -831 3
Affinity against ET B receptorAffinity against ET B receptor
ChEMBL None None None None 10.1016/0960-894X(95)00019-P
CHEMBL314691 711 None 39 Rat Binding pKi = 5.2 5.2 -831 3
Affinity against ET B receptorAffinity against ET B receptor
ChEMBL None None None None 10.1016/0960-894X(95)00019-P
DB12054 711 None 39 Rat Binding pKi = 5.2 5.2 -831 3
Affinity against ET B receptorAffinity against ET B receptor
ChEMBL None None None None 10.1016/0960-894X(95)00019-P
19934544 208658 None 0 Rat Binding pKi = 5.2 5.2 2 2
Affinity against ET B receptorAffinity against ET B receptor
ChEMBL 482 7 3 4 4.9 CCCN1c2ccccc2C(=O)N(CC(=O)O)c2cc(NC(=O)Cc3c[nH]c4ccccc34)ccc21 10.1016/0960-894X(95)00019-P
CHEMBL86489 208658 None 0 Rat Binding pKi = 5.2 5.2 2 2
Affinity against ET B receptorAffinity against ET B receptor
ChEMBL 482 7 3 4 4.9 CCCN1c2ccccc2C(=O)N(CC(=O)O)c2cc(NC(=O)Cc3c[nH]c4ccccc34)ccc21 10.1016/0960-894X(95)00019-P
44333366 107482 None 0 Human Binding pKi = 7.2 7.2 1 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 570 12 1 8 5.2 COc1ccc(CCOC(c2ccc(C)cc2)(c2ccc(C)cc2)C(Oc2nc3c(c(OC)n2)COC3)C(=O)O)cc1 10.1021/jm9910425
CHEMBL318146 107482 None 0 Human Binding pKi = 7.2 7.2 1 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 570 12 1 8 5.2 COc1ccc(CCOC(c2ccc(C)cc2)(c2ccc(C)cc2)C(Oc2nc3c(c(OC)n2)COC3)C(=O)O)cc1 10.1021/jm9910425
46228116 203679 None 0 Mouse Binding pKi = 7.1 7.1 - 1
Displacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomesDisplacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomes
ChEMBL 598 10 1 9 4.6 COc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OCCBr)cc2)cc(OC)c1OC 10.1016/j.bmc.2009.08.058
CHEMBL603635 203679 None 0 Mouse Binding pKi = 7.1 7.1 - 1
Displacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomesDisplacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomes
ChEMBL 598 10 1 9 4.6 COc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OCCBr)cc2)cc(OC)c1OC 10.1016/j.bmc.2009.08.058
11733544 99289 None 0 Human Binding pKi = 5.1 5.1 -7244 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 480 7 1 7 4.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CC(=O)N(C)C)c1C 10.1021/jm020289q
CHEMBL281668 99289 None 0 Human Binding pKi = 5.1 5.1 -7244 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 480 7 1 7 4.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CC(=O)N(C)C)c1C 10.1021/jm020289q
10503999 41327 None 0 Rat Binding pKi = 5.1 5.1 -6 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 456 8 3 6 3.9 Cc1noc(NS(=O)(=O)c2ccc(NC(=O)CN)cc2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL148953 41327 None 0 Rat Binding pKi = 5.1 5.1 -6 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 456 8 3 6 3.9 Cc1noc(NS(=O)(=O)c2ccc(NC(=O)CN)cc2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
22103385 121149 None 0 Human Binding pKi = 4.1 4.1 -19054 2
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B receptor.
ChEMBL 396 5 1 7 3.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3nnco3)cc2)c1C 10.1016/s0960-894x(01)00791-0
CHEMBL357077 121149 None 0 Human Binding pKi = 4.1 4.1 -19054 2
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B receptor.
ChEMBL 396 5 1 7 3.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3nnco3)cc2)c1C 10.1016/s0960-894x(01)00791-0
10045790 141739 None 0 Human Binding pKi = 6.1 6.1 -17 2
Inhibition of [125I]ET1 binding to cloned human ET-B receptorInhibition of [125I]ET1 binding to cloned human ET-B receptor
ChEMBL 388 4 1 4 4.4 COc1ccc([C@H]2c3ccccc3[C@@H](c3ccc4c(c3)OCO4)[C@@H]2C(=O)O)cc1 10.1021/jm00037a003
CHEMBL38537 141739 None 0 Human Binding pKi = 6.1 6.1 -17 2
Inhibition of [125I]ET1 binding to cloned human ET-B receptorInhibition of [125I]ET1 binding to cloned human ET-B receptor
ChEMBL 388 4 1 4 4.4 COc1ccc([C@H]2c3ccccc3[C@@H](c3ccc4c(c3)OCO4)[C@@H]2C(=O)O)cc1 10.1021/jm00037a003
9958321 79182 None 0 Human Binding pKi = 6.1 6.1 -19498 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 520 7 1 7 5.2 Cc1onc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN2CCC(C)(C)C2=O)c1C 10.1021/jm020289q
CHEMBL2113316 79182 None 0 Human Binding pKi = 6.1 6.1 -19498 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 520 7 1 7 5.2 Cc1onc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN2CCC(C)(C)C2=O)c1C 10.1021/jm020289q
10548722 5482 None 0 Human Binding pKi = 4.1 4.1 -20892 2
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B receptor expressed in CHO Cells.
ChEMBL 395 5 1 6 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3cnco3)cc2)c1C 10.1021/jm000105c
CHEMBL107574 5482 None 0 Human Binding pKi = 4.1 4.1 -20892 2
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B receptor expressed in CHO Cells.
ChEMBL 395 5 1 6 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3cnco3)cc2)c1C 10.1021/jm000105c
11027595 100295 None 0 Human Binding pKi = 6.1 6.1 -19952 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 508 8 1 7 5.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)C(C)C)c1C 10.1021/jm020289q
CHEMBL28863 100295 None 0 Human Binding pKi = 6.1 6.1 -19952 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 508 8 1 7 5.0 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)C(C)C)c1C 10.1021/jm020289q
1009 194 None 25 Human Binding pKi = 8.1 8.1 676 2
125I-labelled ET-1 saturation binding studies with EDNRB125I-labelled ET-1 saturation binding studies with EDNRB
ChEMBL 558 11 2 6 5.8 CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2 10.6019/CHEMBL4507261
5310991 194 None 25 Human Binding pKi = 8.1 8.1 676 2
125I-labelled ET-1 saturation binding studies with EDNRB125I-labelled ET-1 saturation binding studies with EDNRB
ChEMBL 558 11 2 6 5.8 CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2 10.6019/CHEMBL4507261
CHEMBL332794 194 None 25 Human Binding pKi = 8.1 8.1 676 2
125I-labelled ET-1 saturation binding studies with EDNRB125I-labelled ET-1 saturation binding studies with EDNRB
ChEMBL 558 11 2 6 5.8 CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2 10.6019/CHEMBL4507261
104865 706 None 60 Human Binding pKi = 7.1 7.1 -6 4
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm020289q
104865.0 706 None 60 Human Binding pKi = 7.1 7.1 -6 4
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm020289q
3494 706 None 60 Human Binding pKi = 7.1 7.1 -6 4
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm020289q
392 706 None 60 Human Binding pKi = 7.1 7.1 -6 4
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm020289q
CHEMBL957 706 None 60 Human Binding pKi = 7.1 7.1 -6 4
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm020289q
DB00559 706 None 60 Human Binding pKi = 7.1 7.1 -6 4
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 10.1021/jm020289q
15297287 164507 None 0 Rat Binding pKi = 5.1 5.1 3 2
Affinity against ET B receptorAffinity against ET B receptor
ChEMBL 424 5 2 4 5.2 O=C(O)CN1C(=O)c2ccccc2Nc2ccc(OCc3cccc4ccccc34)cc21 10.1016/0960-894X(95)00019-P
CHEMBL421349 164507 None 0 Rat Binding pKi = 5.1 5.1 3 2
Affinity against ET B receptorAffinity against ET B receptor
ChEMBL 424 5 2 4 5.2 O=C(O)CN1C(=O)c2ccccc2Nc2ccc(OCc3cccc4ccccc34)cc21 10.1016/0960-894X(95)00019-P
44277840 98307 None 0 Human Binding pKi = 6.1 6.1 -81283 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 522 7 1 7 5.8 Cc1onc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2N(C)C(=O)CC(C)(C)C)c1C 10.1021/jm020289q
CHEMBL274489 98307 None 0 Human Binding pKi = 6.1 6.1 -81283 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 522 7 1 7 5.8 Cc1onc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2N(C)C(=O)CC(C)(C)C)c1C 10.1021/jm020289q
10836583 39705 None 0 Rat Binding pKi = 5.1 5.1 -43 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 434 7 1 5 5.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(OCc3ccccc3)cc2)c1C 10.1021/jm970872k
CHEMBL147521 39705 None 0 Rat Binding pKi = 5.1 5.1 -43 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 434 7 1 5 5.3 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(OCc3ccccc3)cc2)c1C 10.1021/jm970872k
51003307 58081 None 0 Mouse Binding pKi = 5.1 5.1 - 1
Displacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting
ChEMBL 751 21 1 15 4.0 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCc3cn(CCOCCOCCOCCF)nn3)c2)cc1 10.1021/jm101110w
CHEMBL1672881 58081 None 0 Mouse Binding pKi = 5.1 5.1 - 1
Displacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting
ChEMBL 751 21 1 15 4.0 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCc3cn(CCOCCOCCOCCF)nn3)c2)cc1 10.1021/jm101110w
11071765 169310 None 0 Human Binding pKi = 7.1 7.1 -8709 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 556 9 1 7 5.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)Cc2ccccc2)c1C 10.1021/jm020289q
CHEMBL440780 169310 None 0 Human Binding pKi = 7.1 7.1 -8709 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 556 9 1 7 5.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN(C)C(=O)Cc2ccccc2)c1C 10.1021/jm020289q
51002601 58085 None 0 Mouse Binding pKi = 6.1 6.1 - 1
Displacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting
ChEMBL 906 24 2 17 4.2 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCOCCOCCOCCn3cc(CNS(=O)(=O)c4ccc(F)cc4)nn3)c2)cc1 10.1021/jm101110w
CHEMBL1672885 58085 None 0 Mouse Binding pKi = 6.1 6.1 - 1
Displacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma countingDisplacement of [125I]ET1 from ETB receptor in CD1 Nu/Nu mouse myocardial ventricles membranes after 2 hrs by gamma counting
ChEMBL 906 24 2 17 4.2 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCOCCOCCOCCn3cc(CNS(=O)(=O)c4ccc(F)cc4)nn3)c2)cc1 10.1021/jm101110w
9934204 107001 None 0 Rat Binding pKi = 5.1 5.1 1 2
Affinity against ET B receptorAffinity against ET B receptor
ChEMBL 465 7 2 4 6.0 CCCN1c2ccccc2C(=O)N(CC(=O)O)c2cc(NCc3cccc4ccccc34)ccc21 10.1016/0960-894X(95)00019-P
CHEMBL314915 107001 None 0 Rat Binding pKi = 5.1 5.1 1 2
Affinity against ET B receptorAffinity against ET B receptor
ChEMBL 465 7 2 4 6.0 CCCN1c2ccccc2C(=O)N(CC(=O)O)c2cc(NCc3cccc4ccccc34)ccc21 10.1016/0960-894X(95)00019-P
11049336 99994 None 0 Human Binding pKi = 5.0 5.0 -3630 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 497 7 1 6 6.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2/C=C/c2ccccc2)c1C 10.1021/jm020289q
CHEMBL286279 99994 None 0 Human Binding pKi = 5.0 5.0 -3630 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 497 7 1 6 6.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2/C=C/c2ccccc2)c1C 10.1021/jm020289q
10673091 163420 None 0 Human Binding pKi = 7.0 7.0 -4 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 502 10 1 5 5.8 Cc1cc(C)nc(OC(C(=O)O)C(OCCc2ccc(Cl)cc2)(c2ccccc2)c2ccccc2)n1 10.1021/jm9910425
CHEMBL418992 163420 None 0 Human Binding pKi = 7.0 7.0 -4 2
Inhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cellsInhibition of [125I]ET-3 (ETB assay) binding to human cloned Endothelin B receptor in CHO cells
ChEMBL 502 10 1 5 5.8 Cc1cc(C)nc(OC(C(=O)O)C(OCCc2ccc(Cl)cc2)(c2ccccc2)c2ccccc2)n1 10.1021/jm9910425
10621010 164957 None 0 Rat Binding pKi = 6.0 6.0 -186 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 400 6 2 5 4.7 Cc1noc(NS(=O)(=O)c2cccc(O)c2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
CHEMBL421955 164957 None 0 Rat Binding pKi = 6.0 6.0 -186 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 400 6 2 5 4.7 Cc1noc(NS(=O)(=O)c2cccc(O)c2-c2ccc(CC(C)C)cc2)c1C 10.1021/jm970872k
22103787 41005 None 0 Human Binding pKi = 5.0 5.0 -1380 2
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B receptor.
ChEMBL 394 5 1 6 3.9 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-n3cccn3)cc2)c1C 10.1016/s0960-894x(01)00791-0
CHEMBL148719 41005 None 0 Human Binding pKi = 5.0 5.0 -1380 2
Binding affinity to CHO cells stably expressing human Endothelin B receptor.Binding affinity to CHO cells stably expressing human Endothelin B receptor.
ChEMBL 394 5 1 6 3.9 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-n3cccn3)cc2)c1C 10.1016/s0960-894x(01)00791-0
10811477 4820 None 0 Human Binding pKi = 4.0 4.0 -19952 2
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B receptor expressed in CHO Cells.
ChEMBL 409 5 1 6 4.7 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncoc3C)cc2)c1C 10.1021/jm000105c
CHEMBL104172 4820 None 0 Human Binding pKi = 4.0 4.0 -19952 2
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B receptor expressed in CHO Cells.
ChEMBL 409 5 1 6 4.7 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncoc3C)cc2)c1C 10.1021/jm000105c
10813228 107716 None 0 Human Binding pKi = 4.0 4.0 -46 2
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B receptor expressed in CHO Cells.
ChEMBL 445 5 1 6 5.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3nc4ccccc4o3)cc2)c1C 10.1021/jm000105c
CHEMBL319036 107716 None 0 Human Binding pKi = 4.0 4.0 -46 2
Inhibition of Human Endothelin B receptor expressed in CHO Cells.Inhibition of Human Endothelin B receptor expressed in CHO Cells.
ChEMBL 445 5 1 6 5.6 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3nc4ccccc4o3)cc2)c1C 10.1021/jm000105c
10918368 102578 None 0 Human Binding pKi = 6.0 6.0 -21379 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 520 7 1 7 5.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN2CC(C)(C)CC2=O)c1C 10.1021/jm020289q
CHEMBL30405 102578 None 0 Human Binding pKi = 6.0 6.0 -21379 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 520 7 1 7 5.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CN2CC(C)(C)CC2=O)c1C 10.1021/jm020289q
46228118 204999 None 0 Mouse Binding pKi = 7.0 7.0 - 1
Displacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomesDisplacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomes
ChEMBL 690 13 1 12 4.7 COc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OCCOc3ccc(S(C)(=O)=O)cc3)cc2)cc(OC)c1OC 10.1016/j.bmc.2009.08.058
CHEMBL611626 204999 None 0 Mouse Binding pKi = 7.0 7.0 - 1
Displacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomesDisplacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomes
ChEMBL 690 13 1 12 4.7 COc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OCCOc3ccc(S(C)(=O)=O)cc3)cc2)cc(OC)c1OC 10.1016/j.bmc.2009.08.058
10573784 165432 None 0 Rat Binding pKi = 5.0 5.0 -95 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 413 7 2 5 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2CN)c1C 10.1021/jm970872k
CHEMBL423583 165432 None 0 Rat Binding pKi = 5.0 5.0 -95 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 413 7 2 5 4.4 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2CN)c1C 10.1021/jm970872k
10671031 102749 None 0 Human Binding pKi = 6.0 6.0 -29 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 446 9 1 7 3.2 COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2ccc(F)cc2)c2ccc(F)cc2)n1 10.1021/jm960274q
CHEMBL304721 102749 None 0 Human Binding pKi = 6.0 6.0 -29 2
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellumBinding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
ChEMBL 446 9 1 7 3.2 COc1cc(OC)nc(OC(C(=O)O)C(OC)(c2ccc(F)cc2)c2ccc(F)cc2)n1 10.1021/jm960274q
45257115 203789 None 0 Mouse Binding pKi = 7.0 7.0 - 1
Displacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomesDisplacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomes
ChEMBL 538 10 1 9 4.2 COc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OCCF)cc2)cc(OC)c1OC 10.1016/j.bmc.2009.08.058
CHEMBL604286 203789 None 0 Mouse Binding pKi = 7.0 7.0 - 1
Displacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomesDisplacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomes
ChEMBL 538 10 1 9 4.2 COc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OCCF)cc2)cc(OC)c1OC 10.1016/j.bmc.2009.08.058
10973161 101098 None 0 Human Binding pKi = 6.0 6.0 -6456 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 502 8 2 9 4.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CNc2ccncn2)c1C 10.1021/jm020289q
CHEMBL29464 101098 None 0 Human Binding pKi = 6.0 6.0 -6456 2
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL 502 8 2 9 4.8 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(-c3ncco3)cc2CNc2ccncn2)c1C 10.1021/jm020289q
10741830 42857 None 0 Rat Binding pKi = 5.0 5.0 -3 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 441 7 2 5 4.9 CC(=O)Nc1ccc(S(=O)(=O)Nc2onc(C)c2C)c(-c2ccc(CC(C)C)cc2)c1 10.1021/jm970872k
CHEMBL150269 42857 None 0 Rat Binding pKi = 5.0 5.0 -3 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 441 7 2 5 4.9 CC(=O)Nc1ccc(S(=O)(=O)Nc2onc(C)c2C)c(-c2ccc(CC(C)C)cc2)c1 10.1021/jm970872k
10668703 165278 None 0 Rat Binding pKi = 5.0 5.0 -1230 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 400 6 2 5 4.7 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2O)c1C 10.1021/jm970872k
CHEMBL422851 165278 None 0 Rat Binding pKi = 5.0 5.0 -1230 2
Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor)
ChEMBL 400 6 2 5 4.7 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(CC(C)C)cc2O)c1C 10.1021/jm970872k
6662 14452 None 40 Human Binding pIC50 = 8.3 8.3 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
Drug Central 309 3 1 6 1.6 CC(=O)N(c1onc(C)c1C)S(=O)(=O)c1ccc(N)cc1 None
CHEMBL1200910 14452 None 40 Human Binding pIC50 = 8.3 8.3 - 0
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
Drug Central 309 3 1 6 1.6 CC(=O)N(c1onc(C)c1C)S(=O)(=O)c1ccc(N)cc1 None
5344 173577 None 67 Human Binding pIC50 = 8.3 8.3 - 1
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
Drug Central 267 3 2 5 1.7 Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C None
CHEMBL453 173577 None 67 Human Binding pIC50 = 8.3 8.3 - 1
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparationBinding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
Drug Central 267 3 2 5 1.7 Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C None
11477084 3610 None 36 Human Binding pIC50 = 8.3 8.3 - 2
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
Drug Central 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C None
216235 3610 None 36 Human Binding pIC50 = 8.3 8.3 - 2
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
Drug Central 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C None
3548 3610 None 36 Human Binding pIC50 = 8.3 8.3 - 2
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
Drug Central 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C None
3950 3610 None 36 Human Binding pIC50 = 8.3 8.3 - 2
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
Drug Central 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C None
CHEMBL282724 3610 None 36 Human Binding pIC50 = 8.3 8.3 - 2
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
Drug Central 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C None
DB06268 3610 None 36 Human Binding pIC50 = 8.3 8.3 - 2
In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay
Drug Central 454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C None
16004692 2454 None 59 Human Binding pIC50 = 8.2 8.2 - 1
IC50 value as determined in binding assays using membranes of Chinese hamster ovary (CHO) cells containing recombinant ETBIC50 value as determined in binding assays using membranes of Chinese hamster ovary (CHO) cells containing recombinant ETB
Drug Central 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br None
16004692.0 2454 None 59 Human Binding pIC50 = 8.2 8.2 - 1
IC50 value as determined in binding assays using membranes of Chinese hamster ovary (CHO) cells containing recombinant ETBIC50 value as determined in binding assays using membranes of Chinese hamster ovary (CHO) cells containing recombinant ETB
Drug Central 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br None
4809 2454 None 59 Human Binding pIC50 = 8.2 8.2 - 1
IC50 value as determined in binding assays using membranes of Chinese hamster ovary (CHO) cells containing recombinant ETBIC50 value as determined in binding assays using membranes of Chinese hamster ovary (CHO) cells containing recombinant ETB
Drug Central 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br None
7352 2454 None 59 Human Binding pIC50 = 8.2 8.2 - 1
IC50 value as determined in binding assays using membranes of Chinese hamster ovary (CHO) cells containing recombinant ETBIC50 value as determined in binding assays using membranes of Chinese hamster ovary (CHO) cells containing recombinant ETB
Drug Central 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br None
CHEMBL2103873 2454 None 59 Human Binding pIC50 = 8.2 8.2 - 1
IC50 value as determined in binding assays using membranes of Chinese hamster ovary (CHO) cells containing recombinant ETBIC50 value as determined in binding assays using membranes of Chinese hamster ovary (CHO) cells containing recombinant ETB
Drug Central 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br None
DB08932 2454 None 59 Human Binding pIC50 = 8.2 8.2 - 1
IC50 value as determined in binding assays using membranes of Chinese hamster ovary (CHO) cells containing recombinant ETBIC50 value as determined in binding assays using membranes of Chinese hamster ovary (CHO) cells containing recombinant ETB
Drug Central 586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br None
1007 3641 None 0 Human Binding pKd = 10 10.0 -3 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
16130933 3641 None 0 Human Binding pKd = 10 10.0 -3 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
16133819 3641 None 0 Human Binding pKd = 10 10.0 -3 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
3886 3641 None 0 Human Binding pKd = 10 10.0 -3 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
44210030 3641 None 0 Human Binding pKd = 10 10.0 -3 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
56947141 3641 None 0 Human Binding pKd = 10 10.0 -3 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
CHEMBL3188091 3641 None 0 Human Binding pKd = 10 10.0 -3 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
DB06138 3641 None 0 Human Binding pKd = 10 10.0 -3 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
3887 2072 None 35 Human Binding pKd = 7.2 7.2 -7 4
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
5311192 2072 None 35 Human Binding pKd = 7.2 7.2 -7 4
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
CHEMBL72410 2072 None 35 Human Binding pKd = 7.2 7.2 -7 4
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
1010 713 None 0 Human Binding pKd = 8.0 8.0 2 2
UnclassifiedUnclassified
Guide to Pharmacology 641 11 3 8 4.9 CCCC[C@@H](N(C(=O)[C@H](CC(C)(C)C)NC(=O)N1[C@H](C)CCC[C@@H]1C)C(=O)[C@@H](Cc1cn(c2c1cccc2)C(=O)OC)N)C(=O)O 8904635
3081333 713 None 0 Human Binding pKd = 8.0 8.0 2 2
UnclassifiedUnclassified
Guide to Pharmacology 641 11 3 8 4.9 CCCC[C@@H](N(C(=O)[C@H](CC(C)(C)C)NC(=O)N1[C@H](C)CCC[C@@H]1C)C(=O)[C@@H](Cc1cn(c2c1cccc2)C(=O)OC)N)C(=O)O 8904635
1009 194 None 25 Human Binding pKd = 8.1 8.1 676 2
UnclassifiedUnclassified
Guide to Pharmacology 558 11 2 6 5.8 CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2 10479298
5310991 194 None 25 Human Binding pKd = 8.1 8.1 676 2
UnclassifiedUnclassified
Guide to Pharmacology 558 11 2 6 5.8 CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2 10479298
CHEMBL332794 194 None 25 Human Binding pKd = 8.1 8.1 676 2
UnclassifiedUnclassified
Guide to Pharmacology 558 11 2 6 5.8 CCCOc1ccc(cc1)[C@@H]1N(CC(=O)Nc2c(CC)cccc2CC)C[C@@H]([C@H]1C(=O)O)c1ccc2c(c1)OCO2 10479298
3837 334 None 0 Human Binding pKd = 9.0 9.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1472961
1008 3473 None 0 Human Binding pKd = 9.3 9.3 -15 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8587419
1008 3473 None 0 Human Binding pKd = 9.3 9.3 -15 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
16132429 3473 None 0 Human Binding pKd = 9.3 9.3 -15 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8587419
16132429 3473 None 0 Human Binding pKd = 9.3 9.3 -15 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
CHEMBL1790178 3473 None 0 Human Binding pKd = 9.3 9.3 -15 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8587419
CHEMBL1790178 3473 None 0 Human Binding pKd = 9.3 9.3 -15 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
1007 3641 None 0 Rat Binding pKd = 10.0 10.0 3 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
16130933 3641 None 0 Rat Binding pKd = 10.0 10.0 3 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
16133819 3641 None 0 Rat Binding pKd = 10.0 10.0 3 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
3886 3641 None 0 Rat Binding pKd = 10.0 10.0 3 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
44210030 3641 None 0 Rat Binding pKd = 10.0 10.0 3 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
56947141 3641 None 0 Rat Binding pKd = 10.0 10.0 3 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
CHEMBL3188091 3641 None 0 Rat Binding pKd = 10.0 10.0 3 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
DB06138 3641 None 0 Rat Binding pKd = 10.0 10.0 3 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8301559
1004 1565 None 0 Rat Binding pKd None 10.3 10.3 -2 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1850245
1004 1565 None 0 Rat Binding pKd None 10.3 10.3 -2 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
16219334 1565 None 0 Rat Binding pKd None 10.3 10.3 -2 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1850245
16219334 1565 None 0 Rat Binding pKd None 10.3 10.3 -2 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
1008 3473 None 0 Rat Binding pKd None 10.5 10.5 15 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1850245
1008 3473 None 0 Rat Binding pKd None 10.5 10.5 15 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
16132429 3473 None 0 Rat Binding pKd None 10.5 10.5 15 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1850245
16132429 3473 None 0 Rat Binding pKd None 10.5 10.5 15 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
CHEMBL1790178 3473 None 0 Rat Binding pKd None 10.5 10.5 15 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1850245
CHEMBL1790178 3473 None 0 Rat Binding pKd None 10.5 10.5 15 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
1004 1565 None 0 Human Binding pKd None 10.7 10.7 2 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7524189
1004 1565 None 0 Human Binding pKd None 10.7 10.7 2 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8460684
1004 1565 None 0 Human Binding pKd None 10.7 10.7 2 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
16219334 1565 None 0 Human Binding pKd None 10.7 10.7 2 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7524189
16219334 1565 None 0 Human Binding pKd None 10.7 10.7 2 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8460684
16219334 1565 None 0 Human Binding pKd None 10.7 10.7 2 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8904635
1010 713 None 0 Rat Binding pKd None 7.5 7.5 -2 2
UnclassifiedUnclassified
Guide to Pharmacology 641 11 3 8 4.9 CCCC[C@@H](N(C(=O)[C@H](CC(C)(C)C)NC(=O)N1[C@H](C)CCC[C@@H]1C)C(=O)[C@@H](Cc1cn(c2c1cccc2)C(=O)OC)N)C(=O)O 8904635
3081333 713 None 0 Rat Binding pKd None 7.5 7.5 -2 2
UnclassifiedUnclassified
Guide to Pharmacology 641 11 3 8 4.9 CCCC[C@@H](N(C(=O)[C@H](CC(C)(C)C)NC(=O)N1[C@H](C)CCC[C@@H]1C)C(=O)[C@@H](Cc1cn(c2c1cccc2)C(=O)OC)N)C(=O)O 8904635
186002 102897 125I-ENDOTHELIN 18 Human Binding pKi = 10 10.0 -3 3
NoneNone
PDSP KiDatabase 531 10 2 6 5.4 CCCCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1C[C@H](C)C(=O)O)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 None
CHEMBL305576 102897 125I-ENDOTHELIN 18 Human Binding pKi = 10 10.0 -3 3
NoneNone
PDSP KiDatabase 531 10 2 6 5.4 CCCCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1C[C@H](C)C(=O)O)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2 None
44208932 140794 UNDEFINED 4 Human Binding pKi = 5 5.0 -89125 37
NoneNone
PDSP KiDatabase 475 5 1 3 6.8 Cc1ccc(Cn2nc(C(=O)NC3C4(C)CCC(C4)C3(C)C)cc2-c2ccc(Cl)c(C)c2)cc1 None
CHEMBL381689 140794 UNDEFINED 4 Human Binding pKi = 5 5.0 -89125 37
NoneNone
PDSP KiDatabase 475 5 1 3 6.8 Cc1ccc(Cn2nc(C(=O)NC3C4(C)CCC(C4)C3(C)C)cc2-c2ccc(Cl)c(C)c2)cc1 None
1973 205941 125I-ENDOTHELIN 12 Rat Binding pKi = 5 5.0 -3 36
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
CHEMBL1394464 205941 125I-ENDOTHELIN 12 Rat Binding pKi = 5 5.0 -3 36
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
CHEMBL66089 205941 125I-ENDOTHELIN 12 Rat Binding pKi = 5 5.0 -3 36
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
None 218979 125I-ENDOTHELIN 0 Rat Binding pKi = 5 5.0 -10471285 17
NoneNone
PDSP KiDatabase 372 2 1 3 4.4 CC(C)(C)C1=CC=C(C=C1)NC(=O)N2CCN(CC2)C3=C(C=CC=N3)Cl None
104865 706 125I-ENDOTHELIN 60 Human Binding pKi = 7.0 7.0 -6 4
NoneNone
PDSP KiDatabase 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
104865.0 706 125I-ENDOTHELIN 60 Human Binding pKi = 7.0 7.0 -6 4
NoneNone
PDSP KiDatabase 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
3494 706 125I-ENDOTHELIN 60 Human Binding pKi = 7.0 7.0 -6 4
NoneNone
PDSP KiDatabase 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
392 706 125I-ENDOTHELIN 60 Human Binding pKi = 7.0 7.0 -6 4
NoneNone
PDSP KiDatabase 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
CHEMBL957 706 125I-ENDOTHELIN 60 Human Binding pKi = 7.0 7.0 -6 4
NoneNone
PDSP KiDatabase 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
DB00559 706 125I-ENDOTHELIN 60 Human Binding pKi = 7.0 7.0 -6 4
NoneNone
PDSP KiDatabase 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
104865 706 125I-ENDOTHELIN 60 Human Binding pKi = 6.9 6.9 -6 4
NoneNone
PDSP KiDatabase 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
104865.0 706 125I-ENDOTHELIN 60 Human Binding pKi = 6.9 6.9 -6 4
NoneNone
PDSP KiDatabase 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
3494 706 125I-ENDOTHELIN 60 Human Binding pKi = 6.9 6.9 -6 4
NoneNone
PDSP KiDatabase 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
392 706 125I-ENDOTHELIN 60 Human Binding pKi = 6.9 6.9 -6 4
NoneNone
PDSP KiDatabase 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
CHEMBL957 706 125I-ENDOTHELIN 60 Human Binding pKi = 6.9 6.9 -6 4
NoneNone
PDSP KiDatabase 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
DB00559 706 125I-ENDOTHELIN 60 Human Binding pKi = 6.9 6.9 -6 4
NoneNone
PDSP KiDatabase 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
None 218565 125I-ENDOTHELIN 0 Human Binding pKi = 7.7 7.7 -52 2
NoneNone
PDSP KiDatabase 520 10 2 7 4.7 CCCOC1=CC2=C(C=C1)C(C(C2C3=C(C=C(C=C3)OC)OCC(=O)O)C(=O)O)C4=CC5=C(C=C4)OCO5 None
3951 391 None 55 Human Binding pKi = 8.2 8.2 1 2
NoneNone
Drug Central 378 7 1 5 3.5 COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1 None
4337 391 None 55 Human Binding pKi = 8.2 8.2 1 2
NoneNone
Drug Central 378 7 1 5 3.5 COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1 None
6918493 391 None 55 Human Binding pKi = 8.2 8.2 1 2
NoneNone
Drug Central 378 7 1 5 3.5 COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1 None
6918493.0 391 None 55 Human Binding pKi = 8.2 8.2 1 2
NoneNone
Drug Central 378 7 1 5 3.5 COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1 None
CHEMBL1111 391 None 55 Human Binding pKi = 8.2 8.2 1 2
NoneNone
Drug Central 378 7 1 5 3.5 COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1 None
DB06403 391 None 55 Human Binding pKi = 8.2 8.2 1 2
NoneNone
Drug Central 378 7 1 5 3.5 COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1 None
104865 706 None 60 Human Binding pKi = 8.2 8.2 -6 4
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
Drug Central 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
104865.0 706 None 60 Human Binding pKi = 8.2 8.2 -6 4
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
Drug Central 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
3494 706 None 60 Human Binding pKi = 8.2 8.2 -6 4
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
Drug Central 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
392 706 None 60 Human Binding pKi = 8.2 8.2 -6 4
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
Drug Central 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
CHEMBL957 706 None 60 Human Binding pKi = 8.2 8.2 -6 4
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
Drug Central 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
DB00559 706 None 60 Human Binding pKi = 8.2 8.2 -6 4
Inhibitory activity against human endothelin B receptor expressed in CHO cellsInhibitory activity against human endothelin B receptor expressed in CHO cells
Drug Central 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 None
12286 948 None 29 Human Binding pKi = 6.8 6.8 -1348 2
Binding affinity measured as displacement of ET-3 from CHO cells expressing hET<sub>B</sub>Binding affinity measured as displacement of ET-3 from CHO cells expressing hET<sub>B</sub>
Guide to Pharmacology 577 11 3 13 2.4 Cc1cnc(cc1)S(=O)(=O)Nc1c(c(nc(n1)c1cc(ncc1)c1n[nH]nn1)OCCO)Oc1ccccc1OC 9703472
6433095 948 None 29 Human Binding pKi = 6.8 6.8 -1348 2
Binding affinity measured as displacement of ET-3 from CHO cells expressing hET<sub>B</sub>Binding affinity measured as displacement of ET-3 from CHO cells expressing hET<sub>B</sub>
Guide to Pharmacology 577 11 3 13 2.4 Cc1cnc(cc1)S(=O)(=O)Nc1c(c(nc(n1)c1cc(ncc1)c1n[nH]nn1)OCCO)Oc1ccccc1OC 9703472
6433095.0 948 None 29 Human Binding pKi = 6.8 6.8 -1348 2
Binding affinity measured as displacement of ET-3 from CHO cells expressing hET<sub>B</sub>Binding affinity measured as displacement of ET-3 from CHO cells expressing hET<sub>B</sub>
Guide to Pharmacology 577 11 3 13 2.4 Cc1cnc(cc1)S(=O)(=O)Nc1c(c(nc(n1)c1cc(ncc1)c1n[nH]nn1)OCCO)Oc1ccccc1OC 9703472
CHEMBL109648 948 None 29 Human Binding pKi = 6.8 6.8 -1348 2
Binding affinity measured as displacement of ET-3 from CHO cells expressing hET<sub>B</sub>Binding affinity measured as displacement of ET-3 from CHO cells expressing hET<sub>B</sub>
Guide to Pharmacology 577 11 3 13 2.4 Cc1cnc(cc1)S(=O)(=O)Nc1c(c(nc(n1)c1cc(ncc1)c1n[nH]nn1)OCCO)Oc1ccccc1OC 9703472
DB06677 948 None 29 Human Binding pKi = 6.8 6.8 -1348 2
Binding affinity measured as displacement of ET-3 from CHO cells expressing hET<sub>B</sub>Binding affinity measured as displacement of ET-3 from CHO cells expressing hET<sub>B</sub>
Guide to Pharmacology 577 11 3 13 2.4 Cc1cnc(cc1)S(=O)(=O)Nc1c(c(nc(n1)c1cc(ncc1)c1n[nH]nn1)OCCO)Oc1ccccc1OC 9703472
159594 522 None 36 Human Binding pKi = 6.9 6.9 -4073 3
CHO cells expressing human ET<sub>B</sub> receptor.CHO cells expressing human ET<sub>B</sub> receptor.
Guide to Pharmacology 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 8676339
159594.0 522 None 36 Human Binding pKi = 6.9 6.9 -4073 3
CHO cells expressing human ET<sub>B</sub> receptor.CHO cells expressing human ET<sub>B</sub> receptor.
Guide to Pharmacology 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 8676339
3487 522 None 36 Human Binding pKi = 6.9 6.9 -4073 3
CHO cells expressing human ET<sub>B</sub> receptor.CHO cells expressing human ET<sub>B</sub> receptor.
Guide to Pharmacology 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 8676339
CHEMBL9194 522 None 36 Human Binding pKi = 6.9 6.9 -4073 3
CHO cells expressing human ET<sub>B</sub> receptor.CHO cells expressing human ET<sub>B</sub> receptor.
Guide to Pharmacology 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 8676339
DB06199 522 None 36 Human Binding pKi = 6.9 6.9 -4073 3
CHO cells expressing human ET<sub>B</sub> receptor.CHO cells expressing human ET<sub>B</sub> receptor.
Guide to Pharmacology 510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC 8676339
13016 670 None 14 Human Binding pKi = 4.7 4.7 -13182 4
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 6 4.4 CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4 10956219
9843631 670 None 14 Human Binding pKi = 4.7 4.7 -13182 4
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 6 4.4 CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4 10956219
CHEMBL24461 670 None 14 Human Binding pKi = 4.7 4.7 -13182 4
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 6 4.4 CC1=C(ON=C1C)NS(=O)(=O)C2=CC=CC=C2C3=CC=C(C=C3)C4=NC=CO4 10956219
104865 706 None 60 Human Binding pKi = 7.1 7.1 -6 4
UnclassifiedUnclassified
Guide to Pharmacology 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 8035319
104865.0 706 None 60 Human Binding pKi = 7.1 7.1 -6 4
UnclassifiedUnclassified
Guide to Pharmacology 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 8035319
3494 706 None 60 Human Binding pKi = 7.1 7.1 -6 4
UnclassifiedUnclassified
Guide to Pharmacology 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 8035319
392 706 None 60 Human Binding pKi = 7.1 7.1 -6 4
UnclassifiedUnclassified
Guide to Pharmacology 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 8035319
CHEMBL957 706 None 60 Human Binding pKi = 7.1 7.1 -6 4
UnclassifiedUnclassified
Guide to Pharmacology 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 8035319
DB00559 706 None 60 Human Binding pKi = 7.1 7.1 -6 4
UnclassifiedUnclassified
Guide to Pharmacology 551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1 8035319
1007 3641 None 0 Human Binding pKi = 8.7 8.7 -3 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1320877
1007 3641 None 0 Human Binding pKi = 8.7 8.7 -3 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 35328566
16130933 3641 None 0 Human Binding pKi = 8.7 8.7 -3 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1320877
16130933 3641 None 0 Human Binding pKi = 8.7 8.7 -3 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 35328566
16133819 3641 None 0 Human Binding pKi = 8.7 8.7 -3 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1320877
16133819 3641 None 0 Human Binding pKi = 8.7 8.7 -3 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 35328566
3886 3641 None 0 Human Binding pKi = 8.7 8.7 -3 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1320877
3886 3641 None 0 Human Binding pKi = 8.7 8.7 -3 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 35328566
44210030 3641 None 0 Human Binding pKi = 8.7 8.7 -3 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1320877
44210030 3641 None 0 Human Binding pKi = 8.7 8.7 -3 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 35328566
56947141 3641 None 0 Human Binding pKi = 8.7 8.7 -3 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1320877
56947141 3641 None 0 Human Binding pKi = 8.7 8.7 -3 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 35328566
CHEMBL3188091 3641 None 0 Human Binding pKi = 8.7 8.7 -3 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1320877
CHEMBL3188091 3641 None 0 Human Binding pKi = 8.7 8.7 -3 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 35328566
DB06138 3641 None 0 Human Binding pKi = 8.7 8.7 -3 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1320877
DB06138 3641 None 0 Human Binding pKi = 8.7 8.7 -3 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 35328566
16133801 712 None 0 Human Binding pKi = 9.7 9.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7733918
3859 712 None 0 Human Binding pKi = 9.7 9.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7733918
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