Ligand source activities (1 row/activity)





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

59304608 75285 None 0 Human Functional pEC50 = 9 9.0 3 4
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 262 3 2 4 0.9 O=c1[nH]c(=O)c2c(CCC3CCC3)cc(=O)oc2[nH]1 10.1021/ml200243g
CHEMBL2036954 75285 None 0 Human Functional pEC50 = 9 9.0 3 4
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 262 3 2 4 0.9 O=c1[nH]c(=O)c2c(CCC3CCC3)cc(=O)oc2[nH]1 10.1021/ml200243g
46890269 7376 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 381 7 3 3 4.5 CCCC1CCC(NC(=O)CCc2ccc3cc(O)ccc3c2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
CHEMBL1086353 7376 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 381 7 3 3 4.5 CCCC1CCC(NC(=O)CCc2ccc3cc(O)ccc3c2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
15605648 75283 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 290 3 2 4 1.1 O=c1[nH]c(=O)c2c(CCCC(F)(F)F)cc(=O)oc2[nH]1 10.1021/ml200243g
CHEMBL2036952 75283 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 290 3 2 4 1.1 O=c1[nH]c(=O)c2c(CCCC(F)(F)F)cc(=O)oc2[nH]1 10.1021/ml200243g
15604638 75288 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 276 5 2 4 1.3 O=c1[nH]c(=O)c2c(CCCCC3CC3)cc(=O)oc2[nH]1 10.1021/ml200243g
CHEMBL2036957 75288 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 276 5 2 4 1.3 O=c1[nH]c(=O)c2c(CCCCC3CC3)cc(=O)oc2[nH]1 10.1021/ml200243g
145957566 162381 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 426 3 1 5 5.0 COc1ccc(-c2cc3cc(C4Nc5ccccc5C(=O)N4C)cc(C)c3oc2=O)cc1 10.1016/j.ejmech.2018.04.037
CHEMBL4164140 162381 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 426 3 1 5 5.0 COc1ccc(-c2cc3cc(C4Nc5ccccc5C(=O)N4C)cc(C)c3oc2=O)cc1 10.1016/j.ejmech.2018.04.037
145957566 162381 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 426 3 1 5 5.0 COc1ccc(-c2cc3cc(C4Nc5ccccc5C(=O)N4C)cc(C)c3oc2=O)cc1 10.1016/j.ejmech.2018.04.037
CHEMBL4164140 162381 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 426 3 1 5 5.0 COc1ccc(-c2cc3cc(C4Nc5ccccc5C(=O)N4C)cc(C)c3oc2=O)cc1 10.1016/j.ejmech.2018.04.037
156010038 177135 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 414 8 3 4 5.1 CCCCn1cc(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
CHEMBL4632359 177135 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 414 8 3 4 5.1 CCCCn1cc(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
776464 93762 None 59 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 152 2 2 2 1.0 O=C(O)c1cc(C2CC2)n[nH]1 10.1016/j.bmcl.2007.07.101
CHEMBL247098 93762 None 59 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 152 2 2 2 1.0 O=C(O)c1cc(C2CC2)n[nH]1 10.1016/j.bmcl.2007.07.101
117629482 2823 None 82 Human Functional pEC50 = 7 7.0 -4 4
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2011.12.041
1588 2823 None 82 Human Functional pEC50 = 7 7.0 -4 4
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2011.12.041
1594 2823 None 82 Human Functional pEC50 = 7 7.0 -4 4
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2011.12.041
2835 2823 None 82 Human Functional pEC50 = 7 7.0 -4 4
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2011.12.041
938 2823 None 82 Human Functional pEC50 = 7 7.0 -4 4
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2011.12.041
CHEMBL573 2823 None 82 Human Functional pEC50 = 7 7.0 -4 4
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2011.12.041
DB00627 2823 None 82 Human Functional pEC50 = 7 7.0 -4 4
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2011.12.041
17751630 6747 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 487 7 3 7 2.8 NC(Cc1nc(-c2ccc(F)cn2)no1)C(=O)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1083743 6747 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 487 7 3 7 2.8 NC(Cc1nc(-c2ccc(F)cn2)no1)C(=O)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
117629482 2823 None 82 Human Functional pEC50 = 7 7.0 -4 4
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml100251u
1588 2823 None 82 Human Functional pEC50 = 7 7.0 -4 4
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml100251u
1594 2823 None 82 Human Functional pEC50 = 7 7.0 -4 4
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml100251u
2835 2823 None 82 Human Functional pEC50 = 7 7.0 -4 4
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml100251u
938 2823 None 82 Human Functional pEC50 = 7 7.0 -4 4
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml100251u
CHEMBL573 2823 None 82 Human Functional pEC50 = 7 7.0 -4 4
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml100251u
DB00627 2823 None 82 Human Functional pEC50 = 7 7.0 -4 4
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml100251u
156016715 177780 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 415 8 3 5 4.5 CCCCn1cc(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)c(C(=O)O)n1 10.1016/j.bmcl.2020.127105
CHEMBL4641756 177780 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 415 8 3 5 4.5 CCCCn1cc(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)c(C(=O)O)n1 10.1016/j.bmcl.2020.127105
117629482 2823 None 82 Human Functional pEC50 = 6 6.0 -4 4
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.10.055
1588 2823 None 82 Human Functional pEC50 = 6 6.0 -4 4
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.10.055
1594 2823 None 82 Human Functional pEC50 = 6 6.0 -4 4
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.10.055
2835 2823 None 82 Human Functional pEC50 = 6 6.0 -4 4
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.10.055
938 2823 None 82 Human Functional pEC50 = 6 6.0 -4 4
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.10.055
CHEMBL573 2823 None 82 Human Functional pEC50 = 6 6.0 -4 4
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.10.055
DB00627 2823 None 82 Human Functional pEC50 = 6 6.0 -4 4
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.10.055
117629482 2823 None 82 Human Functional pEC50 = 6 6.0 -4 4
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
1588 2823 None 82 Human Functional pEC50 = 6 6.0 -4 4
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
1594 2823 None 82 Human Functional pEC50 = 6 6.0 -4 4
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
2835 2823 None 82 Human Functional pEC50 = 6 6.0 -4 4
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
938 2823 None 82 Human Functional pEC50 = 6 6.0 -4 4
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
CHEMBL573 2823 None 82 Human Functional pEC50 = 6 6.0 -4 4
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
DB00627 2823 None 82 Human Functional pEC50 = 6 6.0 -4 4
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
11594881 88672 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 319 5 2 2 4.1 O=C(CCc1ccc2ccccc2c1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL235740 88672 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 319 5 2 2 4.1 O=C(CCc1ccc2ccccc2c1)Nc1ccccc1C(=O)O 10.1021/jm700942d
117629482 2823 None 82 Human Functional pEC50 = 6 6.0 -4 4
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm900151e
1588 2823 None 82 Human Functional pEC50 = 6 6.0 -4 4
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm900151e
1594 2823 None 82 Human Functional pEC50 = 6 6.0 -4 4
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm900151e
2835 2823 None 82 Human Functional pEC50 = 6 6.0 -4 4
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm900151e
938 2823 None 82 Human Functional pEC50 = 6 6.0 -4 4
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm900151e
CHEMBL573 2823 None 82 Human Functional pEC50 = 6 6.0 -4 4
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm900151e
DB00627 2823 None 82 Human Functional pEC50 = 6 6.0 -4 4
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm900151e
11523095 184293 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 347 7 2 2 4.9 O=C(CCCCc1ccc2ccccc2c1)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL483153 184293 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 347 7 2 2 4.9 O=C(CCCCc1ccc2ccccc2c1)Nc1ccccc1C(=O)O 10.1021/jm900151e
117629482 2823 None 82 Human Functional pEC50 = 6 6.0 -4 4
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.039
1588 2823 None 82 Human Functional pEC50 = 6 6.0 -4 4
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.039
1594 2823 None 82 Human Functional pEC50 = 6 6.0 -4 4
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.039
2835 2823 None 82 Human Functional pEC50 = 6 6.0 -4 4
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.039
938 2823 None 82 Human Functional pEC50 = 6 6.0 -4 4
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.039
CHEMBL573 2823 None 82 Human Functional pEC50 = 6 6.0 -4 4
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.039
DB00627 2823 None 82 Human Functional pEC50 = 6 6.0 -4 4
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.039
11594881 88672 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assayAgonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assay
ChEMBL 319 5 2 2 4.1 O=C(CCc1ccc2ccccc2c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2008.08.030
CHEMBL235740 88672 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assayAgonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assay
ChEMBL 319 5 2 2 4.1 O=C(CCc1ccc2ccccc2c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2008.08.030
776464 93762 None 59 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 152 2 2 2 1.0 O=C(O)c1cc(C2CC2)n[nH]1 10.1016/j.bmcl.2007.06.028
CHEMBL247098 93762 None 59 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 152 2 2 2 1.0 O=C(O)c1cc(C2CC2)n[nH]1 10.1016/j.bmcl.2007.06.028
117629482 2823 None 82 Human Functional pEC50 = 6 6.0 -4 4
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.001
1588 2823 None 82 Human Functional pEC50 = 6 6.0 -4 4
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.001
1594 2823 None 82 Human Functional pEC50 = 6 6.0 -4 4
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.001
2835 2823 None 82 Human Functional pEC50 = 6 6.0 -4 4
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.001
938 2823 None 82 Human Functional pEC50 = 6 6.0 -4 4
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.001
CHEMBL573 2823 None 82 Human Functional pEC50 = 6 6.0 -4 4
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.001
DB00627 2823 None 82 Human Functional pEC50 = 6 6.0 -4 4
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.001
117629482 2823 None 82 Human Functional pEC50 = 6 6.0 -4 4
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.06.054
1588 2823 None 82 Human Functional pEC50 = 6 6.0 -4 4
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.06.054
1594 2823 None 82 Human Functional pEC50 = 6 6.0 -4 4
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.06.054
2835 2823 None 82 Human Functional pEC50 = 6 6.0 -4 4
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.06.054
938 2823 None 82 Human Functional pEC50 = 6 6.0 -4 4
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.06.054
CHEMBL573 2823 None 82 Human Functional pEC50 = 6 6.0 -4 4
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.06.054
DB00627 2823 None 82 Human Functional pEC50 = 6 6.0 -4 4
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.06.054
54585613 61419 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 392 5 4 6 1.9 NC(Cc1cc2n(n1)-c1ccc(O)cc1CC2)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1770174 61419 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 392 5 4 6 1.9 NC(Cc1cc2n(n1)-c1ccc(O)cc1CC2)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
57402396 69939 None 0 Human Functional pEC50 = 5 5.0 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 236 3 1 5 0.8 CCOc1nc2oc(=O)cc(CC)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
CHEMBL1939012 69939 None 0 Human Functional pEC50 = 5 5.0 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 236 3 1 5 0.8 CCOc1nc2oc(=O)cc(CC)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
57397200 69942 None 0 Human Functional pEC50 = 5 5.0 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 312 5 1 5 2.1 CCc1cc(=O)oc2nc(OCCc3ccccc3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939015 69942 None 0 Human Functional pEC50 = 5 5.0 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 312 5 1 5 2.1 CCc1cc(=O)oc2nc(OCCc3ccccc3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
57400597 69961 None 0 Human Functional pEC50 = 5 5.0 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 303 4 1 7 1.3 CCc1cc(=O)oc2nc(OCc3cc(C)on3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939034 69961 None 0 Human Functional pEC50 = 5 5.0 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 303 4 1 7 1.3 CCc1cc(=O)oc2nc(OCc3cc(C)on3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
145954324 162607 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 402 2 1 5 5.0 Cc1cc(C2Nc3ccccc3C(=O)N2C)cc2cc(-c3cccs3)c(=O)oc12 10.1016/j.ejmech.2018.04.037
CHEMBL4167588 162607 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 402 2 1 5 5.0 Cc1cc(C2Nc3ccccc3C(=O)N2C)cc2cc(-c3cccs3)c(=O)oc12 10.1016/j.ejmech.2018.04.037
90645405 112596 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 295 3 2 2 2.6 O=C(/C=C/C#Cc1ccccc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL3299113 112596 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 295 3 2 2 2.6 O=C(/C=C/C#Cc1ccccc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
145954324 162607 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 402 2 1 5 5.0 Cc1cc(C2Nc3ccccc3C(=O)N2C)cc2cc(-c3cccs3)c(=O)oc12 10.1016/j.ejmech.2018.04.037
CHEMBL4167588 162607 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 402 2 1 5 5.0 Cc1cc(C2Nc3ccccc3C(=O)N2C)cc2cc(-c3cccs3)c(=O)oc12 10.1016/j.ejmech.2018.04.037
11672831 76067 None 4 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 192 1 2 2 1.4 CC1(C)C2Cc3c(C(=O)O)n[nH]c3C21 10.1021/jm2010964
CHEMBL2057235 76067 None 4 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 192 1 2 2 1.4 CC1(C)C2Cc3c(C(=O)O)n[nH]c3C21 10.1021/jm2010964
776416 18945 None 63 Human Functional pEC50 = 5.0 5.0 -5 2
Agonist activity against human GPR109a assessed as GTPgammaS bindingAgonist activity against human GPR109a assessed as GTPgammaS binding
ChEMBL 152 1 2 2 0.6 O=C(O)c1n[nH]c2c1CCC2 10.1021/jm800258p
CHEMBL128604 18945 None 63 Human Functional pEC50 = 5.0 5.0 -5 2
Agonist activity against human GPR109a assessed as GTPgammaS bindingAgonist activity against human GPR109a assessed as GTPgammaS binding
ChEMBL 152 1 2 2 0.6 O=C(O)c1n[nH]c2c1CCC2 10.1021/jm800258p
11550911 95241 None 0 Human Functional pEC50 = 5.0 5.0 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 280 3 2 2 2.5 O=C(O)c1cc(Cc2cccc(Br)c2)[nH]n1 10.1016/j.bmcl.2007.06.028
CHEMBL255877 95241 None 0 Human Functional pEC50 = 5.0 5.0 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 280 3 2 2 2.5 O=C(O)c1cc(Cc2cccc(Br)c2)[nH]n1 10.1016/j.bmcl.2007.06.028
57397201 69950 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 328 5 1 6 2.0 CCc1cc(=O)oc2nc(OCc3ccc(OC)cc3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939023 69950 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 328 5 1 6 2.0 CCc1cc(=O)oc2nc(OCc3ccc(OC)cc3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
53325342 58055 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 336 6 1 4 3.3 O=c1cc(CCCC2(C3CC3)CC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
CHEMBL1672642 58055 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 336 6 1 4 3.3 O=c1cc(CCCC2(C3CC3)CC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
24954941 58058 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 296 4 1 4 2.5 O=c1cc(CCC2CCC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
CHEMBL1672732 58058 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 296 4 1 4 2.5 O=c1cc(CCC2CCC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
11159621 2548 None 38 Mouse Functional pEC50 = 6.0 6.0 1 3
Agonist activity against mouse GPR109a assessed as forskolin-induced cAMP accumulationAgonist activity against mouse GPR109a assessed as forskolin-induced cAMP accumulation
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
5784 2548 None 38 Mouse Functional pEC50 = 6.0 6.0 1 3
Agonist activity against mouse GPR109a assessed as forskolin-induced cAMP accumulationAgonist activity against mouse GPR109a assessed as forskolin-induced cAMP accumulation
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
CHEMBL456145 2548 None 38 Mouse Functional pEC50 = 6.0 6.0 1 3
Agonist activity against mouse GPR109a assessed as forskolin-induced cAMP accumulationAgonist activity against mouse GPR109a assessed as forskolin-induced cAMP accumulation
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
DB05939 2548 None 38 Mouse Functional pEC50 = 6.0 6.0 1 3
Agonist activity against mouse GPR109a assessed as forskolin-induced cAMP accumulationAgonist activity against mouse GPR109a assessed as forskolin-induced cAMP accumulation
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
776421 89962 None 65 Human Functional pEC50 = 7.0 7.0 30 2
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 154 2 2 2 1.2 CC(C)c1cc(C(=O)O)n[nH]1 10.1016/j.bmcl.2007.07.101
CHEMBL238002 89962 None 65 Human Functional pEC50 = 7.0 7.0 30 2
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 154 2 2 2 1.2 CC(C)c1cc(C(=O)O)n[nH]1 10.1016/j.bmcl.2007.07.101
13153555 93916 None 26 Human Functional pEC50 = 7.0 7.0 42 2
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 182 5 2 2 1.8 CCCCCc1cc(C(=O)O)[nH]n1 10.1016/j.bmcl.2007.07.101
CHEMBL247921 93916 None 26 Human Functional pEC50 = 7.0 7.0 42 2
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 182 5 2 2 1.8 CCCCCc1cc(C(=O)O)[nH]n1 10.1016/j.bmcl.2007.07.101
46890327 6602 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 451 6 3 3 5.2 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1083138 6602 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 451 6 3 3 5.2 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
59304946 75273 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 268 4 2 5 0.5 CSCCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
CHEMBL2036828 75273 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 268 4 2 5 0.5 CSCCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
11483496 126 None 0 Human Functional pEC50 = 7.0 7.0 14 2
Activity at GPR109a assessed as inhibition of forskolin-stimulated cAMP productionActivity at GPR109a assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 302 2 1 4 2.3 Brc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 10.1021/jm800896z
1589 126 None 0 Human Functional pEC50 = 7.0 7.0 14 2
Activity at GPR109a assessed as inhibition of forskolin-stimulated cAMP productionActivity at GPR109a assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 302 2 1 4 2.3 Brc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 10.1021/jm800896z
CHEMBL375493 126 None 0 Human Functional pEC50 = 7.0 7.0 14 2
Activity at GPR109a assessed as inhibition of forskolin-stimulated cAMP productionActivity at GPR109a assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 302 2 1 4 2.3 Brc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 10.1021/jm800896z
11483496 126 None 0 Human Functional pEC50 = 7.0 7.0 14 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 302 2 1 4 2.3 Brc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 10.1021/jm070022x
1589 126 None 0 Human Functional pEC50 = 7.0 7.0 14 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 302 2 1 4 2.3 Brc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 10.1021/jm070022x
CHEMBL375493 126 None 0 Human Functional pEC50 = 7.0 7.0 14 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 302 2 1 4 2.3 Brc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 10.1021/jm070022x
135416383 185015 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 368 5 3 5 2.7 O=C(CCc1noc2c1CCc1cc(O)ccc1-2)NC1=C(C(=O)O)CCC1 10.1021/jm900151e
CHEMBL485326 185015 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 368 5 3 5 2.7 O=C(CCc1noc2c1CCc1cc(O)ccc1-2)NC1=C(C(=O)O)CCC1 10.1021/jm900151e
59304655 75272 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 252 4 2 5 -0.3 COCCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
CHEMBL2036827 75272 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 252 4 2 5 -0.3 COCCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
137652577 158852 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 329 3 3 3 2.5 O=C(/C=C/C#Cc1ccc(O)cc1F)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4093990 158852 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 329 3 3 3 2.5 O=C(/C=C/C#Cc1ccc(O)cc1F)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
11184165 83487 None 0 Human Functional pEC50 = 6.0 6.0 5 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 246 3 1 3 2.0 CCc1cccc(C2(C)OC(C(=O)O)=CC2=O)c1 10.1021/jm070022x
CHEMBL219950 83487 None 0 Human Functional pEC50 = 6.0 6.0 5 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 246 3 1 3 2.0 CCc1cccc(C2(C)OC(C(=O)O)=CC2=O)c1 10.1021/jm070022x
12003788 196265 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 278 2 2 2 2.7 O=C(O)c1n[nH]c2c1CC(c1cc(F)ccc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL1237148 196265 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 278 2 2 2 2.7 O=C(O)c1n[nH]c2c1CC(c1cc(F)ccc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL542000 196265 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 278 2 2 2 2.7 O=C(O)c1n[nH]c2c1CC(c1cc(F)ccc1F)CC2 10.1016/j.bmcl.2009.06.054
12003787 198298 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 296 2 2 2 2.8 O=C(O)c1n[nH]c2c1CC(c1cc(F)cc(F)c1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL558463 198298 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 296 2 2 2 2.8 O=C(O)c1n[nH]c2c1CC(c1cc(F)cc(F)c1F)CC2 10.1016/j.bmcl.2009.06.054
16048917 154103 None 0 Human Functional pEC50 = 5.0 5.0 - 1
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 407 4 2 6 2.7 COc1cccc2ncc(N3CCN(C(=O)Nc4ccccc4C(=O)O)CC3)nc12 10.1016/j.bmcl.2007.10.055
CHEMBL398414 154103 None 0 Human Functional pEC50 = 5.0 5.0 - 1
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 407 4 2 6 2.7 COc1cccc2ncc(N3CCN(C(=O)Nc4ccccc4C(=O)O)CC3)nc12 10.1016/j.bmcl.2007.10.055
135401974 154813 None 0 Human Functional pEC50 = 5.0 5.0 - 1
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 393 3 3 6 2.4 O=C(O)c1ccccc1NC(=O)N1CCN(c2cnc3cccc(O)c3n2)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL399859 154813 None 0 Human Functional pEC50 = 5.0 5.0 - 1
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 393 3 3 6 2.4 O=C(O)c1ccccc1NC(=O)N1CCN(c2cnc3cccc(O)c3n2)CC1 10.1016/j.bmcl.2007.10.055
46889338 6726 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 214 2 2 4 0.7 C=C[C@H]1[C@H]2Cc3c(-c4nnn[nH]4)n[nH]c3[C@@H]12 10.1016/j.bmcl.2010.03.062
CHEMBL1083683 6726 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 214 2 2 4 0.7 C=C[C@H]1[C@H]2Cc3c(-c4nnn[nH]4)n[nH]c3[C@@H]12 10.1016/j.bmcl.2010.03.062
53317449 58078 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 222 2 2 5 -0.1 CCc1cc(=O)oc2nc(CO)[nH]c(=O)c12 10.1021/ml100251u
CHEMBL1672767 58078 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 222 2 2 5 -0.1 CCc1cc(=O)oc2nc(CO)[nH]c(=O)c12 10.1021/ml100251u
57413448 76378 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 234 5 2 2 2.6 CCCCC[C@@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
CHEMBL2059226 76378 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 234 5 2 2 2.6 CCCCC[C@@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
57395376 69948 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 328 5 1 6 2.0 CCc1cc(=O)oc2nc(OCc3ccccc3OC)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939021 69948 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 328 5 1 6 2.0 CCc1cc(=O)oc2nc(OCc3ccccc3OC)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
57412210 76142 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 178 1 2 2 1.0 C[C@@H]1[C@@H]2c3[nH]nc(C(=O)O)c3C[C@H]12 10.1021/jm2010964
CHEMBL2057616 76142 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 178 1 2 2 1.0 C[C@@H]1[C@@H]2c3[nH]nc(C(=O)O)c3C[C@H]12 10.1021/jm2010964
15605571 75261 None 0 Mouse Functional pEC50 = 7.9 7.9 -1 5
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 236 3 2 4 0.5 CCCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
CHEMBL2036813 75261 None 0 Mouse Functional pEC50 = 7.9 7.9 -1 5
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 236 3 2 4 0.5 CCCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
49763030 76144 None 25 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 164 1 2 2 0.8 O=C(O)c1n[nH]c2c1C[C@H]1C[C@@H]21 10.1021/jm2010964
CHEMBL2057618 76144 None 25 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 164 1 2 2 0.8 O=C(O)c1n[nH]c2c1C[C@H]1C[C@@H]21 10.1021/jm2010964
117629482 2823 None 82 Human Functional pEC50 = 6.9 6.9 -4 4
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm070022x
1588 2823 None 82 Human Functional pEC50 = 6.9 6.9 -4 4
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm070022x
1594 2823 None 82 Human Functional pEC50 = 6.9 6.9 -4 4
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm070022x
2835 2823 None 82 Human Functional pEC50 = 6.9 6.9 -4 4
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm070022x
938 2823 None 82 Human Functional pEC50 = 6.9 6.9 -4 4
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm070022x
CHEMBL573 2823 None 82 Human Functional pEC50 = 6.9 6.9 -4 4
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm070022x
DB00627 2823 None 82 Human Functional pEC50 = 6.9 6.9 -4 4
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm070022x
135800177 146039 None 5 Human Functional pEC50 = 6.9 6.9 24 2
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 353 6 3 6 2.7 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL391813 146039 None 5 Human Functional pEC50 = 6.9 6.9 24 2
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 353 6 3 6 2.7 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1ccccc1C(=O)O 10.1021/jm700942d
11617852 184641 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 381 5 3 6 3.5 O=C(CCc1cn2c(n1)sc1cc(O)ccc12)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL484783 184641 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 381 5 3 6 3.5 O=C(CCc1cn2c(n1)sc1cc(O)ccc12)Nc1ccccc1C(=O)O 10.1021/jm900151e
25101223 1152 None 7 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 428 7 1 5 5.0 C[C@@H](NC(=O)c1cnc2n(c1C)ncc2c1ccc(cc1)C(C)C)COc1ccccc1 10.1016/j.bmcl.2008.08.039
5795 1152 None 7 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 428 7 1 5 5.0 C[C@@H](NC(=O)c1cnc2n(c1C)ncc2c1ccc(cc1)C(C)C)COc1ccccc1 10.1016/j.bmcl.2008.08.039
CHEMBL490599 1152 None 7 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 428 7 1 5 5.0 C[C@@H](NC(=O)c1cnc2n(c1C)ncc2c1ccc(cc1)C(C)C)COc1ccccc1 10.1016/j.bmcl.2008.08.039
117629482 2823 None 82 Human Functional pEC50 = 6.9 6.9 -4 4
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.06.028
1588 2823 None 82 Human Functional pEC50 = 6.9 6.9 -4 4
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.06.028
1594 2823 None 82 Human Functional pEC50 = 6.9 6.9 -4 4
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.06.028
2835 2823 None 82 Human Functional pEC50 = 6.9 6.9 -4 4
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.06.028
938 2823 None 82 Human Functional pEC50 = 6.9 6.9 -4 4
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.06.028
CHEMBL573 2823 None 82 Human Functional pEC50 = 6.9 6.9 -4 4
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.06.028
DB00627 2823 None 82 Human Functional pEC50 = 6.9 6.9 -4 4
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.06.028
135800177 146039 None 5 Human Functional pEC50 = 6.9 6.9 24 2
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 353 6 3 6 2.7 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL391813 146039 None 5 Human Functional pEC50 = 6.9 6.9 24 2
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 353 6 3 6 2.7 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
11992586 197956 None 5 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 217 4 3 3 1.7 O=C(O)c1cc(NCc2ccccc2)[nH]n1 10.1016/j.bmcl.2009.05.108
CHEMBL553435 197956 None 5 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 217 4 3 3 1.7 O=C(O)c1cc(NCc2ccccc2)[nH]n1 10.1016/j.bmcl.2009.05.108
11160694 138243 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 236 2 1 3 1.6 CC1(c2cccc(F)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL376889 138243 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 236 2 1 3 1.6 CC1(c2cccc(F)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
4268702 169755 None 5 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assayAgonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assay
ChEMBL 327 5 2 3 3.7 CC(C)(C)c1ccc(OCC(=O)Nc2ccccc2C(=O)O)cc1 10.1016/j.bmcl.2008.08.030
CHEMBL443733 169755 None 5 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assayAgonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assay
ChEMBL 327 5 2 3 3.7 CC(C)(C)c1ccc(OCC(=O)Nc2ccccc2C(=O)O)cc1 10.1016/j.bmcl.2008.08.030
145984458 165590 None 0 Rat Functional pEC50 = 5.9 5.9 -1 2
Agonist activity at rat GPR109A expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assayAgonist activity at rat GPR109A expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assay
ChEMBL 600 7 2 8 4.6 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3c(s2)C[Si](C)(c2ccc(OC)cc2)CC3)cc1N1CCOCC1 10.1021/acs.jmedchem.7b00718
CHEMBL4240407 165590 None 0 Rat Functional pEC50 = 5.9 5.9 -1 2
Agonist activity at rat GPR109A expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assayAgonist activity at rat GPR109A expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assay
ChEMBL 600 7 2 8 4.6 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3c(s2)C[Si](C)(c2ccc(OC)cc2)CC3)cc1N1CCOCC1 10.1021/acs.jmedchem.7b00718
11322761 141693 None 0 Human Functional pEC50 = 4.9 4.9 1 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 254 2 1 3 1.7 CC1(c2ccc(F)cc2F)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL385103 141693 None 0 Human Functional pEC50 = 4.9 4.9 1 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 254 2 1 3 1.7 CC1(c2ccc(F)cc2F)OC(C(=O)O)=CC1=O 10.1021/jm070022x
44441318 93844 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 228 2 2 2 2.2 O=C(O)c1[nH]nc2c1CCC2c1ccccc1 10.1016/j.bmcl.2007.06.028
CHEMBL247527 93844 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 228 2 2 2 2.2 O=C(O)c1[nH]nc2c1CCC2c1ccccc1 10.1016/j.bmcl.2007.06.028
11845295 149666 None 35 Mouse Functional pEC50 = 4.9 4.9 -1 2
Agonist activity against mouse GPR109a assessed as forskolin-induced cAMP accumulationAgonist activity against mouse GPR109a assessed as forskolin-induced cAMP accumulation
ChEMBL 166 1 2 2 1.2 CC1CCc2c(C(=O)O)n[nH]c21 10.1021/jm800258p
CHEMBL394688 149666 None 35 Mouse Functional pEC50 = 4.9 4.9 -1 2
Agonist activity against mouse GPR109a assessed as forskolin-induced cAMP accumulationAgonist activity against mouse GPR109a assessed as forskolin-induced cAMP accumulation
ChEMBL 166 1 2 2 1.2 CC1CCc2c(C(=O)O)n[nH]c21 10.1021/jm800258p
44441310 149371 None 3 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 170 4 2 3 0.3 COCCc1cc(C(=O)O)[nH]n1 10.1016/j.bmcl.2007.06.028
CHEMBL394464 149371 None 3 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 170 4 2 3 0.3 COCCc1cc(C(=O)O)[nH]n1 10.1016/j.bmcl.2007.06.028
57393654 69938 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 222 2 1 5 0.4 CCc1cc(=O)oc2nc(OC)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939011 69938 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 222 2 1 5 0.4 CCc1cc(=O)oc2nc(OC)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
882926 85641 None 10 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at GPR109aAgonist activity at GPR109a
ChEMBL 301 6 2 4 2.4 COc1ccc(OCC(=O)Nc2ccccc2C(=O)O)cc1 10.1021/jm200371q
CHEMBL228244 85641 None 10 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at GPR109aAgonist activity at GPR109a
ChEMBL 301 6 2 4 2.4 COc1ccc(OCC(=O)Nc2ccccc2C(=O)O)cc1 10.1021/jm200371q
882926 85641 None 10 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assayAgonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assay
ChEMBL 301 6 2 4 2.4 COc1ccc(OCC(=O)Nc2ccccc2C(=O)O)cc1 10.1016/j.bmcl.2008.08.030
CHEMBL228244 85641 None 10 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assayAgonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assay
ChEMBL 301 6 2 4 2.4 COc1ccc(OCC(=O)Nc2ccccc2C(=O)O)cc1 10.1016/j.bmcl.2008.08.030
90645413 112546 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 335 4 2 2 4.0 O=C(O)C1=C(NC(=O)[C@@H]2C[C@H]2c2ccc3ccccc3c2)CCCC1 10.1016/j.bmc.2014.05.011
CHEMBL3298703 112546 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 335 4 2 2 4.0 O=C(O)C1=C(NC(=O)[C@@H]2C[C@H]2c2ccc3ccccc3c2)CCCC1 10.1016/j.bmc.2014.05.011
53326893 58065 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 260 1 1 4 1.5 CCc1cc(=O)oc2nc(C(F)(F)F)[nH]c(=O)c12 10.1021/ml100251u
CHEMBL1672742 58065 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 260 1 1 4 1.5 CCc1cc(=O)oc2nc(C(F)(F)F)[nH]c(=O)c12 10.1021/ml100251u
24954204 58073 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 284 5 1 4 2.5 CCCCCc1cc(=O)oc2nc(C(F)F)[nH]c(=O)c12 10.1021/ml100251u
CHEMBL1672751 58073 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 284 5 1 4 2.5 CCCCCc1cc(=O)oc2nc(C(F)F)[nH]c(=O)c12 10.1021/ml100251u
57413453 76500 None 1 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 190 2 2 2 1.2 C=C[C@@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
CHEMBL2059825 76500 None 1 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 190 2 2 2 1.2 C=C[C@@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
46889360 7109 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 228 3 2 4 1.1 C=CC[C@@H]1[C@@H]2c3[nH]nc(-c4nnn[nH]4)c3C[C@H]12 10.1016/j.bmcl.2010.03.062
CHEMBL1085200 7109 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 228 3 2 4 1.1 C=CC[C@@H]1[C@@H]2c3[nH]nc(-c4nnn[nH]4)c3C[C@H]12 10.1016/j.bmcl.2010.03.062
15605654 75284 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 248 3 2 4 0.5 O=c1[nH]c(=O)c2c(CCC3CC3)cc(=O)oc2[nH]1 10.1021/ml200243g
CHEMBL2036953 75284 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 248 3 2 4 0.5 O=c1[nH]c(=O)c2c(CCC3CC3)cc(=O)oc2[nH]1 10.1021/ml200243g
46890299 7217 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 433 6 3 3 5.0 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2ccc(F)cc2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1085655 7217 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 433 6 3 3 5.0 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2ccc(F)cc2)CC1 10.1016/j.bmcl.2010.04.001
53322717 58063 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 322 4 1 4 2.9 O=c1cc(CCC2CC3(CC3)C2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
CHEMBL1672738 58063 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 322 4 1 4 2.9 O=c1cc(CCC2CC3(CC3)C2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
137633734 156412 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 311 3 3 3 2.3 O=C(/C=C/C#Cc1ccc(O)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4065654 156412 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 311 3 3 3 2.3 O=C(/C=C/C#Cc1ccc(O)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
137641317 157103 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 383 6 2 2 5.0 O=C(CCc1ccc(-c2ccccc2Cl)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4073374 157103 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 383 6 2 2 5.0 O=C(CCc1ccc(-c2ccccc2Cl)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
1595 259 None 36 Human Functional pEC50 = 5.9 5.9 4 2
Activity at GPR109a assessed as inhibition of forskolin-stimulated cAMP productionActivity at GPR109a assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1021/jm800896z
51576 259 None 36 Human Functional pEC50 = 5.9 5.9 4 2
Activity at GPR109a assessed as inhibition of forskolin-stimulated cAMP productionActivity at GPR109a assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1021/jm800896z
CHEMBL278488 259 None 36 Human Functional pEC50 = 5.9 5.9 4 2
Activity at GPR109a assessed as inhibition of forskolin-stimulated cAMP productionActivity at GPR109a assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1021/jm800896z
1595 259 None 36 Human Functional pEC50 = 5.9 5.9 4 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1021/jm070022x
51576 259 None 36 Human Functional pEC50 = 5.9 5.9 4 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1021/jm070022x
CHEMBL278488 259 None 36 Human Functional pEC50 = 5.9 5.9 4 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1021/jm070022x
1595 259 None 36 Human Functional pEC50 = 5.9 5.9 4 2
Agonist activity at N-terminal HA-tagged GPR109a receptor transfected in forskolin-stimulated cells assessed as cAMP accumulation by flashplate assayAgonist activity at N-terminal HA-tagged GPR109a receptor transfected in forskolin-stimulated cells assessed as cAMP accumulation by flashplate assay
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1016/j.bmcl.2009.05.108
51576 259 None 36 Human Functional pEC50 = 5.9 5.9 4 2
Agonist activity at N-terminal HA-tagged GPR109a receptor transfected in forskolin-stimulated cells assessed as cAMP accumulation by flashplate assayAgonist activity at N-terminal HA-tagged GPR109a receptor transfected in forskolin-stimulated cells assessed as cAMP accumulation by flashplate assay
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1016/j.bmcl.2009.05.108
CHEMBL278488 259 None 36 Human Functional pEC50 = 5.9 5.9 4 2
Agonist activity at N-terminal HA-tagged GPR109a receptor transfected in forskolin-stimulated cells assessed as cAMP accumulation by flashplate assayAgonist activity at N-terminal HA-tagged GPR109a receptor transfected in forskolin-stimulated cells assessed as cAMP accumulation by flashplate assay
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1016/j.bmcl.2009.05.108
24741310 89656 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 352 6 3 6 2.2 O=C(CCc1ccn(-c2ccc(O)cn2)n1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL237543 89656 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 352 6 3 6 2.2 O=C(CCc1ccn(-c2ccc(O)cn2)n1)Nc1ccccc1C(=O)O 10.1021/jm700942d
44580038 187055 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 444 8 1 6 4.6 COc1ccc(OCCNC(=O)c2cnc3c(-c4ccc(C(C)C)cc4)cnn3c2C)cc1 10.1016/j.bmcl.2008.08.039
CHEMBL490221 187055 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 444 8 1 6 4.6 COc1ccc(OCCNC(=O)c2cnc3c(-c4ccc(C(C)C)cc4)cnn3c2C)cc1 10.1016/j.bmcl.2008.08.039
44579693 187197 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 428 7 1 5 4.9 Cc1cccc(OCCNC(=O)c2cnc3c(-c4ccc(C(C)C)cc4)cnn3c2C)c1 10.1016/j.bmcl.2008.08.039
CHEMBL491396 187197 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 428 7 1 5 4.9 Cc1cccc(OCCNC(=O)c2cnc3c(-c4ccc(C(C)C)cc4)cnn3c2C)c1 10.1016/j.bmcl.2008.08.039
13557 1106 None 64 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 127 1 1 3 0.7 CC1=NOC(=C1)C(=O)O 10.1016/j.bmcl.2007.06.028
853085 1106 None 64 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 127 1 1 3 0.7 CC1=NOC(=C1)C(=O)O 10.1016/j.bmcl.2007.06.028
CHEMBL393428 1106 None 64 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 127 1 1 3 0.7 CC1=NOC(=C1)C(=O)O 10.1016/j.bmcl.2007.06.028
12003788 196265 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 278 2 2 2 2.7 O=C(O)c1n[nH]c2c1CC(c1cc(F)ccc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL1237148 196265 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 278 2 2 2 2.7 O=C(O)c1n[nH]c2c1CC(c1cc(F)ccc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL542000 196265 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 278 2 2 2 2.7 O=C(O)c1n[nH]c2c1CC(c1cc(F)ccc1F)CC2 10.1016/j.bmcl.2009.06.054
12002717 199198 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 302 2 2 4 2.1 Fc1ccc(F)c(C2CCc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.06.054
CHEMBL565163 199198 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 302 2 2 4 2.1 Fc1ccc(F)c(C2CCc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.06.054
15605357 75266 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 224 1 3 5 -0.8 CC(O)c1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
CHEMBL2036821 75266 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 224 1 3 5 -0.8 CC(O)c1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
145984088 165910 None 0 Rat Functional pEC50 = 5.9 5.9 -1 2
Agonist activity at rat GPR109A expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assayAgonist activity at rat GPR109A expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assay
ChEMBL 630 8 2 9 4.6 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3c(s2)C[Si](C)(c2c(OC)cccc2OC)CC3)cc1N1CCOCC1 10.1021/acs.jmedchem.7b00718
CHEMBL4248415 165910 None 0 Rat Functional pEC50 = 5.9 5.9 -1 2
Agonist activity at rat GPR109A expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assayAgonist activity at rat GPR109A expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assay
ChEMBL 630 8 2 9 4.6 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3c(s2)C[Si](C)(c2c(OC)cccc2OC)CC3)cc1N1CCOCC1 10.1021/acs.jmedchem.7b00718
16048995 94708 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 375 3 2 3 3.9 O=C(O)c1ccccc1NC(=O)N1CCN(c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL252505 94708 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 375 3 2 3 3.9 O=C(O)c1ccccc1NC(=O)N1CCN(c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2007.10.055
16048992 94735 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 403 4 2 5 3.2 O=C(O)c1ccccc1NC(=O)N1CCN(c2nccc(-c3ccccc3)n2)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL252707 94735 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 403 4 2 5 3.2 O=C(O)c1ccccc1NC(=O)N1CCN(c2nccc(-c3ccccc3)n2)CC1 10.1016/j.bmcl.2007.10.055
15605498 69951 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 366 4 1 5 3.0 CCc1cc(=O)oc2nc(OCc3ccccc3C(F)(F)F)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939024 69951 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 366 4 1 5 3.0 CCc1cc(=O)oc2nc(OCc3ccccc3C(F)(F)F)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
88707 93810 None 77 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 201 1 1 2 1.5 O=C(O)c1cncc(Br)c1 10.1016/j.bmcl.2007.06.028
CHEMBL247336 93810 None 77 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 201 1 1 2 1.5 O=C(O)c1cncc(Br)c1 10.1016/j.bmcl.2007.06.028
24954940 69971 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 336 4 1 5 2.3 CCC#CCOc1nc2oc(=O)cc(Cc3ccccc3)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
CHEMBL1939044 69971 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 336 4 1 5 2.3 CCC#CCOc1nc2oc(=O)cc(Cc3ccccc3)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
46890401 7289 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 460 7 3 4 4.9 O=C(CCc1ccc(-c2ccc(O)cc2)cc1)NC1=C(C(=O)O)CC(c2cccnc2F)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1086031 7289 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 460 7 3 4 4.9 O=C(CCc1ccc(-c2ccc(O)cc2)cc1)NC1=C(C(=O)O)CC(c2cccnc2F)CC1 10.1016/j.bmcl.2010.04.001
57393655 69943 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 266 5 1 6 0.5 CCc1cc(=O)oc2nc(OCCOC)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939016 69943 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 266 5 1 6 0.5 CCc1cc(=O)oc2nc(OCCOC)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
57392461 69893 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 240 1 1 5 -0.1 Cc1cc(=O)oc2nc([S+](C)[O-])[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1938888 69893 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 240 1 1 5 -0.1 Cc1cc(=O)oc2nc([S+](C)[O-])[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
11514051 76139 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 218 1 2 2 1.9 O=C(O)c1n[nH]c2c1CC1C2C12CCCC2 10.1021/jm2010964
CHEMBL2057610 76139 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 218 1 2 2 1.9 O=C(O)c1n[nH]c2c1CC1C2C12CCCC2 10.1021/jm2010964
135899178 16217 None 0 Rat Functional pEC50 = 6.9 6.9 -2 2
Agonist activity at rat GPR109A receptor assessed as GTPgammaS bindingAgonist activity at rat GPR109A receptor assessed as GTPgammaS binding
ChEMBL 315 5 1 4 2.7 O=c1[nH]c(COCCc2cccc(Cl)c2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1224219 16217 None 0 Rat Functional pEC50 = 6.9 6.9 -2 2
Agonist activity at rat GPR109A receptor assessed as GTPgammaS bindingAgonist activity at rat GPR109A receptor assessed as GTPgammaS binding
ChEMBL 315 5 1 4 2.7 O=c1[nH]c(COCCc2cccc(Cl)c2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
156016157 177883 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 430 8 3 4 3.2 CCCCN1CC(C(=O)O)=C(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)C1=O 10.1016/j.bmcl.2020.127105
CHEMBL4643073 177883 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 430 8 3 4 3.2 CCCCN1CC(C(=O)O)=C(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)C1=O 10.1016/j.bmcl.2020.127105
44579780 187266 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 442 8 1 5 4.8 COCC(Cc1ccccc1)NC(=O)c1cnc2c(-c3ccc(C(C)C)cc3)cnn2c1C 10.1016/j.bmcl.2008.08.039
CHEMBL492027 187266 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 442 8 1 5 4.8 COCC(Cc1ccccc1)NC(=O)c1cnc2c(-c3ccc(C(C)C)cc3)cnn2c1C 10.1016/j.bmcl.2008.08.039
117629482 2823 None 82 Human Functional pEC50 = 5.9 5.9 -4 4
Agonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assayAgonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.030
1588 2823 None 82 Human Functional pEC50 = 5.9 5.9 -4 4
Agonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assayAgonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.030
1594 2823 None 82 Human Functional pEC50 = 5.9 5.9 -4 4
Agonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assayAgonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.030
2835 2823 None 82 Human Functional pEC50 = 5.9 5.9 -4 4
Agonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assayAgonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.030
938 2823 None 82 Human Functional pEC50 = 5.9 5.9 -4 4
Agonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assayAgonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.030
CHEMBL573 2823 None 82 Human Functional pEC50 = 5.9 5.9 -4 4
Agonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assayAgonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.030
DB00627 2823 None 82 Human Functional pEC50 = 5.9 5.9 -4 4
Agonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assayAgonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.030
90645401 112544 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 337 4 3 3 3.6 O=C(/C=C/c1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
CHEMBL3298701 112544 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 337 4 3 3 3.6 O=C(/C=C/c1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
1591 131 None 45 Human Functional pEC50 = 5.9 5.9 33 2
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 168 4 2 2 1.5 CCCCc1cc(n[nH]1)C(=O)O 10.1016/j.bmcl.2007.06.028
6485181 131 None 45 Human Functional pEC50 = 5.9 5.9 33 2
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 168 4 2 2 1.5 CCCCc1cc(n[nH]1)C(=O)O 10.1016/j.bmcl.2007.06.028
CHEMBL428730 131 None 45 Human Functional pEC50 = 5.9 5.9 33 2
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 168 4 2 2 1.5 CCCCc1cc(n[nH]1)C(=O)O 10.1016/j.bmcl.2007.06.028
156020831 178175 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 386 8 4 8 1.5 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1cn(CCO)cc1C(=O)O 10.1016/j.bmcl.2020.127105
CHEMBL4647398 178175 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 386 8 4 8 1.5 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1cn(CCO)cc1C(=O)O 10.1016/j.bmcl.2020.127105
24954566 58049 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 310 4 1 4 2.9 O=c1cc(CCC2CCCC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
CHEMBL1672637 58049 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 310 4 1 4 2.9 O=c1cc(CCC2CCCC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
57413544 76134 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 208 3 2 3 0.6 COC[C@H]1[C@H]2c3[nH]nc(C(=O)O)c3C[C@H]21 10.1021/jm2010964
CHEMBL2057603 76134 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 208 3 2 3 0.6 COC[C@H]1[C@H]2c3[nH]nc(C(=O)O)c3C[C@H]21 10.1021/jm2010964
46889361 6833 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 228 3 2 4 1.1 C=CC[C@H]1[C@@H]2c3[nH]nc(-c4nnn[nH]4)c3C[C@@H]21 10.1016/j.bmcl.2010.03.062
CHEMBL1083988 6833 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 228 3 2 4 1.1 C=CC[C@H]1[C@@H]2c3[nH]nc(-c4nnn[nH]4)c3C[C@@H]21 10.1016/j.bmcl.2010.03.062
11660694 178173 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 369 5 3 3 4.5 O=C(CCc1ccc2c(Cl)c(O)ccc2c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2020.127105
CHEMBL4647392 178173 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 369 5 3 3 4.5 O=C(CCc1ccc2c(Cl)c(O)ccc2c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2020.127105
24955646 58051 None 0 Mouse Functional pEC50 = 7.8 7.8 -2 4
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 310 5 1 4 2.9 CC1(CCCc2cc(=O)oc3nc(C(F)F)[nH]c(=O)c23)CC1 10.1021/ml100251u
CHEMBL1672639 58051 None 0 Mouse Functional pEC50 = 7.8 7.8 -2 4
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 310 5 1 4 2.9 CC1(CCCc2cc(=O)oc3nc(C(F)F)[nH]c(=O)c23)CC1 10.1021/ml100251u
156019027 177902 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 415 8 3 5 4.5 CCCCn1cc(C(=O)O)c(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)n1 10.1016/j.bmcl.2020.127105
CHEMBL4643451 177902 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 415 8 3 5 4.5 CCCCn1cc(C(=O)O)c(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)n1 10.1016/j.bmcl.2020.127105
156020512 178209 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 403 9 3 8 2.3 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1cn(CCCF)cc1C(=O)O 10.1016/j.bmcl.2020.127105
CHEMBL4647933 178209 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 403 9 3 8 2.3 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1cn(CCCF)cc1C(=O)O 10.1016/j.bmcl.2020.127105
12430656 147822 None 55 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 129 1 1 3 0.8 O=C(O)c1cnsc1 10.1016/j.bmcl.2007.06.028
CHEMBL393226 147822 None 55 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 129 1 1 3 0.8 O=C(O)c1cnsc1 10.1016/j.bmcl.2007.06.028
136000669 61424 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 382 7 4 7 1.9 CN[C@@H](Cc1nc(-c2ccc(O)cc2)no1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1770179 61424 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 382 7 4 7 1.9 CN[C@@H](Cc1nc(-c2ccc(O)cc2)no1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
44433527 88568 None 8 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 150 1 2 4 -0.1 Cc1cc(-c2nnn[nH]2)n[nH]1 10.1016/j.bmcl.2007.07.101
CHEMBL235228 88568 None 8 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 150 1 2 4 -0.1 Cc1cc(-c2nnn[nH]2)n[nH]1 10.1016/j.bmcl.2007.07.101
44433531 88571 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 168 1 2 4 0.0 Cc1[nH]nc(-c2nnn[nH]2)c1F 10.1016/j.bmcl.2007.07.101
CHEMBL235231 88571 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 168 1 2 4 0.0 Cc1[nH]nc(-c2nnn[nH]2)c1F 10.1016/j.bmcl.2007.07.101
46889339 7182 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 214 2 2 4 0.7 C=C[C@@H]1[C@H]2Cc3c(-c4nnn[nH]4)n[nH]c3[C@@H]12 10.1016/j.bmcl.2010.03.062
CHEMBL1085534 7182 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 214 2 2 4 0.7 C=C[C@@H]1[C@H]2Cc3c(-c4nnn[nH]4)n[nH]c3[C@@H]12 10.1016/j.bmcl.2010.03.062
135416394 2560 None 43 Human Functional pEC50 = 7.8 7.8 15 3
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 10.1021/jm100022r
5788 2560 None 43 Human Functional pEC50 = 7.8 7.8 15 3
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 10.1021/jm100022r
73755154 2560 None 43 Human Functional pEC50 = 7.8 7.8 15 3
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 10.1021/jm100022r
CHEMBL1086657 2560 None 43 Human Functional pEC50 = 7.8 7.8 15 3
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 10.1021/jm100022r
70683908 75066 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 280 4 2 4 1.0 O=c1[nH]c(=O)c2c(CCCC3(F)CC3)cc(=O)oc2[nH]1 10.1021/ml200243g
CHEMBL2035002 75066 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 280 4 2 4 1.0 O=c1[nH]c(=O)c2c(CCCC3(F)CC3)cc(=O)oc2[nH]1 10.1021/ml200243g
59343651 75289 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 290 5 2 4 1.7 CCC1(CCCc2cc(=O)oc3[nH]c(=O)[nH]c(=O)c23)CC1 10.1021/ml200243g
CHEMBL2036959 75289 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 290 5 2 4 1.7 CCC1(CCCc2cc(=O)oc3[nH]c(=O)[nH]c(=O)c23)CC1 10.1021/ml200243g
57413367 76140 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 178 1 2 2 1.0 C[C@@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
CHEMBL2057614 76140 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 178 1 2 2 1.0 C[C@@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
137635325 156240 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 313 4 3 3 2.6 O=C(CCC#Cc1ccc(O)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4063682 156240 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 313 4 3 3 2.6 O=C(CCC#Cc1ccc(O)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
11322738 136853 None 0 Human Functional pEC50 = 5.8 5.8 13 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 252 2 1 3 2.1 CC1(c2cccc(Cl)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL374111 136853 None 0 Human Functional pEC50 = 5.8 5.8 13 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 252 2 1 3 2.1 CC1(c2cccc(Cl)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
136375410 177422 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 370 7 3 7 2.5 CCn1cc(NC(=O)CCc2nc(-c3ccc(O)cc3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
CHEMBL4636989 177422 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 370 7 3 7 2.5 CCn1cc(NC(=O)CCc2nc(-c3ccc(O)cc3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
16048770 94684 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 377 3 2 5 2.7 O=C(O)c1ccccc1NC(=O)N1CCN(c2cnc3ccccc3n2)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL252306 94684 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 377 3 2 5 2.7 O=C(O)c1ccccc1NC(=O)N1CCN(c2cnc3ccccc3n2)CC1 10.1016/j.bmcl.2007.10.055
59304808 75263 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 262 1 2 4 0.3 O=c1[nH]c(=O)c2c(CC(F)(F)F)cc(=O)oc2[nH]1 10.1021/ml200243g
CHEMBL2036816 75263 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 262 1 2 4 0.3 O=c1[nH]c(=O)c2c(CC(F)(F)F)cc(=O)oc2[nH]1 10.1021/ml200243g
135800177 146039 None 5 Mouse Functional pEC50 = 5.8 5.8 -24 2
Agonist activity at mouse GPR109A by [35S]GTP-gamma-S binding assayAgonist activity at mouse GPR109A by [35S]GTP-gamma-S binding assay
ChEMBL 353 6 3 6 2.7 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL391813 146039 None 5 Mouse Functional pEC50 = 5.8 5.8 -24 2
Agonist activity at mouse GPR109A by [35S]GTP-gamma-S binding assayAgonist activity at mouse GPR109A by [35S]GTP-gamma-S binding assay
ChEMBL 353 6 3 6 2.7 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1ccccc1C(=O)O 10.1021/jm700942d
135899325 16200 None 0 Rat Functional pEC50 = 5.8 5.8 -1 2
Agonist activity at rat GPR109A receptor assessed as GTPgammaS bindingAgonist activity at rat GPR109A receptor assessed as GTPgammaS binding
ChEMBL 299 5 1 4 2.2 O=c1[nH]c(COCCc2ccc(F)cc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1224147 16200 None 0 Rat Functional pEC50 = 5.8 5.8 -1 2
Agonist activity at rat GPR109A receptor assessed as GTPgammaS bindingAgonist activity at rat GPR109A receptor assessed as GTPgammaS binding
ChEMBL 299 5 1 4 2.2 O=c1[nH]c(COCCc2ccc(F)cc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
1592 144 None 71 Human Functional pEC50 = 4.8 4.8 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 137 1 1 2 1.1 Cc1cc(cnc1)C(=O)O 10.1016/j.bmcl.2007.06.028
256208 144 None 71 Human Functional pEC50 = 4.8 4.8 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 137 1 1 2 1.1 Cc1cc(cnc1)C(=O)O 10.1016/j.bmcl.2007.06.028
CHEMBL247132 144 None 71 Human Functional pEC50 = 4.8 4.8 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 137 1 1 2 1.1 Cc1cc(cnc1)C(=O)O 10.1016/j.bmcl.2007.06.028
44441302 93408 None 23 Human Functional pEC50 = 4.8 4.8 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 166 2 2 2 1.4 O=C(O)c1cc(C2CCC2)n[nH]1 10.1016/j.bmcl.2007.06.028
CHEMBL245491 93408 None 23 Human Functional pEC50 = 4.8 4.8 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 166 2 2 2 1.4 O=C(O)c1cc(C2CCC2)n[nH]1 10.1016/j.bmcl.2007.06.028
57412217 76375 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 206 3 2 2 1.8 CCC[C@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@H]12 10.1021/jm2010964
CHEMBL2059223 76375 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 206 3 2 2 1.8 CCC[C@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@H]12 10.1021/jm2010964
11159621 2548 None 38 Human Functional pEC50 = 5.8 5.8 -1 3
Agonist activity against human GPR109a assessed as forskolin-induced cAMP accumulationAgonist activity against human GPR109a assessed as forskolin-induced cAMP accumulation
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
5784 2548 None 38 Human Functional pEC50 = 5.8 5.8 -1 3
Agonist activity against human GPR109a assessed as forskolin-induced cAMP accumulationAgonist activity against human GPR109a assessed as forskolin-induced cAMP accumulation
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
CHEMBL456145 2548 None 38 Human Functional pEC50 = 5.8 5.8 -1 3
Agonist activity against human GPR109a assessed as forskolin-induced cAMP accumulationAgonist activity against human GPR109a assessed as forskolin-induced cAMP accumulation
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
DB05939 2548 None 38 Human Functional pEC50 = 5.8 5.8 -1 3
Agonist activity against human GPR109a assessed as forskolin-induced cAMP accumulationAgonist activity against human GPR109a assessed as forskolin-induced cAMP accumulation
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
145957566 162381 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 426 3 1 5 5.0 COc1ccc(-c2cc3cc(C4Nc5ccccc5C(=O)N4C)cc(C)c3oc2=O)cc1 10.1016/j.ejmech.2018.04.037
CHEMBL4164140 162381 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 426 3 1 5 5.0 COc1ccc(-c2cc3cc(C4Nc5ccccc5C(=O)N4C)cc(C)c3oc2=O)cc1 10.1016/j.ejmech.2018.04.037
145957566 162381 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 426 3 1 5 5.0 COc1ccc(-c2cc3cc(C4Nc5ccccc5C(=O)N4C)cc(C)c3oc2=O)cc1 10.1016/j.ejmech.2018.04.037
CHEMBL4164140 162381 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 426 3 1 5 5.0 COc1ccc(-c2cc3cc(C4Nc5ccccc5C(=O)N4C)cc(C)c3oc2=O)cc1 10.1016/j.ejmech.2018.04.037
21660892 147606 None 0 Human Functional pEC50 = 4.8 4.8 - 1
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 136 1 2 4 -0.4 c1cc(-c2nnn[nH]2)n[nH]1 10.1016/j.bmcl.2007.07.101
CHEMBL393063 147606 None 0 Human Functional pEC50 = 4.8 4.8 - 1
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 136 1 2 4 -0.4 c1cc(-c2nnn[nH]2)n[nH]1 10.1016/j.bmcl.2007.07.101
136086823 6971 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 400 8 3 7 2.8 CCCC1CCC(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
CHEMBL1084576 6971 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 400 8 3 7 2.8 CCCC1CCC(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
15605571 75261 None 0 Human Functional pEC50 = 7.8 7.8 -3 5
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 236 3 2 4 0.5 CCCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
CHEMBL2036813 75261 None 0 Human Functional pEC50 = 7.8 7.8 -3 5
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 236 3 2 4 0.5 CCCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
117629482 2823 None 82 Human Functional pEC50 = 7.8 7.8 -4 4
Agonist activity at GPR109A (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 15 mins by fluorescence assayAgonist activity at GPR109A (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 15 mins by fluorescence assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/acs.jmedchem.8b00435
1588 2823 None 82 Human Functional pEC50 = 7.8 7.8 -4 4
Agonist activity at GPR109A (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 15 mins by fluorescence assayAgonist activity at GPR109A (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 15 mins by fluorescence assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/acs.jmedchem.8b00435
1594 2823 None 82 Human Functional pEC50 = 7.8 7.8 -4 4
Agonist activity at GPR109A (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 15 mins by fluorescence assayAgonist activity at GPR109A (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 15 mins by fluorescence assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/acs.jmedchem.8b00435
2835 2823 None 82 Human Functional pEC50 = 7.8 7.8 -4 4
Agonist activity at GPR109A (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 15 mins by fluorescence assayAgonist activity at GPR109A (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 15 mins by fluorescence assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/acs.jmedchem.8b00435
938 2823 None 82 Human Functional pEC50 = 7.8 7.8 -4 4
Agonist activity at GPR109A (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 15 mins by fluorescence assayAgonist activity at GPR109A (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 15 mins by fluorescence assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/acs.jmedchem.8b00435
CHEMBL573 2823 None 82 Human Functional pEC50 = 7.8 7.8 -4 4
Agonist activity at GPR109A (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 15 mins by fluorescence assayAgonist activity at GPR109A (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 15 mins by fluorescence assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/acs.jmedchem.8b00435
DB00627 2823 None 82 Human Functional pEC50 = 7.8 7.8 -4 4
Agonist activity at GPR109A (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 15 mins by fluorescence assayAgonist activity at GPR109A (unknown origin) assessed as inhibition of forskolin-mediated cAMP accumulation after 15 mins by fluorescence assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/acs.jmedchem.8b00435
135399731 184263 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 391 5 3 5 3.2 Cn1nc2c(c1CCC(=O)Nc1ccccc1C(=O)O)CCc1cc(O)ccc1-2 10.1021/jm900151e
CHEMBL482963 184263 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 391 5 3 5 3.2 Cn1nc2c(c1CCC(=O)Nc1ccccc1C(=O)O)CCc1cc(O)ccc1-2 10.1021/jm900151e
70681781 75265 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 288 2 2 4 0.9 O=c1[nH]c(=O)c2c(Cc3ccc(F)cc3)cc(=O)oc2[nH]1 10.1021/ml200243g
CHEMBL2036820 75265 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 288 2 2 4 0.9 O=c1[nH]c(=O)c2c(Cc3ccc(F)cc3)cc(=O)oc2[nH]1 10.1021/ml200243g
136127010 16093 None 13 Human Functional pEC50 = 5.8 5.8 -9 2
Agonist activity at human GPR109A receptor assessed as GTPgammaS bindingAgonist activity at human GPR109A receptor assessed as GTPgammaS binding
ChEMBL 215 0 1 3 1.3 O=c1[nH]c(C(F)(F)F)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1223819 16093 None 13 Human Functional pEC50 = 5.8 5.8 -9 2
Agonist activity at human GPR109A receptor assessed as GTPgammaS bindingAgonist activity at human GPR109A receptor assessed as GTPgammaS binding
ChEMBL 215 0 1 3 1.3 O=c1[nH]c(C(F)(F)F)nc2ncccc12 10.1016/j.bmcl.2010.07.108
16048843 154480 None 0 Human Functional pEC50 = 4.8 4.8 - 1
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 392 3 3 6 2.3 Nc1ccc2nc(N3CCN(C(=O)Nc4ccccc4C(=O)O)CC3)cnc2c1 10.1016/j.bmcl.2007.10.055
CHEMBL398762 154480 None 0 Human Functional pEC50 = 4.8 4.8 - 1
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 392 3 3 6 2.3 Nc1ccc2nc(N3CCN(C(=O)Nc4ccccc4C(=O)O)CC3)cnc2c1 10.1016/j.bmcl.2007.10.055
24953857 69973 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 342 5 1 5 2.8 CCC#CCOc1nc2oc(=O)cc(CCC3CCCC3)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
CHEMBL1939046 69973 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 342 5 1 5 2.8 CCC#CCOc1nc2oc(=O)cc(CCC3CCCC3)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
57400598 69967 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 328 3 1 5 2.4 CCc1cc(=O)oc2nc(OCC#CC3CCCCC3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939040 69967 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 328 3 1 5 2.4 CCc1cc(=O)oc2nc(OCC#CC3CCCCC3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
57413446 76374 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 206 3 2 2 1.8 CCC[C@@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
CHEMBL2059222 76374 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 206 3 2 2 1.8 CCC[C@@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
24954572 69969 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 290 4 2 6 0.2 CCc1cc(=O)oc2nc(OCC#CCCO)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939042 69969 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 290 4 2 6 0.2 CCc1cc(=O)oc2nc(OCC#CCCO)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
44579646 187071 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 432 7 1 5 4.8 Cc1c(C(=O)NCCOc2ccccc2F)cnc2c(-c3ccc(C(C)C)cc3)cnn12 10.1016/j.bmcl.2008.08.039
CHEMBL490413 187071 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 432 7 1 5 4.8 Cc1c(C(=O)NCCOc2ccccc2F)cnc2c(-c3ccc(C(C)C)cc3)cnn12 10.1016/j.bmcl.2008.08.039
13153555 93916 None 26 Human Functional pEC50 = 5.8 5.8 42 2
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 182 5 2 2 1.8 CCCCCc1cc(C(=O)O)[nH]n1 10.1016/j.bmcl.2007.06.028
CHEMBL247921 93916 None 26 Human Functional pEC50 = 5.8 5.8 42 2
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 182 5 2 2 1.8 CCCCCc1cc(C(=O)O)[nH]n1 10.1016/j.bmcl.2007.06.028
676464 89910 None 48 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 154 3 2 2 1.1 CCCc1cc(C(=O)O)n[nH]1 10.1016/j.bmcl.2007.07.101
CHEMBL237788 89910 None 48 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 154 3 2 2 1.1 CCCc1cc(C(=O)O)n[nH]1 10.1016/j.bmcl.2007.07.101
44433529 88570 None 0 Human Functional pEC50 = 4.7 4.7 -5 2
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 176 2 2 4 0.5 c1c(-c2nnn[nH]2)n[nH]c1C1CC1 10.1016/j.bmcl.2007.07.101
CHEMBL235230 88570 None 0 Human Functional pEC50 = 4.7 4.7 -5 2
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 176 2 2 4 0.5 c1c(-c2nnn[nH]2)n[nH]c1C1CC1 10.1016/j.bmcl.2007.07.101
46889397 6727 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 232 3 2 5 0.1 COC[C@@H]1[C@H]2Cc3c(-c4nnn[nH]4)n[nH]c3[C@H]21 10.1016/j.bmcl.2010.03.062
CHEMBL1083688 6727 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 232 3 2 5 0.1 COC[C@@H]1[C@H]2Cc3c(-c4nnn[nH]4)n[nH]c3[C@H]21 10.1016/j.bmcl.2010.03.062
44433530 147612 None 0 Human Functional pEC50 = 4.7 4.7 -2 2
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 192 4 2 4 0.9 CCCCc1cc(-c2nnn[nH]2)n[nH]1 10.1016/j.bmcl.2007.07.101
CHEMBL393065 147612 None 0 Human Functional pEC50 = 4.7 4.7 -2 2
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 192 4 2 4 0.9 CCCCc1cc(-c2nnn[nH]2)n[nH]1 10.1016/j.bmcl.2007.07.101
135416384 184930 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 382 5 3 5 3.1 O=C(CCc1noc2c1CCc1cc(O)ccc1-2)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
CHEMBL485196 184930 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 382 5 3 5 3.1 O=C(CCc1noc2c1CCc1cc(O)ccc1-2)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
15605645 75270 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 250 4 2 4 0.9 CCCCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
CHEMBL2036825 75270 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 250 4 2 4 0.9 CCCCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
57397199 69941 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 298 4 1 5 2.0 CCc1cc(=O)oc2nc(OCc3ccccc3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939014 69941 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 298 4 1 5 2.0 CCc1cc(=O)oc2nc(OCc3ccccc3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
135899171 16177 None 0 Rat Functional pEC50 = 6.7 6.7 -18 3
Agonist activity at rat GPR109A receptor assessed as GTPgammaS bindingAgonist activity at rat GPR109A receptor assessed as GTPgammaS binding
ChEMBL 331 6 1 5 2.8 O=c1[nH]c(OCCCOc2ccccc2Cl)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1224070 16177 None 0 Rat Functional pEC50 = 6.7 6.7 -18 3
Agonist activity at rat GPR109A receptor assessed as GTPgammaS bindingAgonist activity at rat GPR109A receptor assessed as GTPgammaS binding
ChEMBL 331 6 1 5 2.8 O=c1[nH]c(OCCCOc2ccccc2Cl)nc2ncccc12 10.1016/j.bmcl.2010.07.108
137661636 159356 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 331 4 2 2 3.5 O=C(CCC#Cc1ccccc1Cl)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4099238 159356 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 331 4 2 2 3.5 O=C(CCC#Cc1ccccc1Cl)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
137662135 159444 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 367 6 2 2 4.5 O=C(CCc1ccc(-c2ccccc2F)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4100231 159444 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 367 6 2 2 4.5 O=C(CCc1ccc(-c2ccccc2F)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
44579779 187001 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 428 7 1 5 4.9 COCC(NC(=O)c1cnc2c(-c3ccc(C(C)C)cc3)cnn2c1C)c1ccccc1 10.1016/j.bmcl.2008.08.039
CHEMBL489787 187001 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 428 7 1 5 4.9 COCC(NC(=O)c1cnc2c(-c3ccc(C(C)C)cc3)cnn2c1C)c1ccccc1 10.1016/j.bmcl.2008.08.039
15986755 184224 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 339 5 3 3 3.5 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
CHEMBL482698 184224 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 339 5 3 3 3.5 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
16125020 137705 None 0 Human Functional pEC50 = 4.7 4.7 - 1
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 230 1 1 3 1.4 O=C(O)C1=CC(=O)C2(CCc3ccccc32)O1 10.1021/jm070022x
CHEMBL375753 137705 None 0 Human Functional pEC50 = 4.7 4.7 - 1
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 230 1 1 3 1.4 O=C(O)C1=CC(=O)C2(CCc3ccccc32)O1 10.1021/jm070022x
57413546 76138 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 222 4 2 3 1.0 CCOC[C@H]1[C@H]2c3[nH]nc(C(=O)O)c3C[C@H]21 10.1021/jm2010964
CHEMBL2057607 76138 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 222 4 2 3 1.0 CCOC[C@H]1[C@H]2c3[nH]nc(C(=O)O)c3C[C@H]21 10.1021/jm2010964
137645601 157943 None 0 Human Functional pEC50 = 4.7 4.7 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 299 6 2 2 3.2 O=C(/C=C/CCc1ccccc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4083723 157943 None 0 Human Functional pEC50 = 4.7 4.7 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 299 6 2 2 3.2 O=C(/C=C/CCc1ccccc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
57413542 76503 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 204 2 2 2 1.4 O=C(O)c1n[nH]c2c1C[C@@H]1[C@H]2[C@@H]1C1CC1 10.1021/jm2010964
CHEMBL2059829 76503 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 204 2 2 2 1.4 O=C(O)c1n[nH]c2c1C[C@@H]1[C@H]2[C@@H]1C1CC1 10.1021/jm2010964
56950369 3559 None 16 Human Functional pEC50 = 8.7 8.7 3 4
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 276 4 2 4 1.3 O=c1cc(CCCC2(C)CC2)c2c(o1)[nH]c(=O)[nH]c2=O 10.1021/ml200243g
8469 3559 None 16 Human Functional pEC50 = 8.7 8.7 3 4
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 276 4 2 4 1.3 O=c1cc(CCCC2(C)CC2)c2c(o1)[nH]c(=O)[nH]c2=O 10.1021/ml200243g
CHEMBL2036958 3559 None 16 Human Functional pEC50 = 8.7 8.7 3 4
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 276 4 2 4 1.3 O=c1cc(CCCC2(C)CC2)c2c(o1)[nH]c(=O)[nH]c2=O 10.1021/ml200243g
DB12433 3559 None 16 Human Functional pEC50 = 8.7 8.7 3 4
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 276 4 2 4 1.3 O=c1cc(CCCC2(C)CC2)c2c(o1)[nH]c(=O)[nH]c2=O 10.1021/ml200243g
59343664 75282 None 0 Rat Functional pEC50 = 8.7 8.7 1 4
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 272 4 2 4 0.8 O=c1[nH]c(=O)c2c(CCCC(F)F)cc(=O)oc2[nH]1 10.1021/ml200243g
CHEMBL2036951 75282 None 0 Rat Functional pEC50 = 8.7 8.7 1 4
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 272 4 2 4 0.8 O=c1[nH]c(=O)c2c(CCCC(F)F)cc(=O)oc2[nH]1 10.1021/ml200243g
15604637 75286 None 0 Rat Functional pEC50 = 8.7 8.7 1 3
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 262 4 2 4 0.9 O=c1[nH]c(=O)c2c(CCCC3CC3)cc(=O)oc2[nH]1 10.1021/ml200243g
CHEMBL2036955 75286 None 0 Rat Functional pEC50 = 8.7 8.7 1 3
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 262 4 2 4 0.9 O=c1[nH]c(=O)c2c(CCCC3CC3)cc(=O)oc2[nH]1 10.1021/ml200243g
117629482 2823 None 82 Human Functional pEC50 = 7.7 7.7 -4 4
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
1588 2823 None 82 Human Functional pEC50 = 7.7 7.7 -4 4
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
1594 2823 None 82 Human Functional pEC50 = 7.7 7.7 -4 4
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
2835 2823 None 82 Human Functional pEC50 = 7.7 7.7 -4 4
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
938 2823 None 82 Human Functional pEC50 = 7.7 7.7 -4 4
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
CHEMBL573 2823 None 82 Human Functional pEC50 = 7.7 7.7 -4 4
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
DB00627 2823 None 82 Human Functional pEC50 = 7.7 7.7 -4 4
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
117629482 2823 None 82 Human Functional pEC50 = 7.7 7.7 -4 4
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
1588 2823 None 82 Human Functional pEC50 = 7.7 7.7 -4 4
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
1594 2823 None 82 Human Functional pEC50 = 7.7 7.7 -4 4
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
2835 2823 None 82 Human Functional pEC50 = 7.7 7.7 -4 4
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
938 2823 None 82 Human Functional pEC50 = 7.7 7.7 -4 4
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
CHEMBL573 2823 None 82 Human Functional pEC50 = 7.7 7.7 -4 4
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
DB00627 2823 None 82 Human Functional pEC50 = 7.7 7.7 -4 4
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
11379903 84305 None 0 Human Functional pEC50 = 6.7 6.7 6 2
Activity at GPR109a assessed as inhibition of forskolin-stimulated cAMP productionActivity at GPR109a assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 258 2 1 4 2.2 CC1(c2csc(Cl)c2)OC(C(=O)O)=CC1=O 10.1021/jm800896z
CHEMBL221282 84305 None 0 Human Functional pEC50 = 6.7 6.7 6 2
Activity at GPR109a assessed as inhibition of forskolin-stimulated cAMP productionActivity at GPR109a assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 258 2 1 4 2.2 CC1(c2csc(Cl)c2)OC(C(=O)O)=CC1=O 10.1021/jm800896z
11379903 84305 None 0 Human Functional pEC50 = 6.7 6.7 6 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 258 2 1 4 2.2 CC1(c2csc(Cl)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL221282 84305 None 0 Human Functional pEC50 = 6.7 6.7 6 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 258 2 1 4 2.2 CC1(c2csc(Cl)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
11206816 84941 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 222 2 1 3 1.8 CC1(C2=CCCCC2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL223706 84941 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 222 2 1 3 1.8 CC1(C2=CCCCC2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
136375465 177238 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 357 6 3 8 1.4 Cn1cc(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
CHEMBL4633857 177238 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 357 6 3 8 1.4 Cn1cc(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
46889399 6835 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 242 1 2 4 1.4 C1CCC2(C1)[C@H]1Cc3c(-c4nnn[nH]4)n[nH]c3[C@H]12 10.1016/j.bmcl.2010.03.062
CHEMBL1083990 6835 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 242 1 2 4 1.4 C1CCC2(C1)[C@H]1Cc3c(-c4nnn[nH]4)n[nH]c3[C@H]12 10.1016/j.bmcl.2010.03.062
28400056 152312 None 1 Human Functional pEC50 = 4.7 4.7 -74 2
Agonist activity at human GPR109a receptor transfected in CHOK1 cells assessed as reversal of forskolin induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109a receptor transfected in CHOK1 cells assessed as reversal of forskolin induced cAMP elevating effect by whole cell assay
ChEMBL 208 5 2 3 2.4 CCC(CC)Nc1ccc(C(=O)O)cn1 10.1016/j.bmcl.2007.09.058
CHEMBL396879 152312 None 1 Human Functional pEC50 = 4.7 4.7 -74 2
Agonist activity at human GPR109a receptor transfected in CHOK1 cells assessed as reversal of forskolin induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109a receptor transfected in CHOK1 cells assessed as reversal of forskolin induced cAMP elevating effect by whole cell assay
ChEMBL 208 5 2 3 2.4 CCC(CC)Nc1ccc(C(=O)O)cn1 10.1016/j.bmcl.2007.09.058
57398904 69944 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 280 6 1 6 0.9 CCOCCOc1nc2oc(=O)cc(CC)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
CHEMBL1939017 69944 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 280 6 1 6 0.9 CCOCCOc1nc2oc(=O)cc(CC)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
135416388 7526 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 358 6 3 7 1.8 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CCCC1 10.1021/jm100022r
CHEMBL1087302 7526 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 358 6 3 7 1.8 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CCCC1 10.1021/jm100022r
135416388 7526 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 358 6 3 7 1.8 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.001
CHEMBL1087302 7526 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 358 6 3 7 1.8 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.001
11672811 1001 None 4 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 188 1 2 4 0.2 n1nnc([nH]1)c1n[nH]c2c1CC1C2C1 10.1016/j.bmcl.2010.03.062
5790 1001 None 4 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 188 1 2 4 0.2 n1nnc([nH]1)c1n[nH]c2c1CC1C2C1 10.1016/j.bmcl.2010.03.062
CHEMBL1169573 1001 None 4 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 188 1 2 4 0.2 n1nnc([nH]1)c1n[nH]c2c1CC1C2C1 10.1016/j.bmcl.2010.03.062
11311474 165877 None 0 Human Functional pEC50 = 5.7 5.7 1 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 258 2 1 4 2.2 CC1(c2ccc(Cl)s2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL424750 165877 None 0 Human Functional pEC50 = 5.7 5.7 1 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 258 2 1 4 2.2 CC1(c2ccc(Cl)s2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
24741306 167052 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 334 6 3 2 4.0 O=C(CCc1ccc(-c2ccc[nH]2)cc1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL428724 167052 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 334 6 3 2 4.0 O=C(CCc1ccc(-c2ccc[nH]2)cc1)Nc1ccccc1C(=O)O 10.1021/jm700942d
44579761 187264 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 428 7 1 5 4.9 Cc1ccc(OCCNC(=O)c2cnc3c(-c4ccc(C(C)C)cc4)cnn3c2C)cc1 10.1016/j.bmcl.2008.08.039
CHEMBL492019 187264 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 428 7 1 5 4.9 Cc1ccc(OCCNC(=O)c2cnc3c(-c4ccc(C(C)C)cc4)cnn3c2C)cc1 10.1016/j.bmcl.2008.08.039
44441322 147651 None 1 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 196 3 2 3 1.5 CCCC1OCc2c1n[nH]c2C(=O)O 10.1016/j.bmcl.2007.06.028
CHEMBL393086 147651 None 1 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 196 3 2 3 1.5 CCCC1OCc2c1n[nH]c2C(=O)O 10.1016/j.bmcl.2007.06.028
145985690 165538 None 0 Rat Functional pEC50 = 5.7 5.7 -17 3
Agonist activity at rat GPR109A expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assayAgonist activity at rat GPR109A expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assay
ChEMBL 464 5 2 7 3.9 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3c(s2)CCCC3)cc1N1CCOCC1 10.1021/acs.jmedchem.7b00718
CHEMBL4239086 165538 None 0 Rat Functional pEC50 = 5.7 5.7 -17 3
Agonist activity at rat GPR109A expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assayAgonist activity at rat GPR109A expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assay
ChEMBL 464 5 2 7 3.9 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3c(s2)CCCC3)cc1N1CCOCC1 10.1021/acs.jmedchem.7b00718
57412211 76143 None 1 Human Functional pEC50 = 4.7 4.7 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 178 1 2 2 1.0 C[C@H]1[C@@H]2c3[nH]nc(C(=O)O)c3C[C@@H]21 10.1021/jm2010964
CHEMBL2057617 76143 None 1 Human Functional pEC50 = 4.7 4.7 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 178 1 2 2 1.0 C[C@H]1[C@@H]2c3[nH]nc(C(=O)O)c3C[C@@H]21 10.1021/jm2010964
53238781 1027 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 389 6 3 7 1.4 C[C@@H]1CCC(=C(C1)NC(=O)[C@H](Cc1onc(n1)c1ccc(cn1)F)N)C(=O)O 10.1016/j.bmcl.2010.11.116
5789 1027 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 389 6 3 7 1.4 C[C@@H]1CCC(=C(C1)NC(=O)[C@H](Cc1onc(n1)c1ccc(cn1)F)N)C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1770358 1027 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 389 6 3 7 1.4 C[C@@H]1CCC(=C(C1)NC(=O)[C@H](Cc1onc(n1)c1ccc(cn1)F)N)C(=O)O 10.1016/j.bmcl.2010.11.116
135416392 7439 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 372 6 3 7 2.0 CC(Cc1nc(-c2ccc(O)cn2)no1)C(=O)NC1=C(C(=O)O)CCCC1 10.1021/jm100022r
CHEMBL1086656 7439 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 372 6 3 7 2.0 CC(Cc1nc(-c2ccc(O)cn2)no1)C(=O)NC1=C(C(=O)O)CCCC1 10.1021/jm100022r
24953854 69974 None 0 Human Functional pEC50 = 7.7 7.7 1 2
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 328 5 1 5 2.4 CCC#CCOc1nc2oc(=O)cc(CCC3CCC3)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
CHEMBL1939047 69974 None 0 Human Functional pEC50 = 7.7 7.7 1 2
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 328 5 1 5 2.4 CCC#CCOc1nc2oc(=O)cc(CCC3CCC3)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
46890539 7042 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 472 7 2 6 3.9 O=C(CCc1nc(-c2ccc(F)cn2)no1)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1084841 7042 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 472 7 2 6 3.9 O=C(CCc1nc(-c2ccc(F)cn2)no1)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
57412216 76145 None 1 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 192 2 2 2 1.4 CC[C@@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
CHEMBL2057619 76145 None 1 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 192 2 2 2 1.4 CC[C@@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
59304931 75262 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 222 1 2 4 0.3 CC(C)c1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
CHEMBL2036814 75262 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 222 1 2 4 0.3 CC(C)c1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
44441326 150266 None 2 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 170 1 2 3 0.8 O=C(O)c1[nH]nc2c1SCC2 10.1016/j.bmcl.2007.06.028
CHEMBL395177 150266 None 2 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 170 1 2 3 0.8 O=C(O)c1[nH]nc2c1SCC2 10.1016/j.bmcl.2007.06.028
16048921 155107 None 0 Human Functional pEC50 = 4.7 4.7 - 1
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 366 3 2 5 2.9 O=C(O)c1ccccc1NC(=O)N1CCN(c2nc3ccccc3o2)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL401470 155107 None 0 Human Functional pEC50 = 4.7 4.7 - 1
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 366 3 2 5 2.9 O=C(O)c1ccccc1NC(=O)N1CCN(c2nc3ccccc3o2)CC1 10.1016/j.bmcl.2007.10.055
44441302 93408 None 23 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 166 2 2 2 1.4 O=C(O)c1cc(C2CCC2)n[nH]1 10.1016/j.bmcl.2007.07.101
CHEMBL245491 93408 None 23 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 166 2 2 2 1.4 O=C(O)c1cc(C2CCC2)n[nH]1 10.1016/j.bmcl.2007.07.101
57413447 76376 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 220 4 2 2 2.2 CCCC[C@@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
CHEMBL2059224 76376 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 220 4 2 2 2.2 CCCC[C@@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
57412300 76502 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 204 3 2 2 1.6 C=CC[C@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@H]12 10.1021/jm2010964
CHEMBL2059828 76502 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 204 3 2 2 1.6 C=CC[C@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@H]12 10.1021/jm2010964
46890537 7040 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 454 7 2 6 3.8 O=C(CCc1nc(-c2ccc(F)cn2)no1)NC1=C(C(=O)O)CC(c2cccc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1084839 7040 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 454 7 2 6 3.8 O=C(CCc1nc(-c2ccc(F)cn2)no1)NC1=C(C(=O)O)CC(c2cccc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
59304949 75275 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 250 3 2 4 1.1 CCCC(C)c1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
CHEMBL2036830 75275 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 250 3 2 4 1.1 CCCC(C)c1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
137647495 157948 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 365 6 3 3 4.0 O=C(CCc1ccc(-c2cccc(O)c2)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4083762 157948 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 365 6 3 3 4.0 O=C(CCc1ccc(-c2cccc(O)c2)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
11159621 2548 None 38 Human Functional pEC50 = 5.6 5.6 -1 3
Agonist activity against human GPR109a assessed as GTPgammaS bindingAgonist activity against human GPR109a assessed as GTPgammaS binding
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
5784 2548 None 38 Human Functional pEC50 = 5.6 5.6 -1 3
Agonist activity against human GPR109a assessed as GTPgammaS bindingAgonist activity against human GPR109a assessed as GTPgammaS binding
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
CHEMBL456145 2548 None 38 Human Functional pEC50 = 5.6 5.6 -1 3
Agonist activity against human GPR109a assessed as GTPgammaS bindingAgonist activity against human GPR109a assessed as GTPgammaS binding
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
DB05939 2548 None 38 Human Functional pEC50 = 5.6 5.6 -1 3
Agonist activity against human GPR109a assessed as GTPgammaS bindingAgonist activity against human GPR109a assessed as GTPgammaS binding
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
11159621 2548 None 38 Rat Functional pEC50 = 5.6 5.6 -2 3
Agonist activity against rat GPR109a assessed as GTPgammaS bindingAgonist activity against rat GPR109a assessed as GTPgammaS binding
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
5784 2548 None 38 Rat Functional pEC50 = 5.6 5.6 -2 3
Agonist activity against rat GPR109a assessed as GTPgammaS bindingAgonist activity against rat GPR109a assessed as GTPgammaS binding
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
CHEMBL456145 2548 None 38 Rat Functional pEC50 = 5.6 5.6 -2 3
Agonist activity against rat GPR109a assessed as GTPgammaS bindingAgonist activity against rat GPR109a assessed as GTPgammaS binding
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
DB05939 2548 None 38 Rat Functional pEC50 = 5.6 5.6 -2 3
Agonist activity against rat GPR109a assessed as GTPgammaS bindingAgonist activity against rat GPR109a assessed as GTPgammaS binding
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
44579648 187072 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 448 7 1 5 5.3 Cc1c(C(=O)NCCOc2ccc(Cl)cc2)cnc2c(-c3ccc(C(C)C)cc3)cnn12 10.1016/j.bmcl.2008.08.039
CHEMBL490414 187072 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 448 7 1 5 5.3 Cc1c(C(=O)NCCOc2ccc(Cl)cc2)cnc2c(-c3ccc(C(C)C)cc3)cnn12 10.1016/j.bmcl.2008.08.039
44580036 187207 None 1 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 464 7 1 5 5.8 Cc1c(C(=O)NCCOc2ccc3ccccc3c2)cnc2c(-c3ccc(C(C)C)cc3)cnn12 10.1016/j.bmcl.2008.08.039
CHEMBL491439 187207 None 1 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 464 7 1 5 5.8 Cc1c(C(=O)NCCOc2ccc3ccccc3c2)cnc2c(-c3ccc(C(C)C)cc3)cnn12 10.1016/j.bmcl.2008.08.039
12003791 194954 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 261 2 2 3 1.9 O=C(O)c1n[nH]c2c1CC(c1cccnc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL1237147 194954 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 261 2 2 3 1.9 O=C(O)c1n[nH]c2c1CC(c1cccnc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL539398 194954 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 261 2 2 3 1.9 O=C(O)c1n[nH]c2c1CC(c1cccnc1F)CC2 10.1016/j.bmcl.2009.06.054
11390981 136637 None 0 Human Functional pEC50 = 4.6 4.6 - 1
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 248 3 1 4 1.5 COc1cccc(C2(C)OC(C(=O)O)=CC2=O)c1 10.1021/jm070022x
CHEMBL373752 136637 None 0 Human Functional pEC50 = 4.6 4.6 - 1
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 248 3 1 4 1.5 COc1cccc(C2(C)OC(C(=O)O)=CC2=O)c1 10.1021/jm070022x
2761046 148871 None 72 Human Functional pEC50 = 4.6 4.6 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 124 1 1 3 0.2 O=C(O)c1ccnnc1 10.1016/j.bmcl.2007.06.028
CHEMBL394068 148871 None 72 Human Functional pEC50 = 4.6 4.6 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 124 1 1 3 0.2 O=C(O)c1ccnnc1 10.1016/j.bmcl.2007.06.028
46889362 7186 None 0 Human Functional pEC50 = 4.6 4.6 - 1
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 244 3 2 4 1.5 CC(C)C[C@H]1C2Cc3c(-c4nnn[nH]4)n[nH]c3[C@H]21 10.1016/j.bmcl.2010.03.062
CHEMBL1085538 7186 None 0 Human Functional pEC50 = 4.6 4.6 - 1
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 244 3 2 4 1.5 CC(C)C[C@H]1C2Cc3c(-c4nnn[nH]4)n[nH]c3[C@H]21 10.1016/j.bmcl.2010.03.062
145949989 163055 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 410 2 1 4 5.3 Cc1ccc(-c2cc3cc(C4Nc5ccccc5C(=O)N4C)cc(C)c3oc2=O)cc1 10.1016/j.ejmech.2018.04.037
CHEMBL4174798 163055 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 410 2 1 4 5.3 Cc1ccc(-c2cc3cc(C4Nc5ccccc5C(=O)N4C)cc(C)c3oc2=O)cc1 10.1016/j.ejmech.2018.04.037
145949989 163055 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 410 2 1 4 5.3 Cc1ccc(-c2cc3cc(C4Nc5ccccc5C(=O)N4C)cc(C)c3oc2=O)cc1 10.1016/j.ejmech.2018.04.037
CHEMBL4174798 163055 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 410 2 1 4 5.3 Cc1ccc(-c2cc3cc(C4Nc5ccccc5C(=O)N4C)cc(C)c3oc2=O)cc1 10.1016/j.ejmech.2018.04.037
46889320 6656 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 202 1 2 4 0.5 C[C@@H]1[C@@H]2c3[nH]nc(-c4nnn[nH]4)c3C[C@H]12 10.1016/j.bmcl.2010.03.062
CHEMBL1083380 6656 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 202 1 2 4 0.5 C[C@@H]1[C@@H]2c3[nH]nc(-c4nnn[nH]4)c3C[C@H]12 10.1016/j.bmcl.2010.03.062
57390148 69954 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 399 5 1 6 3.6 CCc1cc(=O)oc2nc(OCc3ccccc3-c3cccc(C#N)c3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939027 69954 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 399 5 1 6 3.6 CCc1cc(=O)oc2nc(OCc3ccccc3-c3cccc(C#N)c3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
42625218 184285 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 398 5 3 5 3.8 O=C(CCc1noc2c1ccc1c(F)c(O)ccc12)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
CHEMBL483140 184285 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 398 5 3 5 3.8 O=C(CCc1noc2c1ccc1c(F)c(O)ccc12)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
135416388 7526 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 358 6 3 7 1.8 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.11.116
CHEMBL1087302 7526 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 358 6 3 7 1.8 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.11.116
9822 145726 None 78 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 126 1 2 2 0.4 Cc1cc(C(=O)O)n[nH]1 10.1016/j.bmcl.2007.07.101
CHEMBL391574 145726 None 78 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 126 1 2 2 0.4 Cc1cc(C(=O)O)n[nH]1 10.1016/j.bmcl.2007.07.101
11436345 143 None 0 Human Functional pEC50 = 6.6 6.6 1 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 238 2 1 4 1.8 Cc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 10.1021/jm070022x
1599 143 None 0 Human Functional pEC50 = 6.6 6.6 1 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 238 2 1 4 1.8 Cc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 10.1021/jm070022x
CHEMBL424938 143 None 0 Human Functional pEC50 = 6.6 6.6 1 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 238 2 1 4 1.8 Cc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 10.1021/jm070022x
24741312 89433 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 358 6 3 7 2.3 O=C(CCc1cnc(-n2cc(O)cn2)s1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL237036 89433 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 358 6 3 7 2.3 O=C(CCc1cnc(-n2cc(O)cn2)s1)Nc1ccccc1C(=O)O 10.1021/jm700942d
135416394 2560 None 43 Mouse Functional pEC50 = 6.6 6.6 -15 3
Agonist activity at mouse GPR109A receptor by [35S]GTPgammaS binding assayAgonist activity at mouse GPR109A receptor by [35S]GTPgammaS binding assay
ChEMBL 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 10.1021/jm100022r
5788 2560 None 43 Mouse Functional pEC50 = 6.6 6.6 -15 3
Agonist activity at mouse GPR109A receptor by [35S]GTPgammaS binding assayAgonist activity at mouse GPR109A receptor by [35S]GTPgammaS binding assay
ChEMBL 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 10.1021/jm100022r
73755154 2560 None 43 Mouse Functional pEC50 = 6.6 6.6 -15 3
Agonist activity at mouse GPR109A receptor by [35S]GTPgammaS binding assayAgonist activity at mouse GPR109A receptor by [35S]GTPgammaS binding assay
ChEMBL 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 10.1021/jm100022r
CHEMBL1086657 2560 None 43 Mouse Functional pEC50 = 6.6 6.6 -15 3
Agonist activity at mouse GPR109A receptor by [35S]GTPgammaS binding assayAgonist activity at mouse GPR109A receptor by [35S]GTPgammaS binding assay
ChEMBL 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 10.1021/jm100022r
11183678 84806 None 0 Human Functional pEC50 = 5.6 5.6 1 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 224 2 1 4 1.5 CC1(c2ccsc2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL223140 84806 None 0 Human Functional pEC50 = 5.6 5.6 1 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 224 2 1 4 1.5 CC1(c2ccsc2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
11148966 1122 None 2 Human Functional pEC50 = 4.6 4.6 -4 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 232 3 1 3 1.9 CCC1(OC(=CC1=O)C(=O)O)c1ccccc1 10.1021/jm070022x
1598 1122 None 2 Human Functional pEC50 = 4.6 4.6 -4 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 232 3 1 3 1.9 CCC1(OC(=CC1=O)C(=O)O)c1ccccc1 10.1021/jm070022x
CHEMBL436301 1122 None 2 Human Functional pEC50 = 4.6 4.6 -4 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 232 3 1 3 1.9 CCC1(OC(=CC1=O)C(=O)O)c1ccccc1 10.1021/jm070022x
46889336 7066 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 202 1 2 4 0.5 C[C@H]1[C@@H]2c3[nH]nc(-c4nnn[nH]4)c3C[C@@H]21 10.1016/j.bmcl.2010.03.062
CHEMBL1084950 7066 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 202 1 2 4 0.5 C[C@H]1[C@@H]2c3[nH]nc(-c4nnn[nH]4)c3C[C@@H]21 10.1016/j.bmcl.2010.03.062
24955288 58072 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 270 4 1 4 2.2 CCCCc1cc(=O)oc2nc(C(F)F)[nH]c(=O)c12 10.1021/ml100251u
CHEMBL1672750 58072 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 270 4 1 4 2.2 CCCCc1cc(=O)oc2nc(C(F)F)[nH]c(=O)c12 10.1021/ml100251u
46889363 7187 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 244 3 2 4 1.5 CC(C)C[C@H]1[C@@H]2c3[nH]nc(-c4nnn[nH]4)c3C[C@@H]21 10.1016/j.bmcl.2010.03.062
CHEMBL1085539 7187 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 244 3 2 4 1.5 CC(C)C[C@H]1[C@@H]2c3[nH]nc(-c4nnn[nH]4)c3C[C@@H]21 10.1016/j.bmcl.2010.03.062
57412302 76135 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 208 3 2 3 0.6 COC[C@@H]1[C@H]2c3[nH]nc(C(=O)O)c3C[C@@H]12 10.1021/jm2010964
CHEMBL2057604 76135 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 208 3 2 3 0.6 COC[C@@H]1[C@H]2c3[nH]nc(C(=O)O)c3C[C@@H]12 10.1021/jm2010964
135416392 7439 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 372 6 3 7 2.0 CC(Cc1nc(-c2ccc(O)cn2)no1)C(=O)NC1=C(C(=O)O)CCCC1 10.1021/jm100022r
CHEMBL1086656 7439 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 372 6 3 7 2.0 CC(Cc1nc(-c2ccc(O)cn2)no1)C(=O)NC1=C(C(=O)O)CCCC1 10.1021/jm100022r
46890538 7041 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 469 7 3 7 2.7 NC(Cc1nc(-c2ccc(F)cn2)no1)C(=O)NC1=C(C(=O)O)CC(c2cccc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1084840 7041 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 469 7 3 7 2.7 NC(Cc1nc(-c2ccc(F)cn2)no1)C(=O)NC1=C(C(=O)O)CC(c2cccc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
137632012 156748 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 311 3 3 3 2.3 O=C(/C=C/C#Cc1ccccc1O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4069406 156748 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 311 3 3 3 2.3 O=C(/C=C/C#Cc1ccccc1O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
11413114 137706 None 0 Human Functional pEC50 = 5.6 5.6 2 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 208 2 1 3 1.4 CC1(C2=CCCC2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL375754 137706 None 0 Human Functional pEC50 = 5.6 5.6 2 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 208 2 1 3 1.4 CC1(C2=CCCC2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
135899325 16200 None 0 Human Functional pEC50 = 5.6 5.6 1 2
Agonist activity at human GPR109A receptor assessed as GTPgammaS bindingAgonist activity at human GPR109A receptor assessed as GTPgammaS binding
ChEMBL 299 5 1 4 2.2 O=c1[nH]c(COCCc2ccc(F)cc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1224147 16200 None 0 Human Functional pEC50 = 5.6 5.6 1 2
Agonist activity at human GPR109A receptor assessed as GTPgammaS bindingAgonist activity at human GPR109A receptor assessed as GTPgammaS binding
ChEMBL 299 5 1 4 2.2 O=c1[nH]c(COCCc2ccc(F)cc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
44441311 93720 None 36 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 142 2 3 3 -0.4 O=C(O)c1cc(CO)n[nH]1 10.1016/j.bmcl.2007.06.028
CHEMBL246903 93720 None 36 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 142 2 3 3 -0.4 O=C(O)c1cc(CO)n[nH]1 10.1016/j.bmcl.2007.06.028
44441320 147650 None 1 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 168 1 2 3 0.7 CC1OCc2c1n[nH]c2C(=O)O 10.1016/j.bmcl.2007.06.028
CHEMBL393085 147650 None 1 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 168 1 2 3 0.7 CC1OCc2c1n[nH]c2C(=O)O 10.1016/j.bmcl.2007.06.028
12003790 198511 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 276 2 2 2 3.0 O=C(O)c1n[nH]c2c1CC(c1ccccc1Cl)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL560406 198511 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 276 2 2 2 3.0 O=C(O)c1n[nH]c2c1CC(c1ccccc1Cl)CC2 10.1016/j.bmcl.2009.06.054
17688981 147605 None 37 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 160 1 2 2 1.1 Cc1[nH]nc(C(=O)O)c1Cl 10.1016/j.bmcl.2007.07.101
CHEMBL393062 147605 None 37 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 160 1 2 2 1.1 Cc1[nH]nc(C(=O)O)c1Cl 10.1016/j.bmcl.2007.07.101
57400599 69970 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 304 5 2 6 0.6 CCc1cc(=O)oc2nc(OCC#CCCCO)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939043 69970 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 304 5 2 6 0.6 CCc1cc(=O)oc2nc(OCC#CCCCO)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
15604644 75268 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 304 4 2 5 1.4 O=c1[nH]c(=O)c2c(CCCc3cccs3)cc(=O)oc2[nH]1 10.1021/ml200243g
CHEMBL2036823 75268 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 304 4 2 5 1.4 O=c1[nH]c(=O)c2c(CCCc3cccs3)cc(=O)oc2[nH]1 10.1021/ml200243g
117629482 2823 None 82 Human Functional pEC50 = 7.6 7.6 -4 4
Agonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.05.108
1588 2823 None 82 Human Functional pEC50 = 7.6 7.6 -4 4
Agonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.05.108
1594 2823 None 82 Human Functional pEC50 = 7.6 7.6 -4 4
Agonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.05.108
2835 2823 None 82 Human Functional pEC50 = 7.6 7.6 -4 4
Agonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.05.108
938 2823 None 82 Human Functional pEC50 = 7.6 7.6 -4 4
Agonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.05.108
CHEMBL573 2823 None 82 Human Functional pEC50 = 7.6 7.6 -4 4
Agonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.05.108
DB00627 2823 None 82 Human Functional pEC50 = 7.6 7.6 -4 4
Agonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.05.108
57393656 69947 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 264 4 1 5 1.5 COc1nc2oc(=O)cc(CCC(C)C)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
CHEMBL1939020 69947 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 264 4 1 5 1.5 COc1nc2oc(=O)cc(CCC(C)C)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
137637662 156332 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 383 6 3 3 4.2 O=C(CCc1ccc(-c2ccc(O)cc2F)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4064786 156332 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 383 6 3 3 4.2 O=C(CCc1ccc(-c2ccc(O)cc2F)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
11817645 84940 None 0 Human Functional pEC50 = 5.6 5.6 12 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 254 2 1 3 1.7 CC1(c2cc(F)cc(F)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL223700 84940 None 0 Human Functional pEC50 = 5.6 5.6 12 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 254 2 1 3 1.7 CC1(c2cc(F)cc(F)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
42625382 184918 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 416 5 3 5 3.7 Cn1c(=O)c2cc(O)ccc2c2ccc(CCC(=O)Nc3ccccc3C(=O)O)cc21 10.1021/jm900151e
CHEMBL485184 184918 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 416 5 3 5 3.7 Cn1c(=O)c2cc(O)ccc2c2ccc(CCC(=O)Nc3ccccc3C(=O)O)cc21 10.1021/jm900151e
156012920 177554 None 0 Human Functional pEC50 = 4.6 4.6 - 1
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 433 8 3 8 3.0 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1cn(Cc2ccncc2)cc1C(=O)O 10.1016/j.bmcl.2020.127105
CHEMBL4638809 177554 None 0 Human Functional pEC50 = 4.6 4.6 - 1
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 433 8 3 8 3.0 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1cn(Cc2ccncc2)cc1C(=O)O 10.1016/j.bmcl.2020.127105
90645412 112478 None 0 Human Functional pEC50 = 4.6 4.6 - 1
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 365 6 2 4 3.4 COc1ccc(/C=C/C(=O)NC2=C(C(=O)O)CCCC2)c(Cl)c1OC 10.1016/j.bmc.2014.05.011
CHEMBL3297797 112478 None 0 Human Functional pEC50 = 4.6 4.6 - 1
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 365 6 2 4 3.4 COc1ccc(/C=C/C(=O)NC2=C(C(=O)O)CCCC2)c(Cl)c1OC 10.1016/j.bmc.2014.05.011
46890400 7288 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 419 6 3 5 3.6 Cn1cc(C2CCC(NC(=O)CCc3ccc4cc(O)ccc4c3)=C(C(=O)O)C2)cn1 10.1016/j.bmcl.2010.04.001
CHEMBL1086030 7288 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 419 6 3 5 3.6 Cn1cc(C2CCC(NC(=O)CCc3ccc4cc(O)ccc4c3)=C(C(=O)O)C2)cn1 10.1016/j.bmcl.2010.04.001
44433525 147343 None 23 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 170 2 2 2 1.1 O=C(O)c1n[nH]c(C2CC2)c1F 10.1016/j.bmcl.2007.07.101
CHEMBL392859 147343 None 23 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 170 2 2 2 1.1 O=C(O)c1n[nH]c(C2CC2)c1F 10.1016/j.bmcl.2007.07.101
117629482 2823 None 82 Human Functional pEC50 = 7.6 7.6 -4 4
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.03.062
1588 2823 None 82 Human Functional pEC50 = 7.6 7.6 -4 4
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.03.062
1594 2823 None 82 Human Functional pEC50 = 7.6 7.6 -4 4
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.03.062
2835 2823 None 82 Human Functional pEC50 = 7.6 7.6 -4 4
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.03.062
938 2823 None 82 Human Functional pEC50 = 7.6 7.6 -4 4
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.03.062
CHEMBL573 2823 None 82 Human Functional pEC50 = 7.6 7.6 -4 4
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.03.062
DB00627 2823 None 82 Human Functional pEC50 = 7.6 7.6 -4 4
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.03.062
135800194 89525 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 354 6 3 7 2.1 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1ccccc1C(=O)O 10.1021/jm100022r
CHEMBL237248 89525 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 354 6 3 7 2.1 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1ccccc1C(=O)O 10.1021/jm100022r
135800194 89525 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 354 6 3 7 2.1 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL237248 89525 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 354 6 3 7 2.1 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1ccccc1C(=O)O 10.1021/jm700942d
135966934 6844 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 452 7 3 7 3.3 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CC(c2cccc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1084030 6844 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 452 7 3 7 3.3 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CC(c2cccc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
135800194 89525 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 354 6 3 7 2.1 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL237248 89525 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 354 6 3 7 2.1 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
11607970 2552 None 14 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 164 1 2 2 0.8 OC(=O)c1n[nH]c2c1CC1C2C1 10.1021/jm2010964
5785 2552 None 14 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 164 1 2 2 0.8 OC(=O)c1n[nH]c2c1CC1C2C1 10.1021/jm2010964
CHEMBL2059221 2552 None 14 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 164 1 2 2 0.8 OC(=O)c1n[nH]c2c1CC1C2C1 10.1021/jm2010964
11646179 184919 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 359 5 3 3 4.0 O=C(CCc1ccc2c(ccc3[nH]ncc32)c1)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL485185 184919 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 359 5 3 3 4.0 O=C(CCc1ccc2c(ccc3[nH]ncc32)c1)Nc1ccccc1C(=O)O 10.1021/jm900151e
57400595 69953 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 366 4 1 5 3.0 CCc1cc(=O)oc2nc(OCc3ccc(C(F)(F)F)cc3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939026 69953 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 366 4 1 5 3.0 CCc1cc(=O)oc2nc(OCc3ccc(C(F)(F)F)cc3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
117629482 2823 None 82 Mouse Functional pEC50 = 6.6 6.6 3 4
Agonist activity at mouse GPR109A by [35S]GTP-gamma-S binding assayAgonist activity at mouse GPR109A by [35S]GTP-gamma-S binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
1588 2823 None 82 Mouse Functional pEC50 = 6.6 6.6 3 4
Agonist activity at mouse GPR109A by [35S]GTP-gamma-S binding assayAgonist activity at mouse GPR109A by [35S]GTP-gamma-S binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
1594 2823 None 82 Mouse Functional pEC50 = 6.6 6.6 3 4
Agonist activity at mouse GPR109A by [35S]GTP-gamma-S binding assayAgonist activity at mouse GPR109A by [35S]GTP-gamma-S binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
2835 2823 None 82 Mouse Functional pEC50 = 6.6 6.6 3 4
Agonist activity at mouse GPR109A by [35S]GTP-gamma-S binding assayAgonist activity at mouse GPR109A by [35S]GTP-gamma-S binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
938 2823 None 82 Mouse Functional pEC50 = 6.6 6.6 3 4
Agonist activity at mouse GPR109A by [35S]GTP-gamma-S binding assayAgonist activity at mouse GPR109A by [35S]GTP-gamma-S binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
CHEMBL573 2823 None 82 Mouse Functional pEC50 = 6.6 6.6 3 4
Agonist activity at mouse GPR109A by [35S]GTP-gamma-S binding assayAgonist activity at mouse GPR109A by [35S]GTP-gamma-S binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
DB00627 2823 None 82 Mouse Functional pEC50 = 6.6 6.6 3 4
Agonist activity at mouse GPR109A by [35S]GTP-gamma-S binding assayAgonist activity at mouse GPR109A by [35S]GTP-gamma-S binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
137653026 158799 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 329 3 2 2 3.3 O=C(/C=C/C#Cc1ccccc1Cl)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4093294 158799 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 329 3 2 2 3.3 O=C(/C=C/C#Cc1ccccc1Cl)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
44351665 116910 None 22 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 154 1 2 3 0.1 O=C(O)c1[nH]nc2c1COC2 10.1016/j.bmcl.2007.06.028
CHEMBL338071 116910 None 22 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 154 1 2 3 0.1 O=C(O)c1[nH]nc2c1COC2 10.1016/j.bmcl.2007.06.028
11494579 1058 None 0 Rat Functional pEC50 = 5.6 5.6 -123 2
Agonist activity at rat GPR109A expressed by [35S]GTPgammaS binding assayAgonist activity at rat GPR109A expressed by [35S]GTPgammaS binding assay
ChEMBL 377 5 3 5 2.9 O=C(Nc1ccccc1C(=O)O)CCc1cnn2c1CCc1c2ccc(c1)O 10.1021/jm900151e
5791 1058 None 0 Rat Functional pEC50 = 5.6 5.6 -123 2
Agonist activity at rat GPR109A expressed by [35S]GTPgammaS binding assayAgonist activity at rat GPR109A expressed by [35S]GTPgammaS binding assay
ChEMBL 377 5 3 5 2.9 O=C(Nc1ccccc1C(=O)O)CCc1cnn2c1CCc1c2ccc(c1)O 10.1021/jm900151e
CHEMBL482768 1058 None 0 Rat Functional pEC50 = 5.6 5.6 -123 2
Agonist activity at rat GPR109A expressed by [35S]GTPgammaS binding assayAgonist activity at rat GPR109A expressed by [35S]GTPgammaS binding assay
ChEMBL 377 5 3 5 2.9 O=C(Nc1ccccc1C(=O)O)CCc1cnn2c1CCc1c2ccc(c1)O 10.1021/jm900151e
53324022 58068 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 258 2 1 4 1.6 CCc1cc(=O)oc2nc(C(F)Cl)[nH]c(=O)c12 10.1021/ml100251u
CHEMBL1672745 58068 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 258 2 1 4 1.6 CCc1cc(=O)oc2nc(C(F)Cl)[nH]c(=O)c12 10.1021/ml100251u
117629482 2823 None 82 Human Functional pEC50 = 5.6 5.6 -4 4
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
1588 2823 None 82 Human Functional pEC50 = 5.6 5.6 -4 4
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
1594 2823 None 82 Human Functional pEC50 = 5.6 5.6 -4 4
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
2835 2823 None 82 Human Functional pEC50 = 5.6 5.6 -4 4
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
938 2823 None 82 Human Functional pEC50 = 5.6 5.6 -4 4
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
CHEMBL573 2823 None 82 Human Functional pEC50 = 5.6 5.6 -4 4
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
DB00627 2823 None 82 Human Functional pEC50 = 5.6 5.6 -4 4
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
90645407 112582 None 0 Human Functional pEC50 = 4.6 4.6 - 1
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 356 4 2 3 3.9 O=C(/C=C/c1cc2ccccc2nc1Cl)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
CHEMBL3299016 112582 None 0 Human Functional pEC50 = 4.6 4.6 - 1
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 356 4 2 3 3.9 O=C(/C=C/c1cc2ccccc2nc1Cl)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
53324024 58075 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 284 4 1 4 2.4 CC(C)CCc1cc(=O)oc2nc(C(F)F)[nH]c(=O)c12 10.1021/ml100251u
CHEMBL1672753 58075 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 284 4 1 4 2.4 CC(C)CCc1cc(=O)oc2nc(C(F)F)[nH]c(=O)c12 10.1021/ml100251u
145960556 162316 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 454 3 1 6 4.9 CCc1cc(C2Nc3ccccc3C(=O)N2C)cc2cc(-c3ccc4c(c3)OCO4)c(=O)oc12 10.1016/j.ejmech.2018.04.037
CHEMBL4163051 162316 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 454 3 1 6 4.9 CCc1cc(C2Nc3ccccc3C(=O)N2C)cc2cc(-c3ccc4c(c3)OCO4)c(=O)oc12 10.1016/j.ejmech.2018.04.037
117629482 2823 None 82 Human Functional pEC50 = 5.6 5.6 -4 4
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
1588 2823 None 82 Human Functional pEC50 = 5.6 5.6 -4 4
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
1594 2823 None 82 Human Functional pEC50 = 5.6 5.6 -4 4
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
2835 2823 None 82 Human Functional pEC50 = 5.6 5.6 -4 4
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
938 2823 None 82 Human Functional pEC50 = 5.6 5.6 -4 4
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
CHEMBL573 2823 None 82 Human Functional pEC50 = 5.6 5.6 -4 4
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
DB00627 2823 None 82 Human Functional pEC50 = 5.6 5.6 -4 4
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.ejmech.2018.04.037
46889342 7185 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 228 2 2 4 1.1 C/C=C/[C@@H]1[C@H]2Cc3c(-c4nnn[nH]4)n[nH]c3[C@@H]12 10.1016/j.bmcl.2010.03.062
CHEMBL1085537 7185 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 228 2 2 4 1.1 C/C=C/[C@@H]1[C@H]2Cc3c(-c4nnn[nH]4)n[nH]c3[C@@H]12 10.1016/j.bmcl.2010.03.062
57412400 76146 None 1 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 192 2 2 2 1.4 CC[C@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@H]12 10.1021/jm2010964
CHEMBL2057620 76146 None 1 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 192 2 2 2 1.4 CC[C@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@H]12 10.1021/jm2010964
145960556 162316 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 454 3 1 6 4.9 CCc1cc(C2Nc3ccccc3C(=O)N2C)cc2cc(-c3ccc4c(c3)OCO4)c(=O)oc12 10.1016/j.ejmech.2018.04.037
CHEMBL4163051 162316 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 454 3 1 6 4.9 CCc1cc(C2Nc3ccccc3C(=O)N2C)cc2cc(-c3ccc4c(c3)OCO4)c(=O)oc12 10.1016/j.ejmech.2018.04.037
57413541 76501 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 204 3 2 2 1.6 C=CC[C@@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
CHEMBL2059827 76501 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 204 3 2 2 1.6 C=CC[C@@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
46890298 7164 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 433 6 3 3 5.0 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2cccc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1085414 7164 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 433 6 3 3 5.0 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2cccc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
15605646 75271 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 264 5 2 4 1.3 CCCCCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
CHEMBL2036826 75271 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 264 5 2 4 1.3 CCCCCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
24953854 69974 None 0 Rat Functional pEC50 = 7.6 7.6 -1 2
Agonist activity at rat nicotinic acid receptorAgonist activity at rat nicotinic acid receptor
ChEMBL 328 5 1 5 2.4 CCC#CCOc1nc2oc(=O)cc(CCC3CCC3)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
CHEMBL1939047 69974 None 0 Rat Functional pEC50 = 7.6 7.6 -1 2
Agonist activity at rat nicotinic acid receptorAgonist activity at rat nicotinic acid receptor
ChEMBL 328 5 1 5 2.4 CCC#CCOc1nc2oc(=O)cc(CCC3CCC3)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
11218626 84926 None 0 Human Functional pEC50 = 5.6 5.6 -1 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 238 2 1 4 1.8 Cc1csc(C2(C)OC(C(=O)O)=CC2=O)c1 10.1021/jm070022x
CHEMBL223623 84926 None 0 Human Functional pEC50 = 5.6 5.6 -1 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 238 2 1 4 1.8 Cc1csc(C2(C)OC(C(=O)O)=CC2=O)c1 10.1021/jm070022x
156011372 177457 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 415 10 3 9 1.9 COCCCn1cc(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
CHEMBL4637548 177457 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 415 10 3 9 1.9 COCCCn1cc(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
11557600 167478 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 220 3 2 2 1.8 O=C(O)c1cc(Cc2cccc(F)c2)[nH]n1 10.1016/j.bmcl.2007.06.028
CHEMBL429495 167478 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 220 3 2 2 1.8 O=C(O)c1cc(Cc2cccc(F)c2)[nH]n1 10.1016/j.bmcl.2007.06.028
12003699 198510 None 2 Human Functional pEC50 = 4.6 4.6 - 1
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 242 2 2 2 2.4 O=C(O)c1n[nH]c2c1CC(c1ccccc1)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL560405 198510 None 2 Human Functional pEC50 = 4.6 4.6 - 1
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 242 2 2 2 2.4 O=C(O)c1n[nH]c2c1CC(c1ccccc1)CC2 10.1016/j.bmcl.2009.06.054
53326591 58057 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 314 5 1 4 2.6 O=c1cc(CCCC2(F)CC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
CHEMBL1672645 58057 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 314 5 1 4 2.6 O=c1cc(CCCC2(F)CC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
15605364 69940 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 262 4 1 5 1.2 CCc1cc(=O)oc2nc(OCC3CC3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939013 69940 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 262 4 1 5 1.2 CCc1cc(=O)oc2nc(OCC3CC3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
11159621 2548 None 38 Human Functional pEC50 = 6.5 6.5 -1 3
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2010.03.062
5784 2548 None 38 Human Functional pEC50 = 6.5 6.5 -1 3
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2010.03.062
CHEMBL456145 2548 None 38 Human Functional pEC50 = 6.5 6.5 -1 3
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2010.03.062
DB05939 2548 None 38 Human Functional pEC50 = 6.5 6.5 -1 3
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2010.03.062
11159621 2548 None 38 Human Functional pEC50 = 6.5 6.5 -1 3
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm2010964
5784 2548 None 38 Human Functional pEC50 = 6.5 6.5 -1 3
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm2010964
CHEMBL456145 2548 None 38 Human Functional pEC50 = 6.5 6.5 -1 3
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm2010964
DB05939 2548 None 38 Human Functional pEC50 = 6.5 6.5 -1 3
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm2010964
46889398 6834 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 216 1 2 4 0.9 CC1(C)[C@H]2Cc3c(-c4nnn[nH]4)n[nH]c3[C@H]21 10.1016/j.bmcl.2010.03.062
CHEMBL1083989 6834 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 216 1 2 4 0.9 CC1(C)[C@H]2Cc3c(-c4nnn[nH]4)n[nH]c3[C@H]21 10.1016/j.bmcl.2010.03.062
117629482 2823 None 82 Mouse Functional pEC50 = 7.5 7.5 3 4
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml100251u
117629482 2823 None 82 Mouse Functional pEC50 = 7.5 7.5 3 4
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml200243g
1588 2823 None 82 Mouse Functional pEC50 = 7.5 7.5 3 4
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml100251u
1588 2823 None 82 Mouse Functional pEC50 = 7.5 7.5 3 4
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml200243g
1594 2823 None 82 Mouse Functional pEC50 = 7.5 7.5 3 4
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml100251u
1594 2823 None 82 Mouse Functional pEC50 = 7.5 7.5 3 4
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml200243g
2835 2823 None 82 Mouse Functional pEC50 = 7.5 7.5 3 4
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml100251u
2835 2823 None 82 Mouse Functional pEC50 = 7.5 7.5 3 4
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml200243g
938 2823 None 82 Mouse Functional pEC50 = 7.5 7.5 3 4
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml100251u
938 2823 None 82 Mouse Functional pEC50 = 7.5 7.5 3 4
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml200243g
CHEMBL573 2823 None 82 Mouse Functional pEC50 = 7.5 7.5 3 4
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml100251u
CHEMBL573 2823 None 82 Mouse Functional pEC50 = 7.5 7.5 3 4
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml200243g
DB00627 2823 None 82 Mouse Functional pEC50 = 7.5 7.5 3 4
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml100251u
DB00627 2823 None 82 Mouse Functional pEC50 = 7.5 7.5 3 4
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml200243g
11380943 83492 None 0 Human Functional pEC50 = 6.5 6.5 20 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 296 2 1 3 2.2 CC1(c2cccc(Br)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL219980 83492 None 0 Human Functional pEC50 = 6.5 6.5 20 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 296 2 1 3 2.2 CC1(c2cccc(Br)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
135416391 6922 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 372 6 3 7 2.4 CC(CC(=O)NC1=C(C(=O)O)CCCC1)c1nc(-c2ccc(O)cn2)no1 10.1021/jm100022r
CHEMBL1084393 6922 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 372 6 3 7 2.4 CC(CC(=O)NC1=C(C(=O)O)CCCC1)c1nc(-c2ccc(O)cn2)no1 10.1021/jm100022r
135416393 7631 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 374 6 4 8 0.8 O=C(O)C1=C(NC(=O)C(O)Cc2nc(-c3ccc(O)cn3)no2)CCCC1 10.1021/jm100022r
CHEMBL1088213 7631 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 374 6 4 8 0.8 O=C(O)C1=C(NC(=O)C(O)Cc2nc(-c3ccc(O)cn3)no2)CCCC1 10.1021/jm100022r
57400594 69952 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 366 4 1 5 3.0 CCc1cc(=O)oc2nc(OCc3cccc(C(F)(F)F)c3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939025 69952 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 366 4 1 5 3.0 CCc1cc(=O)oc2nc(OCc3cccc(C(F)(F)F)c3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
136000579 61420 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 368 6 4 7 1.6 N[C@@H](Cc1nc(-c2ccc(O)cc2)no1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1770175 61420 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 368 6 4 7 1.6 N[C@@H](Cc1nc(-c2ccc(O)cc2)no1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
59304795 75259 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 194 0 2 4 -0.5 Cc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
CHEMBL2036811 75259 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 194 0 2 4 -0.5 Cc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
156017210 177835 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 414 8 4 3 5.1 CCCCc1cc(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)c(C(=O)O)[nH]1 10.1016/j.bmcl.2020.127105
CHEMBL4642367 177835 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 414 8 4 3 5.1 CCCCc1cc(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)c(C(=O)O)[nH]1 10.1016/j.bmcl.2020.127105
78346 93803 None 72 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 124 1 1 3 0.2 O=C(O)c1cncnc1 10.1016/j.bmcl.2007.06.028
CHEMBL247316 93803 None 72 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 124 1 1 3 0.2 O=C(O)c1cncnc1 10.1016/j.bmcl.2007.06.028
57402398 69956 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 394 5 1 7 2.6 CCc1cc(=O)oc2nc(OCc3ccc(-c4cncnc4)cc3F)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939029 69956 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 394 5 1 7 2.6 CCc1cc(=O)oc2nc(OCc3ccc(-c4cncnc4)cc3F)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
3159638 162005 None 42 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 154 2 2 2 1.0 CCc1[nH]nc(C(=O)O)c1C 10.1016/j.bmcl.2007.07.101
CHEMBL415261 162005 None 42 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 154 2 2 2 1.0 CCc1[nH]nc(C(=O)O)c1C 10.1016/j.bmcl.2007.07.101
136000718 61422 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 368 6 4 7 2.2 N[C@H](CC(=O)Nc1ccccc1C(=O)O)c1nc(-c2ccc(O)cc2)no1 10.1016/j.bmcl.2010.11.116
CHEMBL1770177 61422 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 368 6 4 7 2.2 N[C@H](CC(=O)Nc1ccccc1C(=O)O)c1nc(-c2ccc(O)cc2)no1 10.1016/j.bmcl.2010.11.116
137655320 158630 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 313 4 3 3 2.6 O=C(CCC#Cc1cccc(O)c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4091501 158630 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 313 4 3 3 2.6 O=C(CCC#Cc1cccc(O)c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
59343664 75282 None 0 Human Functional pEC50 = 8.5 8.5 -1 4
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 272 4 2 4 0.8 O=c1[nH]c(=O)c2c(CCCC(F)F)cc(=O)oc2[nH]1 10.1021/ml200243g
CHEMBL2036951 75282 None 0 Human Functional pEC50 = 8.5 8.5 -1 4
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 272 4 2 4 0.8 O=c1[nH]c(=O)c2c(CCCC(F)F)cc(=O)oc2[nH]1 10.1021/ml200243g
51346919 57860 None 5 Rat Functional pEC50 = 8.5 8.5 1 4
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 296 5 1 4 2.5 O=c1cc(CCCC2CC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
CHEMBL1671877 57860 None 5 Rat Functional pEC50 = 8.5 8.5 1 4
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 296 5 1 4 2.5 O=c1cc(CCCC2CC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
46890270 7377 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 395 8 3 3 4.9 CCCCC1CCC(NC(=O)CCc2ccc3cc(O)ccc3c2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
CHEMBL1086354 7377 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 395 8 3 3 4.9 CCCCC1CCC(NC(=O)CCc2ccc3cc(O)ccc3c2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
145949989 163055 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 410 2 1 4 5.3 Cc1ccc(-c2cc3cc(C4Nc5ccccc5C(=O)N4C)cc(C)c3oc2=O)cc1 10.1016/j.ejmech.2018.04.037
CHEMBL4174798 163055 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 410 2 1 4 5.3 Cc1ccc(-c2cc3cc(C4Nc5ccccc5C(=O)N4C)cc(C)c3oc2=O)cc1 10.1016/j.ejmech.2018.04.037
145949989 163055 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 410 2 1 4 5.3 Cc1ccc(-c2cc3cc(C4Nc5ccccc5C(=O)N4C)cc(C)c3oc2=O)cc1 10.1016/j.ejmech.2018.04.037
CHEMBL4174798 163055 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
ChEMBL 410 2 1 4 5.3 Cc1ccc(-c2cc3cc(C4Nc5ccccc5C(=O)N4C)cc(C)c3oc2=O)cc1 10.1016/j.ejmech.2018.04.037
44579763 187089 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 428 7 1 5 5.0 Cc1c(C(=O)N[C@@H](C)COc2ccccc2)cnc2c(-c3ccc(C(C)C)cc3)cnn12 10.1016/j.bmcl.2008.08.039
CHEMBL490600 187089 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 428 7 1 5 5.0 Cc1c(C(=O)N[C@@H](C)COc2ccccc2)cnc2c(-c3ccc(C(C)C)cc3)cnn12 10.1016/j.bmcl.2008.08.039
24955642 58074 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 298 6 1 4 2.9 CCCCCCc1cc(=O)oc2nc(C(F)F)[nH]c(=O)c12 10.1021/ml100251u
CHEMBL1672752 58074 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 298 6 1 4 2.9 CCCCCCc1cc(=O)oc2nc(C(F)F)[nH]c(=O)c12 10.1021/ml100251u
46890297 7216 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 433 6 3 3 5.0 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2ccccc2F)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1085653 7216 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 433 6 3 3 5.0 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2ccccc2F)CC1 10.1016/j.bmcl.2010.04.001
15605287 75258 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 208 1 2 4 -0.3 CCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
CHEMBL2036810 75258 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 208 1 2 4 -0.3 CCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
70686047 75279 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 250 3 2 4 0.8 CCC(C)Cc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
CHEMBL2036947 75279 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 250 3 2 4 0.8 CCC(C)Cc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
53324033 58050 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 298 4 1 5 2.0 CCc1cc(=O)oc2nc(COc3ccccc3)[nH]c(=O)c12 10.1021/ml100251u
CHEMBL1672638 58050 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 298 4 1 5 2.0 CCc1cc(=O)oc2nc(COc3ccccc3)[nH]c(=O)c12 10.1021/ml100251u
57412214 76141 None 1 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 178 1 2 2 1.0 C[C@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@H]12 10.1021/jm2010964
CHEMBL2057615 76141 None 1 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 178 1 2 2 1.0 C[C@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@H]12 10.1021/jm2010964
53317467 58056 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 372 6 1 4 3.9 O=c1cc(CCCC2(c3ccccc3)CC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
CHEMBL1672643 58056 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 372 6 1 4 3.9 O=c1cc(CCCC2(c3ccccc3)CC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
57390149 69968 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 276 3 2 6 -0.2 CCc1cc(=O)oc2nc(OCC#CCO)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939041 69968 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 276 3 2 6 -0.2 CCc1cc(=O)oc2nc(OCC#CCO)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
57390147 69946 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 290 4 1 5 2.0 COc1nc2oc(=O)cc(CCC3CCCC3)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
CHEMBL1939019 69946 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 290 4 1 5 2.0 COc1nc2oc(=O)cc(CCC3CCCC3)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
136375437 178186 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 432 8 3 7 3.6 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1cn(Cc2ccccc2)cc1C(=O)O 10.1016/j.bmcl.2020.127105
CHEMBL4647670 178186 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 432 8 3 7 3.6 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1cn(Cc2ccccc2)cc1C(=O)O 10.1016/j.bmcl.2020.127105
44580007 187053 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 366 6 1 5 3.6 COCC(C)NC(=O)c1cnc2c(-c3ccc(C(C)C)cc3)cnn2c1C 10.1016/j.bmcl.2008.08.039
CHEMBL490215 187053 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 366 6 1 5 3.6 COCC(C)NC(=O)c1cnc2c(-c3ccc(C(C)C)cc3)cnn2c1C 10.1016/j.bmcl.2008.08.039
54587625 61416 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 376 6 4 4 3.3 N[C@@H](Cc1ccc(-c2ccc(O)cc2)cc1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1770171 61416 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 376 6 4 4 3.3 N[C@@H](Cc1ccc(-c2ccc(O)cc2)cc1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
53318746 58053 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 324 6 1 4 3.3 CCC1(CCCc2cc(=O)oc3nc(C(F)F)[nH]c(=O)c23)CC1 10.1021/ml100251u
CHEMBL1672640 58053 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 324 6 1 4 3.3 CCC1(CCCc2cc(=O)oc3nc(C(F)F)[nH]c(=O)c23)CC1 10.1021/ml100251u
16048919 94736 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 407 4 2 6 2.7 COc1cccc2nc(N3CCN(C(=O)Nc4ccccc4C(=O)O)CC3)cnc12 10.1016/j.bmcl.2007.10.055
CHEMBL252708 94736 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 407 4 2 6 2.7 COc1cccc2nc(N3CCN(C(=O)Nc4ccccc4C(=O)O)CC3)cnc12 10.1016/j.bmcl.2007.10.055
11470032 84782 None 0 Human Functional pEC50 = 4.5 4.5 - 1
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 219 2 1 4 0.9 CC1(c2cccnc2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL222949 84782 None 0 Human Functional pEC50 = 4.5 4.5 - 1
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 219 2 1 4 0.9 CC1(c2cccnc2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
53326616 58067 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 224 2 1 4 0.9 CCc1cc(=O)oc2nc(CF)[nH]c(=O)c12 10.1021/ml100251u
CHEMBL1672744 58067 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 224 2 1 4 0.9 CCc1cc(=O)oc2nc(CF)[nH]c(=O)c12 10.1021/ml100251u
137659759 159360 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 314 4 3 4 1.9 O=C(CCC#Cc1ccc(O)cn1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4099278 159360 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 314 4 3 4 1.9 O=C(CCC#Cc1ccc(O)cn1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
53325309 58079 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 236 3 1 5 0.6 CCc1cc(=O)oc2nc(COC)[nH]c(=O)c12 10.1021/ml100251u
CHEMBL1672768 58079 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 236 3 1 5 0.6 CCc1cc(=O)oc2nc(COC)[nH]c(=O)c12 10.1021/ml100251u
11516324 184322 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 375 5 4 4 3.7 O=C(CCc1[nH]nc2c1ccc1cc(O)ccc12)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL483352 184322 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 375 5 4 4 3.7 O=C(CCc1[nH]nc2c1ccc1cc(O)ccc12)Nc1ccccc1C(=O)O 10.1021/jm900151e
57398906 69966 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 286 3 1 5 1.2 CCc1cc(=O)oc2nc(OCC#CC3CC3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939039 69966 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 286 3 1 5 1.2 CCc1cc(=O)oc2nc(OCC#CC3CC3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
11493732 193209 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 335 5 3 3 3.8 O=C(CCc1ccc2cc(O)ccc2c1)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL522649 193209 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 335 5 3 3 3.8 O=C(CCc1ccc2cc(O)ccc2c1)Nc1ccccc1C(=O)O 10.1021/jm900151e
135899178 16217 None 0 Human Functional pEC50 = 6.5 6.5 2 2
Agonist activity at human GPR109A receptor assessed as GTPgammaS bindingAgonist activity at human GPR109A receptor assessed as GTPgammaS binding
ChEMBL 315 5 1 4 2.7 O=c1[nH]c(COCCc2cccc(Cl)c2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1224219 16217 None 0 Human Functional pEC50 = 6.5 6.5 2 2
Agonist activity at human GPR109A receptor assessed as GTPgammaS bindingAgonist activity at human GPR109A receptor assessed as GTPgammaS binding
ChEMBL 315 5 1 4 2.7 O=c1[nH]c(COCCc2cccc(Cl)c2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
11610260 146037 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 364 6 2 4 4.2 Cc1noc(C)c1-c1ccc(CCC(=O)Nc2ccccc2C(=O)O)cc1 10.1021/jm700942d
CHEMBL391812 146037 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 364 6 2 4 4.2 Cc1noc(C)c1-c1ccc(CCC(=O)Nc2ccccc2C(=O)O)cc1 10.1021/jm700942d
136088957 61423 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 368 6 4 7 2.2 N[C@@H](CC(=O)Nc1ccccc1C(=O)O)c1nc(-c2ccc(O)cc2)no1 10.1016/j.bmcl.2010.11.116
CHEMBL1770178 61423 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 368 6 4 7 2.2 N[C@@H](CC(=O)Nc1ccccc1C(=O)O)c1nc(-c2ccc(O)cc2)no1 10.1016/j.bmcl.2010.11.116
44433534 152500 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 210 4 2 4 1.1 CCCCc1[nH]nc(-c2nnn[nH]2)c1F 10.1016/j.bmcl.2007.07.101
CHEMBL397056 152500 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 210 4 2 4 1.1 CCCCc1[nH]nc(-c2nnn[nH]2)c1F 10.1016/j.bmcl.2007.07.101
28400046 89844 None 2 Human Functional pEC50 = 4.5 4.5 -32 2
Agonist activity at human GPR109a receptor transfected in CHOK1 cells assessed as reversal of forskolin induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109a receptor transfected in CHOK1 cells assessed as reversal of forskolin induced cAMP elevating effect by whole cell assay
ChEMBL 194 4 2 3 1.8 CC(C)CNc1ccc(C(=O)O)cn1 10.1016/j.bmcl.2007.09.058
CHEMBL237737 89844 None 2 Human Functional pEC50 = 4.5 4.5 -32 2
Agonist activity at human GPR109a receptor transfected in CHOK1 cells assessed as reversal of forskolin induced cAMP elevating effect by whole cell assayAgonist activity at human GPR109a receptor transfected in CHOK1 cells assessed as reversal of forskolin induced cAMP elevating effect by whole cell assay
ChEMBL 194 4 2 3 1.8 CC(C)CNc1ccc(C(=O)O)cn1 10.1016/j.bmcl.2007.09.058
53318768 58066 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 242 2 1 4 1.4 CCc1cc(=O)oc2nc(C(F)F)[nH]c(=O)c12 10.1021/ml100251u
CHEMBL1672743 58066 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 242 2 1 4 1.4 CCc1cc(=O)oc2nc(C(F)F)[nH]c(=O)c12 10.1021/ml100251u
136088958 61466 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 369 6 4 8 1.0 N[C@H](Cc1nc(-c2ccc(O)cn2)no1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1770353 61466 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 369 6 4 8 1.0 N[C@H](Cc1nc(-c2ccc(O)cn2)no1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
137639493 157003 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 315 4 2 2 3.0 O=C(CCC#Cc1ccccc1F)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4072283 157003 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 315 4 2 2 3.0 O=C(CCC#Cc1ccccc1F)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
90645405 112596 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 295 3 2 2 2.6 O=C(/C=C/C#Cc1ccccc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
CHEMBL3299113 112596 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 295 3 2 2 2.6 O=C(/C=C/C#Cc1ccccc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
90645414 112484 None 0 Human Functional pEC50 = 4.4 4.4 - 1
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 338 5 2 3 3.5 Cc1ccc2cc(CCC(=O)NC3=C(C(=O)O)CCCC3)ccc2n1 10.1016/j.bmc.2014.05.011
CHEMBL3297874 112484 None 0 Human Functional pEC50 = 4.4 4.4 - 1
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 338 5 2 3 3.5 Cc1ccc2cc(CCC(=O)NC3=C(C(=O)O)CCCC3)ccc2n1 10.1016/j.bmc.2014.05.011
57413367 76140 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 178 1 2 2 1.0 C[C@@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
CHEMBL2057614 76140 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 178 1 2 2 1.0 C[C@@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
11436345 143 None 0 Human Functional pEC50 = 6.4 6.4 1 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 238 2 1 4 1.8 Cc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 10.1021/jm070022x
1599 143 None 0 Human Functional pEC50 = 6.4 6.4 1 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 238 2 1 4 1.8 Cc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 10.1021/jm070022x
CHEMBL424938 143 None 0 Human Functional pEC50 = 6.4 6.4 1 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 238 2 1 4 1.8 Cc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 10.1021/jm070022x
11446592 149921 None 2 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 172 3 2 3 1.0 CSCc1cc(C(=O)O)[nH]n1 10.1016/j.bmcl.2007.06.028
CHEMBL394885 149921 None 2 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 172 3 2 3 1.0 CSCc1cc(C(=O)O)[nH]n1 10.1016/j.bmcl.2007.06.028
46889364 7240 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 244 4 2 4 1.7 CCCC[C@H]1[C@@H]2c3[nH]nc(-c4nnn[nH]4)c3C[C@@H]21 10.1016/j.bmcl.2010.03.062
CHEMBL1085760 7240 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 244 4 2 4 1.7 CCCC[C@H]1[C@@H]2c3[nH]nc(-c4nnn[nH]4)c3C[C@@H]21 10.1016/j.bmcl.2010.03.062
53317492 58062 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 310 4 1 4 2.8 CC1CC(CCc2cc(=O)oc3nc(C(F)F)[nH]c(=O)c23)C1 10.1021/ml100251u
CHEMBL1672737 58062 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 310 4 1 4 2.8 CC1CC(CCc2cc(=O)oc3nc(C(F)F)[nH]c(=O)c23)C1 10.1021/ml100251u
56659539 63839 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at GPR109aAgonist activity at GPR109a
ChEMBL 337 5 3 4 3.3 O=C(COc1ccc2cc(O)ccc2c1)Nc1ccccc1C(=O)O 10.1021/jm200371q
CHEMBL1802361 63839 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at GPR109aAgonist activity at GPR109a
ChEMBL 337 5 3 4 3.3 O=C(COc1ccc2cc(O)ccc2c1)Nc1ccccc1C(=O)O 10.1021/jm200371q
11493732 193209 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assayAgonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assay
ChEMBL 335 5 3 3 3.8 O=C(CCc1ccc2cc(O)ccc2c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2008.08.030
CHEMBL522649 193209 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assayAgonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assay
ChEMBL 335 5 3 3 3.8 O=C(CCc1ccc2cc(O)ccc2c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2008.08.030
12002802 198289 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 285 2 2 5 1.4 Fc1ncccc1C1CCc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.06.054
CHEMBL558334 198289 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 285 2 2 5 1.4 Fc1ncccc1C1CCc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.06.054
136088960 61468 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 373 6 4 8 0.7 N[C@@H](Cc1nc(-c2ccc(O)cn2)no1)C(=O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.11.116
CHEMBL1770355 61468 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 373 6 4 8 0.7 N[C@@H](Cc1nc(-c2ccc(O)cn2)no1)C(=O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.11.116
59304954 75287 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 276 4 2 4 1.3 O=c1[nH]c(=O)c2c(CCCC3CCC3)cc(=O)oc2[nH]1 10.1021/ml200243g
CHEMBL2036956 75287 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 276 4 2 4 1.3 O=c1[nH]c(=O)c2c(CCCC3CCC3)cc(=O)oc2[nH]1 10.1021/ml200243g
117629482 2823 None 82 Rat Functional pEC50 = 7.4 7.4 -3 4
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml100251u
117629482 2823 None 82 Rat Functional pEC50 = 7.4 7.4 -3 4
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml200243g
1588 2823 None 82 Rat Functional pEC50 = 7.4 7.4 -3 4
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml100251u
1588 2823 None 82 Rat Functional pEC50 = 7.4 7.4 -3 4
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml200243g
1594 2823 None 82 Rat Functional pEC50 = 7.4 7.4 -3 4
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml100251u
1594 2823 None 82 Rat Functional pEC50 = 7.4 7.4 -3 4
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml200243g
2835 2823 None 82 Rat Functional pEC50 = 7.4 7.4 -3 4
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml100251u
2835 2823 None 82 Rat Functional pEC50 = 7.4 7.4 -3 4
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml200243g
938 2823 None 82 Rat Functional pEC50 = 7.4 7.4 -3 4
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml100251u
938 2823 None 82 Rat Functional pEC50 = 7.4 7.4 -3 4
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml200243g
CHEMBL573 2823 None 82 Rat Functional pEC50 = 7.4 7.4 -3 4
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml100251u
CHEMBL573 2823 None 82 Rat Functional pEC50 = 7.4 7.4 -3 4
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml200243g
DB00627 2823 None 82 Rat Functional pEC50 = 7.4 7.4 -3 4
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml100251u
DB00627 2823 None 82 Rat Functional pEC50 = 7.4 7.4 -3 4
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml200243g
137654580 159114 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 311 3 3 3 2.3 O=C(/C=C/C#Cc1cccc(O)c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4096635 159114 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 311 3 3 3 2.3 O=C(/C=C/C#Cc1cccc(O)c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
676464 89910 None 48 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 154 3 2 2 1.1 CCCc1cc(C(=O)O)n[nH]1 10.1016/j.bmcl.2007.06.028
CHEMBL237788 89910 None 48 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 154 3 2 2 1.1 CCCc1cc(C(=O)O)n[nH]1 10.1016/j.bmcl.2007.06.028
15604642 75280 None 0 Human Functional pEC50 = 8.4 8.4 1 3
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 250 3 2 4 0.8 CC(C)CCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
CHEMBL2036948 75280 None 0 Human Functional pEC50 = 8.4 8.4 1 3
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 250 3 2 4 0.8 CC(C)CCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
15604637 75286 None 0 Human Functional pEC50 = 8.4 8.4 -1 3
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 262 4 2 4 0.9 O=c1[nH]c(=O)c2c(CCCC3CC3)cc(=O)oc2[nH]1 10.1021/ml200243g
CHEMBL2036955 75286 None 0 Human Functional pEC50 = 8.4 8.4 -1 3
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 262 4 2 4 0.9 O=c1[nH]c(=O)c2c(CCCC3CC3)cc(=O)oc2[nH]1 10.1021/ml200243g
51346919 57860 None 5 Mouse Functional pEC50 = 8.4 8.4 -1 4
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 296 5 1 4 2.5 O=c1cc(CCCC2CC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
CHEMBL1671877 57860 None 5 Mouse Functional pEC50 = 8.4 8.4 -1 4
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 296 5 1 4 2.5 O=c1cc(CCCC2CC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
59304608 75285 None 0 Mouse Functional pEC50 = 8.4 8.4 -3 4
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 262 3 2 4 0.9 O=c1[nH]c(=O)c2c(CCC3CCC3)cc(=O)oc2[nH]1 10.1021/ml200243g
CHEMBL2036954 75285 None 0 Mouse Functional pEC50 = 8.4 8.4 -3 4
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 262 3 2 4 0.9 O=c1[nH]c(=O)c2c(CCC3CCC3)cc(=O)oc2[nH]1 10.1021/ml200243g
15604642 75280 None 0 Rat Functional pEC50 = 8.4 8.4 -1 3
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 250 3 2 4 0.8 CC(C)CCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
CHEMBL2036948 75280 None 0 Rat Functional pEC50 = 8.4 8.4 -1 3
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 250 3 2 4 0.8 CC(C)CCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
11501698 192679 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 376 5 3 6 2.9 O=C(CCc1nnn2c1ccc1cc(O)ccc12)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL521326 192679 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 376 5 3 6 2.9 O=C(CCc1nnn2c1ccc1cc(O)ccc12)Nc1ccccc1C(=O)O 10.1021/jm900151e
1597 1965 None 47 Human Functional pEC50 = 6.4 6.4 1 2
Activity at GPR109a assessed as inhibition of forskolin-stimulated cAMP productionActivity at GPR109a assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 205 2 1 4 1.7 OC(=O)c1ccc2c(c1)nnn2C(C)C 10.1021/jm800896z
2736690 1965 None 47 Human Functional pEC50 = 6.4 6.4 1 2
Activity at GPR109a assessed as inhibition of forskolin-stimulated cAMP productionActivity at GPR109a assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 205 2 1 4 1.7 OC(=O)c1ccc2c(c1)nnn2C(C)C 10.1021/jm800896z
CHEMBL381638 1965 None 47 Human Functional pEC50 = 6.4 6.4 1 2
Activity at GPR109a assessed as inhibition of forskolin-stimulated cAMP productionActivity at GPR109a assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 205 2 1 4 1.7 OC(=O)c1ccc2c(c1)nnn2C(C)C 10.1021/jm800896z
11159621 2548 None 38 Mouse Functional pEC50 = 6.4 6.4 1 3
Agonist activity against mouse GPR109a assessed as GTPgammaS bindingAgonist activity against mouse GPR109a assessed as GTPgammaS binding
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
5784 2548 None 38 Mouse Functional pEC50 = 6.4 6.4 1 3
Agonist activity against mouse GPR109a assessed as GTPgammaS bindingAgonist activity against mouse GPR109a assessed as GTPgammaS binding
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
CHEMBL456145 2548 None 38 Mouse Functional pEC50 = 6.4 6.4 1 3
Agonist activity against mouse GPR109a assessed as GTPgammaS bindingAgonist activity against mouse GPR109a assessed as GTPgammaS binding
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
DB05939 2548 None 38 Mouse Functional pEC50 = 6.4 6.4 1 3
Agonist activity against mouse GPR109a assessed as GTPgammaS bindingAgonist activity against mouse GPR109a assessed as GTPgammaS binding
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
11693991 88569 None 0 Human Functional pEC50 = 4.4 4.4 - 1
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 178 2 2 4 0.7 CC(C)c1cc(-c2nnn[nH]2)n[nH]1 10.1016/j.bmcl.2007.07.101
CHEMBL235229 88569 None 0 Human Functional pEC50 = 4.4 4.4 - 1
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 178 2 2 4 0.7 CC(C)c1cc(-c2nnn[nH]2)n[nH]1 10.1016/j.bmcl.2007.07.101
24180571 89963 None 23 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 144 1 2 2 0.6 Cc1[nH]nc(C(=O)O)c1F 10.1016/j.bmcl.2007.07.101
CHEMBL238004 89963 None 23 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 144 1 2 2 0.6 Cc1[nH]nc(C(=O)O)c1F 10.1016/j.bmcl.2007.07.101
24811199 6603 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 434 6 3 4 4.4 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2cccnc2F)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1083139 6603 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 434 6 3 4 4.4 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2cccnc2F)CC1 10.1016/j.bmcl.2010.04.001
54584718 61471 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 374 6 2 6 2.5 C[C@@H]1CCC(C(=O)O)=C(NC(=O)CCc2nc(-c3ccc(F)cn3)no2)C1 10.1016/j.bmcl.2010.11.116
CHEMBL1770359 61471 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 374 6 2 6 2.5 C[C@@H]1CCC(C(=O)O)=C(NC(=O)CCc2nc(-c3ccc(F)cn3)no2)C1 10.1016/j.bmcl.2010.11.116
137650474 157371 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 365 6 3 3 4.0 O=C(CCc1ccc(-c2ccccc2O)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4076822 157371 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 365 6 3 3 4.0 O=C(CCc1ccc(-c2ccccc2O)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
90645406 112485 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 388 6 2 4 3.9 COc1ccc2nc(Cl)c(CCC(=O)NC3=C(C(=O)O)CCCC3)cc2c1 10.1016/j.bmc.2014.05.011
CHEMBL3297875 112485 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 388 6 2 4 3.9 COc1ccc2nc(Cl)c(CCC(=O)NC3=C(C(=O)O)CCCC3)cc2c1 10.1016/j.bmc.2014.05.011
90645404 112581 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 322 4 2 3 3.3 O=C(/C=C/c1ccc2ccccc2n1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
CHEMBL3299009 112581 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 322 4 2 3 3.3 O=C(/C=C/c1ccc2ccccc2n1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
11323649 84783 None 0 Human Functional pEC50 = 4.4 4.4 - 1
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 286 2 1 3 2.8 CC1(c2cc(Cl)ccc2Cl)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL222955 84783 None 0 Human Functional pEC50 = 4.4 4.4 - 1
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 286 2 1 3 2.8 CC1(c2cc(Cl)ccc2Cl)OC(C(=O)O)=CC1=O 10.1021/jm070022x
53321368 58076 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 324 4 1 4 3.3 O=c1cc(CCC2CCCCC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
CHEMBL1672754 58076 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 324 4 1 4 3.3 O=c1cc(CCC2CCCCC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
57402397 69945 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 250 4 1 5 1.2 CCCCc1cc(=O)oc2nc(OC)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939018 69945 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 250 4 1 5 1.2 CCCCc1cc(=O)oc2nc(OC)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
136086829 7340 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 466 7 3 7 3.6 C[C@H]1CC(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)=C(C(=O)O)C[C@H]1c1cccc(F)c1 10.1016/j.bmcl.2010.04.001
CHEMBL1086225 7340 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 466 7 3 7 3.6 C[C@H]1CC(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)=C(C(=O)O)C[C@H]1c1cccc(F)c1 10.1016/j.bmcl.2010.04.001
11219885 83495 None 0 Human Functional pEC50 = 5.4 5.4 3 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 286 2 1 3 2.5 CC1(c2cccc(C(F)(F)F)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL220001 83495 None 0 Human Functional pEC50 = 5.4 5.4 3 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 286 2 1 3 2.5 CC1(c2cccc(C(F)(F)F)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
57397203 69977 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 274 4 1 5 1.2 CC#CCCOc1nc2oc(=O)cc(CC)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
CHEMBL1939050 69977 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 274 4 1 5 1.2 CC#CCCOc1nc2oc(=O)cc(CC)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
15605359 69963 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 260 3 1 5 0.8 CC#CCOc1nc2oc(=O)cc(CC)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
CHEMBL1939036 69963 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 260 3 1 5 0.8 CC#CCOc1nc2oc(=O)cc(CC)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
42625475 184315 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 414 5 3 5 4.3 O=C(CCc1noc2c1ccc1c(Cl)c(O)ccc12)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
CHEMBL483336 184315 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 414 5 3 5 4.3 O=C(CCc1noc2c1ccc1c(Cl)c(O)ccc12)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
57412216 76145 None 1 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 192 2 2 2 1.4 CC[C@@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
CHEMBL2057619 76145 None 1 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 192 2 2 2 1.4 CC[C@@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
11739420 84791 None 0 Human Functional pEC50 = 6.4 6.4 12 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 344 2 1 3 2.1 CC1(c2cccc(I)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL223013 84791 None 0 Human Functional pEC50 = 6.4 6.4 12 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 344 2 1 3 2.1 CC1(c2cccc(I)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
135800176 89434 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 369 6 3 6 3.2 O=C(CCc1cnc(-c2ccc(O)cn2)s1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL237037 89434 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 369 6 3 6 3.2 O=C(CCc1cnc(-c2ccc(O)cn2)s1)Nc1ccccc1C(=O)O 10.1021/jm700942d
46890268 6608 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 353 5 3 3 3.8 CC1CCC(NC(=O)CCc2ccc3cc(O)ccc3c2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
CHEMBL1083174 6608 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 353 5 3 3 3.8 CC1CCC(NC(=O)CCc2ccc3cc(O)ccc3c2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
44433526 88524 None 14 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 246 4 2 2 2.2 CCCCc1[nH]nc(C(=O)O)c1Br 10.1016/j.bmcl.2007.07.101
CHEMBL235010 88524 None 14 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 246 4 2 2 2.2 CCCCc1[nH]nc(C(=O)O)c1Br 10.1016/j.bmcl.2007.07.101
16048768 94503 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 405 3 2 5 3.5 C[C@H]1CN(C(=O)Nc2ccccc2C(=O)O)[C@H](C)CN1c1cnc2ccccc2n1 10.1016/j.bmcl.2007.10.055
CHEMBL251222 94503 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 405 3 2 5 3.5 C[C@H]1CN(C(=O)Nc2ccccc2C(=O)O)[C@H](C)CN1c1cnc2ccccc2n1 10.1016/j.bmcl.2007.10.055
12003785 198835 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 260 2 2 2 2.5 O=C(O)c1n[nH]c2c1CC(c1ccccc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL562632 198835 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 260 2 2 2 2.5 O=C(O)c1n[nH]c2c1CC(c1ccccc1F)CC2 10.1016/j.bmcl.2009.06.054
53318741 58071 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 256 3 1 4 1.8 CCCc1cc(=O)oc2nc(C(F)F)[nH]c(=O)c12 10.1021/ml100251u
CHEMBL1672749 58071 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 256 3 1 4 1.8 CCCc1cc(=O)oc2nc(C(F)F)[nH]c(=O)c12 10.1021/ml100251u
46889319 7132 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 188 1 2 4 0.2 C1c2c(-c3nnn[nH]3)n[nH]c2[C@H]2C[C@@H]12 10.1016/j.bmcl.2010.03.062
CHEMBL1085289 7132 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 188 1 2 4 0.2 C1c2c(-c3nnn[nH]3)n[nH]c2[C@H]2C[C@@H]12 10.1016/j.bmcl.2010.03.062
11560300 88573 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 395 6 3 3 5.0 O=C(CCc1ccc(-c2ccc(O)cc2Cl)cc1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL235256 88573 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 395 6 3 3 5.0 O=C(CCc1ccc(-c2ccc(O)cc2Cl)cc1)Nc1ccccc1C(=O)O 10.1021/jm700942d
46890577 6674 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 490 7 2 6 4.0 O=C(CCc1nc(-c2ccc(F)cn2)no1)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2F)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1083442 6674 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 490 7 2 6 4.0 O=C(CCc1nc(-c2ccc(F)cn2)no1)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2F)CC1 10.1016/j.bmcl.2010.04.001
137640776 157096 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 313 3 2 2 2.8 O=C(/C=C/C#Cc1ccccc1F)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4073322 157096 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 313 3 2 2 2.8 O=C(/C=C/C#Cc1ccccc1F)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
90645403 112543 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 321 4 2 2 3.9 O=C(/C=C/c1ccc2ccccc2c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
CHEMBL3298700 112543 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 321 4 2 2 3.9 O=C(/C=C/c1ccc2ccccc2c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
12003791 194954 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 261 2 2 3 1.9 O=C(O)c1n[nH]c2c1CC(c1cccnc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL1237147 194954 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 261 2 2 3 1.9 O=C(O)c1n[nH]c2c1CC(c1cccnc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL539398 194954 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 261 2 2 3 1.9 O=C(O)c1n[nH]c2c1CC(c1cccnc1F)CC2 10.1016/j.bmcl.2009.06.054
24955294 58059 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 282 4 1 4 2.2 O=c1cc(CCC2CC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
CHEMBL1672733 58059 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 282 4 1 4 2.2 O=c1cc(CCC2CC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
145957123 162111 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 440 2 1 6 4.7 Cc1cc(C2Nc3ccccc3C(=O)N2C)cc2cc(-c3ccc4c(c3)OCO4)c(=O)oc12 10.1016/j.ejmech.2018.04.037
CHEMBL4159670 162111 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 440 2 1 6 4.7 Cc1cc(C2Nc3ccccc3C(=O)N2C)cc2cc(-c3ccc4c(c3)OCO4)c(=O)oc12 10.1016/j.ejmech.2018.04.037
145957123 162111 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 440 2 1 6 4.7 Cc1cc(C2Nc3ccccc3C(=O)N2C)cc2cc(-c3ccc4c(c3)OCO4)c(=O)oc12 10.1016/j.ejmech.2018.04.037
CHEMBL4159670 162111 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assayAgonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
ChEMBL 440 2 1 6 4.7 Cc1cc(C2Nc3ccccc3C(=O)N2C)cc2cc(-c3ccc4c(c3)OCO4)c(=O)oc12 10.1016/j.ejmech.2018.04.037
46890578 6393 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 505 7 3 7 3.0 NC(Cc1nc(-c2ccc(F)cn2)no1)C(=O)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2F)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1082294 6393 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 505 7 3 7 3.0 NC(Cc1nc(-c2ccc(F)cn2)no1)C(=O)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2F)CC1 10.1016/j.bmcl.2010.04.001
44579647 193130 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 432 7 1 5 4.8 Cc1c(C(=O)NCCOc2ccc(F)cc2)cnc2c(-c3ccc(C(C)C)cc3)cnn12 10.1016/j.bmcl.2008.08.039
CHEMBL522281 193130 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 432 7 1 5 4.8 Cc1c(C(=O)NCCOc2ccc(F)cc2)cnc2c(-c3ccc(C(C)C)cc3)cnn12 10.1016/j.bmcl.2008.08.039
9822 145726 None 78 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 126 1 2 2 0.4 Cc1cc(C(=O)O)n[nH]1 10.1016/j.bmcl.2007.06.028
CHEMBL391574 145726 None 78 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 126 1 2 2 0.4 Cc1cc(C(=O)O)n[nH]1 10.1016/j.bmcl.2007.06.028
46890501 7248 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 375 6 3 7 1.2 NC(Cc1nc(-c2ccc(F)cn2)no1)C(=O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.001
CHEMBL1085816 7248 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 375 6 3 7 1.2 NC(Cc1nc(-c2ccc(F)cn2)no1)C(=O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.001
16048840 94097 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 391 3 2 5 3.1 O=C(O)c1ccccc1NC(=O)N1CCCN(c2cnc3ccccc3n2)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL248851 94097 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 391 3 2 5 3.1 O=C(O)c1ccccc1NC(=O)N1CCCN(c2cnc3ccccc3n2)CC1 10.1016/j.bmcl.2007.10.055
135416394 2560 None 43 Rat Functional pEC50 = 5.3 5.3 -288 3
Agonist activity at rat GPR109A receptor by [35S]GTPgammaS binding assayAgonist activity at rat GPR109A receptor by [35S]GTPgammaS binding assay
ChEMBL 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 10.1021/jm100022r
5788 2560 None 43 Rat Functional pEC50 = 5.3 5.3 -288 3
Agonist activity at rat GPR109A receptor by [35S]GTPgammaS binding assayAgonist activity at rat GPR109A receptor by [35S]GTPgammaS binding assay
ChEMBL 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 10.1021/jm100022r
73755154 2560 None 43 Rat Functional pEC50 = 5.3 5.3 -288 3
Agonist activity at rat GPR109A receptor by [35S]GTPgammaS binding assayAgonist activity at rat GPR109A receptor by [35S]GTPgammaS binding assay
ChEMBL 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 10.1021/jm100022r
CHEMBL1086657 2560 None 43 Rat Functional pEC50 = 5.3 5.3 -288 3
Agonist activity at rat GPR109A receptor by [35S]GTPgammaS binding assayAgonist activity at rat GPR109A receptor by [35S]GTPgammaS binding assay
ChEMBL 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 10.1021/jm100022r
11367769 136651 None 0 Human Functional pEC50 = 4.3 4.3 - 1
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 208 2 1 4 1.1 CC1(c2ccco2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL373880 136651 None 0 Human Functional pEC50 = 4.3 4.3 - 1
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 208 2 1 4 1.1 CC1(c2ccco2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
11379903 84305 None 0 Human Functional pEC50 = 5.3 5.3 6 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 258 2 1 4 2.2 CC1(c2csc(Cl)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL221282 84305 None 0 Human Functional pEC50 = 5.3 5.3 6 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 258 2 1 4 2.2 CC1(c2csc(Cl)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
59304594 75269 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 290 3 2 5 1.0 O=c1[nH]c(=O)c2c(CCc3cccs3)cc(=O)oc2[nH]1 10.1021/ml200243g
CHEMBL2036824 75269 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 290 3 2 5 1.0 O=c1[nH]c(=O)c2c(CCc3cccs3)cc(=O)oc2[nH]1 10.1021/ml200243g
135401973 1022 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 393 3 3 6 2.4 Oc1ccc2c(c1)ncc(n2)N1CCN(CC1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2007.10.055
5792 1022 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 393 3 3 6 2.4 Oc1ccc2c(c1)ncc(n2)N1CCN(CC1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2007.10.055
CHEMBL398496 1022 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 393 3 3 6 2.4 Oc1ccc2c(c1)ncc(n2)N1CCN(CC1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2007.10.055
53322689 58077 None 0 Human Functional pEC50 = 6.3 6.3 1 2
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 224 1 2 5 0.7 CCc1cc(=O)oc2nc(S)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1672755 58077 None 0 Human Functional pEC50 = 6.3 6.3 1 2
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 224 1 2 5 0.7 CCc1cc(=O)oc2nc(S)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
59304859 75274 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 300 4 2 6 -0.9 CS(=O)(=O)CCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
CHEMBL2036829 75274 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 300 4 2 6 -0.9 CS(=O)(=O)CCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
53322689 58077 None 0 Human Functional pEC50 = 6.3 6.3 1 2
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 224 1 2 5 0.7 CCc1cc(=O)oc2nc(S)[nH]c(=O)c12 10.1021/ml100251u
CHEMBL1672755 58077 None 0 Human Functional pEC50 = 6.3 6.3 1 2
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 224 1 2 5 0.7 CCc1cc(=O)oc2nc(S)[nH]c(=O)c12 10.1021/ml100251u
53321396 58061 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 310 5 1 4 2.9 O=c1cc(CCCC2CCC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
CHEMBL1672736 58061 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 310 5 1 4 2.9 O=c1cc(CCCC2CCC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
11483496 126 None 0 Human Functional pEC50 = 7.3 7.3 14 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 302 2 1 4 2.3 Brc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 10.1021/jm070022x
1589 126 None 0 Human Functional pEC50 = 7.3 7.3 14 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 302 2 1 4 2.3 Brc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 10.1021/jm070022x
CHEMBL375493 126 None 0 Human Functional pEC50 = 7.3 7.3 14 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 302 2 1 4 2.3 Brc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 10.1021/jm070022x
42625476 184316 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 379 5 3 5 3.2 O=C(CCc1cnn2c1ccc1cc(O)ccc12)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
CHEMBL483337 184316 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 379 5 3 5 3.2 O=C(CCc1cnn2c1ccc1cc(O)ccc12)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
11276453 84910 None 0 Human Functional pEC50 = 6.3 6.3 -1 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 238 2 1 4 1.8 Cc1ccc(C2(C)OC(C(=O)O)=CC2=O)s1 10.1021/jm070022x
CHEMBL223566 84910 None 0 Human Functional pEC50 = 6.3 6.3 -1 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 238 2 1 4 1.8 Cc1ccc(C2(C)OC(C(=O)O)=CC2=O)s1 10.1021/jm070022x
46890399 7287 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 419 6 3 5 3.6 Cn1nccc1C1CCC(NC(=O)CCc2ccc3cc(O)ccc3c2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
CHEMBL1086029 7287 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 419 6 3 5 3.6 Cn1nccc1C1CCC(NC(=O)CCc2ccc3cc(O)ccc3c2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
156013148 177573 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 356 6 3 7 2.1 Cn1cc(NC(=O)CCc2nc(-c3ccc(O)cc3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
CHEMBL4639053 177573 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 356 6 3 7 2.1 Cn1cc(NC(=O)CCc2nc(-c3ccc(O)cc3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
24955646 58051 None 0 Human Functional pEC50 = 7.3 7.3 -8 4
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 310 5 1 4 2.9 CC1(CCCc2cc(=O)oc3nc(C(F)F)[nH]c(=O)c23)CC1 10.1021/ml100251u
CHEMBL1672639 58051 None 0 Human Functional pEC50 = 7.3 7.3 -8 4
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 310 5 1 4 2.9 CC1(CCCc2cc(=O)oc3nc(C(F)F)[nH]c(=O)c23)CC1 10.1021/ml100251u
46890500 7247 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 360 6 2 6 2.2 O=C(CCc1nc(-c2ccc(F)cn2)no1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.001
CHEMBL1085815 7247 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 360 6 2 6 2.2 O=C(CCc1nc(-c2ccc(F)cn2)no1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.001
44441305 150209 None 1 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 188 3 2 3 -0.0 C[S+]([O-])Cc1cc(C(=O)O)[nH]n1 10.1016/j.bmcl.2007.06.028
CHEMBL395118 150209 None 1 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 188 3 2 3 -0.0 C[S+]([O-])Cc1cc(C(=O)O)[nH]n1 10.1016/j.bmcl.2007.06.028
15604641 75281 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 264 4 2 4 1.1 CC(C)CCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
CHEMBL2036950 75281 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 264 4 2 4 1.1 CC(C)CCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
59343664 75282 None 0 Mouse Functional pEC50 = 8.3 8.3 -2 4
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 272 4 2 4 0.8 O=c1[nH]c(=O)c2c(CCCC(F)F)cc(=O)oc2[nH]1 10.1021/ml200243g
CHEMBL2036951 75282 None 0 Mouse Functional pEC50 = 8.3 8.3 -2 4
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 272 4 2 4 0.8 O=c1[nH]c(=O)c2c(CCCC(F)F)cc(=O)oc2[nH]1 10.1021/ml200243g
59304608 75285 None 0 Rat Functional pEC50 = 8.3 8.3 -5 4
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 262 3 2 4 0.9 O=c1[nH]c(=O)c2c(CCC3CCC3)cc(=O)oc2[nH]1 10.1021/ml200243g
CHEMBL2036954 75285 None 0 Rat Functional pEC50 = 8.3 8.3 -5 4
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 262 3 2 4 0.9 O=c1[nH]c(=O)c2c(CCC3CCC3)cc(=O)oc2[nH]1 10.1021/ml200243g
135466520 184323 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 378 5 3 5 3.4 O=C(CCc1noc2c1CCc1cc(O)ccc1-2)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL483353 184323 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 378 5 3 5 3.4 O=C(CCc1noc2c1CCc1cc(O)ccc1-2)Nc1ccccc1C(=O)O 10.1021/jm900151e
135899171 16177 None 0 Human Functional pEC50 = 7.3 7.3 18 3
Agonist activity at human GPR109A receptor assessed as GTPgammaS bindingAgonist activity at human GPR109A receptor assessed as GTPgammaS binding
ChEMBL 331 6 1 5 2.8 O=c1[nH]c(OCCCOc2ccccc2Cl)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1224070 16177 None 0 Human Functional pEC50 = 7.3 7.3 18 3
Agonist activity at human GPR109A receptor assessed as GTPgammaS bindingAgonist activity at human GPR109A receptor assessed as GTPgammaS binding
ChEMBL 331 6 1 5 2.8 O=c1[nH]c(OCCCOc2ccccc2Cl)nc2ncccc12 10.1016/j.bmcl.2010.07.108
776416 18945 None 63 Mouse Functional pEC50 = 6.3 6.3 5 2
Agonist activity against mouse GPR109a assessed as forskolin-induced cAMP accumulationAgonist activity against mouse GPR109a assessed as forskolin-induced cAMP accumulation
ChEMBL 152 1 2 2 0.6 O=C(O)c1n[nH]c2c1CCC2 10.1021/jm800258p
CHEMBL128604 18945 None 63 Mouse Functional pEC50 = 6.3 6.3 5 2
Agonist activity against mouse GPR109a assessed as forskolin-induced cAMP accumulationAgonist activity against mouse GPR109a assessed as forskolin-induced cAMP accumulation
ChEMBL 152 1 2 2 0.6 O=C(O)c1n[nH]c2c1CCC2 10.1021/jm800258p
11594881 88672 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 319 5 2 2 4.1 O=C(CCc1ccc2ccccc2c1)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL235740 88672 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 319 5 2 2 4.1 O=C(CCc1ccc2ccccc2c1)Nc1ccccc1C(=O)O 10.1021/jm900151e
98845 93769 None 71 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 143 1 1 3 1.2 Cc1ncc(C(=O)O)s1 10.1016/j.bmcl.2007.06.028
CHEMBL247134 93769 None 71 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 143 1 1 3 1.2 Cc1ncc(C(=O)O)s1 10.1016/j.bmcl.2007.06.028
136088959 61467 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 383 6 4 8 1.6 CC(c1nc(-c2ccc(O)cn2)no1)[C@H](N)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1770354 61467 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 383 6 4 8 1.6 CC(c1nc(-c2ccc(O)cn2)no1)[C@H](N)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
11183677 83496 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 224 2 1 4 1.5 CC1(c2cccs2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL220004 83496 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 224 2 1 4 1.5 CC1(c2cccs2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
117629482 2823 None 82 Human Functional pEC50 = 5.3 5.3 -4 4
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2020.127105
1588 2823 None 82 Human Functional pEC50 = 5.3 5.3 -4 4
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2020.127105
1594 2823 None 82 Human Functional pEC50 = 5.3 5.3 -4 4
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2020.127105
2835 2823 None 82 Human Functional pEC50 = 5.3 5.3 -4 4
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2020.127105
938 2823 None 82 Human Functional pEC50 = 5.3 5.3 -4 4
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2020.127105
CHEMBL573 2823 None 82 Human Functional pEC50 = 5.3 5.3 -4 4
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2020.127105
DB00627 2823 None 82 Human Functional pEC50 = 5.3 5.3 -4 4
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2020.127105
16048839 155106 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 382 3 2 5 3.3 O=C(O)c1ccccc1NC(=O)N1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL401469 155106 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 382 3 2 5 3.3 O=C(O)c1ccccc1NC(=O)N1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmcl.2007.10.055
46889337 6725 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 216 2 2 4 0.9 CC[C@H]1[C@@H]2c3[nH]nc(-c4nnn[nH]4)c3C[C@@H]21 10.1016/j.bmcl.2010.03.062
CHEMBL1083682 6725 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 216 2 2 4 0.9 CC[C@H]1[C@@H]2c3[nH]nc(-c4nnn[nH]4)c3C[C@@H]21 10.1016/j.bmcl.2010.03.062
46889340 7183 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 228 2 2 4 0.9 C1CC1[C@@H]1[C@H]2Cc3c(-c4nnn[nH]4)n[nH]c3[C@H]21 10.1016/j.bmcl.2010.03.062
CHEMBL1085535 7183 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 228 2 2 4 0.9 C1CC1[C@@H]1[C@H]2Cc3c(-c4nnn[nH]4)n[nH]c3[C@H]21 10.1016/j.bmcl.2010.03.062
42625379 192200 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 376 5 3 5 4.0 O=C(CCc1noc2c1ccc1cc(O)ccc12)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL520299 192200 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 376 5 3 5 4.0 O=C(CCc1noc2c1ccc1cc(O)ccc12)Nc1ccccc1C(=O)O 10.1021/jm900151e
117629482 2823 None 82 Human Functional pEC50 = 7.3 7.3 -4 4
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm2010964
1588 2823 None 82 Human Functional pEC50 = 7.3 7.3 -4 4
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm2010964
1594 2823 None 82 Human Functional pEC50 = 7.3 7.3 -4 4
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm2010964
2835 2823 None 82 Human Functional pEC50 = 7.3 7.3 -4 4
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm2010964
938 2823 None 82 Human Functional pEC50 = 7.3 7.3 -4 4
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm2010964
CHEMBL573 2823 None 82 Human Functional pEC50 = 7.3 7.3 -4 4
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm2010964
DB00627 2823 None 82 Human Functional pEC50 = 7.3 7.3 -4 4
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm2010964
90645411 112486 None 0 Human Functional pEC50 = 4.3 4.3 - 1
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 317 5 2 4 2.4 O=C(CCc1ccc2c(c1)OCO2)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
CHEMBL3297876 112486 None 0 Human Functional pEC50 = 4.3 4.3 - 1
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 317 5 2 4 2.4 O=C(CCc1ccc2c(c1)OCO2)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
1595 259 None 36 Human Functional pEC50 = 6.3 6.3 4 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1021/jm070022x
51576 259 None 36 Human Functional pEC50 = 6.3 6.3 4 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1021/jm070022x
CHEMBL278488 259 None 36 Human Functional pEC50 = 6.3 6.3 4 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1021/jm070022x
117629482 2823 None 82 Human Functional pEC50 = 6.3 6.3 -4 4
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm100022r
1588 2823 None 82 Human Functional pEC50 = 6.3 6.3 -4 4
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm100022r
1594 2823 None 82 Human Functional pEC50 = 6.3 6.3 -4 4
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm100022r
2835 2823 None 82 Human Functional pEC50 = 6.3 6.3 -4 4
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm100022r
938 2823 None 82 Human Functional pEC50 = 6.3 6.3 -4 4
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm100022r
CHEMBL573 2823 None 82 Human Functional pEC50 = 6.3 6.3 -4 4
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm100022r
DB00627 2823 None 82 Human Functional pEC50 = 6.3 6.3 -4 4
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm100022r
24954935 69965 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 288 4 1 5 1.6 CCCC#CCOc1nc2oc(=O)cc(CC)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
CHEMBL1939038 69965 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 288 4 1 5 1.6 CCCC#CCOc1nc2oc(=O)cc(CC)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
1596 260 None 60 Human Functional pEC50 = 5.3 5.3 - 1
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O 10.1021/jm070022x
5310993 260 None 60 Human Functional pEC50 = 5.3 5.3 - 1
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O 10.1021/jm070022x
76 260 None 60 Human Functional pEC50 = 5.3 5.3 - 1
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O 10.1021/jm070022x
CHEMBL345714 260 None 60 Human Functional pEC50 = 5.3 5.3 - 1
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O 10.1021/jm070022x
DB09055 260 None 60 Human Functional pEC50 = 5.3 5.3 - 1
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O 10.1021/jm070022x
120232 153374 None 69 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 141 1 1 2 0.9 O=C(O)c1cncc(F)c1 10.1016/j.bmcl.2007.06.028
CHEMBL397783 153374 None 69 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 141 1 1 2 0.9 O=C(O)c1cncc(F)c1 10.1016/j.bmcl.2007.06.028
46890296 7215 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 364 5 3 4 3.3 N#CC1CCC(NC(=O)CCc2ccc3cc(O)ccc3c2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
CHEMBL1085652 7215 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 364 5 3 4 3.3 N#CC1CCC(NC(=O)CCc2ccc3cc(O)ccc3c2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
57412297 76499 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 220 3 2 2 2.0 CC(C)C[C@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
CHEMBL2059822 76499 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 220 3 2 2 2.0 CC(C)C[C@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
11638560 187149 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assayAgonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assay
ChEMBL 334 5 3 3 3.7 Nc1ccc2cc(CCC(=O)Nc3ccccc3C(=O)O)ccc2c1 10.1016/j.bmcl.2008.08.030
CHEMBL491002 187149 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assayAgonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assay
ChEMBL 334 5 3 3 3.7 Nc1ccc2cc(CCC(=O)Nc3ccccc3C(=O)O)ccc2c1 10.1016/j.bmcl.2008.08.030
11345283 85045 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 232 2 1 3 1.8 Cc1cccc(C2(C)OC(C(=O)O)=CC2=O)c1 10.1021/jm070022x
CHEMBL223878 85045 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 232 2 1 3 1.8 Cc1cccc(C2(C)OC(C(=O)O)=CC2=O)c1 10.1021/jm070022x
11264843 137707 None 0 Human Functional pEC50 = 5.3 5.3 1 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 236 2 1 3 1.6 CC1(c2ccc(F)cc2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL375762 137707 None 0 Human Functional pEC50 = 5.3 5.3 1 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 236 2 1 3 1.6 CC1(c2ccc(F)cc2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
46889341 7184 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 230 3 2 4 1.3 CCC[C@H]1[C@@H]2c3[nH]nc(-c4nnn[nH]4)c3C[C@@H]21 10.1016/j.bmcl.2010.03.062
CHEMBL1085536 7184 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assayAgonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
ChEMBL 230 3 2 4 1.3 CCC[C@H]1[C@@H]2c3[nH]nc(-c4nnn[nH]4)c3C[C@@H]21 10.1016/j.bmcl.2010.03.062
57412218 76377 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 220 4 2 2 2.2 CCCC[C@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@H]12 10.1021/jm2010964
CHEMBL2059225 76377 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 220 4 2 2 2.2 CCCC[C@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@H]12 10.1021/jm2010964
52941721 54981 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 283 1 0 7 4.2 Fc1ncccc1C1CCC2=C(C1)C(=C1N=NN=N1)N=N2 10.1016/j.bmcl.2009.06.054
CHEMBL1204125 54981 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 283 1 0 7 4.2 Fc1ncccc1C1CCC2=C(C1)C(=C1N=NN=N1)N=N2 10.1016/j.bmcl.2009.06.054
CHEMBL1615577 54981 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CKO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 283 1 0 7 4.2 Fc1ncccc1C1CCC2=C(C1)C(=C1N=NN=N1)N=N2 10.1016/j.bmcl.2009.06.054
44441323 93886 None 5 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 170 1 2 3 0.9 O=C(O)c1[nH]nc2c1CSC2 10.1016/j.bmcl.2007.06.028
CHEMBL247724 93886 None 5 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 170 1 2 3 0.9 O=C(O)c1[nH]nc2c1CSC2 10.1016/j.bmcl.2007.06.028
44441312 93917 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 196 6 2 2 2.2 CCCCCCc1cc(C(=O)O)[nH]n1 10.1016/j.bmcl.2007.06.028
CHEMBL247922 93917 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 196 6 2 2 2.2 CCCCCCc1cc(C(=O)O)[nH]n1 10.1016/j.bmcl.2007.06.028
137648318 157724 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 341 5 3 3 2.5 O=C(CCC#Cc1ccc(C(=O)O)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4081260 157724 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 341 5 3 3 2.5 O=C(CCC#Cc1ccc(C(=O)O)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
44433524 152297 None 25 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 158 2 2 2 0.8 CCc1[nH]nc(C(=O)O)c1F 10.1016/j.bmcl.2007.07.101
CHEMBL396864 152297 None 25 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 158 2 2 2 0.8 CCc1[nH]nc(C(=O)O)c1F 10.1016/j.bmcl.2007.07.101
11380943 83492 None 0 Human Functional pEC50 = 6.2 6.2 20 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 296 2 1 3 2.2 CC1(c2cccc(Br)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL219980 83492 None 0 Human Functional pEC50 = 6.2 6.2 20 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 296 2 1 3 2.2 CC1(c2cccc(Br)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
11368347 84980 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 236 2 1 3 1.6 CC1(c2ccccc2F)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL223754 84980 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 236 2 1 3 1.6 CC1(c2ccccc2F)OC(C(=O)O)=CC1=O 10.1021/jm070022x
57412214 76141 None 1 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 178 1 2 2 1.0 C[C@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@H]12 10.1021/jm2010964
CHEMBL2057615 76141 None 1 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 178 1 2 2 1.0 C[C@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@H]12 10.1021/jm2010964
135401975 94801 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 393 3 3 6 2.4 O=C(O)c1ccccc1NC(=O)N1CCN(c2cnc3ccc(O)cc3n2)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL253128 94801 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 393 3 3 6 2.4 O=C(O)c1ccccc1NC(=O)N1CCN(c2cnc3ccc(O)cc3n2)CC1 10.1016/j.bmcl.2007.10.055
90645410 112597 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 315 4 2 4 2.5 O=C(/C=C/c1ccc2c(c1)OCO2)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
CHEMBL3299114 112597 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 315 4 2 4 2.5 O=C(/C=C/c1ccc2c(c1)OCO2)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
57391931 69960 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 345 6 1 7 2.1 CCc1noc(CC)c1COc1nc2oc(=O)cc(CC)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
CHEMBL1939033 69960 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 345 6 1 7 2.1 CCc1noc(CC)c1COc1nc2oc(=O)cc(CC)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
44433533 89224 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 194 2 2 4 0.6 Fc1c(-c2nnn[nH]2)n[nH]c1C1CC1 10.1016/j.bmcl.2007.07.101
CHEMBL236728 89224 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 194 2 2 4 0.6 Fc1c(-c2nnn[nH]2)n[nH]c1C1CC1 10.1016/j.bmcl.2007.07.101
51346919 57860 None 5 Human Functional pEC50 = 7.2 7.2 -19 4
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 296 5 1 4 2.5 O=c1cc(CCCC2CC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
CHEMBL1671877 57860 None 5 Human Functional pEC50 = 7.2 7.2 -19 4
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 296 5 1 4 2.5 O=c1cc(CCCC2CC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
11617151 88673 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 345 6 2 2 4.6 O=C(CCc1ccc(-c2ccccc2)cc1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL235741 88673 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 345 6 2 2 4.6 O=C(CCc1ccc(-c2ccccc2)cc1)Nc1ccccc1C(=O)O 10.1021/jm700942d
11617151 88673 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 345 6 2 2 4.6 O=C(CCc1ccc(-c2ccccc2)cc1)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL235741 88673 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 345 6 2 2 4.6 O=C(CCc1ccc(-c2ccccc2)cc1)Nc1ccccc1C(=O)O 10.1021/jm900151e
16048998 94685 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 376 3 2 4 3.3 O=C(O)c1ccccc1NC(=O)N1CCN(c2ccc3ccccc3n2)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL252307 94685 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 376 3 2 4 3.3 O=C(O)c1ccccc1NC(=O)N1CCN(c2ccc3ccccc3n2)CC1 10.1016/j.bmcl.2007.10.055
53324057 58064 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 310 6 1 4 2.9 O=c1cc(CCCCC2CC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
CHEMBL1672741 58064 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 310 6 1 4 2.9 O=c1cc(CCCCC2CC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
135453098 88768 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 402 6 3 5 4.4 O=C(CCc1cnc(-c2ccc(O)cc2Cl)s1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL236162 88768 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 402 6 3 5 4.4 O=C(CCc1cnc(-c2ccc(O)cc2Cl)s1)Nc1ccccc1C(=O)O 10.1021/jm700942d
136086828 7195 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 502 7 3 7 3.9 C[C@H]1CC(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)=C(C(=O)O)C[C@H]1c1cc(F)cc(F)c1F 10.1016/j.bmcl.2010.04.001
CHEMBL1085589 7195 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 502 7 3 7 3.9 C[C@H]1CC(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)=C(C(=O)O)C[C@H]1c1cc(F)cc(F)c1F 10.1016/j.bmcl.2010.04.001
135453098 88768 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 402 6 3 5 4.4 O=C(CCc1cnc(-c2ccc(O)cc2Cl)s1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL236162 88768 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 402 6 3 5 4.4 O=C(CCc1cnc(-c2ccc(O)cc2Cl)s1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
56950369 3559 None 16 Mouse Functional pEC50 = 8.2 8.2 -3 4
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 276 4 2 4 1.3 O=c1cc(CCCC2(C)CC2)c2c(o1)[nH]c(=O)[nH]c2=O 10.1021/ml200243g
8469 3559 None 16 Mouse Functional pEC50 = 8.2 8.2 -3 4
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 276 4 2 4 1.3 O=c1cc(CCCC2(C)CC2)c2c(o1)[nH]c(=O)[nH]c2=O 10.1021/ml200243g
CHEMBL2036958 3559 None 16 Mouse Functional pEC50 = 8.2 8.2 -3 4
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 276 4 2 4 1.3 O=c1cc(CCCC2(C)CC2)c2c(o1)[nH]c(=O)[nH]c2=O 10.1021/ml200243g
DB12433 3559 None 16 Mouse Functional pEC50 = 8.2 8.2 -3 4
Agonist activity at mouse GPR109aAgonist activity at mouse GPR109a
ChEMBL 276 4 2 4 1.3 O=c1cc(CCCC2(C)CC2)c2c(o1)[nH]c(=O)[nH]c2=O 10.1021/ml200243g
24955646 58051 None 0 Rat Functional pEC50 = 8.2 8.2 2 4
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 310 5 1 4 2.9 CC1(CCCc2cc(=O)oc3nc(C(F)F)[nH]c(=O)c23)CC1 10.1021/ml100251u
CHEMBL1672639 58051 None 0 Rat Functional pEC50 = 8.2 8.2 2 4
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 310 5 1 4 2.9 CC1(CCCc2cc(=O)oc3nc(C(F)F)[nH]c(=O)c23)CC1 10.1021/ml100251u
42625474 184284 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 380 5 3 5 3.6 O=C(CCc1noc2c1ccc1cc(O)ccc12)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
CHEMBL483139 184284 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 380 5 3 5 3.6 O=C(CCc1noc2c1ccc1cc(O)ccc12)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
11624691 7229 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 361 6 3 3 4.3 O=C(CCc1ccc(-c2ccc(O)cc2)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1085711 7229 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 361 6 3 3 4.3 O=C(CCc1ccc(-c2ccc(O)cc2)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
136127010 16093 None 13 Rat Functional pEC50 = 7.2 7.2 9 2
Agonist activity at rat GPR109A receptor assessed as GTPgammaS bindingAgonist activity at rat GPR109A receptor assessed as GTPgammaS binding
ChEMBL 215 0 1 3 1.3 O=c1[nH]c(C(F)(F)F)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1223819 16093 None 13 Rat Functional pEC50 = 7.2 7.2 9 2
Agonist activity at rat GPR109A receptor assessed as GTPgammaS bindingAgonist activity at rat GPR109A receptor assessed as GTPgammaS binding
ChEMBL 215 0 1 3 1.3 O=c1[nH]c(C(F)(F)F)nc2ncccc12 10.1016/j.bmcl.2010.07.108
882926 85641 None 10 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 301 6 2 4 2.4 COc1ccc(OCC(=O)Nc2ccccc2C(=O)O)cc1 10.1021/jm700942d
CHEMBL228244 85641 None 10 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 301 6 2 4 2.4 COc1ccc(OCC(=O)Nc2ccccc2C(=O)O)cc1 10.1021/jm700942d
882926 85641 None 10 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 301 6 2 4 2.4 COc1ccc(OCC(=O)Nc2ccccc2C(=O)O)cc1 10.1021/jm900151e
CHEMBL228244 85641 None 10 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 301 6 2 4 2.4 COc1ccc(OCC(=O)Nc2ccccc2C(=O)O)cc1 10.1021/jm900151e
44580008 187054 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 414 7 1 5 4.6 Cc1c(C(=O)NCCOc2ccccc2)cnc2c(-c3ccc(C(C)C)cc3)cnn12 10.1016/j.bmcl.2008.08.039
CHEMBL490216 187054 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 414 7 1 5 4.6 Cc1c(C(=O)NCCOc2ccccc2)cnc2c(-c3ccc(C(C)C)cc3)cnn12 10.1016/j.bmcl.2008.08.039
53318740 58069 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 238 2 1 4 1.5 CCc1cc(=O)oc2nc(C(C)F)[nH]c(=O)c12 10.1021/ml100251u
CHEMBL1672746 58069 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 238 2 1 4 1.5 CCc1cc(=O)oc2nc(C(C)F)[nH]c(=O)c12 10.1021/ml100251u
11322762 137689 None 0 Human Functional pEC50 = 5.2 5.2 5 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 254 2 1 3 1.7 CC1(c2c(F)cccc2F)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL375625 137689 None 0 Human Functional pEC50 = 5.2 5.2 5 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 254 2 1 3 1.7 CC1(c2c(F)cccc2F)OC(C(=O)O)=CC1=O 10.1021/jm070022x
17925840 93674 None 15 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 140 2 2 3 -0.1 O=Cc1cc(C(=O)O)[nH]n1 10.1016/j.bmcl.2007.06.028
CHEMBL246692 93674 None 15 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 140 2 2 3 -0.1 O=Cc1cc(C(=O)O)[nH]n1 10.1016/j.bmcl.2007.06.028
70683894 75267 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 298 4 2 4 1.3 O=c1[nH]c(=O)c2c(CCCc3ccccc3)cc(=O)oc2[nH]1 10.1021/ml200243g
CHEMBL2036822 75267 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 298 4 2 4 1.3 O=c1[nH]c(=O)c2c(CCCc3ccccc3)cc(=O)oc2[nH]1 10.1021/ml200243g
15986930 185016 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 371 5 3 6 2.8 O=C(CCc1cn2c(n1)sc1cc(O)ccc12)NC1=C(C(=O)O)CCC1 10.1021/jm900151e
CHEMBL485327 185016 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 371 5 3 6 2.8 O=C(CCc1cn2c(n1)sc1cc(O)ccc12)NC1=C(C(=O)O)CCC1 10.1021/jm900151e
11776293 149345 None 4 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 236 3 2 2 2.4 O=C(O)c1cc(Cc2cccc(Cl)c2)n[nH]1 10.1016/j.bmcl.2007.06.028
CHEMBL394441 149345 None 4 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 236 3 2 2 2.4 O=C(O)c1cc(Cc2cccc(Cl)c2)n[nH]1 10.1016/j.bmcl.2007.06.028
56950649 69959 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 331 5 1 7 1.9 CCc1noc(C)c1COc1nc2oc(=O)cc(CC)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
CHEMBL1939032 69959 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 331 5 1 7 1.9 CCc1noc(C)c1COc1nc2oc(=O)cc(CC)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
137653428 158635 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 315 4 2 2 3.0 O=C(CCC#Cc1ccc(F)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4091542 158635 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 315 4 2 2 3.0 O=C(CCC#Cc1ccc(F)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
44445341 154337 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 376 4 2 5 3.2 O=C(O)c1ccccc1NC(=O)C1CCN(c2cnc3ccccc3n2)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL398625 154337 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 376 4 2 5 3.2 O=C(O)c1ccccc1NC(=O)C1CCN(c2cnc3ccccc3n2)CC1 10.1016/j.bmcl.2007.10.055
90645409 112595 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 386 5 2 4 3.9 COc1ccc2nc(Cl)c(/C=C/C(=O)NC3=C(C(=O)O)CCCC3)cc2c1 10.1016/j.bmc.2014.05.011
CHEMBL3299112 112595 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 386 5 2 4 3.9 COc1ccc2nc(Cl)c(/C=C/C(=O)NC3=C(C(=O)O)CCCC3)cc2c1 10.1016/j.bmc.2014.05.011
1047 205093 None 78 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 124 1 1 3 0.2 O=C(O)c1cnccn1 10.1016/j.bmcl.2007.06.028
CHEMBL613 205093 None 78 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 124 1 1 3 0.2 O=C(O)c1cnccn1 10.1016/j.bmcl.2007.06.028
11494579 1058 None 0 Human Functional pEC50 = 7.2 7.2 123 2
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 377 5 3 5 2.9 O=C(Nc1ccccc1C(=O)O)CCc1cnn2c1CCc1c2ccc(c1)O 10.1021/jm900151e
5791 1058 None 0 Human Functional pEC50 = 7.2 7.2 123 2
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 377 5 3 5 2.9 O=C(Nc1ccccc1C(=O)O)CCc1cnn2c1CCc1c2ccc(c1)O 10.1021/jm900151e
CHEMBL482768 1058 None 0 Human Functional pEC50 = 7.2 7.2 123 2
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 377 5 3 5 2.9 O=C(Nc1ccccc1C(=O)O)CCc1cnn2c1CCc1c2ccc(c1)O 10.1021/jm900151e
24811550 6682 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 434 6 3 4 4.4 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2ccc(F)nc2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1083450 6682 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 434 6 3 4 4.4 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2ccc(F)nc2)CC1 10.1016/j.bmcl.2010.04.001
156021045 178236 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 399 9 3 8 2.7 CCCCn1cc(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
CHEMBL4648435 178236 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 399 9 3 8 2.7 CCCCn1cc(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
135887289 6923 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 386 6 3 7 2.5 CC(C)(CC(=O)NC1=C(C(=O)O)CCCC1)c1nc(-c2ccc(O)cn2)no1 10.1021/jm100022r
CHEMBL1084394 6923 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 386 6 3 7 2.5 CC(C)(CC(=O)NC1=C(C(=O)O)CCCC1)c1nc(-c2ccc(O)cn2)no1 10.1021/jm100022r
54580748 61418 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 377 5 3 5 2.9 O=C(CCc1cc2n(n1)-c1ccc(O)cc1CC2)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1770173 61418 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 377 5 3 5 2.9 O=C(CCc1cc2n(n1)-c1ccc(O)cc1CC2)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
53321367 58070 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 228 1 1 4 1.1 Cc1cc(=O)oc2nc(C(F)F)[nH]c(=O)c12 10.1021/ml100251u
CHEMBL1672748 58070 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 228 1 1 4 1.1 Cc1cc(=O)oc2nc(C(F)F)[nH]c(=O)c12 10.1021/ml100251u
11379903 84305 None 0 Human Functional pEC50 = 7.2 7.2 6 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 258 2 1 4 2.2 CC1(c2csc(Cl)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL221282 84305 None 0 Human Functional pEC50 = 7.2 7.2 6 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 258 2 1 4 2.2 CC1(c2csc(Cl)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
24953855 69972 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 316 5 1 5 2.3 CCC#CCOc1nc2oc(=O)cc(CCC(C)C)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
CHEMBL1939045 69972 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 316 5 1 5 2.3 CCC#CCOc1nc2oc(=O)cc(CCC(C)C)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
44441316 93843 None 1 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 194 3 2 2 1.9 CCCC1CCc2c1n[nH]c2C(=O)O 10.1016/j.bmcl.2007.06.028
CHEMBL247526 93843 None 1 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 194 3 2 2 1.9 CCCC1CCc2c1n[nH]c2C(=O)O 10.1016/j.bmcl.2007.06.028
24953853 69976 None 0 Human Functional pEC50 = 7.2 7.2 1 2
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 328 6 1 5 2.4 CCC#CCOc1nc2oc(=O)cc(CCCC3CC3)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
CHEMBL1939049 69976 None 0 Human Functional pEC50 = 7.2 7.2 1 2
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 328 6 1 5 2.4 CCC#CCOc1nc2oc(=O)cc(CCCC3CC3)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
117629482 2823 None 82 Rat Functional pEC50 = 6.2 6.2 -3 4
Agonist activity at rat GPR109A expressed by [35S]GTPgammaS binding assayAgonist activity at rat GPR109A expressed by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm900151e
1588 2823 None 82 Rat Functional pEC50 = 6.2 6.2 -3 4
Agonist activity at rat GPR109A expressed by [35S]GTPgammaS binding assayAgonist activity at rat GPR109A expressed by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm900151e
1594 2823 None 82 Rat Functional pEC50 = 6.2 6.2 -3 4
Agonist activity at rat GPR109A expressed by [35S]GTPgammaS binding assayAgonist activity at rat GPR109A expressed by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm900151e
2835 2823 None 82 Rat Functional pEC50 = 6.2 6.2 -3 4
Agonist activity at rat GPR109A expressed by [35S]GTPgammaS binding assayAgonist activity at rat GPR109A expressed by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm900151e
938 2823 None 82 Rat Functional pEC50 = 6.2 6.2 -3 4
Agonist activity at rat GPR109A expressed by [35S]GTPgammaS binding assayAgonist activity at rat GPR109A expressed by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm900151e
CHEMBL573 2823 None 82 Rat Functional pEC50 = 6.2 6.2 -3 4
Agonist activity at rat GPR109A expressed by [35S]GTPgammaS binding assayAgonist activity at rat GPR109A expressed by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm900151e
DB00627 2823 None 82 Rat Functional pEC50 = 6.2 6.2 -3 4
Agonist activity at rat GPR109A expressed by [35S]GTPgammaS binding assayAgonist activity at rat GPR109A expressed by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm900151e
90645408 112598 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 329 4 2 4 2.5 O=C(/C=C/c1ccc2c(c1)OCCO2)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
CHEMBL3299115 112598 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 329 4 2 4 2.5 O=C(/C=C/c1ccc2c(c1)OCCO2)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
42625213 192412 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 365 5 2 5 3.8 O=C(CCc1cn2c(n1)sc1ccccc12)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL520620 192412 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 365 5 2 5 3.8 O=C(CCc1cn2c(n1)sc1ccccc12)Nc1ccccc1C(=O)O 10.1021/jm900151e
59343597 75291 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 296 4 2 4 1.3 O=c1[nH]c(=O)c2c(CCCC3(Cl)CC3)cc(=O)oc2[nH]1 10.1021/ml200243g
CHEMBL2036960 75291 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 296 4 2 4 1.3 O=c1[nH]c(=O)c2c(CCCC3(Cl)CC3)cc(=O)oc2[nH]1 10.1021/ml200243g
57412301 76133 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 218 3 2 2 1.8 O=C(O)c1n[nH]c2c1C[C@H]1[C@@H](CC3CC3)[C@@H]21 10.1021/jm2010964
CHEMBL2057602 76133 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 218 3 2 2 1.8 O=C(O)c1n[nH]c2c1C[C@H]1[C@@H](CC3CC3)[C@@H]21 10.1021/jm2010964
122181142 121896 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 365 6 3 3 4.0 O=C(CCc1ccc(-c2ccc(O)cc2)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL3589836 121896 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 365 6 3 3 4.0 O=C(CCc1ccc(-c2ccc(O)cc2)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
44579762 187265 None 1 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 428 7 1 5 5.0 Cc1c(C(=O)NC(C)COc2ccccc2)cnc2c(-c3ccc(C(C)C)cc3)cnn12 10.1016/j.bmcl.2008.08.039
CHEMBL492020 187265 None 1 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 428 7 1 5 5.0 Cc1c(C(=O)NC(C)COc2ccccc2)cnc2c(-c3ccc(C(C)C)cc3)cnn12 10.1016/j.bmcl.2008.08.039
11415838 136444 None 0 Human Functional pEC50 = 5.2 5.2 1 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 316 2 1 4 2.6 Cc1sc(C2(C)OC(C(=O)O)=CC2=O)cc1Br 10.1021/jm070022x
CHEMBL373484 136444 None 0 Human Functional pEC50 = 5.2 5.2 1 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 316 2 1 4 2.6 Cc1sc(C2(C)OC(C(=O)O)=CC2=O)cc1Br 10.1021/jm070022x
137661033 159581 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 313 4 3 3 2.6 O=C(CCC#Cc1ccccc1O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4101720 159581 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 313 4 3 3 2.6 O=C(CCC#Cc1ccccc1O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
11470798 138054 None 0 Human Functional pEC50 = 5.1 5.1 2 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 254 2 1 3 1.7 CC1(c2ccc(F)c(F)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL376419 138054 None 0 Human Functional pEC50 = 5.1 5.1 2 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 254 2 1 3 1.7 CC1(c2ccc(F)c(F)c2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
156020475 178179 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 429 8 3 5 4.5 CCCCc1nc(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)c(C(=O)O)n1C 10.1016/j.bmcl.2020.127105
CHEMBL4647545 178179 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 429 8 3 5 4.5 CCCCc1nc(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)c(C(=O)O)n1C 10.1016/j.bmcl.2020.127105
136088961 61470 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 387 6 4 8 1.0 CC1CCC(NC(=O)[C@@H](N)Cc2nc(-c3ccc(O)cn3)no2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.11.116
CHEMBL1770357 61470 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 387 6 4 8 1.0 CC1CCC(NC(=O)[C@@H](N)Cc2nc(-c3ccc(O)cn3)no2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.11.116
57397202 69955 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 399 5 1 6 3.6 CCc1cc(=O)oc2nc(OCc3cccc(-c4cccc(C#N)c4)c3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939028 69955 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 399 5 1 6 3.6 CCc1cc(=O)oc2nc(OCc3cccc(-c4cccc(C#N)c4)c3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
135887288 7618 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 398 6 3 7 2.6 O=C(O)C1=C(NC(=O)C2(Cc3nc(-c4ccc(O)cn4)no3)CCC2)CCCC1 10.1021/jm100022r
CHEMBL1088074 7618 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAgonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
ChEMBL 398 6 3 7 2.6 O=C(O)C1=C(NC(=O)C2(Cc3nc(-c4ccc(O)cn4)no3)CCC2)CCCC1 10.1021/jm100022r
135922719 184393 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 377 5 3 5 3.0 Cn1nc(CCC(=O)Nc2ccccc2C(=O)O)c2c1-c1ccc(O)cc1C2 10.1021/jm900151e
CHEMBL483996 184393 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 377 5 3 5 3.0 Cn1nc(CCC(=O)Nc2ccccc2C(=O)O)c2c1-c1ccc(O)cc1C2 10.1021/jm900151e
15605503 69957 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 299 4 1 6 1.4 CCc1cc(=O)oc2nc(OCc3cccnc3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939030 69957 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 299 4 1 6 1.4 CCc1cc(=O)oc2nc(OCc3cccnc3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
135502978 192098 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 377 5 4 4 3.2 O=C(CCc1[nH]nc2c1CCc1cc(O)ccc1-2)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL520136 192098 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 377 5 4 4 3.2 O=C(CCc1[nH]nc2c1CCc1cc(O)ccc1-2)Nc1ccccc1C(=O)O 10.1021/jm900151e
11324121 84700 None 0 Human Functional pEC50 = 6.1 6.1 5 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 302 2 1 4 2.3 CC1(c2cc(Br)cs2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
CHEMBL222472 84700 None 0 Human Functional pEC50 = 6.1 6.1 5 2
Activity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generationActivity at GPR109a in CHO cells assessed as inhibition of forskolin-induced cAMP generation
ChEMBL 302 2 1 4 2.3 CC1(c2cc(Br)cs2)OC(C(=O)O)=CC1=O 10.1021/jm070022x
46890579 7018 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 455 7 2 7 3.2 O=C(CCc1nc(-c2ccc(F)cn2)no1)NC1=C(C(=O)O)CC(c2ccc(F)nc2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1084798 7018 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 455 7 2 7 3.2 O=C(CCc1nc(-c2ccc(F)cn2)no1)NC1=C(C(=O)O)CC(c2ccc(F)nc2)CC1 10.1016/j.bmcl.2010.04.001
46890580 7019 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 504 7 2 6 4.3 C[C@H]1CC(NC(=O)CCc2nc(-c3ccc(F)cn3)no2)=C(C(=O)O)C[C@H]1c1cc(F)cc(F)c1F 10.1016/j.bmcl.2010.04.001
CHEMBL1084799 7019 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 504 7 2 6 4.3 C[C@H]1CC(NC(=O)CCc2nc(-c3ccc(F)cn3)no2)=C(C(=O)O)C[C@H]1c1cc(F)cc(F)c1F 10.1016/j.bmcl.2010.04.001
44433532 152498 None 0 Human Functional pEC50 = 6.1 6.1 16 2
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 182 2 2 4 0.3 CCc1[nH]nc(-c2nnn[nH]2)c1F 10.1016/j.bmcl.2007.07.101
CHEMBL397055 152498 None 0 Human Functional pEC50 = 6.1 6.1 16 2
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 182 2 2 4 0.3 CCc1[nH]nc(-c2nnn[nH]2)c1F 10.1016/j.bmcl.2007.07.101
15986931 192345 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 385 5 3 6 3.2 O=C(CCc1cn2c(n1)sc1cc(O)ccc12)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
CHEMBL520513 192345 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 385 5 3 6 3.2 O=C(CCc1cn2c(n1)sc1cc(O)ccc12)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
15986755 184224 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 339 5 3 3 3.5 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.001
CHEMBL482698 184224 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 339 5 3 3 3.5 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.001
156021546 178291 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 401 9 4 9 1.3 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1cn(CCCO)cc1C(=O)O 10.1016/j.bmcl.2020.127105
CHEMBL4649305 178291 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 401 9 4 9 1.3 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1cn(CCCO)cc1C(=O)O 10.1016/j.bmcl.2020.127105
247986 150268 None 73 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 157 1 1 2 1.4 O=C(O)c1cncc(Cl)c1 10.1016/j.bmcl.2007.06.028
CHEMBL395178 150268 None 73 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 157 1 1 2 1.4 O=C(O)c1cncc(Cl)c1 10.1016/j.bmcl.2007.06.028
11647028 88716 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 401 6 3 4 5.0 O=C(CCc1ccc(-c2ccc(O)cc2Cl)s1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL235954 88716 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 401 6 3 4 5.0 O=C(CCc1ccc(-c2ccc(O)cc2Cl)s1)Nc1ccccc1C(=O)O 10.1021/jm700942d
574310 18963 None 77 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 112 1 2 2 0.1 O=C(O)c1cc[nH]n1 10.1016/j.bmcl.2007.07.101
CHEMBL128679 18963 None 77 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 112 1 2 2 0.1 O=C(O)c1cc[nH]n1 10.1016/j.bmcl.2007.07.101
44433528 147610 None 0 Human Functional pEC50 = 5.1 5.1 -10 2
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 178 3 2 4 0.5 CCCc1cc(-c2nnn[nH]2)n[nH]1 10.1016/j.bmcl.2007.07.101
CHEMBL393064 147610 None 0 Human Functional pEC50 = 5.1 5.1 -10 2
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 178 3 2 4 0.5 CCCc1cc(-c2nnn[nH]2)n[nH]1 10.1016/j.bmcl.2007.07.101
117629482 2823 None 82 Human Functional pEC50 = 6.1 6.1 -4 4
Agonist activity at human recombinant GPR109a transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109a transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml3000676
1588 2823 None 82 Human Functional pEC50 = 6.1 6.1 -4 4
Agonist activity at human recombinant GPR109a transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109a transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml3000676
1594 2823 None 82 Human Functional pEC50 = 6.1 6.1 -4 4
Agonist activity at human recombinant GPR109a transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109a transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml3000676
2835 2823 None 82 Human Functional pEC50 = 6.1 6.1 -4 4
Agonist activity at human recombinant GPR109a transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109a transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml3000676
938 2823 None 82 Human Functional pEC50 = 6.1 6.1 -4 4
Agonist activity at human recombinant GPR109a transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109a transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml3000676
CHEMBL573 2823 None 82 Human Functional pEC50 = 6.1 6.1 -4 4
Agonist activity at human recombinant GPR109a transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109a transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml3000676
DB00627 2823 None 82 Human Functional pEC50 = 6.1 6.1 -4 4
Agonist activity at human recombinant GPR109a transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109a transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml3000676
16048993 169080 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 377 3 2 5 2.7 O=C(O)c1ccccc1NC(=O)N1CCN(c2ncc3ccccc3n2)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL439060 169080 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 377 3 2 5 2.7 O=C(O)c1ccccc1NC(=O)N1CCN(c2ncc3ccccc3n2)CC1 10.1016/j.bmcl.2007.10.055
53324034 58054 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 338 6 1 4 3.6 CC(C)C1(CCCc2cc(=O)oc3nc(C(F)F)[nH]c(=O)c23)CC1 10.1021/ml100251u
CHEMBL1672641 58054 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 338 6 1 4 3.6 CC(C)C1(CCCc2cc(=O)oc3nc(C(F)F)[nH]c(=O)c23)CC1 10.1021/ml100251u
10197980 88523 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 186 4 2 2 1.6 CCCCc1[nH]nc(C(=O)O)c1F 10.1016/j.bmcl.2007.07.101
CHEMBL235009 88523 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 186 4 2 2 1.6 CCCCc1[nH]nc(C(=O)O)c1F 10.1016/j.bmcl.2007.07.101
4913402 149410 None 45 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 140 2 2 2 0.7 CCc1cc(C(=O)O)[nH]n1 10.1016/j.bmcl.2007.07.101
CHEMBL394498 149410 None 45 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 140 2 2 2 0.7 CCc1cc(C(=O)O)[nH]n1 10.1016/j.bmcl.2007.07.101
16048845 167271 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 420 4 3 6 1.8 NC(=O)c1ccc2ncc(N3CCN(C(=O)Nc4ccccc4C(=O)O)CC3)nc2c1 10.1016/j.bmcl.2007.10.055
CHEMBL429120 167271 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 420 4 3 6 1.8 NC(=O)c1ccc2ncc(N3CCN(C(=O)Nc4ccccc4C(=O)O)CC3)nc2c1 10.1016/j.bmcl.2007.10.055
56950369 3559 None 16 Rat Functional pEC50 = 8.1 8.1 -3 4
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 276 4 2 4 1.3 O=c1cc(CCCC2(C)CC2)c2c(o1)[nH]c(=O)[nH]c2=O 10.1021/ml200243g
8469 3559 None 16 Rat Functional pEC50 = 8.1 8.1 -3 4
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 276 4 2 4 1.3 O=c1cc(CCCC2(C)CC2)c2c(o1)[nH]c(=O)[nH]c2=O 10.1021/ml200243g
CHEMBL2036958 3559 None 16 Rat Functional pEC50 = 8.1 8.1 -3 4
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 276 4 2 4 1.3 O=c1cc(CCCC2(C)CC2)c2c(o1)[nH]c(=O)[nH]c2=O 10.1021/ml200243g
DB12433 3559 None 16 Rat Functional pEC50 = 8.1 8.1 -3 4
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 276 4 2 4 1.3 O=c1cc(CCCC2(C)CC2)c2c(o1)[nH]c(=O)[nH]c2=O 10.1021/ml200243g
15605571 75261 None 0 Rat Functional pEC50 = 8.1 8.1 1 5
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 236 3 2 4 0.5 CCCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
CHEMBL2036813 75261 None 0 Rat Functional pEC50 = 8.1 8.1 1 5
Agonist activity at rat GPR109aAgonist activity at rat GPR109a
ChEMBL 236 3 2 4 0.5 CCCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
117629482 2823 None 82 Human Functional pEC50 = 8.1 8.1 -4 4
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.07.101
1588 2823 None 82 Human Functional pEC50 = 8.1 8.1 -4 4
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.07.101
1594 2823 None 82 Human Functional pEC50 = 8.1 8.1 -4 4
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.07.101
2835 2823 None 82 Human Functional pEC50 = 8.1 8.1 -4 4
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.07.101
938 2823 None 82 Human Functional pEC50 = 8.1 8.1 -4 4
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.07.101
CHEMBL573 2823 None 82 Human Functional pEC50 = 8.1 8.1 -4 4
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.07.101
DB00627 2823 None 82 Human Functional pEC50 = 8.1 8.1 -4 4
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.07.101
137635425 156012 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 331 4 3 3 2.7 O=C(CCC#Cc1ccc(O)cc1F)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4060899 156012 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 331 4 3 3 2.7 O=C(CCC#Cc1ccc(O)cc1F)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
4913402 149410 None 45 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 140 2 2 2 0.7 CCc1cc(C(=O)O)[nH]n1 10.1016/j.bmcl.2007.06.028
CHEMBL394498 149410 None 45 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 140 2 2 2 0.7 CCc1cc(C(=O)O)[nH]n1 10.1016/j.bmcl.2007.06.028
57413450 76498 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 220 3 2 2 2.0 CC(C)C[C@@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
CHEMBL2059821 76498 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 220 3 2 2 2.0 CC(C)C[C@@H]1[C@@H]2Cc3c(C(=O)O)n[nH]c3[C@@H]21 10.1021/jm2010964
156022048 178306 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 383 7 3 8 2.2 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1cn(C2CC2)cc1C(=O)O 10.1016/j.bmcl.2020.127105
CHEMBL4649587 178306 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 383 7 3 8 2.2 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1cn(C2CC2)cc1C(=O)O 10.1016/j.bmcl.2020.127105
53317491 58060 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 282 3 1 4 2.2 O=c1cc(CC2CCC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
CHEMBL1672735 58060 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 282 3 1 4 2.2 O=c1cc(CC2CCC2)c2c(=O)[nH]c(C(F)F)nc2o1 10.1021/ml100251u
57413545 76136 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 224 3 2 3 1.4 CSC[C@H]1[C@H]2c3[nH]nc(C(=O)O)c3C[C@H]21 10.1021/jm2010964
CHEMBL2057605 76136 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 224 3 2 3 1.4 CSC[C@H]1[C@H]2c3[nH]nc(C(=O)O)c3C[C@H]21 10.1021/jm2010964
24953853 69976 None 0 Rat Functional pEC50 = 7.1 7.1 -1 2
Agonist activity at rat nicotinic acid receptorAgonist activity at rat nicotinic acid receptor
ChEMBL 328 6 1 5 2.4 CCC#CCOc1nc2oc(=O)cc(CCCC3CC3)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
CHEMBL1939049 69976 None 0 Rat Functional pEC50 = 7.1 7.1 -1 2
Agonist activity at rat nicotinic acid receptorAgonist activity at rat nicotinic acid receptor
ChEMBL 328 6 1 5 2.4 CCC#CCOc1nc2oc(=O)cc(CCCC3CC3)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
11845295 149666 None 35 Human Functional pEC50 = 5.1 5.1 1 2
Agonist activity against human GPR109a assessed as forskolin-induced cAMP accumulationAgonist activity against human GPR109a assessed as forskolin-induced cAMP accumulation
ChEMBL 166 1 2 2 1.2 CC1CCc2c(C(=O)O)n[nH]c21 10.1021/jm800258p
CHEMBL394688 149666 None 35 Human Functional pEC50 = 5.1 5.1 1 2
Agonist activity against human GPR109a assessed as forskolin-induced cAMP accumulationAgonist activity against human GPR109a assessed as forskolin-induced cAMP accumulation
ChEMBL 166 1 2 2 1.2 CC1CCc2c(C(=O)O)n[nH]c21 10.1021/jm800258p
15986754 184596 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 323 5 2 2 3.8 O=C(CCc1ccc2ccccc2c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
CHEMBL484719 184596 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 323 5 2 2 3.8 O=C(CCc1ccc2ccccc2c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
776421 89962 None 65 Human Functional pEC50 = 5.1 5.1 30 2
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 154 2 2 2 1.2 CC(C)c1cc(C(=O)O)n[nH]1 10.1016/j.bmcl.2007.06.028
CHEMBL238002 89962 None 65 Human Functional pEC50 = 5.1 5.1 30 2
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 154 2 2 2 1.2 CC(C)c1cc(C(=O)O)n[nH]1 10.1016/j.bmcl.2007.06.028
11845295 149666 None 35 Human Functional pEC50 = 5.1 5.1 1 2
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 166 1 2 2 1.2 CC1CCc2c(C(=O)O)n[nH]c21 10.1016/j.bmcl.2007.06.028
CHEMBL394688 149666 None 35 Human Functional pEC50 = 5.1 5.1 1 2
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 166 1 2 2 1.2 CC1CCc2c(C(=O)O)n[nH]c21 10.1016/j.bmcl.2007.06.028
135922722 184297 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 391 5 3 5 3.2 Cn1nc(CCC(=O)Nc2ccccc2C(=O)O)c2c1-c1ccc(O)cc1CC2 10.1021/jm900151e
CHEMBL483160 184297 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
ChEMBL 391 5 3 5 3.2 Cn1nc(CCC(=O)Nc2ccccc2C(=O)O)c2c1-c1ccc(O)cc1CC2 10.1021/jm900151e
57412301 76133 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 218 3 2 2 1.8 O=C(O)c1n[nH]c2c1C[C@H]1[C@@H](CC3CC3)[C@@H]21 10.1021/jm2010964
CHEMBL2057602 76133 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 218 3 2 2 1.8 O=C(O)c1n[nH]c2c1C[C@H]1[C@@H](CC3CC3)[C@@H]21 10.1021/jm2010964
136000580 61469 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 387 6 4 8 1.0 C[C@@H]1CCC(C(=O)O)=C(NC(=O)[C@@H](N)Cc2nc(-c3ccc(O)cn3)no2)C1 10.1016/j.bmcl.2010.11.116
CHEMBL1770356 61469 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 387 6 4 8 1.0 C[C@@H]1CCC(C(=O)O)=C(NC(=O)[C@@H](N)Cc2nc(-c3ccc(O)cn3)no2)C1 10.1016/j.bmcl.2010.11.116
1591 131 None 45 Human Functional pEC50 = 7.1 7.1 33 2
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 168 4 2 2 1.5 CCCCc1cc(n[nH]1)C(=O)O 10.1016/j.bmcl.2007.07.101
6485181 131 None 45 Human Functional pEC50 = 7.1 7.1 33 2
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 168 4 2 2 1.5 CCCCc1cc(n[nH]1)C(=O)O 10.1016/j.bmcl.2007.07.101
CHEMBL428730 131 None 45 Human Functional pEC50 = 7.1 7.1 33 2
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assayAgonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL 168 4 2 2 1.5 CCCCc1cc(n[nH]1)C(=O)O 10.1016/j.bmcl.2007.07.101
57412303 76137 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 224 3 2 3 1.4 CSC[C@@H]1[C@H]2c3[nH]nc(C(=O)O)c3C[C@@H]12 10.1021/jm2010964
CHEMBL2057606 76137 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assayAgonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
ChEMBL 224 3 2 3 1.4 CSC[C@@H]1[C@H]2c3[nH]nc(C(=O)O)c3C[C@@H]12 10.1021/jm2010964
11617480 88715 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 362 6 3 4 3.7 O=C(CCc1ccc(-c2ccc(O)cn2)cc1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL235952 88715 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 362 6 3 4 3.7 O=C(CCc1ccc(-c2ccc(O)cn2)cc1)Nc1ccccc1C(=O)O 10.1021/jm700942d
776416 18945 None 63 Human Functional pEC50 = 6.1 6.1 -5 2
Agonist activity against human GPR109a assessed as forskolin-induced cAMP accumulationAgonist activity against human GPR109a assessed as forskolin-induced cAMP accumulation
ChEMBL 152 1 2 2 0.6 O=C(O)c1n[nH]c2c1CCC2 10.1021/jm800258p
CHEMBL128604 18945 None 63 Human Functional pEC50 = 6.1 6.1 -5 2
Agonist activity against human GPR109a assessed as forskolin-induced cAMP accumulationAgonist activity against human GPR109a assessed as forskolin-induced cAMP accumulation
ChEMBL 152 1 2 2 0.6 O=C(O)c1n[nH]c2c1CCC2 10.1021/jm800258p
57398905 69949 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 328 5 1 6 2.0 CCc1cc(=O)oc2nc(OCc3cccc(OC)c3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939022 69949 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 328 5 1 6 2.0 CCc1cc(=O)oc2nc(OCc3cccc(OC)c3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
776416 18945 None 63 Human Functional pEC50 = 6.1 6.1 -5 2
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 152 1 2 2 0.6 O=C(O)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2007.06.028
CHEMBL128604 18945 None 63 Human Functional pEC50 = 6.1 6.1 -5 2
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 152 1 2 2 0.6 O=C(O)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2007.06.028
44441304 93471 None 21 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 156 3 2 3 0.3 COCc1cc(C(=O)O)[nH]n1 10.1016/j.bmcl.2007.06.028
CHEMBL245858 93471 None 21 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 156 3 2 3 0.3 COCc1cc(C(=O)O)[nH]n1 10.1016/j.bmcl.2007.06.028
44441321 93885 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 182 2 2 3 1.1 CCC1OCc2c1n[nH]c2C(=O)O 10.1016/j.bmcl.2007.06.028
CHEMBL247723 93885 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 182 2 2 3 1.1 CCC1OCc2c1n[nH]c2C(=O)O 10.1016/j.bmcl.2007.06.028
136088962 61421 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 368 6 4 7 1.6 N[C@H](Cc1nc(-c2ccc(O)cc2)no1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1770176 61421 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 368 6 4 7 1.6 N[C@H](Cc1nc(-c2ccc(O)cc2)no1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
11041813 93804 None 21 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 202 3 2 2 1.7 O=C(O)c1cc(Cc2ccccc2)n[nH]1 10.1016/j.bmcl.2007.06.028
CHEMBL247317 93804 None 21 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production testAgonist activity at human cloned GPR109a receptor by forskolin-stimulated cAMP production test
ChEMBL 202 3 2 2 1.7 O=C(O)c1cc(Cc2ccccc2)n[nH]1 10.1016/j.bmcl.2007.06.028
137648386 157864 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 347 4 3 3 3.2 O=C(CCC#Cc1ccc(O)cc1Cl)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4082765 157864 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at recombinant human HCA2 receptor expressed in Flp-IN HEK cells assessed as reduction in forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 347 4 3 3 3.2 O=C(CCC#Cc1ccc(O)cc1Cl)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
24954201 69975 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 314 5 1 5 2.0 CCC#CCOc1nc2oc(=O)cc(CCC3CC3)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
CHEMBL1939048 69975 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 314 5 1 5 2.0 CCC#CCOc1nc2oc(=O)cc(CCC3CC3)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
90645402 112545 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 335 2 3 3 2.9 O=C(C#Cc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
CHEMBL3298702 112545 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsAgonist activity at human HCA2 receptor expressed in Flp-In-293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins
ChEMBL 335 2 3 3 2.9 O=C(C#Cc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2014.05.011
16048923 94709 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 376 3 2 4 3.3 O=C(O)c1ccccc1NC(=O)N1CCN(c2nccc3ccccc23)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL252506 94709 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 376 3 2 4 3.3 O=C(O)c1ccccc1NC(=O)N1CCN(c2nccc3ccccc23)CC1 10.1016/j.bmcl.2007.10.055
15981408 94399 None 0 Human Functional pEC50 = 5.0 5.0 - 1
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 405 3 2 5 3.5 C[C@H]1CN(c2cnc3ccccc3n2)C[C@@H](C)N1C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2007.10.055
CHEMBL250690 94399 None 0 Human Functional pEC50 = 5.0 5.0 - 1
Agonist activity at human GPR106A by [35S]GTPgammaS binding assayAgonist activity at human GPR106A by [35S]GTPgammaS binding assay
ChEMBL 405 3 2 5 3.5 C[C@H]1CN(c2cnc3ccccc3n2)C[C@@H](C)N1C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2007.10.055
57391932 69962 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 246 3 1 5 0.5 C#CCOc1nc2oc(=O)cc(CC)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
CHEMBL1939035 69962 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 246 3 1 5 0.5 C#CCOc1nc2oc(=O)cc(CC)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
44250176 1131 None 0 Human Functional pEC50 = 5.0 5.0 -2951 2
Agonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 319 6 2 5 3.4 OC(=O)c1n[nH]c(c1)N(Cc1cscc1)Cc1cscc1 10.1016/j.bmcl.2009.05.108
5800 1131 None 0 Human Functional pEC50 = 5.0 5.0 -2951 2
Agonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 319 6 2 5 3.4 OC(=O)c1n[nH]c(c1)N(Cc1cscc1)Cc1cscc1 10.1016/j.bmcl.2009.05.108
CHEMBL564300 1131 None 0 Human Functional pEC50 = 5.0 5.0 -2951 2
Agonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 319 6 2 5 3.4 OC(=O)c1n[nH]c(c1)N(Cc1cscc1)Cc1cscc1 10.1016/j.bmcl.2009.05.108
24811547 7378 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 415 6 3 3 4.9 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2ccccc2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1086355 7378 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 415 6 3 3 4.9 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2ccccc2)CC1 10.1016/j.bmcl.2010.04.001
24741307 88769 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 365 6 3 5 3.2 Cc1c(CCC(=O)Nc2ccccc2C(=O)O)cnn1-c1ccc(O)cc1 10.1021/jm700942d
CHEMBL236163 88769 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 365 6 3 5 3.2 Cc1c(CCC(=O)Nc2ccccc2C(=O)O)cnn1-c1ccc(O)cc1 10.1021/jm700942d
57400596 69958 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 300 4 1 7 0.8 CCc1cc(=O)oc2nc(OCc3ccnnc3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
CHEMBL1939031 69958 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 300 4 1 7 0.8 CCc1cc(=O)oc2nc(OCc3ccnnc3)[nH]c(=O)c12 10.1016/j.bmcl.2011.12.041
11610363 89524 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 369 6 3 6 3.2 O=C(CCc1ncc(-c2ccc(O)cn2)s1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL237247 89524 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 369 6 3 6 3.2 O=C(CCc1ncc(-c2ccc(O)cn2)s1)Nc1ccccc1C(=O)O 10.1021/jm700942d
44579645 187174 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 444 8 1 6 4.6 COc1cccc(OCCNC(=O)c2cnc3c(-c4ccc(C(C)C)cc4)cnn3c2C)c1 10.1016/j.bmcl.2008.08.039
CHEMBL491227 187174 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 444 8 1 6 4.6 COc1cccc(OCCNC(=O)c2cnc3c(-c4ccc(C(C)C)cc4)cnn3c2C)c1 10.1016/j.bmcl.2008.08.039
135627640 61417 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 417 6 4 6 3.4 NC(Cc1cnc(-c2ccc(O)cc2Cl)s1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1770172 61417 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR109A receptor expressed in CHO-K1 cells after 60 mins by [35S]GTPgammaS binding assay
ChEMBL 417 6 4 6 3.4 NC(Cc1cnc(-c2ccc(O)cc2Cl)s1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
15605292 75264 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 266 3 2 6 -0.7 CCOC(=O)Cc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
CHEMBL2036819 75264 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 266 3 2 6 -0.7 CCOC(=O)Cc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
11992789 199054 None 0 Human Functional pEC50 = 5.0 5.0 - 1
Agonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 343 6 2 3 3.6 O=C(O)c1cc(N(Cc2cccc(F)c2)Cc2cccc(F)c2)[nH]n1 10.1016/j.bmcl.2009.05.108
CHEMBL564064 199054 None 0 Human Functional pEC50 = 5.0 5.0 - 1
Agonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assayAgonist activity at GPR109a receptor transfected in CHOK1 cells assessed as inhibition of forskolin-induced cAMP generation by HTRF assay
ChEMBL 343 6 2 3 3.6 O=C(O)c1cc(N(Cc2cccc(F)c2)Cc2cccc(F)c2)[nH]n1 10.1016/j.bmcl.2009.05.108
46890328 6683 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 484 6 3 4 5.3 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2ccc(C(F)(F)F)nc2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1083451 6683 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 484 6 3 4 5.3 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2ccc(C(F)(F)F)nc2)CC1 10.1016/j.bmcl.2010.04.001
44579742 187150 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assayAgonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assay
ChEMBL 347 6 2 3 3.9 O=Cc1ccc2cc(CCC(=O)Nc3ccccc3C(=O)O)ccc2c1 10.1016/j.bmcl.2008.08.030
CHEMBL491003 187150 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assayAgonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assay
ChEMBL 347 6 2 3 3.9 O=Cc1ccc2cc(CCC(=O)Nc3ccccc3C(=O)O)ccc2c1 10.1016/j.bmcl.2008.08.030
136375455 177659 None 0 Human Functional pEC50 = 5.0 5.0 - 1
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 385 7 3 8 2.5 CC(C)n1cc(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
CHEMBL4640349 177659 None 0 Human Functional pEC50 = 5.0 5.0 - 1
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
ChEMBL 385 7 3 8 2.5 CC(C)n1cc(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
57395377 69964 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 274 3 1 5 1.2 CCC#CCOc1nc2oc(=O)cc(CC)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
CHEMBL1939037 69964 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human HM74AAgonist activity at human HM74A
ChEMBL 274 3 1 5 1.2 CCC#CCOc1nc2oc(=O)cc(CC)c2c(=O)[nH]1 10.1016/j.bmcl.2011.12.041
11566404 145759 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 346 6 2 3 4.0 O=C(CCc1ccc(-c2ccccn2)cc1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL391603 145759 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assayAgonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
ChEMBL 346 6 2 3 4.0 O=C(CCc1ccc(-c2ccccn2)cc1)Nc1ccccc1C(=O)O 10.1021/jm700942d
136086824 6845 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 453 7 3 8 2.7 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CC(c2ccc(F)nc2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1084031 6845 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assayAgonist activity at human niacin receptor expressed in CHO-KI cells by [35S]GTPgammaS binding assay
ChEMBL 453 7 3 8 2.7 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CC(c2ccc(F)nc2)CC1 10.1016/j.bmcl.2010.04.001
117629482 2823 None 82 Human Functional pEC50 = 7 7.0 -4 4
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml200243g
1588 2823 None 82 Human Functional pEC50 = 7 7.0 -4 4
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml200243g
1594 2823 None 82 Human Functional pEC50 = 7 7.0 -4 4
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml200243g
2835 2823 None 82 Human Functional pEC50 = 7 7.0 -4 4
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml200243g
938 2823 None 82 Human Functional pEC50 = 7 7.0 -4 4
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml200243g
CHEMBL573 2823 None 82 Human Functional pEC50 = 7 7.0 -4 4
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml200243g
DB00627 2823 None 82 Human Functional pEC50 = 7 7.0 -4 4
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/ml200243g
59304624 75260 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 222 2 2 4 0.1 CCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
CHEMBL2036812 75260 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 222 2 2 4 0.1 CCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1021/ml200243g
13557 1106 None 64 Human Functional pIC50 = 5.9 5.9 - 1
Agonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assayAgonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assay
ChEMBL 127 1 1 3 0.7 CC1=NOC(=C1)C(=O)O 10.1074/jbc.m701866200
853085 1106 None 64 Human Functional pIC50 = 5.9 5.9 - 1
Agonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assayAgonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assay
ChEMBL 127 1 1 3 0.7 CC1=NOC(=C1)C(=O)O 10.1074/jbc.m701866200
CHEMBL393428 1106 None 64 Human Functional pIC50 = 5.9 5.9 - 1
Agonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assayAgonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assay
ChEMBL 127 1 1 3 0.7 CC1=NOC(=C1)C(=O)O 10.1074/jbc.m701866200
11550911 95241 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Agonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assayAgonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assay
ChEMBL 280 3 2 2 2.5 O=C(O)c1cc(Cc2cccc(Br)c2)[nH]n1 10.1074/jbc.m701866200
CHEMBL255877 95241 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Agonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assayAgonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assay
ChEMBL 280 3 2 2 2.5 O=C(O)c1cc(Cc2cccc(Br)c2)[nH]n1 10.1074/jbc.m701866200
11557600 167478 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Agonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assayAgonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assay
ChEMBL 220 3 2 2 1.8 O=C(O)c1cc(Cc2cccc(F)c2)[nH]n1 10.1074/jbc.m701866200
CHEMBL429495 167478 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Agonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assayAgonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assay
ChEMBL 220 3 2 2 1.8 O=C(O)c1cc(Cc2cccc(F)c2)[nH]n1 10.1074/jbc.m701866200
776421 89962 None 65 Human Functional pIC50 = 5.6 5.6 30 2
Agonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assayAgonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assay
ChEMBL 154 2 2 2 1.2 CC(C)c1cc(C(=O)O)n[nH]1 10.1074/jbc.m701866200
CHEMBL238002 89962 None 65 Human Functional pIC50 = 5.6 5.6 30 2
Agonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assayAgonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assay
ChEMBL 154 2 2 2 1.2 CC(C)c1cc(C(=O)O)n[nH]1 10.1074/jbc.m701866200
11776293 149345 None 4 Human Functional pIC50 = 5.4 5.4 - 1
Agonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assayAgonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assay
ChEMBL 236 3 2 2 2.4 O=C(O)c1cc(Cc2cccc(Cl)c2)n[nH]1 10.1074/jbc.m701866200
CHEMBL394441 149345 None 4 Human Functional pIC50 = 5.4 5.4 - 1
Agonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assayAgonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assay
ChEMBL 236 3 2 2 2.4 O=C(O)c1cc(Cc2cccc(Cl)c2)n[nH]1 10.1074/jbc.m701866200
1595 259 None 36 Human Functional pIC50 = 6.3 6.3 4 2
Activity at GPR109a assessed as inhibition of forskolin-stimulated cAMP productionActivity at GPR109a assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1021/jm800896z
51576 259 None 36 Human Functional pIC50 = 6.3 6.3 4 2
Activity at GPR109a assessed as inhibition of forskolin-stimulated cAMP productionActivity at GPR109a assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1021/jm800896z
CHEMBL278488 259 None 36 Human Functional pIC50 = 6.3 6.3 4 2
Activity at GPR109a assessed as inhibition of forskolin-stimulated cAMP productionActivity at GPR109a assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1021/jm800896z
117629482 2823 None 82 Human Functional pIC50 = 4.2 4.2 -4 4
Agonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assayAgonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1074/jbc.m701866200
1588 2823 None 82 Human Functional pIC50 = 4.2 4.2 -4 4
Agonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assayAgonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1074/jbc.m701866200
1594 2823 None 82 Human Functional pIC50 = 4.2 4.2 -4 4
Agonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assayAgonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1074/jbc.m701866200
2835 2823 None 82 Human Functional pIC50 = 4.2 4.2 -4 4
Agonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assayAgonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1074/jbc.m701866200
938 2823 None 82 Human Functional pIC50 = 4.2 4.2 -4 4
Agonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assayAgonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1074/jbc.m701866200
CHEMBL573 2823 None 82 Human Functional pIC50 = 4.2 4.2 -4 4
Agonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assayAgonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1074/jbc.m701866200
DB00627 2823 None 82 Human Functional pIC50 = 4.2 4.2 -4 4
Agonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assayAgonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assay
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1074/jbc.m701866200
108 111 None 0 Human Functional pEC50 = 8.3 8.3 - 1
NoneNone
Drug Central 137 2 1 2 0.7 OC(=O)Cc1cccnc1 None
1590 111 None 0 Human Functional pEC50 = 8.3 8.3 - 1
NoneNone
Drug Central 137 2 1 2 0.7 OC(=O)Cc1cccnc1 None
3505 111 None 0 Human Functional pEC50 = 8.3 8.3 - 1
NoneNone
Drug Central 137 2 1 2 0.7 OC(=O)Cc1cccnc1 None
CHEMBL1741437 111 None 0 Human Functional pEC50 = 8.3 8.3 - 1
NoneNone
Drug Central 137 2 1 2 0.7 OC(=O)Cc1cccnc1 None
1596 260 None 60 Human Functional pEC50 = 8.3 8.3 - 1
NoneNone
Drug Central 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O None
5310993 260 None 60 Human Functional pEC50 = 8.3 8.3 - 1
NoneNone
Drug Central 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O None
76 260 None 60 Human Functional pEC50 = 8.3 8.3 - 1
NoneNone
Drug Central 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O None
CHEMBL345714 260 None 60 Human Functional pEC50 = 8.3 8.3 - 1
NoneNone
Drug Central 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O None
DB09055 260 None 60 Human Functional pEC50 = 8.3 8.3 - 1
NoneNone
Drug Central 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O None
13558 1041 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at HCAR2, determined in a [<sup>35</sup>S]-GTP&gammagS binding assayAgonist activity at HCAR2, determined in a [<sup>35</sup>S]-GTP&gammagS binding assay
Guide to Pharmacology 242 3 2 4 0.9 C(CCC)N1C(NC(C=2NC(=NC12)Cl)=O)=O None
59299562 1041 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at HCAR2, determined in a [<sup>35</sup>S]-GTP&gammagS binding assayAgonist activity at HCAR2, determined in a [<sup>35</sup>S]-GTP&gammagS binding assay
Guide to Pharmacology 242 3 2 4 0.9 C(CCC)N1C(NC(C=2NC(=NC12)Cl)=O)=O None
CHEMBL3732182 1041 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at HCAR2, determined in a [<sup>35</sup>S]-GTP&gammagS binding assayAgonist activity at HCAR2, determined in a [<sup>35</sup>S]-GTP&gammagS binding assay
Guide to Pharmacology 242 3 2 4 0.9 C(CCC)N1C(NC(C=2NC(=NC12)Cl)=O)=O None
13559 1135 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at HCAR2, determined in a [<sup>35</sup>S]-GTP&gammagS binding assayAgonist activity at HCAR2, determined in a [<sup>35</sup>S]-GTP&gammagS binding assay
Guide to Pharmacology 460 9 1 9 2.1 C(CCC)N1C(N(C(C=2NC(=NC12)Cl)=O)CCCN3N=C(N=N3)CC4=CC=C(C=C4)F)=O None
59395852 1135 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at HCAR2, determined in a [<sup>35</sup>S]-GTP&gammagS binding assayAgonist activity at HCAR2, determined in a [<sup>35</sup>S]-GTP&gammagS binding assay
Guide to Pharmacology 460 9 1 9 2.1 C(CCC)N1C(N(C(C=2NC(=NC12)Cl)=O)CCCN3N=C(N=N3)CC4=CC=C(C=C4)F)=O None
1059 750 None 54 Human Functional pEC50 = 2.8 2.8 -67 3
UnclassifiedUnclassified
Guide to Pharmacology 88 2 1 1 0.9 CCCC(=O)O None
264 750 None 54 Human Functional pEC50 = 2.8 2.8 -67 3
UnclassifiedUnclassified
Guide to Pharmacology 88 2 1 1 0.9 CCCC(=O)O None
CHEMBL14227 750 None 54 Human Functional pEC50 = 2.8 2.8 -67 3
UnclassifiedUnclassified
Guide to Pharmacology 88 2 1 1 0.9 CCCC(=O)O None
DB03568 750 None 54 Human Functional pEC50 = 2.8 2.8 -67 3
UnclassifiedUnclassified
Guide to Pharmacology 88 2 1 1 0.9 CCCC(=O)O None
1593 609 None 0 Human Functional pEC50 = 3.1 3.1 -2 2
UnclassifiedUnclassified
Guide to Pharmacology 104 2 2 2 -0.2 C[C@H](CC(=O)O)O 15929991
92135 609 None 0 Human Functional pEC50 = 3.1 3.1 -2 2
UnclassifiedUnclassified
Guide to Pharmacology 104 2 2 2 -0.2 C[C@H](CC(=O)O)O 15929991
CHEMBL1162484 609 None 0 Human Functional pEC50 = 3.1 3.1 -2 2
UnclassifiedUnclassified
Guide to Pharmacology 104 2 2 2 -0.2 C[C@H](CC(=O)O)O 15929991
5787 3005 None 68 Human Functional pEC50 = 3.5 3.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology 164 2 2 2 1.5 OC(=O)/C=C/c1ccc(cc1)O 19136666
637542 3005 None 68 Human Functional pEC50 = 3.5 3.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology 164 2 2 2 1.5 OC(=O)/C=C/c1ccc(cc1)O 19136666
CHEMBL66879 3005 None 68 Human Functional pEC50 = 3.5 3.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology 164 2 2 2 1.5 OC(=O)/C=C/c1ccc(cc1)O 19136666
DB04066 3005 None 68 Human Functional pEC50 = 3.5 3.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology 164 2 2 2 1.5 OC(=O)/C=C/c1ccc(cc1)O 19136666
3203 939 None 65 Human Functional pEC50 = 3.6 3.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology 148 2 1 1 1.8 OC(=O)/C=C/c1ccccc1 19136666
444539 939 None 65 Human Functional pEC50 = 3.6 3.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology 148 2 1 1 1.8 OC(=O)/C=C/c1ccccc1 19136666
CHEMBL27246 939 None 65 Human Functional pEC50 = 3.6 3.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology 148 2 1 1 1.8 OC(=O)/C=C/c1ccccc1 19136666
5369209 2591 None 55 Human Functional pEC50 = 5.0 5.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology 130 2 1 3 -0.2 COC(=O)/C=C/C(=O)O 18722346
5786 2591 None 55 Human Functional pEC50 = 5.0 5.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology 130 2 1 3 -0.2 COC(=O)/C=C/C(=O)O 18722346
CHEMBL589586 2591 None 55 Human Functional pEC50 = 5.0 5.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology 130 2 1 3 -0.2 COC(=O)/C=C/C(=O)O 18722346
DB14219 2591 None 55 Human Functional pEC50 = 5.0 5.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology 130 2 1 3 -0.2 COC(=O)/C=C/C(=O)O 18722346
1596 260 None 60 Human Functional pEC50 = 5.4 5.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O 12522134
1596 260 None 60 Human Functional pEC50 = 5.4 5.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O 12646212
5310993 260 None 60 Human Functional pEC50 = 5.4 5.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O 12522134
5310993 260 None 60 Human Functional pEC50 = 5.4 5.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O 12646212
76 260 None 60 Human Functional pEC50 = 5.4 5.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O 12522134
76 260 None 60 Human Functional pEC50 = 5.4 5.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O 12646212
CHEMBL345714 260 None 60 Human Functional pEC50 = 5.4 5.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O 12522134
CHEMBL345714 260 None 60 Human Functional pEC50 = 5.4 5.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O 12646212
DB09055 260 None 60 Human Functional pEC50 = 5.4 5.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O 12522134
DB09055 260 None 60 Human Functional pEC50 = 5.4 5.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O 12646212
5794 1096 None 0 Human Functional pEC50 = 5.6 5.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology 446 6 1 5 4.3 ClC1CCC(CC1Cl)c1cnn2c1ncc(c2C)C(=O)NCCOc1ccccc1 22420767
73755156 1096 None 0 Human Functional pEC50 = 5.6 5.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology 446 6 1 5 4.3 ClC1CCC(CC1Cl)c1cnn2c1ncc(c2C)C(=O)NCCOc1ccccc1 22420767
11159621 2548 None 38 Human Functional pEC50 = 5.8 5.8 -1 3
UnclassifiedUnclassified
Guide to Pharmacology 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 18665582
5784 2548 None 38 Human Functional pEC50 = 5.8 5.8 -1 3
UnclassifiedUnclassified
Guide to Pharmacology 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 18665582
CHEMBL456145 2548 None 38 Human Functional pEC50 = 5.8 5.8 -1 3
UnclassifiedUnclassified
Guide to Pharmacology 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 18665582
DB05939 2548 None 38 Human Functional pEC50 = 5.8 5.8 -1 3
UnclassifiedUnclassified
Guide to Pharmacology 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 18665582
117629482 2823 None 82 Human Functional pEC50 = 6.6 6.6 -4 4
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12522134
117629482 2823 None 82 Human Functional pEC50 = 6.6 6.6 -4 4
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12563315
117629482 2823 None 82 Human Functional pEC50 = 6.6 6.6 -4 4
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12646212
1588 2823 None 82 Human Functional pEC50 = 6.6 6.6 -4 4
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12522134
1588 2823 None 82 Human Functional pEC50 = 6.6 6.6 -4 4
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12563315
1588 2823 None 82 Human Functional pEC50 = 6.6 6.6 -4 4
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12646212
1594 2823 None 82 Human Functional pEC50 = 6.6 6.6 -4 4
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12522134
1594 2823 None 82 Human Functional pEC50 = 6.6 6.6 -4 4
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12563315
1594 2823 None 82 Human Functional pEC50 = 6.6 6.6 -4 4
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12646212
2835 2823 None 82 Human Functional pEC50 = 6.6 6.6 -4 4
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12522134
2835 2823 None 82 Human Functional pEC50 = 6.6 6.6 -4 4
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12563315
2835 2823 None 82 Human Functional pEC50 = 6.6 6.6 -4 4
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12646212
938 2823 None 82 Human Functional pEC50 = 6.6 6.6 -4 4
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12522134
938 2823 None 82 Human Functional pEC50 = 6.6 6.6 -4 4
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12563315
938 2823 None 82 Human Functional pEC50 = 6.6 6.6 -4 4
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12646212
CHEMBL573 2823 None 82 Human Functional pEC50 = 6.6 6.6 -4 4
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12522134
CHEMBL573 2823 None 82 Human Functional pEC50 = 6.6 6.6 -4 4
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12563315
CHEMBL573 2823 None 82 Human Functional pEC50 = 6.6 6.6 -4 4
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12646212
DB00627 2823 None 82 Human Functional pEC50 = 6.6 6.6 -4 4
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12522134
DB00627 2823 None 82 Human Functional pEC50 = 6.6 6.6 -4 4
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12563315
DB00627 2823 None 82 Human Functional pEC50 = 6.6 6.6 -4 4
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12646212
25101223 1152 None 7 Human Functional pEC50 = 6.8 6.8 - 1
UnclassifiedUnclassified
Guide to Pharmacology 428 7 1 5 5.0 C[C@@H](NC(=O)c1cnc2n(c1C)ncc2c1ccc(cc1)C(C)C)COc1ccccc1 18752940
5795 1152 None 7 Human Functional pEC50 = 6.8 6.8 - 1
UnclassifiedUnclassified
Guide to Pharmacology 428 7 1 5 5.0 C[C@@H](NC(=O)c1cnc2n(c1C)ncc2c1ccc(cc1)C(C)C)COc1ccccc1 18752940
CHEMBL490599 1152 None 7 Human Functional pEC50 = 6.8 6.8 - 1
UnclassifiedUnclassified
Guide to Pharmacology 428 7 1 5 5.0 C[C@@H](NC(=O)c1cnc2n(c1C)ncc2c1ccc(cc1)C(C)C)COc1ccccc1 18752940
11672811 1001 None 4 Human Functional pEC50 = 7.4 7.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 188 1 2 4 0.2 n1nnc([nH]1)c1n[nH]c2c1CC1C2C1 20363624
5790 1001 None 4 Human Functional pEC50 = 7.4 7.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 188 1 2 4 0.2 n1nnc([nH]1)c1n[nH]c2c1CC1C2C1 20363624
CHEMBL1169573 1001 None 4 Human Functional pEC50 = 7.4 7.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 188 1 2 4 0.2 n1nnc([nH]1)c1n[nH]c2c1CC1C2C1 20363624
13359 1099 None 0 Human Functional pEC50 = 7.4 7.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 442 9 3 7 4.8 CNCCNCC1=CC=CC(=C1)C2=NC(C3=C(C)ON=C3C)=C(C)C(NC4=CC=CC=C4)=N2 None
146188223 1099 None 0 Human Functional pEC50 = 7.4 7.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 442 9 3 7 4.8 CNCCNCC1=CC=CC(=C1)C2=NC(C3=C(C)ON=C3C)=C(C)C(NC4=CC=CC=C4)=N2 None
46215799 1880 None 0 Human Functional pEC50 = 7.5 7.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology 256 4 2 4 1.3 CCCCCn1c(=O)[nH]c(=O)c2c1nc([nH]2)Cl 25773497
8470 1880 None 0 Human Functional pEC50 = 7.5 7.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology 256 4 2 4 1.3 CCCCCn1c(=O)[nH]c(=O)c2c1nc([nH]2)Cl 25773497
CHEMBL3730241 1880 None 0 Human Functional pEC50 = 7.5 7.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology 256 4 2 4 1.3 CCCCCn1c(=O)[nH]c(=O)c2c1nc([nH]2)Cl 25773497
11607970 2552 None 14 Human Functional pEC50 = 7.6 7.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology 164 1 2 2 0.8 OC(=O)c1n[nH]c2c1CC1C2C1 22435740
5785 2552 None 14 Human Functional pEC50 = 7.6 7.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology 164 1 2 2 0.8 OC(=O)c1n[nH]c2c1CC1C2C1 22435740
CHEMBL2059221 2552 None 14 Human Functional pEC50 = 7.6 7.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology 164 1 2 2 0.8 OC(=O)c1n[nH]c2c1CC1C2C1 22435740
135416394 2560 None 43 Human Functional pEC50 = 7.8 7.8 15 3
UnclassifiedUnclassified
Guide to Pharmacology 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 20184326
5788 2560 None 43 Human Functional pEC50 = 7.8 7.8 15 3
UnclassifiedUnclassified
Guide to Pharmacology 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 20184326
73755154 2560 None 43 Human Functional pEC50 = 7.8 7.8 15 3
UnclassifiedUnclassified
Guide to Pharmacology 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 20184326
CHEMBL1086657 2560 None 43 Human Functional pEC50 = 7.8 7.8 15 3
UnclassifiedUnclassified
Guide to Pharmacology 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 20184326
56950369 3559 None 16 Human Functional pEC50 = 8.7 8.7 3 4
UnclassifiedUnclassified
Guide to Pharmacology 276 4 2 4 1.3 O=c1cc(CCCC2(C)CC2)c2c(o1)[nH]c(=O)[nH]c2=O 24900372
8469 3559 None 16 Human Functional pEC50 = 8.7 8.7 3 4
UnclassifiedUnclassified
Guide to Pharmacology 276 4 2 4 1.3 O=c1cc(CCCC2(C)CC2)c2c(o1)[nH]c(=O)[nH]c2=O 24900372
CHEMBL2036958 3559 None 16 Human Functional pEC50 = 8.7 8.7 3 4
UnclassifiedUnclassified
Guide to Pharmacology 276 4 2 4 1.3 O=c1cc(CCCC2(C)CC2)c2c(o1)[nH]c(=O)[nH]c2=O 24900372
DB12433 3559 None 16 Human Functional pEC50 = 8.7 8.7 3 4
UnclassifiedUnclassified
Guide to Pharmacology 276 4 2 4 1.3 O=c1cc(CCCC2(C)CC2)c2c(o1)[nH]c(=O)[nH]c2=O 24900372
1593 609 None 0 Mouse Functional pEC50 None 3.5 3.5 2 2
UnclassifiedUnclassified
Guide to Pharmacology 104 2 2 2 -0.2 C[C@H](CC(=O)O)O 15929991
92135 609 None 0 Mouse Functional pEC50 None 3.5 3.5 2 2
UnclassifiedUnclassified
Guide to Pharmacology 104 2 2 2 -0.2 C[C@H](CC(=O)O)O 15929991
CHEMBL1162484 609 None 0 Mouse Functional pEC50 None 3.5 3.5 2 2
UnclassifiedUnclassified
Guide to Pharmacology 104 2 2 2 -0.2 C[C@H](CC(=O)O)O 15929991
1592 144 None 71 Human Functional pEC50 None 5.1 5.1 - 1
UnclassifiedUnclassified
Guide to Pharmacology 137 1 1 2 1.1 Cc1cc(cnc1)C(=O)O 12522134
256208 144 None 71 Human Functional pEC50 None 5.1 5.1 - 1
UnclassifiedUnclassified
Guide to Pharmacology 137 1 1 2 1.1 Cc1cc(cnc1)C(=O)O 12522134
CHEMBL247132 144 None 71 Human Functional pEC50 None 5.1 5.1 - 1
UnclassifiedUnclassified
Guide to Pharmacology 137 1 1 2 1.1 Cc1cc(cnc1)C(=O)O 12522134
108 111 None 0 Human Functional pEC50 None 5.3 5.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology 137 2 1 2 0.7 OC(=O)Cc1cccnc1 12522134
1590 111 None 0 Human Functional pEC50 None 5.3 5.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology 137 2 1 2 0.7 OC(=O)Cc1cccnc1 12522134
3505 111 None 0 Human Functional pEC50 None 5.3 5.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology 137 2 1 2 0.7 OC(=O)Cc1cccnc1 12522134
CHEMBL1741437 111 None 0 Human Functional pEC50 None 5.3 5.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology 137 2 1 2 0.7 OC(=O)Cc1cccnc1 12522134
1595 259 None 36 Human Functional pEC50 None 5.8 5.8 4 2
UnclassifiedUnclassified
Guide to Pharmacology 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 12522134
1595 259 None 36 Human Functional pEC50 None 5.8 5.8 4 2
UnclassifiedUnclassified
Guide to Pharmacology 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 15929991
1595 259 None 36 Human Functional pEC50 None 5.8 5.8 4 2
UnclassifiedUnclassified
Guide to Pharmacology 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 16389067
1595 259 None 36 Human Functional pEC50 None 5.8 5.8 4 2
UnclassifiedUnclassified
Guide to Pharmacology 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 17358052
51576 259 None 36 Human Functional pEC50 None 5.8 5.8 4 2
UnclassifiedUnclassified
Guide to Pharmacology 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 12522134
51576 259 None 36 Human Functional pEC50 None 5.8 5.8 4 2
UnclassifiedUnclassified
Guide to Pharmacology 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 15929991
51576 259 None 36 Human Functional pEC50 None 5.8 5.8 4 2
UnclassifiedUnclassified
Guide to Pharmacology 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 16389067
51576 259 None 36 Human Functional pEC50 None 5.8 5.8 4 2
UnclassifiedUnclassified
Guide to Pharmacology 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 17358052
CHEMBL278488 259 None 36 Human Functional pEC50 None 5.8 5.8 4 2
UnclassifiedUnclassified
Guide to Pharmacology 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 12522134
CHEMBL278488 259 None 36 Human Functional pEC50 None 5.8 5.8 4 2
UnclassifiedUnclassified
Guide to Pharmacology 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 15929991
CHEMBL278488 259 None 36 Human Functional pEC50 None 5.8 5.8 4 2
UnclassifiedUnclassified
Guide to Pharmacology 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 16389067
CHEMBL278488 259 None 36 Human Functional pEC50 None 5.8 5.8 4 2
UnclassifiedUnclassified
Guide to Pharmacology 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 17358052
11483496 126 None 0 Human Functional pEC50 None 7.3 7.3 14 2
UnclassifiedUnclassified
Guide to Pharmacology 302 2 1 4 2.3 Brc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 15929991
11483496 126 None 0 Human Functional pEC50 None 7.3 7.3 14 2
UnclassifiedUnclassified
Guide to Pharmacology 302 2 1 4 2.3 Brc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 17358052
1589 126 None 0 Human Functional pEC50 None 7.3 7.3 14 2
UnclassifiedUnclassified
Guide to Pharmacology 302 2 1 4 2.3 Brc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 15929991
1589 126 None 0 Human Functional pEC50 None 7.3 7.3 14 2
UnclassifiedUnclassified
Guide to Pharmacology 302 2 1 4 2.3 Brc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 17358052
CHEMBL375493 126 None 0 Human Functional pEC50 None 7.3 7.3 14 2
UnclassifiedUnclassified
Guide to Pharmacology 302 2 1 4 2.3 Brc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 15929991
CHEMBL375493 126 None 0 Human Functional pEC50 None 7.3 7.3 14 2
UnclassifiedUnclassified
Guide to Pharmacology 302 2 1 4 2.3 Brc1scc(c1)C1(C)OC(=CC1=O)C(=O)O 17358052
53232 188732 None 57 Human Functional pIC50 = 8.1 8.1 -1 10
NoneNone
Drug Central 404 6 1 5 4.2 CC[C@H](C)C(=O)O[C@H]1C[C@@H](C)C=C2C=C[C@H](C)[C@H](CC[C@@H]3C[C@@H](O)CC(=O)O3)[C@H]21 None
CHEMBL503 188732 None 57 Human Functional pIC50 = 8.1 8.1 -1 10
NoneNone
Drug Central 404 6 1 5 4.2 CC[C@H](C)C(=O)O[C@H]1C[C@@H](C)C=C2C=C[C@H](C)[C@H](CC[C@@H]3C[C@@H](O)CC(=O)O3)[C@H]21 None
13557 1106 None 64 Human Functional pIC50 = 5.9 5.9 - 1
Inhibition of forskolin-stimulated cAMP production in CHO-K1 cells stably transfected with HCAR2.Inhibition of forskolin-stimulated cAMP production in CHO-K1 cells stably transfected with HCAR2.
Guide to Pharmacology 127 1 1 3 0.7 CC1=NOC(=C1)C(=O)O 17452318
853085 1106 None 64 Human Functional pIC50 = 5.9 5.9 - 1
Inhibition of forskolin-stimulated cAMP production in CHO-K1 cells stably transfected with HCAR2.Inhibition of forskolin-stimulated cAMP production in CHO-K1 cells stably transfected with HCAR2.
Guide to Pharmacology 127 1 1 3 0.7 CC1=NOC(=C1)C(=O)O 17452318
CHEMBL393428 1106 None 64 Human Functional pIC50 = 5.9 5.9 - 1
Inhibition of forskolin-stimulated cAMP production in CHO-K1 cells stably transfected with HCAR2.Inhibition of forskolin-stimulated cAMP production in CHO-K1 cells stably transfected with HCAR2.
Guide to Pharmacology 127 1 1 3 0.7 CC1=NOC(=C1)C(=O)O 17452318
12003694 1144 None 0 Human Functional pIC50 = 6.4 6.4 1 2
UnclassifiedUnclassified
Guide to Pharmacology 232 2 2 4 0.7 OC(=O)c1n[nH]c2c1CC(C2)c1ccnn1C 20615702
5793 1144 None 0 Human Functional pIC50 = 6.4 6.4 1 2
UnclassifiedUnclassified
Guide to Pharmacology 232 2 2 4 0.7 OC(=O)c1n[nH]c2c1CC(C2)c1ccnn1C 20615702
CHEMBL1208986 1144 None 0 Human Functional pIC50 = 6.4 6.4 1 2
UnclassifiedUnclassified
Guide to Pharmacology 232 2 2 4 0.7 OC(=O)c1n[nH]c2c1CC(C2)c1ccnn1C 20615702
135401973 1022 None 0 Human Functional pIC50 = 6.9 6.9 - 1
UnclassifiedUnclassified
Guide to Pharmacology 393 3 3 6 2.4 Oc1ccc2c(c1)ncc(n2)N1CCN(CC1)C(=O)Nc1ccccc1C(=O)O 18029181
5792 1022 None 0 Human Functional pIC50 = 6.9 6.9 - 1
UnclassifiedUnclassified
Guide to Pharmacology 393 3 3 6 2.4 Oc1ccc2c(c1)ncc(n2)N1CCN(CC1)C(=O)Nc1ccccc1C(=O)O 18029181
CHEMBL398496 1022 None 0 Human Functional pIC50 = 6.9 6.9 - 1
UnclassifiedUnclassified
Guide to Pharmacology 393 3 3 6 2.4 Oc1ccc2c(c1)ncc(n2)N1CCN(CC1)C(=O)Nc1ccccc1C(=O)O 18029181
11494579 1058 None 0 Human Functional pIC50 = 7.9 7.9 123 2
UnclassifiedUnclassified
Guide to Pharmacology 377 5 3 5 2.9 O=C(Nc1ccccc1C(=O)O)CCc1cnn2c1CCc1c2ccc(c1)O 19309152
5791 1058 None 0 Human Functional pIC50 = 7.9 7.9 123 2
UnclassifiedUnclassified
Guide to Pharmacology 377 5 3 5 2.9 O=C(Nc1ccccc1C(=O)O)CCc1cnn2c1CCc1c2ccc(c1)O 19309152
CHEMBL482768 1058 None 0 Human Functional pIC50 = 7.9 7.9 123 2
UnclassifiedUnclassified
Guide to Pharmacology 377 5 3 5 2.9 O=C(Nc1ccccc1C(=O)O)CCc1cnn2c1CCc1c2ccc(c1)O 19309152
53238781 1027 None 0 Human Functional pIC50 = 7.9 7.9 - 1
UnclassifiedUnclassified
Guide to Pharmacology 389 6 3 7 1.4 C[C@@H]1CCC(=C(C1)NC(=O)[C@H](Cc1onc(n1)c1ccc(cn1)F)N)C(=O)O 21185185
5789 1027 None 0 Human Functional pIC50 = 7.9 7.9 - 1
UnclassifiedUnclassified
Guide to Pharmacology 389 6 3 7 1.4 C[C@@H]1CCC(=C(C1)NC(=O)[C@H](Cc1onc(n1)c1ccc(cn1)F)N)C(=O)O 21185185
CHEMBL1770358 1027 None 0 Human Functional pIC50 = 7.9 7.9 - 1
UnclassifiedUnclassified
Guide to Pharmacology 389 6 3 7 1.4 C[C@@H]1CCC(=C(C1)NC(=O)[C@H](Cc1onc(n1)c1ccc(cn1)F)N)C(=O)O 21185185




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

1596 260 None 60 Human Binding pAC50 = 5.4 5.4 - 0
Binding affinity towards human HCAR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human HCAR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O 10.1038/s41467-023-40064-9
5310993 260 None 60 Human Binding pAC50 = 5.4 5.4 - 0
Binding affinity towards human HCAR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human HCAR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O 10.1038/s41467-023-40064-9
76 260 None 60 Human Binding pAC50 = 5.4 5.4 - 0
Binding affinity towards human HCAR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human HCAR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O 10.1038/s41467-023-40064-9
CHEMBL345714 260 None 60 Human Binding pAC50 = 5.4 5.4 - 0
Binding affinity towards human HCAR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human HCAR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O 10.1038/s41467-023-40064-9
DB09055 260 None 60 Human Binding pAC50 = 5.4 5.4 - 0
Binding affinity towards human HCAR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human HCAR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 154 1 1 3 -0.3 [O-][n+]1cc(ncc1C)C(=O)O 10.1038/s41467-023-40064-9
117629482 2823 None 82 Human Binding pEC50 = 6 6.0 -3 2
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.013
1588 2823 None 82 Human Binding pEC50 = 6 6.0 -3 2
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.013
1594 2823 None 82 Human Binding pEC50 = 6 6.0 -3 2
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.013
2835 2823 None 82 Human Binding pEC50 = 6 6.0 -3 2
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.013
938 2823 None 82 Human Binding pEC50 = 6 6.0 -3 2
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.013
CHEMBL573 2823 None 82 Human Binding pEC50 = 6 6.0 -3 2
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.013
DB00627 2823 None 82 Human Binding pEC50 = 6 6.0 -3 2
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.013
11516424 7317 None 0 Human Binding pEC50 = 6.0 6.0 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 379 6 3 5 3.4 Cc1c(CC(C)C(=O)Nc2ccccc2C(=O)O)cnn1-c1ccc(O)cc1 10.1016/j.bmcl.2010.04.013
CHEMBL1086104 7317 None 0 Human Binding pEC50 = 6.0 6.0 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 379 6 3 5 3.4 Cc1c(CC(C)C(=O)Nc2ccccc2C(=O)O)cnn1-c1ccc(O)cc1 10.1016/j.bmcl.2010.04.013
11625092 6686 None 0 Human Binding pEC50 = 6.9 6.9 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 379 6 2 2 5.3 O=C(CCc1ccc(-c2ccccc2Cl)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
CHEMBL1083473 6686 None 0 Human Binding pEC50 = 6.9 6.9 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 379 6 2 2 5.3 O=C(CCc1ccc(-c2ccccc2Cl)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
156017170 177753 None 0 Human Binding pEC50 = 4.9 4.9 - 0
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 417 5 1 6 4.4 CCOc1cc(Cl)c(C(=O)Nc2nc3ccccc3s2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4641449 177753 None 0 Human Binding pEC50 = 4.9 4.9 - 0
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 417 5 1 6 4.4 CCOc1cc(Cl)c(C(=O)Nc2nc3ccccc3s2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
57422810 177766 None 4 Human Binding pEC50 = 6.9 6.9 - 0
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 602 7 2 10 4.4 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)C4CCN(C)CC4)cc3s2)cc1-n1cccn1 10.1016/j.bmcl.2020.126953
CHEMBL4641579 177766 None 4 Human Binding pEC50 = 6.9 6.9 - 0
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 602 7 2 10 4.4 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)C4CCN(C)CC4)cc3s2)cc1-n1cccn1 10.1016/j.bmcl.2020.126953
46890275 6532 None 0 Human Binding pEC50 = 6.9 6.9 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 412 8 3 6 3.2 CCCC1CCC(C(=O)O)=C(NC(=O)C(C)Cc2ccn(-c3ccc(O)cn3)n2)C1 10.1016/j.bmcl.2010.04.013
CHEMBL1082823 6532 None 0 Human Binding pEC50 = 6.9 6.9 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 412 8 3 6 3.2 CCCC1CCC(C(=O)O)=C(NC(=O)C(C)Cc2ccn(-c3ccc(O)cn3)n2)C1 10.1016/j.bmcl.2010.04.013
24741310 89656 None 0 Human Binding pEC50 = 5.9 5.9 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 352 6 3 6 2.2 O=C(CCc1ccn(-c2ccc(O)cn2)n1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
CHEMBL237543 89656 None 0 Human Binding pEC50 = 5.9 5.9 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 352 6 3 6 2.2 O=C(CCc1ccn(-c2ccc(O)cn2)n1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
117629482 2823 None 82 Human Binding pEC50 = 7.8 7.8 -3 2
Agonist activity at GPR109A (unknown origin) assessed as effect on beta-arrestin2 conformational changesAgonist activity at GPR109A (unknown origin) assessed as effect on beta-arrestin2 conformational changes
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/acs.jmedchem.8b00435
1588 2823 None 82 Human Binding pEC50 = 7.8 7.8 -3 2
Agonist activity at GPR109A (unknown origin) assessed as effect on beta-arrestin2 conformational changesAgonist activity at GPR109A (unknown origin) assessed as effect on beta-arrestin2 conformational changes
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/acs.jmedchem.8b00435
1594 2823 None 82 Human Binding pEC50 = 7.8 7.8 -3 2
Agonist activity at GPR109A (unknown origin) assessed as effect on beta-arrestin2 conformational changesAgonist activity at GPR109A (unknown origin) assessed as effect on beta-arrestin2 conformational changes
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/acs.jmedchem.8b00435
2835 2823 None 82 Human Binding pEC50 = 7.8 7.8 -3 2
Agonist activity at GPR109A (unknown origin) assessed as effect on beta-arrestin2 conformational changesAgonist activity at GPR109A (unknown origin) assessed as effect on beta-arrestin2 conformational changes
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/acs.jmedchem.8b00435
938 2823 None 82 Human Binding pEC50 = 7.8 7.8 -3 2
Agonist activity at GPR109A (unknown origin) assessed as effect on beta-arrestin2 conformational changesAgonist activity at GPR109A (unknown origin) assessed as effect on beta-arrestin2 conformational changes
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/acs.jmedchem.8b00435
CHEMBL573 2823 None 82 Human Binding pEC50 = 7.8 7.8 -3 2
Agonist activity at GPR109A (unknown origin) assessed as effect on beta-arrestin2 conformational changesAgonist activity at GPR109A (unknown origin) assessed as effect on beta-arrestin2 conformational changes
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/acs.jmedchem.8b00435
DB00627 2823 None 82 Human Binding pEC50 = 7.8 7.8 -3 2
Agonist activity at GPR109A (unknown origin) assessed as effect on beta-arrestin2 conformational changesAgonist activity at GPR109A (unknown origin) assessed as effect on beta-arrestin2 conformational changes
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/acs.jmedchem.8b00435
156021885 178320 None 0 Human Binding pEC50 = 5.9 5.9 - 0
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 635 10 1 10 4.2 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1N1CCO[C@H](C)C1 10.1016/j.bmcl.2020.126953
CHEMBL4649741 178320 None 0 Human Binding pEC50 = 5.9 5.9 - 0
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 635 10 1 10 4.2 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1N1CCO[C@H](C)C1 10.1016/j.bmcl.2020.126953
1595 259 None 36 Human Binding pEC50 = 6.8 6.8 - 0
Agonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISAAgonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISA
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1016/j.bmc.2015.02.018
51576 259 None 36 Human Binding pEC50 = 6.8 6.8 - 0
Agonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISAAgonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISA
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1016/j.bmc.2015.02.018
CHEMBL278488 259 None 36 Human Binding pEC50 = 6.8 6.8 - 0
Agonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISAAgonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISA
ChEMBL 218 2 1 3 1.5 OC(=O)C1=CC(=O)C(O1)(C)c1ccccc1 10.1016/j.bmc.2015.02.018
156018500 178029 None 0 Human Binding pEC50 = 5.8 5.8 - 0
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 629 7 1 10 4.5 CCOc1cc(Cl)c(-c2ncc(-c3nc4ccc(S(=O)(=O)C5CCN(C)CC5)cc4s3)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4645314 178029 None 0 Human Binding pEC50 = 5.8 5.8 - 0
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 629 7 1 10 4.5 CCOc1cc(Cl)c(-c2ncc(-c3nc4ccc(S(=O)(=O)C5CCN(C)CC5)cc4s3)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
156019324 178079 None 0 Human Binding pEC50 = 5.8 5.8 - 0
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 530 7 1 8 4.9 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(OC4CCN(C)CC4)cc3s2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4646005 178079 None 0 Human Binding pEC50 = 5.8 5.8 - 0
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 530 7 1 8 4.9 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(OC4CCN(C)CC4)cc3s2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
46890274 6908 None 0 Human Binding pEC50 = 6.8 6.8 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 384 6 3 6 2.4 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CC[C@@H](C)C1 10.1016/j.bmcl.2010.04.013
CHEMBL1084332 6908 None 0 Human Binding pEC50 = 6.8 6.8 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 384 6 3 6 2.4 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CC[C@@H](C)C1 10.1016/j.bmcl.2010.04.013
46890273 6851 None 0 Human Binding pEC50 = 4.8 4.8 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 358 6 3 6 1.7 O=C(CCc1ccn(-c2ccc(O)cn2)n1)N[C@@H]1CCCC[C@@H]1C(=O)O 10.1016/j.bmcl.2010.04.013
CHEMBL1084060 6851 None 0 Human Binding pEC50 = 4.8 4.8 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 358 6 3 6 1.7 O=C(CCc1ccn(-c2ccc(O)cn2)n1)N[C@@H]1CCCC[C@@H]1C(=O)O 10.1016/j.bmcl.2010.04.013
156011618 177503 None 0 Human Binding pEC50 = 5.7 5.7 - 0
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 544 7 1 8 3.6 CCOc1cc(Cl)c(-c2ccc(-c3nc4c(s3)CN(C(=O)COC)CC4)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4638263 177503 None 0 Human Binding pEC50 = 5.7 5.7 - 0
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 544 7 1 8 3.6 CCOc1cc(Cl)c(-c2ccc(-c3nc4c(s3)CN(C(=O)COC)CC4)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
15986936 7103 None 0 Human Binding pEC50 = 6.7 6.7 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 356 6 3 6 1.9 O=C(CCc1cnn(-c2ccc(O)cn2)c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.013
CHEMBL1085150 7103 None 0 Human Binding pEC50 = 6.7 6.7 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 356 6 3 6 1.9 O=C(CCc1cnn(-c2ccc(O)cn2)c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.013
11197 1066 None 0 Human Binding pEC50 = 5.7 5.7 - 0
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 572 7 2 9 3.9 CCOc1cc(Cl)c(cc1N1CCOCC1)C(=O)NC(=O)Nc1nc2c(s1)cc(cc2)CN1CCN(CC1)C 10.1016/j.bmcl.2020.126953
154699458 1066 None 0 Human Binding pEC50 = 5.7 5.7 - 0
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 572 7 2 9 3.9 CCOc1cc(Cl)c(cc1N1CCOCC1)C(=O)NC(=O)Nc1nc2c(s1)cc(cc2)CN1CCN(CC1)C 10.1016/j.bmcl.2020.126953
CHEMBL4632411 1066 None 0 Human Binding pEC50 = 5.7 5.7 - 0
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 572 7 2 9 3.9 CCOc1cc(Cl)c(cc1N1CCOCC1)C(=O)NC(=O)Nc1nc2c(s1)cc(cc2)CN1CCN(CC1)C 10.1016/j.bmcl.2020.126953
46890276 6533 None 0 Human Binding pEC50 = 6.6 6.6 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 464 7 3 6 3.7 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CCC(c2cccc(F)c2)C1 10.1016/j.bmcl.2010.04.013
CHEMBL1082824 6533 None 0 Human Binding pEC50 = 6.6 6.6 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 464 7 3 6 3.7 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CCC(c2cccc(F)c2)C1 10.1016/j.bmcl.2010.04.013
46890240 7105 None 0 Human Binding pEC50 = 6.6 6.6 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 356 6 3 6 1.9 O=C(CCc1ccn(-c2ccc(O)cn2)n1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.013
CHEMBL1085156 7105 None 0 Human Binding pEC50 = 6.6 6.6 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 356 6 3 6 1.9 O=C(CCc1ccn(-c2ccc(O)cn2)n1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.013
46890237 7101 None 0 Human Binding pEC50 = 6.6 6.6 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 370 6 3 6 2.2 Cc1c(CCC(=O)NC2=C(C(=O)O)CCCC2)cnn1-c1ccc(O)cn1 10.1016/j.bmcl.2010.04.013
CHEMBL1085148 7101 None 0 Human Binding pEC50 = 6.6 6.6 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 370 6 3 6 2.2 Cc1c(CCC(=O)NC2=C(C(=O)O)CCCC2)cnn1-c1ccc(O)cn1 10.1016/j.bmcl.2010.04.013
46890199 7160 None 0 Human Binding pEC50 = 5.5 5.5 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 380 6 3 6 2.8 Cc1c(CC(C)C(=O)Nc2ccccc2C(=O)O)cnn1-c1ccc(O)cn1 10.1016/j.bmcl.2010.04.013
CHEMBL1085401 7160 None 0 Human Binding pEC50 = 5.5 5.5 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 380 6 3 6 2.8 Cc1c(CC(C)C(=O)Nc2ccccc2C(=O)O)cnn1-c1ccc(O)cn1 10.1016/j.bmcl.2010.04.013
156016073 177760 None 0 Human Binding pEC50 = 5.5 5.5 - 0
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 649 10 1 10 4.6 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1N1C[C@H](C)O[C@@H](C)C1 10.1016/j.bmcl.2020.126953
CHEMBL4641503 177760 None 0 Human Binding pEC50 = 5.5 5.5 - 0
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 649 10 1 10 4.6 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1N1C[C@H](C)O[C@@H](C)C1 10.1016/j.bmcl.2020.126953
46890165 7316 None 0 Human Binding pEC50 = 6.5 6.5 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 351 6 3 5 2.8 O=C(CCc1cnn(-c2ccc(O)cc2)c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
CHEMBL1086103 7316 None 0 Human Binding pEC50 = 6.5 6.5 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 351 6 3 5 2.8 O=C(CCc1cnn(-c2ccc(O)cc2)c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
15986929 7161 None 0 Human Binding pEC50 = 6.5 6.5 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 383 6 3 5 3.1 Cc1c(CC(C)C(=O)NC2=C(C(=O)O)CCCC2)cnn1-c1ccc(O)cc1 10.1016/j.bmcl.2010.04.013
CHEMBL1085402 7161 None 0 Human Binding pEC50 = 6.5 6.5 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 383 6 3 5 3.1 Cc1c(CC(C)C(=O)NC2=C(C(=O)O)CCCC2)cnn1-c1ccc(O)cc1 10.1016/j.bmcl.2010.04.013
156016110 177803 None 0 Human Binding pEC50 = 7.4 7.4 - 0
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 628 7 1 9 5.1 CCOc1cc(Cl)c(-c2ccc(-c3nc4ccc(S(=O)(=O)C5CCN(C)CC5)cc4s3)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4642043 177803 None 0 Human Binding pEC50 = 7.4 7.4 - 0
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 628 7 1 9 5.1 CCOc1cc(Cl)c(-c2ccc(-c3nc4ccc(S(=O)(=O)C5CCN(C)CC5)cc4s3)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
46890272 6849 None 0 Human Binding pEC50 = 6.4 6.4 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 370 6 3 6 2.2 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.013
CHEMBL1084059 6849 None 0 Human Binding pEC50 = 6.4 6.4 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 370 6 3 6 2.2 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.013
46890164 7424 None 0 Human Binding pEC50 = 5.4 5.4 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 335 6 2 4 3.1 O=C(CCc1cnn(-c2ccccc2)c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
CHEMBL1086568 7424 None 0 Human Binding pEC50 = 5.4 5.4 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 335 6 2 4 3.1 O=C(CCc1cnn(-c2ccccc2)c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
11560300 88573 None 0 Human Binding pEC50 = 7.4 7.4 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 395 6 3 3 5.0 O=C(CCc1ccc(-c2ccc(O)cc2Cl)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
CHEMBL235256 88573 None 0 Human Binding pEC50 = 7.4 7.4 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 395 6 3 3 5.0 O=C(CCc1ccc(-c2ccc(O)cc2Cl)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
117629482 2823 None 82 Human Binding pEC50 = 7.3 7.3 -3 2
Agonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISAAgonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISA
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmc.2015.02.018
1588 2823 None 82 Human Binding pEC50 = 7.3 7.3 -3 2
Agonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISAAgonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISA
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmc.2015.02.018
1594 2823 None 82 Human Binding pEC50 = 7.3 7.3 -3 2
Agonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISAAgonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISA
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmc.2015.02.018
2835 2823 None 82 Human Binding pEC50 = 7.3 7.3 -3 2
Agonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISAAgonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISA
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmc.2015.02.018
938 2823 None 82 Human Binding pEC50 = 7.3 7.3 -3 2
Agonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISAAgonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISA
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmc.2015.02.018
CHEMBL573 2823 None 82 Human Binding pEC50 = 7.3 7.3 -3 2
Agonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISAAgonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISA
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmc.2015.02.018
DB00627 2823 None 82 Human Binding pEC50 = 7.3 7.3 -3 2
Agonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISAAgonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISA
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmc.2015.02.018
53322689 58077 None 0 Human Binding pEC50 = 7.3 7.3 - 0
Agonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assayAgonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assay
ChEMBL 224 1 2 5 0.7 CCc1cc(=O)oc2nc(S)[nH]c(=O)c12 10.1039/d2md00076h
CHEMBL1672755 58077 None 0 Human Binding pEC50 = 7.3 7.3 - 0
Agonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assayAgonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assay
ChEMBL 224 1 2 5 0.7 CCc1cc(=O)oc2nc(S)[nH]c(=O)c12 10.1039/d2md00076h
15605571 75261 None 0 Human Binding pEC50 = 7.3 7.3 - 0
Agonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assayAgonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assay
ChEMBL 236 3 2 4 0.5 CCCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1039/d2md00076h
CHEMBL2036813 75261 None 0 Human Binding pEC50 = 7.3 7.3 - 0
Agonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assayAgonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assay
ChEMBL 236 3 2 4 0.5 CCCCc1cc(=O)oc2[nH]c(=O)[nH]c(=O)c12 10.1039/d2md00076h
171343909 193728 None 0 Human Binding pEC50 = 7.3 7.3 - 0
Agonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assayAgonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assay
ChEMBL 252 3 2 4 1.9 CCCCc1cc(=O)oc2[nH]c(=S)[nH]c(=O)c12 10.1039/d2md00076h
CHEMBL5270112 193728 None 0 Human Binding pEC50 = 7.3 7.3 - 0
Agonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assayAgonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assay
ChEMBL 252 3 2 4 1.9 CCCCc1cc(=O)oc2[nH]c(=S)[nH]c(=O)c12 10.1039/d2md00076h
171356818 193981 None 0 Human Binding pEC50 = 7.3 7.3 - 0
Agonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assayAgonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assay
ChEMBL 286 4 2 4 2.1 O=c1cc(CCCCCl)c2c(=O)[nH]c(=S)[nH]c2o1 10.1039/d2md00076h
CHEMBL5275861 193981 None 0 Human Binding pEC50 = 7.3 7.3 - 0
Agonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assayAgonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assay
ChEMBL 286 4 2 4 2.1 O=c1cc(CCCCCl)c2c(=O)[nH]c(=S)[nH]c2o1 10.1039/d2md00076h
171357332 194030 None 0 Human Binding pEC50 = 7.3 7.3 - 0
Agonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assayAgonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assay
ChEMBL 238 2 2 4 1.5 CCCc1cc(=O)oc2[nH]c(=S)[nH]c(=O)c12 10.1039/d2md00076h
CHEMBL5277000 194030 None 0 Human Binding pEC50 = 7.3 7.3 - 0
Agonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assayAgonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assay
ChEMBL 238 2 2 4 1.5 CCCc1cc(=O)oc2[nH]c(=S)[nH]c(=O)c12 10.1039/d2md00076h
766926 194224 None 11 Human Binding pEC50 = 7.3 7.3 - 0
Agonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assayAgonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assay
ChEMBL 210 0 2 4 0.8 Cc1cc(=O)oc2[nH]c(=S)[nH]c(=O)c12 10.1039/d2md00076h
CHEMBL5281556 194224 None 11 Human Binding pEC50 = 7.3 7.3 - 0
Agonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assayAgonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assay
ChEMBL 210 0 2 4 0.8 Cc1cc(=O)oc2[nH]c(=S)[nH]c(=O)c12 10.1039/d2md00076h
171346683 194381 None 0 Human Binding pEC50 = 7.3 7.3 - 0
Agonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assayAgonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assay
ChEMBL 270 4 2 4 0.7 O=c1[nH]c(=O)c2c(CCCCCl)cc(=O)oc2[nH]1 10.1039/d2md00076h
CHEMBL5284951 194381 None 0 Human Binding pEC50 = 7.3 7.3 - 0
Agonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assayAgonist activity at human HCA2 expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assay
ChEMBL 270 4 2 4 0.7 O=c1[nH]c(=O)c2c(CCCCCl)cc(=O)oc2[nH]1 10.1039/d2md00076h
46890239 6936 None 0 Human Binding pEC50 = 6.3 6.3 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 370 6 3 6 2.2 CC(Cc1cnn(-c2ccc(O)cn2)c1)C(=O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.013
CHEMBL1084448 6936 None 0 Human Binding pEC50 = 6.3 6.3 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 370 6 3 6 2.2 CC(Cc1cnn(-c2ccc(O)cn2)c1)C(=O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.013
117629482 2823 None 82 Human Binding pEC50 = 6.2 6.2 -3 2
Activation of GPR109A receptor in CHOK1 cells assessed as ERK1/2 MAP kinase activation by ELISAActivation of GPR109A receptor in CHOK1 cells assessed as ERK1/2 MAP kinase activation by ELISA
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1074/jbc.m701866200
1588 2823 None 82 Human Binding pEC50 = 6.2 6.2 -3 2
Activation of GPR109A receptor in CHOK1 cells assessed as ERK1/2 MAP kinase activation by ELISAActivation of GPR109A receptor in CHOK1 cells assessed as ERK1/2 MAP kinase activation by ELISA
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1074/jbc.m701866200
1594 2823 None 82 Human Binding pEC50 = 6.2 6.2 -3 2
Activation of GPR109A receptor in CHOK1 cells assessed as ERK1/2 MAP kinase activation by ELISAActivation of GPR109A receptor in CHOK1 cells assessed as ERK1/2 MAP kinase activation by ELISA
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1074/jbc.m701866200
2835 2823 None 82 Human Binding pEC50 = 6.2 6.2 -3 2
Activation of GPR109A receptor in CHOK1 cells assessed as ERK1/2 MAP kinase activation by ELISAActivation of GPR109A receptor in CHOK1 cells assessed as ERK1/2 MAP kinase activation by ELISA
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1074/jbc.m701866200
938 2823 None 82 Human Binding pEC50 = 6.2 6.2 -3 2
Activation of GPR109A receptor in CHOK1 cells assessed as ERK1/2 MAP kinase activation by ELISAActivation of GPR109A receptor in CHOK1 cells assessed as ERK1/2 MAP kinase activation by ELISA
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1074/jbc.m701866200
CHEMBL573 2823 None 82 Human Binding pEC50 = 6.2 6.2 -3 2
Activation of GPR109A receptor in CHOK1 cells assessed as ERK1/2 MAP kinase activation by ELISAActivation of GPR109A receptor in CHOK1 cells assessed as ERK1/2 MAP kinase activation by ELISA
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1074/jbc.m701866200
DB00627 2823 None 82 Human Binding pEC50 = 6.2 6.2 -3 2
Activation of GPR109A receptor in CHOK1 cells assessed as ERK1/2 MAP kinase activation by ELISAActivation of GPR109A receptor in CHOK1 cells assessed as ERK1/2 MAP kinase activation by ELISA
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1074/jbc.m701866200
156021336 178272 None 0 Human Binding pEC50 = 6.2 6.2 - 0
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 467 5 1 6 5.2 CCOc1cc(Cl)c(-c2ccc(-c3nc4ccccc4s3)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4649089 178272 None 0 Human Binding pEC50 = 6.2 6.2 - 0
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 467 5 1 6 5.2 CCOc1cc(Cl)c(-c2ccc(-c3nc4ccccc4s3)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
46890301 7201 None 0 Human Binding pEC50 = 7.2 7.2 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 482 7 3 6 3.9 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2010.04.013
CHEMBL1085616 7201 None 0 Human Binding pEC50 = 7.2 7.2 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 482 7 3 6 3.9 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2010.04.013
156012428 177415 None 0 Human Binding pEC50 = 6.2 6.2 - 0
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 649 10 1 10 4.6 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1N1C[C@H](C)O[C@H](C)C1 10.1016/j.bmcl.2020.126953
CHEMBL4636832 177415 None 0 Human Binding pEC50 = 6.2 6.2 - 0
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 649 10 1 10 4.6 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1N1C[C@H](C)O[C@H](C)C1 10.1016/j.bmcl.2020.126953
46890300 7417 None 0 Human Binding pEC50 = 7.2 7.2 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 482 7 3 6 3.9 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CCC(c2cccc(F)c2F)C1 10.1016/j.bmcl.2010.04.013
CHEMBL1086541 7417 None 0 Human Binding pEC50 = 7.2 7.2 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 482 7 3 6 3.9 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CCC(c2cccc(F)c2F)C1 10.1016/j.bmcl.2010.04.013
46890198 7319 None 0 Human Binding pEC50 = 6.1 6.1 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 366 6 3 6 2.6 Cc1c(CCC(=O)Nc2ccccc2C(=O)O)cnn1-c1ccc(O)cn1 10.1016/j.bmcl.2010.04.013
CHEMBL1086108 7319 None 0 Human Binding pEC50 = 6.1 6.1 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 366 6 3 6 2.6 Cc1c(CCC(=O)Nc2ccccc2C(=O)O)cnn1-c1ccc(O)cn1 10.1016/j.bmcl.2010.04.013
46890238 7102 None 0 Human Binding pEC50 = 6.1 6.1 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 384 6 3 6 2.5 Cc1c(CC(C)C(=O)NC2=C(C(=O)O)CCCC2)cnn1-c1ccc(O)cn1 10.1016/j.bmcl.2010.04.013
CHEMBL1085149 7102 None 0 Human Binding pEC50 = 6.1 6.1 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 384 6 3 6 2.5 Cc1c(CC(C)C(=O)NC2=C(C(=O)O)CCCC2)cnn1-c1ccc(O)cn1 10.1016/j.bmcl.2010.04.013
9822 145726 None 78 Human Binding pEC50 = 6.1 6.1 - 0
Activation of GPR109A receptor in CHOK1 cells assessed as ERK1/2 MAP kinase activation by ELISAActivation of GPR109A receptor in CHOK1 cells assessed as ERK1/2 MAP kinase activation by ELISA
ChEMBL 126 1 2 2 0.4 Cc1cc(C(=O)O)n[nH]1 10.1074/jbc.m701866200
CHEMBL391574 145726 None 78 Human Binding pEC50 = 6.1 6.1 - 0
Activation of GPR109A receptor in CHOK1 cells assessed as ERK1/2 MAP kinase activation by ELISAActivation of GPR109A receptor in CHOK1 cells assessed as ERK1/2 MAP kinase activation by ELISA
ChEMBL 126 1 2 2 0.4 Cc1cc(C(=O)O)n[nH]1 10.1074/jbc.m701866200
156014693 177297 None 0 Human Binding pEC50 = 6.0 6.0 - 0
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 530 6 2 8 2.9 CCOc1cc(Cl)c(-c2ccc(-c3nc4c(s3)CN(C(=O)CO)CC4)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4635089 177297 None 0 Human Binding pEC50 = 6.0 6.0 - 0
Agonist activity at human GPR109A receptorAgonist activity at human GPR109A receptor
ChEMBL 530 6 2 8 2.9 CCOc1cc(Cl)c(-c2ccc(-c3nc4c(s3)CN(C(=O)CO)CC4)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
24741307 88769 None 0 Human Binding pEC50 = 7.0 7.0 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 365 6 3 5 3.2 Cc1c(CCC(=O)Nc2ccccc2C(=O)O)cnn1-c1ccc(O)cc1 10.1016/j.bmcl.2010.04.013
CHEMBL236163 88769 None 0 Human Binding pEC50 = 7.0 7.0 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 365 6 3 5 3.2 Cc1c(CCC(=O)Nc2ccccc2C(=O)O)cnn1-c1ccc(O)cc1 10.1016/j.bmcl.2010.04.013
46890197 7261 None 0 Human Binding pEC50 = 6.0 6.0 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 366 6 3 6 2.5 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
CHEMBL1085875 7261 None 0 Human Binding pEC50 = 6.0 6.0 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 366 6 3 6 2.5 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
46890302 7254 None 0 Human Binding pEC50 = 7.0 7.0 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 500 7 3 6 4.0 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CCC(c2cc(F)c(F)c(F)c2)C1 10.1016/j.bmcl.2010.04.013
CHEMBL1085842 7254 None 0 Human Binding pEC50 = 7.0 7.0 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 500 7 3 6 4.0 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CCC(c2cc(F)c(F)c(F)c2)C1 10.1016/j.bmcl.2010.04.013
46890163 7423 None 0 Human Binding pEC50 = 5.0 5.0 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 335 6 2 4 3.1 O=C(CCc1ccn(-c2ccccc2)n1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
CHEMBL1086567 7423 None 0 Human Binding pEC50 = 5.0 5.0 - 0
Displacement of [3H]niacin from GRP109A receptor in presence of 4% human serumDisplacement of [3H]niacin from GRP109A receptor in presence of 4% human serum
ChEMBL 335 6 2 4 3.1 O=C(CCc1ccn(-c2ccccc2)n1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
135453098 88768 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 402 6 3 5 4.4 O=C(CCc1cnc(-c2ccc(O)cc2Cl)s1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL236162 88768 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 402 6 3 5 4.4 O=C(CCc1cnc(-c2ccc(O)cc2Cl)s1)Nc1ccccc1C(=O)O 10.1021/jm700942d
42625475 184315 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 414 5 3 5 4.3 O=C(CCc1noc2c1ccc1c(Cl)c(O)ccc12)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
CHEMBL483336 184315 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 414 5 3 5 4.3 O=C(CCc1noc2c1ccc1c(Cl)c(O)ccc12)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
42625476 184316 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 379 5 3 5 3.2 O=C(CCc1cnn2c1ccc1cc(O)ccc12)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
CHEMBL483337 184316 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 379 5 3 5 3.2 O=C(CCc1cnn2c1ccc1cc(O)ccc12)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
136000619 61465 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 369 6 4 8 1.0 N[C@@H](Cc1nc(-c2ccc(O)cn2)no1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1770352 61465 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 369 6 4 8 1.0 N[C@@H](Cc1nc(-c2ccc(O)cn2)no1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
135453098 88768 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 402 6 3 5 4.4 O=C(CCc1cnc(-c2ccc(O)cc2Cl)s1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL236162 88768 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 402 6 3 5 4.4 O=C(CCc1cnc(-c2ccc(O)cc2Cl)s1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
46890272 6849 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 370 6 3 6 2.2 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.013
CHEMBL1084059 6849 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 370 6 3 6 2.2 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.013
135800177 146039 None 5 Human Binding pIC50 = 8 8.0 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 353 6 3 6 2.7 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL391813 146039 None 5 Human Binding pIC50 = 8 8.0 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 353 6 3 6 2.7 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1ccccc1C(=O)O 10.1021/jm700942d
135800177 146039 None 5 Human Binding pIC50 = 8 8.0 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 353 6 3 6 2.7 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL391813 146039 None 5 Human Binding pIC50 = 8 8.0 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 353 6 3 6 2.7 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
135627640 61417 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 417 6 4 6 3.4 NC(Cc1cnc(-c2ccc(O)cc2Cl)s1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1770172 61417 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 417 6 4 6 3.4 NC(Cc1cnc(-c2ccc(O)cc2Cl)s1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
136088959 61467 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 383 6 4 8 1.6 CC(c1nc(-c2ccc(O)cn2)no1)[C@H](N)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1770354 61467 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 383 6 4 8 1.6 CC(c1nc(-c2ccc(O)cn2)no1)[C@H](N)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
44580008 187054 None 0 Human Binding pIC50 = 6 6.0 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cells
ChEMBL 414 7 1 5 4.6 Cc1c(C(=O)NCCOc2ccccc2)cnc2c(-c3ccc(C(C)C)cc3)cnn12 10.1016/j.bmcl.2008.08.039
CHEMBL490216 187054 None 0 Human Binding pIC50 = 6 6.0 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cells
ChEMBL 414 7 1 5 4.6 Cc1c(C(=O)NCCOc2ccccc2)cnc2c(-c3ccc(C(C)C)cc3)cnn12 10.1016/j.bmcl.2008.08.039
156013291 177610 None 0 Human Binding pIC50 = 4 4.0 - 0
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 455 9 3 9 1.8 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1cn(CCN2CCOCC2)cc1C(=O)O 10.1016/j.bmcl.2020.127105
CHEMBL4639589 177610 None 0 Human Binding pIC50 = 4 4.0 - 0
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 455 9 3 9 1.8 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1cn(CCN2CCOCC2)cc1C(=O)O 10.1016/j.bmcl.2020.127105
122181143 121897 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 367 6 3 4 4.4 O=C(CCc1ccc(-c2ccc(O)cc2)cc1)Nc1sccc1C(=O)O 10.1016/j.bmc.2015.02.018
CHEMBL3589837 121897 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 367 6 3 4 4.4 O=C(CCc1ccc(-c2ccc(O)cc2)cc1)Nc1sccc1C(=O)O 10.1016/j.bmc.2015.02.018
122181142 121896 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 365 6 3 3 4.0 O=C(CCc1ccc(-c2ccc(O)cc2)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2015.02.018
CHEMBL3589836 121896 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 365 6 3 3 4.0 O=C(CCc1ccc(-c2ccc(O)cc2)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2015.02.018
136000718 61422 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 368 6 4 7 2.2 N[C@H](CC(=O)Nc1ccccc1C(=O)O)c1nc(-c2ccc(O)cc2)no1 10.1016/j.bmcl.2010.11.116
CHEMBL1770177 61422 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 368 6 4 7 2.2 N[C@H](CC(=O)Nc1ccccc1C(=O)O)c1nc(-c2ccc(O)cc2)no1 10.1016/j.bmcl.2010.11.116
11617852 184641 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 381 5 3 6 3.5 O=C(CCc1cn2c(n1)sc1cc(O)ccc12)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL484783 184641 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 381 5 3 6 3.5 O=C(CCc1cn2c(n1)sc1cc(O)ccc12)Nc1ccccc1C(=O)O 10.1021/jm900151e
46890297 7216 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 433 6 3 3 5.0 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2ccccc2F)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1085653 7216 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 433 6 3 3 5.0 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2ccccc2F)CC1 10.1016/j.bmcl.2010.04.001
136000580 61469 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 387 6 4 8 1.0 C[C@@H]1CCC(C(=O)O)=C(NC(=O)[C@@H](N)Cc2nc(-c3ccc(O)cn3)no2)C1 10.1016/j.bmcl.2010.11.116
CHEMBL1770356 61469 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 387 6 4 8 1.0 C[C@@H]1CCC(C(=O)O)=C(NC(=O)[C@@H](N)Cc2nc(-c3ccc(O)cn3)no2)C1 10.1016/j.bmcl.2010.11.116
15981408 94399 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 405 3 2 5 3.5 C[C@H]1CN(c2cnc3ccccc3n2)C[C@@H](C)N1C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2007.10.055
CHEMBL250690 94399 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 405 3 2 5 3.5 C[C@H]1CN(c2cnc3ccccc3n2)C[C@@H](C)N1C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2007.10.055
156011372 177457 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 415 10 3 9 1.9 COCCCn1cc(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
CHEMBL4637548 177457 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 415 10 3 9 1.9 COCCCn1cc(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
49862074 14980 None 0 Mouse Binding pIC50 = 6.0 6.0 - 0
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 208 3 2 2 1.9 CCC(C)C1Cc2[nH]nc(C(=O)O)c2C1 10.1016/j.bmcl.2010.06.041
CHEMBL1208921 14980 None 0 Mouse Binding pIC50 = 6.0 6.0 - 0
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 208 3 2 2 1.9 CCC(C)C1Cc2[nH]nc(C(=O)O)c2C1 10.1016/j.bmcl.2010.06.041
135899129 16145 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 315 6 1 5 2.3 O=c1[nH]c(OCCCOc2ccc(F)cc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1223961 16145 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 315 6 1 5 2.3 O=c1[nH]c(OCCCOc2ccc(F)cc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
156012920 177554 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 433 8 3 8 3.0 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1cn(Cc2ccncc2)cc1C(=O)O 10.1016/j.bmcl.2020.127105
CHEMBL4638809 177554 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 433 8 3 8 3.0 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1cn(Cc2ccncc2)cc1C(=O)O 10.1016/j.bmcl.2020.127105
44591603 191811 None 0 Mouse Binding pIC50 = 5.0 5.0 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 266 2 2 4 1.8 Cc1cccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
CHEMBL519689 191811 None 0 Mouse Binding pIC50 = 5.0 5.0 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 266 2 2 4 1.8 Cc1cccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
136000669 61424 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 382 7 4 7 1.9 CN[C@@H](Cc1nc(-c2ccc(O)cc2)no1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1770179 61424 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 382 7 4 7 1.9 CN[C@@H](Cc1nc(-c2ccc(O)cc2)no1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
46890276 6533 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 464 7 3 6 3.7 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CCC(c2cccc(F)c2)C1 10.1016/j.bmcl.2010.04.013
CHEMBL1082824 6533 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 464 7 3 6 3.7 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CCC(c2cccc(F)c2)C1 10.1016/j.bmcl.2010.04.013
136086828 7195 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 502 7 3 7 3.9 C[C@H]1CC(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)=C(C(=O)O)C[C@H]1c1cc(F)cc(F)c1F 10.1016/j.bmcl.2010.04.001
CHEMBL1085589 7195 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 502 7 3 7 3.9 C[C@H]1CC(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)=C(C(=O)O)C[C@H]1c1cc(F)cc(F)c1F 10.1016/j.bmcl.2010.04.001
53238781 1027 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 389 6 3 7 1.4 C[C@@H]1CCC(=C(C1)NC(=O)[C@H](Cc1onc(n1)c1ccc(cn1)F)N)C(=O)O 10.1016/j.bmcl.2010.11.116
5789 1027 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 389 6 3 7 1.4 C[C@@H]1CCC(=C(C1)NC(=O)[C@H](Cc1onc(n1)c1ccc(cn1)F)N)C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1770358 1027 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 389 6 3 7 1.4 C[C@@H]1CCC(=C(C1)NC(=O)[C@H](Cc1onc(n1)c1ccc(cn1)F)N)C(=O)O 10.1016/j.bmcl.2010.11.116
11566404 145759 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 346 6 2 3 4.0 O=C(CCc1ccc(-c2ccccn2)cc1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL391603 145759 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 346 6 2 3 4.0 O=C(CCc1ccc(-c2ccccn2)cc1)Nc1ccccc1C(=O)O 10.1021/jm700942d
46890400 7288 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 419 6 3 5 3.6 Cn1cc(C2CCC(NC(=O)CCc3ccc4cc(O)ccc4c3)=C(C(=O)O)C2)cn1 10.1016/j.bmcl.2010.04.001
CHEMBL1086030 7288 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 419 6 3 5 3.6 Cn1cc(C2CCC(NC(=O)CCc3ccc4cc(O)ccc4c3)=C(C(=O)O)C2)cn1 10.1016/j.bmcl.2010.04.001
54585613 61419 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 392 5 4 6 1.9 NC(Cc1cc2n(n1)-c1ccc(O)cc1CC2)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1770174 61419 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 392 5 4 6 1.9 NC(Cc1cc2n(n1)-c1ccc(O)cc1CC2)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
16048839 155106 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 382 3 2 5 3.3 O=C(O)c1ccccc1NC(=O)N1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL401469 155106 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 382 3 2 5 3.3 O=C(O)c1ccccc1NC(=O)N1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmcl.2007.10.055
4268702 169755 None 5 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cells
ChEMBL 327 5 2 3 3.7 CC(C)(C)c1ccc(OCC(=O)Nc2ccccc2C(=O)O)cc1 10.1016/j.bmcl.2008.08.030
CHEMBL443733 169755 None 5 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cells
ChEMBL 327 5 2 3 3.7 CC(C)(C)c1ccc(OCC(=O)Nc2ccccc2C(=O)O)cc1 10.1016/j.bmcl.2008.08.030
11159621 2548 None 38 Mouse Binding pIC50 = 5.9 5.9 - 1
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2009.03.014
5784 2548 None 38 Mouse Binding pIC50 = 5.9 5.9 - 1
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2009.03.014
CHEMBL456145 2548 None 38 Mouse Binding pIC50 = 5.9 5.9 - 1
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2009.03.014
DB05939 2548 None 38 Mouse Binding pIC50 = 5.9 5.9 - 1
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2009.03.014
11159621 2548 None 38 Mouse Binding pIC50 = 5.9 5.9 - 1
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2010.06.041
5784 2548 None 38 Mouse Binding pIC50 = 5.9 5.9 - 1
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2010.06.041
CHEMBL456145 2548 None 38 Mouse Binding pIC50 = 5.9 5.9 - 1
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2010.06.041
DB05939 2548 None 38 Mouse Binding pIC50 = 5.9 5.9 - 1
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2010.06.041
135899108 16218 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 315 5 1 4 2.7 O=c1[nH]c(COCCc2ccc(Cl)cc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1224220 16218 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 315 5 1 4 2.7 O=c1[nH]c(COCCc2ccc(Cl)cc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
122181139 121893 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 375 6 3 3 4.6 Cc1cc(O)ccc1-c1ccc(CCC(=O)Nc2ccccc2C(=O)O)cc1 10.1016/j.bmc.2015.02.018
CHEMBL3589833 121893 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 375 6 3 3 4.6 Cc1cc(O)ccc1-c1ccc(CCC(=O)Nc2ccccc2C(=O)O)cc1 10.1016/j.bmc.2015.02.018
11494579 1058 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 377 5 3 5 2.9 O=C(Nc1ccccc1C(=O)O)CCc1cnn2c1CCc1c2ccc(c1)O 10.1021/jm900151e
5791 1058 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 377 5 3 5 2.9 O=C(Nc1ccccc1C(=O)O)CCc1cnn2c1CCc1c2ccc(c1)O 10.1021/jm900151e
CHEMBL482768 1058 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 377 5 3 5 2.9 O=C(Nc1ccccc1C(=O)O)CCc1cnn2c1CCc1c2ccc(c1)O 10.1021/jm900151e
135416383 185015 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 368 5 3 5 2.7 O=C(CCc1noc2c1CCc1cc(O)ccc1-2)NC1=C(C(=O)O)CCC1 10.1021/jm900151e
CHEMBL485326 185015 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 368 5 3 5 2.7 O=C(CCc1noc2c1CCc1cc(O)ccc1-2)NC1=C(C(=O)O)CCC1 10.1021/jm900151e
54580748 61418 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 377 5 3 5 2.9 O=C(CCc1cc2n(n1)-c1ccc(O)cc1CC2)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1770173 61418 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 377 5 3 5 2.9 O=C(CCc1cc2n(n1)-c1ccc(O)cc1CC2)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
137635325 156240 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 313 4 3 3 2.6 O=C(CCC#Cc1ccc(O)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4063682 156240 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 313 4 3 3 2.6 O=C(CCC#Cc1ccc(O)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
135922722 184297 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 391 5 3 5 3.2 Cn1nc(CCC(=O)Nc2ccccc2C(=O)O)c2c1-c1ccc(O)cc1CC2 10.1021/jm900151e
CHEMBL483160 184297 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 391 5 3 5 3.2 Cn1nc(CCC(=O)Nc2ccccc2C(=O)O)c2c1-c1ccc(O)cc1CC2 10.1021/jm900151e
117629482 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.030
1588 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.030
1594 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.030
2835 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.030
938 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.030
CHEMBL573 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.030
DB00627 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.030
135899320 16140 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 297 6 1 5 2.2 O=c1[nH]c(OCCCOc2ccccc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1223957 16140 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 297 6 1 5 2.2 O=c1[nH]c(OCCCOc2ccccc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
44579762 187265 None 1 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cells
ChEMBL 428 7 1 5 5.0 Cc1c(C(=O)NC(C)COc2ccccc2)cnc2c(-c3ccc(C(C)C)cc3)cnn12 10.1016/j.bmcl.2008.08.039
CHEMBL492020 187265 None 1 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cells
ChEMBL 428 7 1 5 5.0 Cc1c(C(=O)NC(C)COc2ccccc2)cnc2c(-c3ccc(C(C)C)cc3)cnn12 10.1016/j.bmcl.2008.08.039
49862074 14980 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 208 3 2 2 1.9 CCC(C)C1Cc2[nH]nc(C(=O)O)c2C1 10.1016/j.bmcl.2010.06.041
CHEMBL1208921 14980 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 208 3 2 2 1.9 CCC(C)C1Cc2[nH]nc(C(=O)O)c2C1 10.1016/j.bmcl.2010.06.041
11183317 191579 None 0 Mouse Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 204 2 2 4 0.7 CCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
CHEMBL519338 191579 None 0 Mouse Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 204 2 2 4 0.7 CCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
136127010 16093 None 13 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 215 0 1 3 1.3 O=c1[nH]c(C(F)(F)F)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1223819 16093 None 13 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 215 0 1 3 1.3 O=c1[nH]c(C(F)(F)F)nc2ncccc12 10.1016/j.bmcl.2010.07.108
46890273 6851 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 358 6 3 6 1.7 O=C(CCc1ccn(-c2ccc(O)cn2)n1)N[C@@H]1CCCC[C@@H]1C(=O)O 10.1016/j.bmcl.2010.04.013
CHEMBL1084060 6851 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 358 6 3 6 1.7 O=C(CCc1ccn(-c2ccc(O)cn2)n1)N[C@@H]1CCCC[C@@H]1C(=O)O 10.1016/j.bmcl.2010.04.013
137655320 158630 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 313 4 3 3 2.6 O=C(CCC#Cc1cccc(O)c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4091501 158630 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 313 4 3 3 2.6 O=C(CCC#Cc1cccc(O)c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
46890274 6908 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 384 6 3 6 2.4 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CC[C@@H](C)C1 10.1016/j.bmcl.2010.04.013
CHEMBL1084332 6908 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 384 6 3 6 2.4 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CC[C@@H](C)C1 10.1016/j.bmcl.2010.04.013
46890399 7287 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 419 6 3 5 3.6 Cn1nccc1C1CCC(NC(=O)CCc2ccc3cc(O)ccc3c2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
CHEMBL1086029 7287 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 419 6 3 5 3.6 Cn1nccc1C1CCC(NC(=O)CCc2ccc3cc(O)ccc3c2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
117629482 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.013
1588 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.013
1594 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.013
2835 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.013
938 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.013
CHEMBL573 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.013
DB00627 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.013
135401973 1022 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 393 3 3 6 2.4 Oc1ccc2c(c1)ncc(n2)N1CCN(CC1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2007.10.055
5792 1022 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 393 3 3 6 2.4 Oc1ccc2c(c1)ncc(n2)N1CCN(CC1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2007.10.055
CHEMBL398496 1022 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 393 3 3 6 2.4 Oc1ccc2c(c1)ncc(n2)N1CCN(CC1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2007.10.055
117629482 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.10.055
117629482 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
1588 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.10.055
1588 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
1594 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.10.055
1594 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
2835 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.10.055
2835 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
938 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.10.055
938 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
CHEMBL573 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.10.055
CHEMBL573 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
DB00627 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2007.10.055
DB00627 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
11594881 88672 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 319 5 2 2 4.1 O=C(CCc1ccc2ccccc2c1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL235740 88672 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 319 5 2 2 4.1 O=C(CCc1ccc2ccccc2c1)Nc1ccccc1C(=O)O 10.1021/jm700942d
117629482 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm900151e
1588 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm900151e
1594 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm900151e
2835 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm900151e
938 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm900151e
CHEMBL573 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm900151e
DB00627 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm900151e
117629482 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.001
1588 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.001
1594 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.001
2835 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.001
938 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.001
CHEMBL573 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.001
DB00627 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.04.001
117629482 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.06.054
1588 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.06.054
1594 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.06.054
2835 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.06.054
938 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.06.054
CHEMBL573 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.06.054
DB00627 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.06.054
117629482 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serum
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.06.054
1588 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serum
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.06.054
1594 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serum
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.06.054
2835 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serum
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.06.054
938 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serum
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.06.054
CHEMBL573 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serum
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.06.054
DB00627 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serum
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.06.054
117629482 2823 None 82 Mouse Binding pIC50 = 6.9 6.9 - 2
Displacement of [3H]niacin from mouse GPR109ADisplacement of [3H]niacin from mouse GPR109A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
1588 2823 None 82 Mouse Binding pIC50 = 6.9 6.9 - 2
Displacement of [3H]niacin from mouse GPR109ADisplacement of [3H]niacin from mouse GPR109A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
1594 2823 None 82 Mouse Binding pIC50 = 6.9 6.9 - 2
Displacement of [3H]niacin from mouse GPR109ADisplacement of [3H]niacin from mouse GPR109A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
2835 2823 None 82 Mouse Binding pIC50 = 6.9 6.9 - 2
Displacement of [3H]niacin from mouse GPR109ADisplacement of [3H]niacin from mouse GPR109A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
938 2823 None 82 Mouse Binding pIC50 = 6.9 6.9 - 2
Displacement of [3H]niacin from mouse GPR109ADisplacement of [3H]niacin from mouse GPR109A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
CHEMBL573 2823 None 82 Mouse Binding pIC50 = 6.9 6.9 - 2
Displacement of [3H]niacin from mouse GPR109ADisplacement of [3H]niacin from mouse GPR109A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
DB00627 2823 None 82 Mouse Binding pIC50 = 6.9 6.9 - 2
Displacement of [3H]niacin from mouse GPR109ADisplacement of [3H]niacin from mouse GPR109A
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm700942d
11594881 88672 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cells
ChEMBL 319 5 2 2 4.1 O=C(CCc1ccc2ccccc2c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2008.08.030
CHEMBL235740 88672 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cells
ChEMBL 319 5 2 2 4.1 O=C(CCc1ccc2ccccc2c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2008.08.030
117629482 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.03.014
1588 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.03.014
1594 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.03.014
2835 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.03.014
938 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.03.014
CHEMBL573 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.03.014
DB00627 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.03.014
12002517 191991 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 270 2 2 4 1.6 Fc1cccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
CHEMBL519966 191991 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 270 2 2 4 1.6 Fc1cccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
12002525 192452 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 288 2 2 4 1.8 Fc1cccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1F 10.1016/j.bmcl.2009.03.014
CHEMBL520676 192452 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 288 2 2 4 1.8 Fc1cccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1F 10.1016/j.bmcl.2009.03.014
117629482 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.06.041
1588 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.06.041
1594 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.06.041
2835 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.06.041
938 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.06.041
CHEMBL573 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.06.041
DB00627 2823 None 82 Human Binding pIC50 = 6.9 6.9 -3 2
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.06.041
117629482 2823 None 82 Mouse Binding pIC50 = 6.9 6.9 - 2
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.03.014
1588 2823 None 82 Mouse Binding pIC50 = 6.9 6.9 - 2
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.03.014
1594 2823 None 82 Mouse Binding pIC50 = 6.9 6.9 - 2
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.03.014
2835 2823 None 82 Mouse Binding pIC50 = 6.9 6.9 - 2
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.03.014
938 2823 None 82 Mouse Binding pIC50 = 6.9 6.9 - 2
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.03.014
CHEMBL573 2823 None 82 Mouse Binding pIC50 = 6.9 6.9 - 2
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.03.014
DB00627 2823 None 82 Mouse Binding pIC50 = 6.9 6.9 - 2
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2009.03.014
12002522 188563 None 0 Mouse Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 286 2 2 4 2.1 Clc1cccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
CHEMBL502716 188563 None 0 Mouse Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 286 2 2 4 2.1 Clc1cccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
117629482 2823 None 82 Mouse Binding pIC50 = 6.9 6.9 - 2
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.06.041
1588 2823 None 82 Mouse Binding pIC50 = 6.9 6.9 - 2
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.06.041
1594 2823 None 82 Mouse Binding pIC50 = 6.9 6.9 - 2
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.06.041
2835 2823 None 82 Mouse Binding pIC50 = 6.9 6.9 - 2
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.06.041
938 2823 None 82 Mouse Binding pIC50 = 6.9 6.9 - 2
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.06.041
CHEMBL573 2823 None 82 Mouse Binding pIC50 = 6.9 6.9 - 2
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.06.041
DB00627 2823 None 82 Mouse Binding pIC50 = 6.9 6.9 - 2
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2010.06.041
135899171 16177 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Displacement of radioligand from rat GPR109ADisplacement of radioligand from rat GPR109A
ChEMBL 331 6 1 5 2.8 O=c1[nH]c(OCCCOc2ccccc2Cl)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1224070 16177 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Displacement of radioligand from rat GPR109ADisplacement of radioligand from rat GPR109A
ChEMBL 331 6 1 5 2.8 O=c1[nH]c(OCCCOc2ccccc2Cl)nc2ncccc12 10.1016/j.bmcl.2010.07.108
122181102 121876 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 379 6 2 2 5.3 O=C(CCc1ccc(-c2cccc(Cl)c2)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
CHEMBL3589784 121876 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 379 6 2 2 5.3 O=C(CCc1ccc(-c2cccc(Cl)c2)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
46890302 7254 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 500 7 3 6 4.0 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CCC(c2cc(F)c(F)c(F)c2)C1 10.1016/j.bmcl.2010.04.013
CHEMBL1085842 7254 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 500 7 3 6 4.0 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CCC(c2cc(F)c(F)c(F)c2)C1 10.1016/j.bmcl.2010.04.013
46890198 7319 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 366 6 3 6 2.6 Cc1c(CCC(=O)Nc2ccccc2C(=O)O)cnn1-c1ccc(O)cn1 10.1016/j.bmcl.2010.04.013
CHEMBL1086108 7319 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 366 6 3 6 2.6 Cc1c(CCC(=O)Nc2ccccc2C(=O)O)cnn1-c1ccc(O)cn1 10.1016/j.bmcl.2010.04.013
46890578 6393 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 505 7 3 7 3.0 NC(Cc1nc(-c2ccc(F)cn2)no1)C(=O)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2F)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1082294 6393 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 505 7 3 7 3.0 NC(Cc1nc(-c2ccc(F)cn2)no1)C(=O)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2F)CC1 10.1016/j.bmcl.2010.04.001
135899171 16177 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 331 6 1 5 2.8 O=c1[nH]c(OCCCOc2ccccc2Cl)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1224070 16177 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 331 6 1 5 2.8 O=c1[nH]c(OCCCOc2ccccc2Cl)nc2ncccc12 10.1016/j.bmcl.2010.07.108
52941721 54981 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 283 1 0 7 4.2 Fc1ncccc1C1CCC2=C(C1)C(=C1N=NN=N1)N=N2 10.1016/j.bmcl.2009.06.054
CHEMBL1204125 54981 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 283 1 0 7 4.2 Fc1ncccc1C1CCC2=C(C1)C(=C1N=NN=N1)N=N2 10.1016/j.bmcl.2009.06.054
CHEMBL1615577 54981 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 283 1 0 7 4.2 Fc1ncccc1C1CCC2=C(C1)C(=C1N=NN=N1)N=N2 10.1016/j.bmcl.2009.06.054
12002717 199198 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 302 2 2 4 2.1 Fc1ccc(F)c(C2CCc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.06.054
CHEMBL565163 199198 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 302 2 2 4 2.1 Fc1ccc(F)c(C2CCc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.06.054
52941721 54981 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serum
ChEMBL 283 1 0 7 4.2 Fc1ncccc1C1CCC2=C(C1)C(=C1N=NN=N1)N=N2 10.1016/j.bmcl.2009.06.054
CHEMBL1204125 54981 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serum
ChEMBL 283 1 0 7 4.2 Fc1ncccc1C1CCC2=C(C1)C(=C1N=NN=N1)N=N2 10.1016/j.bmcl.2009.06.054
CHEMBL1615577 54981 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serum
ChEMBL 283 1 0 7 4.2 Fc1ncccc1C1CCC2=C(C1)C(=C1N=NN=N1)N=N2 10.1016/j.bmcl.2009.06.054
54587625 61416 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 376 6 4 4 3.3 N[C@@H](Cc1ccc(-c2ccc(O)cc2)cc1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1770171 61416 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 376 6 4 4 3.3 N[C@@H](Cc1ccc(-c2ccc(O)cc2)cc1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
117629482 2823 None 82 Human Binding pIC50 = 6.8 6.8 -3 2
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.039
1588 2823 None 82 Human Binding pIC50 = 6.8 6.8 -3 2
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.039
1594 2823 None 82 Human Binding pIC50 = 6.8 6.8 -3 2
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.039
2835 2823 None 82 Human Binding pIC50 = 6.8 6.8 -3 2
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.039
938 2823 None 82 Human Binding pIC50 = 6.8 6.8 -3 2
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.039
CHEMBL573 2823 None 82 Human Binding pIC50 = 6.8 6.8 -3 2
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.039
DB00627 2823 None 82 Human Binding pIC50 = 6.8 6.8 -3 2
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2008.08.039
11852982 14981 None 0 Mouse Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 228 2 2 2 2.0 O=C(O)c1n[nH]c2c1CC(c1ccccc1)C2 10.1016/j.bmcl.2010.06.041
CHEMBL1208922 14981 None 0 Mouse Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 228 2 2 2 2.0 O=C(O)c1n[nH]c2c1CC(c1ccccc1)C2 10.1016/j.bmcl.2010.06.041
11159621 2548 None 38 Human Binding pIC50 = 5.8 5.8 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2009.03.014
5784 2548 None 38 Human Binding pIC50 = 5.8 5.8 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2009.03.014
CHEMBL456145 2548 None 38 Human Binding pIC50 = 5.8 5.8 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2009.03.014
DB05939 2548 None 38 Human Binding pIC50 = 5.8 5.8 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2009.03.014
11159621 2548 None 38 Human Binding pIC50 = 5.8 5.8 - 1
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2010.06.041
5784 2548 None 38 Human Binding pIC50 = 5.8 5.8 - 1
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2010.06.041
CHEMBL456145 2548 None 38 Human Binding pIC50 = 5.8 5.8 - 1
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2010.06.041
DB05939 2548 None 38 Human Binding pIC50 = 5.8 5.8 - 1
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1016/j.bmcl.2010.06.041
135899199 16234 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 311 6 1 5 2.1 COc1cccc(CCOCc2nc3ncccc3c(=O)[nH]2)c1 10.1016/j.bmcl.2010.07.108
CHEMBL1224293 16234 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 311 6 1 5 2.1 COc1cccc(CCOCc2nc3ncccc3c(=O)[nH]2)c1 10.1016/j.bmcl.2010.07.108
136088957 61423 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 368 6 4 7 2.2 N[C@@H](CC(=O)Nc1ccccc1C(=O)O)c1nc(-c2ccc(O)cc2)no1 10.1016/j.bmcl.2010.11.116
CHEMBL1770178 61423 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 368 6 4 7 2.2 N[C@@H](CC(=O)Nc1ccccc1C(=O)O)c1nc(-c2ccc(O)cc2)no1 10.1016/j.bmcl.2010.11.116
24811550 6682 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 434 6 3 4 4.4 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2ccc(F)nc2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1083450 6682 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 434 6 3 4 4.4 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2ccc(F)nc2)CC1 10.1016/j.bmcl.2010.04.001
11624691 7229 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 361 6 3 3 4.3 O=C(CCc1ccc(-c2ccc(O)cc2)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1085711 7229 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 361 6 3 3 4.3 O=C(CCc1ccc(-c2ccc(O)cc2)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
137640776 157096 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 313 3 2 2 2.8 O=C(/C=C/C#Cc1ccccc1F)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4073322 157096 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 313 3 2 2 2.8 O=C(/C=C/C#Cc1ccccc1F)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
117629482 2823 None 82 Human Binding pIC50 = 6.8 6.8 -3 2
Agonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysisAgonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2020.127105
1588 2823 None 82 Human Binding pIC50 = 6.8 6.8 -3 2
Agonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysisAgonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2020.127105
1594 2823 None 82 Human Binding pIC50 = 6.8 6.8 -3 2
Agonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysisAgonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2020.127105
2835 2823 None 82 Human Binding pIC50 = 6.8 6.8 -3 2
Agonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysisAgonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2020.127105
938 2823 None 82 Human Binding pIC50 = 6.8 6.8 -3 2
Agonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysisAgonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2020.127105
CHEMBL573 2823 None 82 Human Binding pIC50 = 6.8 6.8 -3 2
Agonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysisAgonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2020.127105
DB00627 2823 None 82 Human Binding pIC50 = 6.8 6.8 -3 2
Agonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysisAgonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2020.127105
44445341 154337 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 376 4 2 5 3.2 O=C(O)c1ccccc1NC(=O)C1CCN(c2cnc3ccccc3n2)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL398625 154337 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 376 4 2 5 3.2 O=C(O)c1ccccc1NC(=O)C1CCN(c2cnc3ccccc3n2)CC1 10.1016/j.bmcl.2007.10.055
156022048 178306 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 383 7 3 8 2.2 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1cn(C2CC2)cc1C(=O)O 10.1016/j.bmcl.2020.127105
CHEMBL4649587 178306 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 383 7 3 8 2.2 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1cn(C2CC2)cc1C(=O)O 10.1016/j.bmcl.2020.127105
12002619 184286 None 0 Mouse Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 288 2 2 4 1.8 Fc1ccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c(F)c1 10.1016/j.bmcl.2009.03.014
CHEMBL483141 184286 None 0 Mouse Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 288 2 2 4 1.8 Fc1ccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c(F)c1 10.1016/j.bmcl.2009.03.014
12003695 14985 None 0 Mouse Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 232 2 2 4 0.7 Cn1cc(C2Cc3[nH]nc(C(=O)O)c3C2)cn1 10.1016/j.bmcl.2010.06.041
CHEMBL1208926 14985 None 0 Mouse Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 232 2 2 4 0.7 Cn1cc(C2Cc3[nH]nc(C(=O)O)c3C2)cn1 10.1016/j.bmcl.2010.06.041
44591603 191811 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 266 2 2 4 1.8 Cc1cccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
CHEMBL519689 191811 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 266 2 2 4 1.8 Cc1cccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
135502978 192098 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 377 5 4 4 3.2 O=C(CCc1[nH]nc2c1CCc1cc(O)ccc1-2)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL520136 192098 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 377 5 4 4 3.2 O=C(CCc1[nH]nc2c1CCc1cc(O)ccc1-2)Nc1ccccc1C(=O)O 10.1021/jm900151e
25101223 1152 None 7 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cells
ChEMBL 428 7 1 5 5.0 C[C@@H](NC(=O)c1cnc2n(c1C)ncc2c1ccc(cc1)C(C)C)COc1ccccc1 10.1016/j.bmcl.2008.08.039
5795 1152 None 7 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cells
ChEMBL 428 7 1 5 5.0 C[C@@H](NC(=O)c1cnc2n(c1C)ncc2c1ccc(cc1)C(C)C)COc1ccccc1 10.1016/j.bmcl.2008.08.039
CHEMBL490599 1152 None 7 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cells
ChEMBL 428 7 1 5 5.0 C[C@@H](NC(=O)c1cnc2n(c1C)ncc2c1ccc(cc1)C(C)C)COc1ccccc1 10.1016/j.bmcl.2008.08.039
49862073 14979 None 1 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 194 2 2 2 1.5 CC(C)C1Cc2[nH]nc(C(=O)O)c2C1 10.1016/j.bmcl.2010.06.041
CHEMBL1208920 14979 None 1 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 194 2 2 2 1.5 CC(C)C1Cc2[nH]nc(C(=O)O)c2C1 10.1016/j.bmcl.2010.06.041
12002520 184259 None 0 Mouse Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 270 2 2 4 1.6 Fc1ccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)cc1 10.1016/j.bmcl.2009.03.014
CHEMBL482943 184259 None 0 Mouse Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 270 2 2 4 1.6 Fc1ccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)cc1 10.1016/j.bmcl.2009.03.014
135899152 16233 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 311 6 1 5 2.1 COc1ccccc1CCOCc1nc2ncccc2c(=O)[nH]1 10.1016/j.bmcl.2010.07.108
CHEMBL1224292 16233 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 311 6 1 5 2.1 COc1ccccc1CCOCc1nc2ncccc2c(=O)[nH]1 10.1016/j.bmcl.2010.07.108
11646179 184919 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 359 5 3 3 4.0 O=C(CCc1ccc2c(ccc3[nH]ncc32)c1)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL485185 184919 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 359 5 3 3 4.0 O=C(CCc1ccc2c(ccc3[nH]ncc32)c1)Nc1ccccc1C(=O)O 10.1021/jm900151e
46890328 6683 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 484 6 3 4 5.3 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2ccc(C(F)(F)F)nc2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1083451 6683 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 484 6 3 4 5.3 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2ccc(C(F)(F)F)nc2)CC1 10.1016/j.bmcl.2010.04.001
156021045 178236 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 399 9 3 8 2.7 CCCCn1cc(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
CHEMBL4648435 178236 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 399 9 3 8 2.7 CCCCn1cc(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
156017210 177835 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 414 8 4 3 5.1 CCCCc1cc(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)c(C(=O)O)[nH]1 10.1016/j.bmcl.2020.127105
CHEMBL4642367 177835 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 414 8 4 3 5.1 CCCCc1cc(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)c(C(=O)O)[nH]1 10.1016/j.bmcl.2020.127105
11625092 6686 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 379 6 2 2 5.3 O=C(CCc1ccc(-c2ccccc2Cl)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
CHEMBL1083473 6686 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 379 6 2 2 5.3 O=C(CCc1ccc(-c2ccccc2Cl)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
46890539 7042 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 472 7 2 6 3.9 O=C(CCc1nc(-c2ccc(F)cn2)no1)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1084841 7042 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 472 7 2 6 3.9 O=C(CCc1nc(-c2ccc(F)cn2)no1)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
136375455 177659 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 385 7 3 8 2.5 CC(C)n1cc(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
CHEMBL4640349 177659 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 385 7 3 8 2.5 CC(C)n1cc(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
12002523 172052 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 286 2 2 4 2.1 Clc1ccccc1C1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
CHEMBL447050 172052 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 286 2 2 4 2.1 Clc1ccccc1C1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
12003601 14986 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 218 2 2 4 0.6 O=C(O)c1n[nH]c2c1CC(n1cccn1)C2 10.1016/j.bmcl.2010.06.041
CHEMBL1208987 14986 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 218 2 2 4 0.6 O=C(O)c1n[nH]c2c1CC(n1cccn1)C2 10.1016/j.bmcl.2010.06.041
135899263 16119 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 307 7 1 3 3.7 O=c1[nH]c(CCCCCCc2ccccc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1223875 16119 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 307 7 1 3 3.7 O=c1[nH]c(CCCCCCc2ccccc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
156021045 178236 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Agonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysisAgonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysis
ChEMBL 399 9 3 8 2.7 CCCCn1cc(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
CHEMBL4648435 178236 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Agonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysisAgonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysis
ChEMBL 399 9 3 8 2.7 CCCCn1cc(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
24741312 89433 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 358 6 3 7 2.3 O=C(CCc1cnc(-n2cc(O)cn2)s1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL237036 89433 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 358 6 3 7 2.3 O=C(CCc1cnc(-n2cc(O)cn2)s1)Nc1ccccc1C(=O)O 10.1021/jm700942d
136088961 61470 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 387 6 4 8 1.0 CC1CCC(NC(=O)[C@@H](N)Cc2nc(-c3ccc(O)cn3)no2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.11.116
CHEMBL1770357 61470 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 387 6 4 8 1.0 CC1CCC(NC(=O)[C@@H](N)Cc2nc(-c3ccc(O)cn3)no2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.11.116
12003490 14982 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 282 2 2 2 2.4 O=C(O)c1n[nH]c2c1CC(c1cc(F)cc(F)c1F)C2 10.1016/j.bmcl.2010.06.041
CHEMBL1208923 14982 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 282 2 2 2 2.4 O=C(O)c1n[nH]c2c1CC(c1cc(F)cc(F)c1F)C2 10.1016/j.bmcl.2010.06.041
12003791 194954 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 261 2 2 3 1.9 O=C(O)c1n[nH]c2c1CC(c1cccnc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL1237147 194954 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 261 2 2 3 1.9 O=C(O)c1n[nH]c2c1CC(c1cccnc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL539398 194954 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 261 2 2 3 1.9 O=C(O)c1n[nH]c2c1CC(c1cccnc1F)CC2 10.1016/j.bmcl.2009.06.054
11852982 14981 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 228 2 2 2 2.0 O=C(O)c1n[nH]c2c1CC(c1ccccc1)C2 10.1016/j.bmcl.2010.06.041
CHEMBL1208922 14981 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 228 2 2 2 2.0 O=C(O)c1n[nH]c2c1CC(c1ccccc1)C2 10.1016/j.bmcl.2010.06.041
16048997 94710 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 394 3 2 4 3.4 O=C(O)c1ccccc1NC(=O)N1CCN(c2c(Cl)cncc2Cl)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL252507 94710 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 394 3 2 4 3.4 O=C(O)c1ccccc1NC(=O)N1CCN(c2c(Cl)cncc2Cl)CC1 10.1016/j.bmcl.2007.10.055
122181105 121883 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 375 6 3 3 4.6 Cc1cc(-c2ccc(CCC(=O)Nc3ccccc3C(=O)O)cc2)ccc1O 10.1016/j.bmc.2015.02.018
CHEMBL3589791 121883 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 375 6 3 3 4.6 Cc1cc(-c2ccc(CCC(=O)Nc3ccccc3C(=O)O)cc2)ccc1O 10.1016/j.bmc.2015.02.018
11493732 193209 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 335 5 3 3 3.8 O=C(CCc1ccc2cc(O)ccc2c1)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL522649 193209 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 335 5 3 3 3.8 O=C(CCc1ccc2cc(O)ccc2c1)Nc1ccccc1C(=O)O 10.1021/jm900151e
54584718 61471 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 374 6 2 6 2.5 C[C@@H]1CCC(C(=O)O)=C(NC(=O)CCc2nc(-c3ccc(F)cn3)no2)C1 10.1016/j.bmcl.2010.11.116
CHEMBL1770359 61471 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 374 6 2 6 2.5 C[C@@H]1CCC(C(=O)O)=C(NC(=O)CCc2nc(-c3ccc(F)cn3)no2)C1 10.1016/j.bmcl.2010.11.116
122181142 121896 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 365 6 3 3 4.0 O=C(CCc1ccc(-c2ccc(O)cc2)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL3589836 121896 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 365 6 3 3 4.0 O=C(CCc1ccc(-c2ccc(O)cc2)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
11736428 189172 None 0 Mouse Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 232 4 2 4 1.5 CCCCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
CHEMBL509541 189172 None 0 Mouse Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 232 4 2 4 1.5 CCCCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
16048992 94735 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 403 4 2 5 3.2 O=C(O)c1ccccc1NC(=O)N1CCN(c2nccc(-c3ccccc3)n2)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL252707 94735 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 403 4 2 5 3.2 O=C(O)c1ccccc1NC(=O)N1CCN(c2nccc(-c3ccccc3)n2)CC1 10.1016/j.bmcl.2007.10.055
135922719 184393 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 377 5 3 5 3.0 Cn1nc(CCC(=O)Nc2ccccc2C(=O)O)c2c1-c1ccc(O)cc1C2 10.1021/jm900151e
CHEMBL483996 184393 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 377 5 3 5 3.0 Cn1nc(CCC(=O)Nc2ccccc2C(=O)O)c2c1-c1ccc(O)cc1C2 10.1021/jm900151e
12003695 14985 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 232 2 2 4 0.7 Cn1cc(C2Cc3[nH]nc(C(=O)O)c3C2)cn1 10.1016/j.bmcl.2010.06.041
CHEMBL1208926 14985 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 232 2 2 4 0.7 Cn1cc(C2Cc3[nH]nc(C(=O)O)c3C2)cn1 10.1016/j.bmcl.2010.06.041
46890239 6936 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 370 6 3 6 2.2 CC(Cc1cnn(-c2ccc(O)cn2)c1)C(=O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.013
CHEMBL1084448 6936 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 370 6 3 6 2.2 CC(Cc1cnn(-c2ccc(O)cn2)c1)C(=O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.013
12003788 196265 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 278 2 2 2 2.7 O=C(O)c1n[nH]c2c1CC(c1cc(F)ccc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL1237148 196265 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 278 2 2 2 2.7 O=C(O)c1n[nH]c2c1CC(c1cc(F)ccc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL542000 196265 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 278 2 2 2 2.7 O=C(O)c1n[nH]c2c1CC(c1cc(F)ccc1F)CC2 10.1016/j.bmcl.2009.06.054
136375410 177422 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 370 7 3 7 2.5 CCn1cc(NC(=O)CCc2nc(-c3ccc(O)cc3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
CHEMBL4636989 177422 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 370 7 3 7 2.5 CCn1cc(NC(=O)CCc2nc(-c3ccc(O)cc3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
135899322 16199 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 299 5 1 4 2.2 O=c1[nH]c(COCCc2ccccc2F)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1224146 16199 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 299 5 1 4 2.2 O=c1[nH]c(COCCc2ccccc2F)nc2ncccc12 10.1016/j.bmcl.2010.07.108
16048923 94709 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 376 3 2 4 3.3 O=C(O)c1ccccc1NC(=O)N1CCN(c2nccc3ccccc23)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL252506 94709 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 376 3 2 4 3.3 O=C(O)c1ccccc1NC(=O)N1CCN(c2nccc3ccccc23)CC1 10.1016/j.bmcl.2007.10.055
137661033 159581 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 313 4 3 3 2.6 O=C(CCC#Cc1ccccc1O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4101720 159581 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 313 4 3 3 2.6 O=C(CCC#Cc1ccccc1O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
122181140 121894 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 379 6 3 3 4.5 O=C(CCc1ccc(-c2ccc(O)cc2F)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
CHEMBL3589834 121894 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 379 6 3 3 4.5 O=C(CCc1ccc(-c2ccc(O)cc2F)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
15986930 185016 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 371 5 3 6 2.8 O=C(CCc1cn2c(n1)sc1cc(O)ccc12)NC1=C(C(=O)O)CCC1 10.1021/jm900151e
CHEMBL485327 185016 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 371 5 3 6 2.8 O=C(CCc1cn2c(n1)sc1cc(O)ccc12)NC1=C(C(=O)O)CCC1 10.1021/jm900151e
156019027 177902 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 415 8 3 5 4.5 CCCCn1cc(C(=O)O)c(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)n1 10.1016/j.bmcl.2020.127105
CHEMBL4643451 177902 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 415 8 3 5 4.5 CCCCn1cc(C(=O)O)c(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)n1 10.1016/j.bmcl.2020.127105
135899198 15598 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 299 5 1 4 2.2 O=c1[nH]c(COCCc2cccc(F)c2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1221438 15598 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 299 5 1 4 2.2 O=c1[nH]c(COCCc2cccc(F)c2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
135899170 16179 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 331 6 1 5 2.8 O=c1[nH]c(OCCCOc2ccc(Cl)cc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1224072 16179 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 331 6 1 5 2.8 O=c1[nH]c(OCCCOc2ccc(Cl)cc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
24741307 88769 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 365 6 3 5 3.2 Cc1c(CCC(=O)Nc2ccccc2C(=O)O)cnn1-c1ccc(O)cc1 10.1016/j.bmcl.2010.04.013
CHEMBL236163 88769 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 365 6 3 5 3.2 Cc1c(CCC(=O)Nc2ccccc2C(=O)O)cnn1-c1ccc(O)cc1 10.1016/j.bmcl.2010.04.013
24741307 88769 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 365 6 3 5 3.2 Cc1c(CCC(=O)Nc2ccccc2C(=O)O)cnn1-c1ccc(O)cc1 10.1021/jm700942d
CHEMBL236163 88769 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 365 6 3 5 3.2 Cc1c(CCC(=O)Nc2ccccc2C(=O)O)cnn1-c1ccc(O)cc1 10.1021/jm700942d
11660694 178173 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 369 5 3 3 4.5 O=C(CCc1ccc2c(Cl)c(O)ccc2c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2020.127105
CHEMBL4647392 178173 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 369 5 3 3 4.5 O=C(CCc1ccc2c(Cl)c(O)ccc2c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2020.127105
11493732 193209 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cells
ChEMBL 335 5 3 3 3.8 O=C(CCc1ccc2cc(O)ccc2c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2008.08.030
CHEMBL522649 193209 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cells
ChEMBL 335 5 3 3 3.8 O=C(CCc1ccc2cc(O)ccc2c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2008.08.030
12003596 14983 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 234 2 2 3 2.1 O=C(O)c1n[nH]c2c1CC(c1cccs1)C2 10.1016/j.bmcl.2010.06.041
CHEMBL1208924 14983 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 234 2 2 3 2.1 O=C(O)c1n[nH]c2c1CC(c1cccs1)C2 10.1016/j.bmcl.2010.06.041
12002619 184286 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 288 2 2 4 1.8 Fc1ccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c(F)c1 10.1016/j.bmcl.2009.03.014
CHEMBL483141 184286 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 288 2 2 4 1.8 Fc1ccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c(F)c1 10.1016/j.bmcl.2009.03.014
117629482 2823 None 82 Human Binding pIC50 = 6.6 6.6 -3 2
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmc.2015.02.018
1588 2823 None 82 Human Binding pIC50 = 6.6 6.6 -3 2
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmc.2015.02.018
1594 2823 None 82 Human Binding pIC50 = 6.6 6.6 -3 2
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmc.2015.02.018
2835 2823 None 82 Human Binding pIC50 = 6.6 6.6 -3 2
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmc.2015.02.018
938 2823 None 82 Human Binding pIC50 = 6.6 6.6 -3 2
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmc.2015.02.018
CHEMBL573 2823 None 82 Human Binding pIC50 = 6.6 6.6 -3 2
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmc.2015.02.018
DB00627 2823 None 82 Human Binding pIC50 = 6.6 6.6 -3 2
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmc.2015.02.018
46890197 7261 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 366 6 3 6 2.5 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
CHEMBL1085875 7261 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 366 6 3 6 2.5 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
137633734 156412 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 311 3 3 3 2.3 O=C(/C=C/C#Cc1ccc(O)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4065654 156412 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 311 3 3 3 2.3 O=C(/C=C/C#Cc1ccc(O)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
49862072 14978 None 0 Mouse Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 194 3 2 2 1.6 CCCC1Cc2[nH]nc(C(=O)O)c2C1 10.1016/j.bmcl.2010.06.041
CHEMBL1208919 14978 None 0 Mouse Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 194 3 2 2 1.6 CCCC1Cc2[nH]nc(C(=O)O)c2C1 10.1016/j.bmcl.2010.06.041
12003596 14983 None 0 Mouse Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 234 2 2 3 2.1 O=C(O)c1n[nH]c2c1CC(c1cccs1)C2 10.1016/j.bmcl.2010.06.041
CHEMBL1208924 14983 None 0 Mouse Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 234 2 2 3 2.1 O=C(O)c1n[nH]c2c1CC(c1cccs1)C2 10.1016/j.bmcl.2010.06.041
135899131 16142 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 315 6 1 5 2.3 O=c1[nH]c(OCCCOc2ccccc2F)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1223959 16142 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 315 6 1 5 2.3 O=c1[nH]c(OCCCOc2ccccc2F)nc2ncccc12 10.1016/j.bmcl.2010.07.108
16048998 94685 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 376 3 2 4 3.3 O=C(O)c1ccccc1NC(=O)N1CCN(c2ccc3ccccc3n2)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL252307 94685 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 376 3 2 4 3.3 O=C(O)c1ccccc1NC(=O)N1CCN(c2ccc3ccccc3n2)CC1 10.1016/j.bmcl.2007.10.055
11299550 192116 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 244 2 2 4 1.5 C1CCC(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)C1 10.1016/j.bmcl.2009.03.014
CHEMBL520159 192116 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 244 2 2 4 1.5 C1CCC(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)C1 10.1016/j.bmcl.2009.03.014
44591602 188491 None 0 Mouse Binding pIC50 = 5.6 5.6 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 216 2 2 4 0.7 C1CC1C1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
CHEMBL501585 188491 None 0 Mouse Binding pIC50 = 5.6 5.6 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 216 2 2 4 0.7 C1CC1C1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
15986936 7103 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 356 6 3 6 1.9 O=C(CCc1cnn(-c2ccc(O)cn2)c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.013
CHEMBL1085150 7103 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 356 6 3 6 1.9 O=C(CCc1cnn(-c2ccc(O)cn2)c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.013
15986929 7161 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 383 6 3 5 3.1 Cc1c(CC(C)C(=O)NC2=C(C(=O)O)CCCC2)cnn1-c1ccc(O)cc1 10.1016/j.bmcl.2010.04.013
CHEMBL1085402 7161 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 383 6 3 5 3.1 Cc1c(CC(C)C(=O)NC2=C(C(=O)O)CCCC2)cnn1-c1ccc(O)cc1 10.1016/j.bmcl.2010.04.013
135800176 89434 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 369 6 3 6 3.2 O=C(CCc1cnc(-c2ccc(O)cn2)s1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL237037 89434 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 369 6 3 6 3.2 O=C(CCc1cnc(-c2ccc(O)cn2)s1)Nc1ccccc1C(=O)O 10.1021/jm700942d
46890164 7424 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 335 6 2 4 3.1 O=C(CCc1cnn(-c2ccccc2)c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
CHEMBL1086568 7424 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 335 6 2 4 3.1 O=C(CCc1cnn(-c2ccccc2)c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
11424509 188395 None 0 Mouse Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 218 3 2 4 1.1 CCCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
CHEMBL500239 188395 None 0 Mouse Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 218 3 2 4 1.1 CCCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
156021546 178291 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 401 9 4 9 1.3 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1cn(CCCO)cc1C(=O)O 10.1016/j.bmcl.2020.127105
CHEMBL4649305 178291 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 401 9 4 9 1.3 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1cn(CCCO)cc1C(=O)O 10.1016/j.bmcl.2020.127105
12003785 198835 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 260 2 2 2 2.5 O=C(O)c1n[nH]c2c1CC(c1ccccc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL562632 198835 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 260 2 2 2 2.5 O=C(O)c1n[nH]c2c1CC(c1ccccc1F)CC2 10.1016/j.bmcl.2009.06.054
12002520 184259 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 270 2 2 4 1.6 Fc1ccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)cc1 10.1016/j.bmcl.2009.03.014
CHEMBL482943 184259 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 270 2 2 4 1.6 Fc1ccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)cc1 10.1016/j.bmcl.2009.03.014
135899325 16200 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
Displacement of radioligand from rat GPR109ADisplacement of radioligand from rat GPR109A
ChEMBL 299 5 1 4 2.2 O=c1[nH]c(COCCc2ccc(F)cc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1224147 16200 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
Displacement of radioligand from rat GPR109ADisplacement of radioligand from rat GPR109A
ChEMBL 299 5 1 4 2.2 O=c1[nH]c(COCCc2ccc(F)cc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
17751630 6747 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 487 7 3 7 2.8 NC(Cc1nc(-c2ccc(F)cn2)no1)C(=O)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1083743 6747 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 487 7 3 7 2.8 NC(Cc1nc(-c2ccc(F)cn2)no1)C(=O)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
137635425 156012 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 331 4 3 3 2.7 O=C(CCC#Cc1ccc(O)cc1F)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4060899 156012 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 331 4 3 3 2.7 O=C(CCC#Cc1ccc(O)cc1F)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
46890579 7018 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 455 7 2 7 3.2 O=C(CCc1nc(-c2ccc(F)cn2)no1)NC1=C(C(=O)O)CC(c2ccc(F)nc2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1084798 7018 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 455 7 2 7 3.2 O=C(CCc1nc(-c2ccc(F)cn2)no1)NC1=C(C(=O)O)CC(c2ccc(F)nc2)CC1 10.1016/j.bmcl.2010.04.001
137662135 159444 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 367 6 2 2 4.5 O=C(CCc1ccc(-c2ccccc2F)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4100231 159444 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 367 6 2 2 4.5 O=C(CCc1ccc(-c2ccccc2F)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
137645601 157943 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 299 6 2 2 3.2 O=C(/C=C/CCc1ccccc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4083723 157943 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 299 6 2 2 3.2 O=C(/C=C/CCc1ccccc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
11559598 121877 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 363 6 2 2 4.8 O=C(CCc1ccc(-c2cccc(F)c2)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
CHEMBL3589785 121877 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 363 6 2 2 4.8 O=C(CCc1ccc(-c2cccc(F)c2)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
11660694 178173 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Agonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysisAgonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysis
ChEMBL 369 5 3 3 4.5 O=C(CCc1ccc2c(Cl)c(O)ccc2c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2020.127105
CHEMBL4647392 178173 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Agonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysisAgonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysis
ChEMBL 369 5 3 3 4.5 O=C(CCc1ccc2c(Cl)c(O)ccc2c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2020.127105
11617151 88673 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 345 6 2 2 4.6 O=C(CCc1ccc(-c2ccccc2)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
CHEMBL235741 88673 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 345 6 2 2 4.6 O=C(CCc1ccc(-c2ccccc2)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
16048919 94736 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 407 4 2 6 2.7 COc1cccc2nc(N3CCN(C(=O)Nc4ccccc4C(=O)O)CC3)cnc12 10.1016/j.bmcl.2007.10.055
CHEMBL252708 94736 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 407 4 2 6 2.7 COc1cccc2nc(N3CCN(C(=O)Nc4ccccc4C(=O)O)CC3)cnc12 10.1016/j.bmcl.2007.10.055
12002522 188563 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 286 2 2 4 2.1 Clc1cccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
CHEMBL502716 188563 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 286 2 2 4 2.1 Clc1cccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
137653428 158635 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 315 4 2 2 3.0 O=C(CCC#Cc1ccc(F)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4091542 158635 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 315 4 2 2 3.0 O=C(CCC#Cc1ccc(F)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
42625474 184284 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 380 5 3 5 3.6 O=C(CCc1noc2c1ccc1cc(O)ccc12)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
CHEMBL483139 184284 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 380 5 3 5 3.6 O=C(CCc1noc2c1ccc1cc(O)ccc12)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
42625379 192200 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 376 5 3 5 4.0 O=C(CCc1noc2c1ccc1cc(O)ccc12)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL520299 192200 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 376 5 3 5 4.0 O=C(CCc1noc2c1ccc1cc(O)ccc12)Nc1ccccc1C(=O)O 10.1021/jm900151e
46890327 6602 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 451 6 3 3 5.2 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1083138 6602 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 451 6 3 3 5.2 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
135416388 7526 None 0 Human Binding pIC50 = 8.5 8.5 - 1
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 358 6 3 7 1.8 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.11.116
CHEMBL1087302 7526 None 0 Human Binding pIC50 = 8.5 8.5 - 1
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 358 6 3 7 1.8 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.11.116
12003490 14982 None 0 Mouse Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 282 2 2 2 2.4 O=C(O)c1n[nH]c2c1CC(c1cc(F)cc(F)c1F)C2 10.1016/j.bmcl.2010.06.041
CHEMBL1208923 14982 None 0 Mouse Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 282 2 2 2 2.4 O=C(O)c1n[nH]c2c1CC(c1cc(F)cc(F)c1F)C2 10.1016/j.bmcl.2010.06.041
42625213 192412 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 365 5 2 5 3.8 O=C(CCc1cn2c(n1)sc1ccccc12)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL520620 192412 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 365 5 2 5 3.8 O=C(CCc1cn2c(n1)sc1ccccc12)Nc1ccccc1C(=O)O 10.1021/jm900151e
46890163 7423 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 335 6 2 4 3.1 O=C(CCc1ccn(-c2ccccc2)n1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
CHEMBL1086567 7423 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 335 6 2 4 3.1 O=C(CCc1ccn(-c2ccccc2)n1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
12003879 192451 None 0 Mouse Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 252 2 2 4 1.5 c1ccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)cc1 10.1016/j.bmcl.2009.03.014
CHEMBL520675 192451 None 0 Mouse Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 252 2 2 4 1.5 c1ccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)cc1 10.1016/j.bmcl.2009.03.014
156020475 178179 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 429 8 3 5 4.5 CCCCc1nc(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)c(C(=O)O)n1C 10.1016/j.bmcl.2020.127105
CHEMBL4647545 178179 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 429 8 3 5 4.5 CCCCc1nc(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)c(C(=O)O)n1C 10.1016/j.bmcl.2020.127105
12002523 172052 None 0 Mouse Binding pIC50 = 5.5 5.5 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 286 2 2 4 2.1 Clc1ccccc1C1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
CHEMBL447050 172052 None 0 Mouse Binding pIC50 = 5.5 5.5 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 286 2 2 4 2.1 Clc1ccccc1C1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
46890165 7316 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 351 6 3 5 2.8 O=C(CCc1cnn(-c2ccc(O)cc2)c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
CHEMBL1086103 7316 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 351 6 3 5 2.8 O=C(CCc1cnn(-c2ccc(O)cc2)c1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
46890501 7248 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 375 6 3 7 1.2 NC(Cc1nc(-c2ccc(F)cn2)no1)C(=O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.001
CHEMBL1085816 7248 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 375 6 3 7 1.2 NC(Cc1nc(-c2ccc(F)cn2)no1)C(=O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.001
137647495 157948 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 365 6 3 3 4.0 O=C(CCc1ccc(-c2cccc(O)c2)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4083762 157948 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 365 6 3 3 4.0 O=C(CCc1ccc(-c2cccc(O)c2)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
11508815 121873 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 363 6 2 2 4.8 O=C(CCc1ccc(-c2ccc(F)cc2)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
CHEMBL3589779 121873 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 363 6 2 2 4.8 O=C(CCc1ccc(-c2ccc(F)cc2)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
122181104 121881 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 413 6 2 2 5.6 O=C(CCc1ccc(-c2ccccc2C(F)(F)F)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
CHEMBL3589789 121881 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 413 6 2 2 5.6 O=C(CCc1ccc(-c2ccccc2C(F)(F)F)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
90645405 112596 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 295 3 2 2 2.6 O=C(/C=C/C#Cc1ccccc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL3299113 112596 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 295 3 2 2 2.6 O=C(/C=C/C#Cc1ccccc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
136127016 16178 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 331 6 1 5 2.8 O=c1[nH]c(OCCCOc2cccc(Cl)c2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1224071 16178 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 331 6 1 5 2.8 O=c1[nH]c(OCCCOc2cccc(Cl)c2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
135800175 88770 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 353 6 3 6 2.7 O=C(CCc1nnc(-c2ccc(O)cc2)o1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL236164 88770 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 353 6 3 6 2.7 O=C(CCc1nnc(-c2ccc(O)cc2)o1)Nc1ccccc1C(=O)O 10.1021/jm700942d
44579763 187089 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cells
ChEMBL 428 7 1 5 5.0 Cc1c(C(=O)N[C@@H](C)COc2ccccc2)cnc2c(-c3ccc(C(C)C)cc3)cnn12 10.1016/j.bmcl.2008.08.039
CHEMBL490600 187089 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cells
ChEMBL 428 7 1 5 5.0 Cc1c(C(=O)N[C@@H](C)COc2ccccc2)cnc2c(-c3ccc(C(C)C)cc3)cnn12 10.1016/j.bmcl.2008.08.039
137652577 158852 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 329 3 3 3 2.5 O=C(/C=C/C#Cc1ccc(O)cc1F)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4093990 158852 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 329 3 3 3 2.5 O=C(/C=C/C#Cc1ccc(O)cc1F)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
11560300 88573 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 395 6 3 3 5.0 O=C(CCc1ccc(-c2ccc(O)cc2Cl)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
CHEMBL235256 88573 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 395 6 3 3 5.0 O=C(CCc1ccc(-c2ccc(O)cc2Cl)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
24811547 7378 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 415 6 3 3 4.9 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2ccccc2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1086355 7378 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 415 6 3 3 4.9 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2ccccc2)CC1 10.1016/j.bmcl.2010.04.001
11638560 187149 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cells
ChEMBL 334 5 3 3 3.7 Nc1ccc2cc(CCC(=O)Nc3ccccc3C(=O)O)ccc2c1 10.1016/j.bmcl.2008.08.030
CHEMBL491002 187149 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cells
ChEMBL 334 5 3 3 3.7 Nc1ccc2cc(CCC(=O)Nc3ccccc3C(=O)O)ccc2c1 10.1016/j.bmcl.2008.08.030
42625382 184918 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 416 5 3 5 3.7 Cn1c(=O)c2cc(O)ccc2c2ccc(CCC(=O)Nc3ccccc3C(=O)O)cc21 10.1021/jm900151e
CHEMBL485184 184918 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 416 5 3 5 3.7 Cn1c(=O)c2cc(O)ccc2c2ccc(CCC(=O)Nc3ccccc3C(=O)O)cc21 10.1021/jm900151e
11736428 189172 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 232 4 2 4 1.5 CCCCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
CHEMBL509541 189172 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 232 4 2 4 1.5 CCCCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
12003880 188842 None 0 Mouse Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 270 2 2 4 1.6 Fc1ccccc1C1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
CHEMBL504980 188842 None 0 Mouse Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 270 2 2 4 1.6 Fc1ccccc1C1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
44580007 187053 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cells
ChEMBL 366 6 1 5 3.6 COCC(C)NC(=O)c1cnc2c(-c3ccc(C(C)C)cc3)cnn2c1C 10.1016/j.bmcl.2008.08.039
CHEMBL490215 187053 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cells
ChEMBL 366 6 1 5 3.6 COCC(C)NC(=O)c1cnc2c(-c3ccc(C(C)C)cc3)cnn2c1C 10.1016/j.bmcl.2008.08.039
12003601 14986 None 0 Mouse Binding pIC50 = 5.5 5.5 - 0
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 218 2 2 4 0.6 O=C(O)c1n[nH]c2c1CC(n1cccn1)C2 10.1016/j.bmcl.2010.06.041
CHEMBL1208987 14986 None 0 Mouse Binding pIC50 = 5.5 5.5 - 0
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 218 2 2 4 0.6 O=C(O)c1n[nH]c2c1CC(n1cccn1)C2 10.1016/j.bmcl.2010.06.041
135399731 184263 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 391 5 3 5 3.2 Cn1nc2c(c1CCC(=O)Nc1ccccc1C(=O)O)CCc1cc(O)ccc1-2 10.1021/jm900151e
CHEMBL482963 184263 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 391 5 3 5 3.2 Cn1nc2c(c1CCC(=O)Nc1ccccc1C(=O)O)CCc1cc(O)ccc1-2 10.1021/jm900151e
46890500 7247 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 360 6 2 6 2.2 O=C(CCc1nc(-c2ccc(F)cn2)no1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.001
CHEMBL1085815 7247 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 360 6 2 6 2.2 O=C(CCc1nc(-c2ccc(F)cn2)no1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.001
24741306 167052 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 334 6 3 2 4.0 O=C(CCc1ccc(-c2ccc[nH]2)cc1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL428724 167052 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 334 6 3 2 4.0 O=C(CCc1ccc(-c2ccc[nH]2)cc1)Nc1ccccc1C(=O)O 10.1021/jm700942d
46890401 7289 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 460 7 3 4 4.9 O=C(CCc1ccc(-c2ccc(O)cc2)cc1)NC1=C(C(=O)O)CC(c2cccnc2F)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1086031 7289 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 460 7 3 4 4.9 O=C(CCc1ccc(-c2ccc(O)cc2)cc1)NC1=C(C(=O)O)CC(c2cccnc2F)CC1 10.1016/j.bmcl.2010.04.001
42625380 184517 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 407 5 3 8 1.6 Cn1c(=O)c2c(CCC(=O)Nc3ccccc3C(=O)O)nnn2c2ccc(O)cc21 10.1021/jm900151e
CHEMBL484605 184517 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 407 5 3 8 1.6 Cn1c(=O)c2c(CCC(=O)Nc3ccccc3C(=O)O)nnn2c2ccc(O)cc21 10.1021/jm900151e
44591586 184267 None 0 Mouse Binding pIC50 = 5.4 5.4 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 246 5 2 4 1.9 CCCCCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
CHEMBL482979 184267 None 0 Mouse Binding pIC50 = 5.4 5.4 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 246 5 2 4 1.9 CCCCCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
137648318 157724 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 341 5 3 3 2.5 O=C(CCC#Cc1ccc(C(=O)O)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4081260 157724 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 341 5 3 3 2.5 O=C(CCC#Cc1ccc(C(=O)O)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
122181106 121884 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 395 6 3 3 5.0 O=C(CCc1ccc(-c2ccc(O)c(Cl)c2)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
CHEMBL3589792 121884 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 395 6 3 3 5.0 O=C(CCc1ccc(-c2ccc(O)c(Cl)c2)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
137632012 156748 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 311 3 3 3 2.3 O=C(/C=C/C#Cc1ccccc1O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4069406 156748 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 311 3 3 3 2.3 O=C(/C=C/C#Cc1ccccc1O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
12003791 194954 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serum
ChEMBL 261 2 2 3 1.9 O=C(O)c1n[nH]c2c1CC(c1cccnc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL1237147 194954 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serum
ChEMBL 261 2 2 3 1.9 O=C(O)c1n[nH]c2c1CC(c1cccnc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL539398 194954 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serum
ChEMBL 261 2 2 3 1.9 O=C(O)c1n[nH]c2c1CC(c1cccnc1F)CC2 10.1016/j.bmcl.2009.06.054
136127015 16139 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 279 4 1 4 2.4 O=c1[nH]c(OC/C=C/c2ccccc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1223956 16139 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 279 4 1 4 2.4 O=c1[nH]c(OC/C=C/c2ccccc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
135899149 16144 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 315 6 1 5 2.3 O=c1[nH]c(OCCCOc2cccc(F)c2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1223960 16144 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 315 6 1 5 2.3 O=c1[nH]c(OCCCOc2cccc(F)c2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
135922723 184268 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 364 5 3 5 3.2 O=C(CCc1noc2c1Cc1cc(O)ccc1-2)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL482980 184268 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 364 5 3 5 3.2 O=C(CCc1noc2c1Cc1cc(O)ccc1-2)Nc1ccccc1C(=O)O 10.1021/jm900151e
49862072 14978 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 194 3 2 2 1.6 CCCC1Cc2[nH]nc(C(=O)O)c2C1 10.1016/j.bmcl.2010.06.041
CHEMBL1208919 14978 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 194 3 2 2 1.6 CCCC1Cc2[nH]nc(C(=O)O)c2C1 10.1016/j.bmcl.2010.06.041
137654580 159114 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 311 3 3 3 2.3 O=C(/C=C/C#Cc1cccc(O)c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4096635 159114 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 311 3 3 3 2.3 O=C(/C=C/C#Cc1cccc(O)c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
12003694 1144 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 232 2 2 4 0.7 OC(=O)c1n[nH]c2c1CC(C2)c1ccnn1C 10.1016/j.bmcl.2010.06.041
5793 1144 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 232 2 2 4 0.7 OC(=O)c1n[nH]c2c1CC(C2)c1ccnn1C 10.1016/j.bmcl.2010.06.041
CHEMBL1208986 1144 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 232 2 2 4 0.7 OC(=O)c1n[nH]c2c1CC(C2)c1ccnn1C 10.1016/j.bmcl.2010.06.041
156017987 178024 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 358 5 3 4 3.4 O=C(CCc1ccc2c(Cl)c(O)ccc2c1)Nn1cccc1C(=O)O 10.1016/j.bmcl.2020.127105
CHEMBL4645273 178024 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 358 5 3 4 3.4 O=C(CCc1ccc2c(Cl)c(O)ccc2c1)Nn1cccc1C(=O)O 10.1016/j.bmcl.2020.127105
11560300 88573 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 395 6 3 3 5.0 O=C(CCc1ccc(-c2ccc(O)cc2Cl)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
CHEMBL235256 88573 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 395 6 3 3 5.0 O=C(CCc1ccc(-c2ccc(O)cc2Cl)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
11560300 88573 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 395 6 3 3 5.0 O=C(CCc1ccc(-c2ccc(O)cc2Cl)cc1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL235256 88573 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 395 6 3 3 5.0 O=C(CCc1ccc(-c2ccc(O)cc2Cl)cc1)Nc1ccccc1C(=O)O 10.1021/jm700942d
135800194 89525 None 0 Human Binding pIC50 = 8.4 8.4 - 1
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 354 6 3 7 2.1 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL237248 89525 None 0 Human Binding pIC50 = 8.4 8.4 - 1
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 354 6 3 7 2.1 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1ccccc1C(=O)O 10.1021/jm700942d
135466520 184323 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 378 5 3 5 3.4 O=C(CCc1noc2c1CCc1cc(O)ccc1-2)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL483353 184323 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 378 5 3 5 3.4 O=C(CCc1noc2c1CCc1cc(O)ccc1-2)Nc1ccccc1C(=O)O 10.1021/jm900151e
135416384 184930 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 382 5 3 5 3.1 O=C(CCc1noc2c1CCc1cc(O)ccc1-2)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
CHEMBL485196 184930 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 382 5 3 5 3.1 O=C(CCc1noc2c1CCc1cc(O)ccc1-2)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
136086823 6971 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 400 8 3 7 2.8 CCCC1CCC(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
CHEMBL1084576 6971 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 400 8 3 7 2.8 CCCC1CCC(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
135416388 7526 None 0 Human Binding pIC50 = 8.4 8.4 - 1
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 358 6 3 7 1.8 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.001
CHEMBL1087302 7526 None 0 Human Binding pIC50 = 8.4 8.4 - 1
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 358 6 3 7 1.8 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.001
136088958 61466 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 369 6 4 8 1.0 N[C@H](Cc1nc(-c2ccc(O)cn2)no1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1770353 61466 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 369 6 4 8 1.0 N[C@H](Cc1nc(-c2ccc(O)cn2)no1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
12002618 192100 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 306 2 2 4 1.9 Fc1cc(F)c(F)c(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
CHEMBL520137 192100 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 306 2 2 4 1.9 Fc1cc(F)c(F)c(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
12002618 192100 None 0 Mouse Binding pIC50 = 7.4 7.4 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 306 2 2 4 1.9 Fc1cc(F)c(F)c(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
CHEMBL520137 192100 None 0 Mouse Binding pIC50 = 7.4 7.4 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 306 2 2 4 1.9 Fc1cc(F)c(F)c(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
137650474 157371 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 365 6 3 3 4.0 O=C(CCc1ccc(-c2ccccc2O)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4076822 157371 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 365 6 3 3 4.0 O=C(CCc1ccc(-c2ccccc2O)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
12003788 196265 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serum
ChEMBL 278 2 2 2 2.7 O=C(O)c1n[nH]c2c1CC(c1cc(F)ccc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL1237148 196265 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serum
ChEMBL 278 2 2 2 2.7 O=C(O)c1n[nH]c2c1CC(c1cc(F)ccc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL542000 196265 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serum
ChEMBL 278 2 2 2 2.7 O=C(O)c1n[nH]c2c1CC(c1cc(F)ccc1F)CC2 10.1016/j.bmcl.2009.06.054
136127010 16093 None 13 Rat Binding pIC50 = 6.4 6.4 - 0
Displacement of radioligand from rat GPR109ADisplacement of radioligand from rat GPR109A
ChEMBL 215 0 1 3 1.3 O=c1[nH]c(C(F)(F)F)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1223819 16093 None 13 Rat Binding pIC50 = 6.4 6.4 - 0
Displacement of radioligand from rat GPR109ADisplacement of radioligand from rat GPR109A
ChEMBL 215 0 1 3 1.3 O=c1[nH]c(C(F)(F)F)nc2ncccc12 10.1016/j.bmcl.2010.07.108
156020831 178175 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 386 8 4 8 1.5 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1cn(CCO)cc1C(=O)O 10.1016/j.bmcl.2020.127105
CHEMBL4647398 178175 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 386 8 4 8 1.5 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1cn(CCO)cc1C(=O)O 10.1016/j.bmcl.2020.127105
12003692 14987 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 219 2 2 5 0.0 O=C(O)c1n[nH]c2c1CC(n1ccnn1)C2 10.1016/j.bmcl.2010.06.041
CHEMBL1208988 14987 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 219 2 2 5 0.0 O=C(O)c1n[nH]c2c1CC(n1ccnn1)C2 10.1016/j.bmcl.2010.06.041
44591604 184929 None 0 Mouse Binding pIC50 = 5.4 5.4 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 286 2 2 4 2.1 Clc1ccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)cc1 10.1016/j.bmcl.2009.03.014
CHEMBL485195 184929 None 0 Mouse Binding pIC50 = 5.4 5.4 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 286 2 2 4 2.1 Clc1ccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)cc1 10.1016/j.bmcl.2009.03.014
136088962 61421 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 368 6 4 7 1.6 N[C@H](Cc1nc(-c2ccc(O)cc2)no1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1770176 61421 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 368 6 4 7 1.6 N[C@H](Cc1nc(-c2ccc(O)cc2)no1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
156016157 177883 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 430 8 3 4 3.2 CCCCN1CC(C(=O)O)=C(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)C1=O 10.1016/j.bmcl.2020.127105
CHEMBL4643073 177883 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 430 8 3 4 3.2 CCCCN1CC(C(=O)O)=C(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)C1=O 10.1016/j.bmcl.2020.127105
12003880 188842 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 270 2 2 4 1.6 Fc1ccccc1C1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
CHEMBL504980 188842 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 270 2 2 4 1.6 Fc1ccccc1C1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
136127017 16220 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 295 5 1 4 2.4 Cc1cccc(CCOCc2nc3ncccc3c(=O)[nH]2)c1 10.1016/j.bmcl.2010.07.108
CHEMBL1224222 16220 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 295 5 1 4 2.4 Cc1cccc(CCOCc2nc3ncccc3c(=O)[nH]2)c1 10.1016/j.bmcl.2010.07.108
136000579 61420 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 368 6 4 7 1.6 N[C@@H](Cc1nc(-c2ccc(O)cc2)no1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL1770175 61420 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 368 6 4 7 1.6 N[C@@H](Cc1nc(-c2ccc(O)cc2)no1)C(=O)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
46890271 7379 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 355 5 4 4 2.5 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(O)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1086356 7379 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 355 5 4 4 2.5 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(O)CC1 10.1016/j.bmcl.2010.04.001
12002521 184927 None 0 Mouse Binding pIC50 = 5.4 5.4 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 266 2 2 4 1.8 Cc1ccccc1C1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
CHEMBL485194 184927 None 0 Mouse Binding pIC50 = 5.4 5.4 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 266 2 2 4 1.8 Cc1ccccc1C1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
46890268 6608 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 353 5 3 3 3.8 CC1CCC(NC(=O)CCc2ccc3cc(O)ccc3c2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
CHEMBL1083174 6608 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 353 5 3 3 3.8 CC1CCC(NC(=O)CCc2ccc3cc(O)ccc3c2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
12003879 192451 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 252 2 2 4 1.5 c1ccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)cc1 10.1016/j.bmcl.2009.03.014
CHEMBL520675 192451 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 252 2 2 4 1.5 c1ccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)cc1 10.1016/j.bmcl.2009.03.014
135899109 16221 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 295 5 1 4 2.4 Cc1ccc(CCOCc2nc3ncccc3c(=O)[nH]2)cc1 10.1016/j.bmcl.2010.07.108
CHEMBL1224223 16221 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 295 5 1 4 2.4 Cc1ccc(CCOCc2nc3ncccc3c(=O)[nH]2)cc1 10.1016/j.bmcl.2010.07.108
135899153 16219 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 295 5 1 4 2.4 Cc1ccccc1CCOCc1nc2ncccc2c(=O)[nH]1 10.1016/j.bmcl.2010.07.108
CHEMBL1224221 16219 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 295 5 1 4 2.4 Cc1ccccc1CCOCc1nc2ncccc2c(=O)[nH]1 10.1016/j.bmcl.2010.07.108
135899247 16095 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 279 5 1 3 2.9 O=c1[nH]c(CCCCc2ccccc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1223823 16095 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 279 5 1 3 2.9 O=c1[nH]c(CCCCc2ccccc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
135899110 16235 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 311 6 1 5 2.1 COc1ccc(CCOCc2nc3ncccc3c(=O)[nH]2)cc1 10.1016/j.bmcl.2010.07.108
CHEMBL1224294 16235 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 311 6 1 5 2.1 COc1ccc(CCOCc2nc3ncccc3c(=O)[nH]2)cc1 10.1016/j.bmcl.2010.07.108
12003694 1144 None 0 Mouse Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 232 2 2 4 0.7 OC(=O)c1n[nH]c2c1CC(C2)c1ccnn1C 10.1016/j.bmcl.2010.06.041
5793 1144 None 0 Mouse Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 232 2 2 4 0.7 OC(=O)c1n[nH]c2c1CC(C2)c1ccnn1C 10.1016/j.bmcl.2010.06.041
CHEMBL1208986 1144 None 0 Mouse Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 232 2 2 4 0.7 OC(=O)c1n[nH]c2c1CC(C2)c1ccnn1C 10.1016/j.bmcl.2010.06.041
135812996 16180 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 311 6 1 5 2.5 Cc1ccccc1OCCCOc1nc2ncccc2c(=O)[nH]1 10.1016/j.bmcl.2010.07.108
CHEMBL1224073 16180 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 311 6 1 5 2.5 Cc1ccccc1OCCCOc1nc2ncccc2c(=O)[nH]1 10.1016/j.bmcl.2010.07.108
46890238 7102 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 384 6 3 6 2.5 Cc1c(CC(C)C(=O)NC2=C(C(=O)O)CCCC2)cnn1-c1ccc(O)cn1 10.1016/j.bmcl.2010.04.013
CHEMBL1085149 7102 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 384 6 3 6 2.5 Cc1c(CC(C)C(=O)NC2=C(C(=O)O)CCCC2)cnn1-c1ccc(O)cn1 10.1016/j.bmcl.2010.04.013
12003790 198511 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 276 2 2 2 3.0 O=C(O)c1n[nH]c2c1CC(c1ccccc1Cl)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL560406 198511 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 276 2 2 2 3.0 O=C(O)c1n[nH]c2c1CC(c1ccccc1Cl)CC2 10.1016/j.bmcl.2009.06.054
135800177 146039 None 5 Mouse Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]niacin from mouse GPR109ADisplacement of [3H]niacin from mouse GPR109A
ChEMBL 353 6 3 6 2.7 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL391813 146039 None 5 Mouse Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]niacin from mouse GPR109ADisplacement of [3H]niacin from mouse GPR109A
ChEMBL 353 6 3 6 2.7 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1ccccc1C(=O)O 10.1021/jm700942d
156016715 177780 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 415 8 3 5 4.5 CCCCn1cc(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)c(C(=O)O)n1 10.1016/j.bmcl.2020.127105
CHEMBL4641756 177780 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 415 8 3 5 4.5 CCCCn1cc(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)c(C(=O)O)n1 10.1016/j.bmcl.2020.127105
11183317 191579 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 204 2 2 4 0.7 CCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
CHEMBL519338 191579 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 204 2 2 4 0.7 CCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
135899130 16182 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 311 6 1 5 2.5 Cc1ccc(OCCCOc2nc3ncccc3c(=O)[nH]2)cc1 10.1016/j.bmcl.2010.07.108
CHEMBL1224075 16182 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 311 6 1 5 2.5 Cc1ccc(OCCCOc2nc3ncccc3c(=O)[nH]2)cc1 10.1016/j.bmcl.2010.07.108
44591586 184267 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 246 5 2 4 1.9 CCCCCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
CHEMBL482979 184267 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 246 5 2 4 1.9 CCCCCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
136127012 16120 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 321 8 1 3 4.1 O=c1[nH]c(CCCCCCCc2ccccc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1223876 16120 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 321 8 1 3 4.1 O=c1[nH]c(CCCCCCCc2ccccc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
46890240 7105 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 356 6 3 6 1.9 O=C(CCc1ccn(-c2ccc(O)cn2)n1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.013
CHEMBL1085156 7105 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 356 6 3 6 1.9 O=C(CCc1ccn(-c2ccc(O)cn2)n1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.013
46890301 7201 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 482 7 3 6 3.9 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2010.04.013
CHEMBL1085616 7201 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 482 7 3 6 3.9 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2010.04.013
11516324 184322 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 375 5 4 4 3.7 O=C(CCc1[nH]nc2c1ccc1cc(O)ccc12)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL483352 184322 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 375 5 4 4 3.7 O=C(CCc1[nH]nc2c1ccc1cc(O)ccc12)Nc1ccccc1C(=O)O 10.1021/jm900151e
15986931 192345 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 385 5 3 6 3.2 O=C(CCc1cn2c(n1)sc1cc(O)ccc12)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
CHEMBL520513 192345 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 385 5 3 6 3.2 O=C(CCc1cn2c(n1)sc1cc(O)ccc12)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
136088960 61468 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 373 6 4 8 0.7 N[C@@H](Cc1nc(-c2ccc(O)cn2)no1)C(=O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.11.116
CHEMBL1770355 61468 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 373 6 4 8 0.7 N[C@@H](Cc1nc(-c2ccc(O)cn2)no1)C(=O)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.11.116
135899178 16217 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 315 5 1 4 2.7 O=c1[nH]c(COCCc2cccc(Cl)c2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1224219 16217 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 315 5 1 4 2.7 O=c1[nH]c(COCCc2cccc(Cl)c2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
12002802 198289 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 285 2 2 5 1.4 Fc1ncccc1C1CCc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.06.054
CHEMBL558334 198289 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 285 2 2 5 1.4 Fc1ncccc1C1CCc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.06.054
117629482 2823 None 82 Human Binding pIC50 = 6.3 6.3 -3 2
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2020.127105
1588 2823 None 82 Human Binding pIC50 = 6.3 6.3 -3 2
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2020.127105
1594 2823 None 82 Human Binding pIC50 = 6.3 6.3 -3 2
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2020.127105
2835 2823 None 82 Human Binding pIC50 = 6.3 6.3 -3 2
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2020.127105
938 2823 None 82 Human Binding pIC50 = 6.3 6.3 -3 2
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2020.127105
CHEMBL573 2823 None 82 Human Binding pIC50 = 6.3 6.3 -3 2
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2020.127105
DB00627 2823 None 82 Human Binding pIC50 = 6.3 6.3 -3 2
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1016/j.bmcl.2020.127105
44591604 184929 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 286 2 2 4 2.1 Clc1ccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)cc1 10.1016/j.bmcl.2009.03.014
CHEMBL485195 184929 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 286 2 2 4 2.1 Clc1ccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)cc1 10.1016/j.bmcl.2009.03.014
11610363 89524 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 369 6 3 6 3.2 O=C(CCc1ncc(-c2ccc(O)cn2)s1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL237247 89524 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 369 6 3 6 3.2 O=C(CCc1ncc(-c2ccc(O)cn2)s1)Nc1ccccc1C(=O)O 10.1021/jm700942d
156010038 177135 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 414 8 3 4 5.1 CCCCn1cc(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
CHEMBL4632359 177135 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 414 8 3 4 5.1 CCCCn1cc(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
24811199 6603 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 434 6 3 4 4.4 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2cccnc2F)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1083139 6603 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 434 6 3 4 4.4 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2cccnc2F)CC1 10.1016/j.bmcl.2010.04.001
12002524 191891 None 0 Mouse Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 288 2 2 4 1.8 Fc1ccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)cc1F 10.1016/j.bmcl.2009.03.014
CHEMBL519811 191891 None 0 Mouse Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 288 2 2 4 1.8 Fc1ccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)cc1F 10.1016/j.bmcl.2009.03.014
44591602 188491 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 216 2 2 4 0.7 C1CC1C1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
CHEMBL501585 188491 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 216 2 2 4 0.7 C1CC1C1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
12003692 14987 None 0 Mouse Binding pIC50 = 5.3 5.3 - 0
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 219 2 2 5 0.0 O=C(O)c1n[nH]c2c1CC(n1ccnn1)C2 10.1016/j.bmcl.2010.06.041
CHEMBL1208988 14987 None 0 Mouse Binding pIC50 = 5.3 5.3 - 0
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 219 2 2 5 0.0 O=C(O)c1n[nH]c2c1CC(n1ccnn1)C2 10.1016/j.bmcl.2010.06.041
44579742 187150 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cells
ChEMBL 347 6 2 3 3.9 O=Cc1ccc2cc(CCC(=O)Nc3ccccc3C(=O)O)ccc2c1 10.1016/j.bmcl.2008.08.030
CHEMBL491003 187150 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cells
ChEMBL 347 6 2 3 3.9 O=Cc1ccc2cc(CCC(=O)Nc3ccccc3C(=O)O)ccc2c1 10.1016/j.bmcl.2008.08.030
16048770 94684 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 377 3 2 5 2.7 O=C(O)c1ccccc1NC(=O)N1CCN(c2cnc3ccccc3n2)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL252306 94684 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 377 3 2 5 2.7 O=C(O)c1ccccc1NC(=O)N1CCN(c2cnc3ccccc3n2)CC1 10.1016/j.bmcl.2007.10.055
156013148 177573 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 356 6 3 7 2.1 Cn1cc(NC(=O)CCc2nc(-c3ccc(O)cc3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
CHEMBL4639053 177573 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 356 6 3 7 2.1 Cn1cc(NC(=O)CCc2nc(-c3ccc(O)cc3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
11523335 121879 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 359 6 2 2 4.9 Cc1ccccc1-c1ccc(CCC(=O)Nc2ccccc2C(=O)O)cc1 10.1016/j.bmc.2015.02.018
CHEMBL3589787 121879 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 359 6 2 2 4.9 Cc1ccccc1-c1ccc(CCC(=O)Nc2ccccc2C(=O)O)cc1 10.1016/j.bmc.2015.02.018
137661636 159356 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 331 4 2 2 3.5 O=C(CCC#Cc1ccccc1Cl)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4099238 159356 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 331 4 2 2 3.5 O=C(CCC#Cc1ccccc1Cl)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
46890537 7040 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 454 7 2 6 3.8 O=C(CCc1nc(-c2ccc(F)cn2)no1)NC1=C(C(=O)O)CC(c2cccc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1084839 7040 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 454 7 2 6 3.8 O=C(CCc1nc(-c2ccc(F)cn2)no1)NC1=C(C(=O)O)CC(c2cccc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
16048921 155107 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 366 3 2 5 2.9 O=C(O)c1ccccc1NC(=O)N1CCN(c2nc3ccccc3o2)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL401470 155107 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 366 3 2 5 2.9 O=C(O)c1ccccc1NC(=O)N1CCN(c2nc3ccccc3o2)CC1 10.1016/j.bmcl.2007.10.055
122181141 121895 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 377 6 4 4 4.0 O=C(CCc1ccc(-c2ccc(O)cc2O)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
CHEMBL3589835 121895 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 377 6 4 4 4.0 O=C(CCc1ccc(-c2ccc(O)cc2O)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
24741310 89656 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 352 6 3 6 2.2 O=C(CCc1ccn(-c2ccc(O)cn2)n1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
CHEMBL237543 89656 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 352 6 3 6 2.2 O=C(CCc1ccn(-c2ccc(O)cn2)n1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.013
24741310 89656 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 352 6 3 6 2.2 O=C(CCc1ccn(-c2ccc(O)cn2)n1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL237543 89656 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 352 6 3 6 2.2 O=C(CCc1ccn(-c2ccc(O)cn2)n1)Nc1ccccc1C(=O)O 10.1021/jm700942d
137637662 156332 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 383 6 3 3 4.2 O=C(CCc1ccc(-c2ccc(O)cc2F)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4064786 156332 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 383 6 3 3 4.2 O=C(CCc1ccc(-c2ccc(O)cc2F)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
135899244 16118 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 293 6 1 3 3.3 O=c1[nH]c(CCCCCc2ccccc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1223874 16118 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 293 6 1 3 3.3 O=c1[nH]c(CCCCCc2ccccc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
46890300 7417 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 482 7 3 6 3.9 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CCC(c2cccc(F)c2F)C1 10.1016/j.bmcl.2010.04.013
CHEMBL1086541 7417 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 482 7 3 6 3.9 CC(Cc1ccn(-c2ccc(O)cn2)n1)C(=O)NC1=C(C(=O)O)CCC(c2cccc(F)c2F)C1 10.1016/j.bmcl.2010.04.013
42625218 184285 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 398 5 3 5 3.8 O=C(CCc1noc2c1ccc1c(F)c(O)ccc12)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
CHEMBL483140 184285 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 398 5 3 5 3.8 O=C(CCc1noc2c1ccc1c(F)c(O)ccc12)NC1=C(C(=O)O)CCCC1 10.1021/jm900151e
46890580 7019 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 504 7 2 6 4.3 C[C@H]1CC(NC(=O)CCc2nc(-c3ccc(F)cn3)no2)=C(C(=O)O)C[C@H]1c1cc(F)cc(F)c1F 10.1016/j.bmcl.2010.04.001
CHEMBL1084799 7019 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 504 7 2 6 4.3 C[C@H]1CC(NC(=O)CCc2nc(-c3ccc(F)cn3)no2)=C(C(=O)O)C[C@H]1c1cc(F)cc(F)c1F 10.1016/j.bmcl.2010.04.001
46890270 7377 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 395 8 3 3 4.9 CCCCC1CCC(NC(=O)CCc2ccc3cc(O)ccc3c2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
CHEMBL1086354 7377 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 395 8 3 3 4.9 CCCCC1CCC(NC(=O)CCc2ccc3cc(O)ccc3c2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
135800194 89525 None 0 Human Binding pIC50 = 8.2 8.2 - 1
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 354 6 3 7 2.1 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
CHEMBL237248 89525 None 0 Human Binding pIC50 = 8.2 8.2 - 1
Displacement of [3H]nicotinic acid from human GPR109A receptorDisplacement of [3H]nicotinic acid from human GPR109A receptor
ChEMBL 354 6 3 7 2.1 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.11.116
11736428 189172 None 0 Mouse Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 232 4 2 4 1.5 CCCCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
CHEMBL509541 189172 None 0 Mouse Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 232 4 2 4 1.5 CCCCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
12003791 194954 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 261 2 2 3 1.9 O=C(O)c1n[nH]c2c1CC(c1cccnc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL1237147 194954 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 261 2 2 3 1.9 O=C(O)c1n[nH]c2c1CC(c1cccnc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL539398 194954 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 261 2 2 3 1.9 O=C(O)c1n[nH]c2c1CC(c1cccnc1F)CC2 10.1016/j.bmcl.2009.06.054
135899154 16216 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 315 5 1 4 2.7 O=c1[nH]c(COCCc2ccccc2Cl)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1224218 16216 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 315 5 1 4 2.7 O=c1[nH]c(COCCc2ccccc2Cl)nc2ncccc12 10.1016/j.bmcl.2010.07.108
12002524 191891 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 288 2 2 4 1.8 Fc1ccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)cc1F 10.1016/j.bmcl.2009.03.014
CHEMBL519811 191891 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 288 2 2 4 1.8 Fc1ccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)cc1F 10.1016/j.bmcl.2009.03.014
136375437 178186 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 432 8 3 7 3.6 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1cn(Cc2ccccc2)cc1C(=O)O 10.1016/j.bmcl.2020.127105
CHEMBL4647670 178186 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 432 8 3 7 3.6 O=C(CCc1nc(-c2ccc(O)cc2)no1)Nc1cn(Cc2ccccc2)cc1C(=O)O 10.1016/j.bmcl.2020.127105
135899325 16200 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 299 5 1 4 2.2 O=c1[nH]c(COCCc2ccc(F)cc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1224147 16200 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 299 5 1 4 2.2 O=c1[nH]c(COCCc2ccc(F)cc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
135899324 16198 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 327 7 1 6 2.2 COc1ccc(OCCCOc2nc3ncccc3c(=O)[nH]2)cc1 10.1016/j.bmcl.2010.07.108
CHEMBL1224145 16198 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 327 7 1 6 2.2 COc1ccc(OCCCOc2nc3ncccc3c(=O)[nH]2)cc1 10.1016/j.bmcl.2010.07.108
135899178 16217 None 0 Rat Binding pIC50 = 6.2 6.2 - 0
Displacement of radioligand from rat GPR109ADisplacement of radioligand from rat GPR109A
ChEMBL 315 5 1 4 2.7 O=c1[nH]c(COCCc2cccc(Cl)c2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1224219 16217 None 0 Rat Binding pIC50 = 6.2 6.2 - 0
Displacement of radioligand from rat GPR109ADisplacement of radioligand from rat GPR109A
ChEMBL 315 5 1 4 2.7 O=c1[nH]c(COCCc2cccc(Cl)c2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
156010038 177135 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Agonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysisAgonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysis
ChEMBL 414 8 3 4 5.1 CCCCn1cc(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
CHEMBL4632359 177135 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Agonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysisAgonist activity at GPR109A receptor in human adipocytes assessed as inhibition of lipolysis
ChEMBL 414 8 3 4 5.1 CCCCn1cc(NC(=O)CCc2ccc3c(Cl)c(O)ccc3c2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
16048768 94503 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 405 3 2 5 3.5 C[C@H]1CN(C(=O)Nc2ccccc2C(=O)O)[C@H](C)CN1c1cnc2ccccc2n1 10.1016/j.bmcl.2007.10.055
CHEMBL251222 94503 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 405 3 2 5 3.5 C[C@H]1CN(C(=O)Nc2ccccc2C(=O)O)[C@H](C)CN1c1cnc2ccccc2n1 10.1016/j.bmcl.2007.10.055
137659759 159360 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 314 4 3 4 1.9 O=C(CCC#Cc1ccc(O)cn1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4099278 159360 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 314 4 3 4 1.9 O=C(CCC#Cc1ccc(O)cn1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
12003787 198298 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 296 2 2 2 2.8 O=C(O)c1n[nH]c2c1CC(c1cc(F)cc(F)c1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL558463 198298 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 296 2 2 2 2.8 O=C(O)c1n[nH]c2c1CC(c1cc(F)cc(F)c1F)CC2 10.1016/j.bmcl.2009.06.054
137639493 157003 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 315 4 2 2 3.0 O=C(CCC#Cc1ccccc1F)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4072283 157003 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 315 4 2 2 3.0 O=C(CCC#Cc1ccccc1F)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
135899321 16122 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 281 5 1 4 2.1 O=c1[nH]c(COCCc2ccccc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1223878 16122 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 281 5 1 4 2.1 O=c1[nH]c(COCCc2ccccc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
16048843 154480 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 392 3 3 6 2.3 Nc1ccc2nc(N3CCN(C(=O)Nc4ccccc4C(=O)O)CC3)cnc2c1 10.1016/j.bmcl.2007.10.055
CHEMBL398762 154480 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 392 3 3 6 2.3 Nc1ccc2nc(N3CCN(C(=O)Nc4ccccc4C(=O)O)CC3)cnc2c1 10.1016/j.bmcl.2007.10.055
11424509 188395 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 218 3 2 4 1.1 CCCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
CHEMBL500239 188395 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 218 3 2 4 1.1 CCCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
46890237 7101 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 370 6 3 6 2.2 Cc1c(CCC(=O)NC2=C(C(=O)O)CCCC2)cnn1-c1ccc(O)cn1 10.1016/j.bmcl.2010.04.013
CHEMBL1085148 7101 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 370 6 3 6 2.2 Cc1c(CCC(=O)NC2=C(C(=O)O)CCCC2)cnn1-c1ccc(O)cn1 10.1016/j.bmcl.2010.04.013
135966934 6844 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 452 7 3 7 3.3 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CC(c2cccc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1084030 6844 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 452 7 3 7 3.3 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CC(c2cccc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
46890298 7164 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 433 6 3 3 5.0 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2cccc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1085414 7164 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 433 6 3 3 5.0 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2cccc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
12002518 188987 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 288 2 2 4 1.8 Fc1cc(F)cc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
CHEMBL507182 188987 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 288 2 2 4 1.8 Fc1cc(F)cc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
12002518 188987 None 0 Mouse Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 288 2 2 4 1.8 Fc1cc(F)cc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
CHEMBL507182 188987 None 0 Mouse Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 288 2 2 4 1.8 Fc1cc(F)cc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
12002618 192100 None 0 Mouse Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 306 2 2 4 1.9 Fc1cc(F)c(F)c(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
CHEMBL520137 192100 None 0 Mouse Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 306 2 2 4 1.9 Fc1cc(F)c(F)c(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
12002618 192100 None 0 Mouse Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 306 2 2 4 1.9 Fc1cc(F)c(F)c(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2010.06.041
CHEMBL520137 192100 None 0 Mouse Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 306 2 2 4 1.9 Fc1cc(F)c(F)c(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2010.06.041
156020512 178209 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 403 9 3 8 2.3 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1cn(CCCF)cc1C(=O)O 10.1016/j.bmcl.2020.127105
CHEMBL4647933 178209 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 403 9 3 8 2.3 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1cn(CCCF)cc1C(=O)O 10.1016/j.bmcl.2020.127105
11624691 7229 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 361 6 3 3 4.3 O=C(CCc1ccc(-c2ccc(O)cc2)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
CHEMBL1085711 7229 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 361 6 3 3 4.3 O=C(CCc1ccc(-c2ccc(O)cc2)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
137641317 157103 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 383 6 2 2 5.0 O=C(CCc1ccc(-c2ccccc2Cl)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4073374 157103 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 383 6 2 2 5.0 O=C(CCc1ccc(-c2ccccc2Cl)cc1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
137648386 157864 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 347 4 3 3 3.2 O=C(CCC#Cc1ccc(O)cc1Cl)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4082765 157864 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 347 4 3 3 3.2 O=C(CCC#Cc1ccc(O)cc1Cl)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
12002616 184287 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 288 2 2 4 1.8 Fc1ccc(F)c(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
CHEMBL483142 184287 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 288 2 2 4 1.8 Fc1ccc(F)c(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
16048995 94708 None 0 Human Binding pIC50 = 4.1 4.1 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 375 3 2 3 3.9 O=C(O)c1ccccc1NC(=O)N1CCN(c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL252505 94708 None 0 Human Binding pIC50 = 4.1 4.1 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 375 3 2 3 3.9 O=C(O)c1ccccc1NC(=O)N1CCN(c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2007.10.055
11646494 121875 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 375 7 2 3 4.6 COc1cccc(-c2ccc(CCC(=O)Nc3ccccc3C(=O)O)cc2)c1 10.1016/j.bmc.2015.02.018
CHEMBL3589783 121875 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 375 7 2 3 4.6 COc1cccc(-c2ccc(CCC(=O)Nc3ccccc3C(=O)O)cc2)c1 10.1016/j.bmc.2015.02.018
11516424 7317 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 379 6 3 5 3.4 Cc1c(CC(C)C(=O)Nc2ccccc2C(=O)O)cnn1-c1ccc(O)cc1 10.1016/j.bmcl.2010.04.013
CHEMBL1086104 7317 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 379 6 3 5 3.4 Cc1c(CC(C)C(=O)Nc2ccccc2C(=O)O)cnn1-c1ccc(O)cc1 10.1016/j.bmcl.2010.04.013
12002521 184927 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 266 2 2 4 1.8 Cc1ccccc1C1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
CHEMBL485194 184927 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 266 2 2 4 1.8 Cc1ccccc1C1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
135401975 94801 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 393 3 3 6 2.4 O=C(O)c1ccccc1NC(=O)N1CCN(c2cnc3ccc(O)cc3n2)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL253128 94801 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 393 3 3 6 2.4 O=C(O)c1ccccc1NC(=O)N1CCN(c2cnc3ccc(O)cc3n2)CC1 10.1016/j.bmcl.2007.10.055
11647028 88716 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 401 6 3 4 5.0 O=C(CCc1ccc(-c2ccc(O)cc2Cl)s1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL235954 88716 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 401 6 3 4 5.0 O=C(CCc1ccc(-c2ccc(O)cc2Cl)s1)Nc1ccccc1C(=O)O 10.1021/jm700942d
11501698 192679 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 376 5 3 6 2.9 O=C(CCc1nnn2c1ccc1cc(O)ccc12)Nc1ccccc1C(=O)O 10.1021/jm900151e
CHEMBL521326 192679 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [3H]niacin from human GPR109A expressed in CHO cellsDisplacement of [3H]niacin from human GPR109A expressed in CHO cells
ChEMBL 376 5 3 6 2.9 O=C(CCc1nnn2c1ccc1cc(O)ccc12)Nc1ccccc1C(=O)O 10.1021/jm900151e
136086829 7340 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 466 7 3 7 3.6 C[C@H]1CC(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)=C(C(=O)O)C[C@H]1c1cccc(F)c1 10.1016/j.bmcl.2010.04.001
CHEMBL1086225 7340 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 466 7 3 7 3.6 C[C@H]1CC(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)=C(C(=O)O)C[C@H]1c1cccc(F)c1 10.1016/j.bmcl.2010.04.001
46890269 7376 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 381 7 3 3 4.5 CCCC1CCC(NC(=O)CCc2ccc3cc(O)ccc3c2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
CHEMBL1086353 7376 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 381 7 3 3 4.5 CCCC1CCC(NC(=O)CCc2ccc3cc(O)ccc3c2)=C(C(=O)O)C1 10.1016/j.bmcl.2010.04.001
15986755 184224 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 339 5 3 3 3.5 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.001
CHEMBL482698 184224 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 339 5 3 3 3.5 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CCCC1 10.1016/j.bmcl.2010.04.001
46890299 7217 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 433 6 3 3 5.0 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2ccc(F)cc2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1085655 7217 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 433 6 3 3 5.0 O=C(CCc1ccc2cc(O)ccc2c1)NC1=C(C(=O)O)CC(c2ccc(F)cc2)CC1 10.1016/j.bmcl.2010.04.001
11736428 189172 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 232 4 2 4 1.5 CCCCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
CHEMBL509541 189172 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 232 4 2 4 1.5 CCCCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
12002618 192100 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 306 2 2 4 1.9 Fc1cc(F)c(F)c(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
CHEMBL520137 192100 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 306 2 2 4 1.9 Fc1cc(F)c(F)c(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
12002618 192100 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 306 2 2 4 1.9 Fc1cc(F)c(F)c(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2010.06.041
CHEMBL520137 192100 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 306 2 2 4 1.9 Fc1cc(F)c(F)c(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2010.06.041
12002517 191991 None 0 Mouse Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 270 2 2 4 1.6 Fc1cccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
CHEMBL519966 191991 None 0 Mouse Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 270 2 2 4 1.6 Fc1cccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
12003597 14984 None 0 Mouse Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 234 2 2 3 2.1 O=C(O)c1n[nH]c2c1CC(c1ccsc1)C2 10.1016/j.bmcl.2010.06.041
CHEMBL1208925 14984 None 0 Mouse Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 234 2 2 3 2.1 O=C(O)c1n[nH]c2c1CC(c1ccsc1)C2 10.1016/j.bmcl.2010.06.041
11710202 121874 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 359 6 2 2 4.9 Cc1cccc(-c2ccc(CCC(=O)Nc3ccccc3C(=O)O)cc2)c1 10.1016/j.bmc.2015.02.018
CHEMBL3589782 121874 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 359 6 2 2 4.9 Cc1cccc(-c2ccc(CCC(=O)Nc3ccccc3C(=O)O)cc2)c1 10.1016/j.bmc.2015.02.018
16048840 94097 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 391 3 2 5 3.1 O=C(O)c1ccccc1NC(=O)N1CCCN(c2cnc3ccccc3n2)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL248851 94097 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 391 3 2 5 3.1 O=C(O)c1ccccc1NC(=O)N1CCCN(c2cnc3ccccc3n2)CC1 10.1016/j.bmcl.2007.10.055
44591601 184417 None 0 Mouse Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 260 6 2 4 2.3 CCCCCCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
CHEMBL484172 184417 None 0 Mouse Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 260 6 2 4 2.3 CCCCCCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
122181103 121880 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 363 6 2 2 4.8 O=C(CCc1ccc(-c2ccccc2F)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
CHEMBL3589788 121880 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 363 6 2 2 4.8 O=C(CCc1ccc(-c2ccccc2F)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
135899300 16121 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 295 6 1 4 2.7 O=c1[nH]c(OCCCCc2ccccc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
CHEMBL1223877 16121 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 295 6 1 4 2.7 O=c1[nH]c(OCCCCc2ccccc2)nc2ncccc12 10.1016/j.bmcl.2010.07.108
46890538 7041 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 469 7 3 7 2.7 NC(Cc1nc(-c2ccc(F)cn2)no1)C(=O)NC1=C(C(=O)O)CC(c2cccc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1084840 7041 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 469 7 3 7 2.7 NC(Cc1nc(-c2ccc(F)cn2)no1)C(=O)NC1=C(C(=O)O)CC(c2cccc(F)c2)CC1 10.1016/j.bmcl.2010.04.001
12003791 194954 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serum
ChEMBL 261 2 2 3 1.9 O=C(O)c1n[nH]c2c1CC(c1cccnc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL1237147 194954 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serum
ChEMBL 261 2 2 3 1.9 O=C(O)c1n[nH]c2c1CC(c1cccnc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL539398 194954 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in presence of 5% human serum
ChEMBL 261 2 2 3 1.9 O=C(O)c1n[nH]c2c1CC(c1cccnc1F)CC2 10.1016/j.bmcl.2009.06.054
12002616 184287 None 0 Mouse Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 288 2 2 4 1.8 Fc1ccc(F)c(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
CHEMBL483142 184287 None 0 Mouse Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 288 2 2 4 1.8 Fc1ccc(F)c(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1 10.1016/j.bmcl.2009.03.014
11581300 121882 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 361 6 3 3 4.3 O=C(CCc1ccc(-c2ccccc2O)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
CHEMBL3589790 121882 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 361 6 3 3 4.3 O=C(CCc1ccc(-c2ccccc2O)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
135899150 16181 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 311 6 1 5 2.5 Cc1cccc(OCCCOc2nc3ncccc3c(=O)[nH]2)c1 10.1016/j.bmcl.2010.07.108
CHEMBL1224074 16181 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 311 6 1 5 2.5 Cc1cccc(OCCCOc2nc3ncccc3c(=O)[nH]2)c1 10.1016/j.bmcl.2010.07.108
11501164 187284 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cells
ChEMBL 349 6 2 3 4.1 COc1ccc2cc(CCC(=O)Nc3ccccc3C(=O)O)ccc2c1 10.1016/j.bmcl.2008.08.030
CHEMBL492220 187284 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cellsDisplacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO-K1 cells
ChEMBL 349 6 2 3 4.1 COc1ccc2cc(CCC(=O)Nc3ccccc3C(=O)O)ccc2c1 10.1016/j.bmcl.2008.08.030
135401974 154813 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 393 3 3 6 2.4 O=C(O)c1ccccc1NC(=O)N1CCN(c2cnc3cccc(O)c3n2)CC1 10.1016/j.bmcl.2007.10.055
CHEMBL399859 154813 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 393 3 3 6 2.4 O=C(O)c1ccccc1NC(=O)N1CCN(c2cnc3cccc(O)c3n2)CC1 10.1016/j.bmcl.2007.10.055
44591601 184417 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 260 6 2 4 2.3 CCCCCCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
CHEMBL484172 184417 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]nicotinic acid from human GPR109a receptorDisplacement of [3H]nicotinic acid from human GPR109a receptor
ChEMBL 260 6 2 4 2.3 CCCCCCC1Cc2[nH]nc(-c3nnn[nH]3)c2C1 10.1016/j.bmcl.2009.03.014
137653026 158799 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 329 3 2 2 3.3 O=C(/C=C/C#Cc1ccccc1Cl)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
CHEMBL4093294 158799 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting methodDisplacement of [5,6-3H]-nicotinic acid from recombinant human HCA2 receptor expressed in Flp-IN HEK cell membranes after 2 hrs by microbeta counting method
ChEMBL 329 3 2 2 3.3 O=C(/C=C/C#Cc1ccccc1Cl)NC1=C(C(=O)O)CCCC1 10.1016/j.bmc.2017.06.028
46890275 6532 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 412 8 3 6 3.2 CCCC1CCC(C(=O)O)=C(NC(=O)C(C)Cc2ccn(-c3ccc(O)cn3)n2)C1 10.1016/j.bmcl.2010.04.013
CHEMBL1082823 6532 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 412 8 3 6 3.2 CCCC1CCC(C(=O)O)=C(NC(=O)C(C)Cc2ccn(-c3ccc(O)cn3)n2)C1 10.1016/j.bmcl.2010.04.013
11617480 88715 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 362 6 3 4 3.7 O=C(CCc1ccc(-c2ccc(O)cn2)cc1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL235952 88715 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 362 6 3 4 3.7 O=C(CCc1ccc(-c2ccc(O)cn2)cc1)Nc1ccccc1C(=O)O 10.1021/jm700942d
46890577 6674 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 490 7 2 6 4.0 O=C(CCc1nc(-c2ccc(F)cn2)no1)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2F)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1083442 6674 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 490 7 2 6 4.0 O=C(CCc1nc(-c2ccc(F)cn2)no1)NC1=C(C(=O)O)CC(c2cc(F)cc(F)c2F)CC1 10.1016/j.bmcl.2010.04.001
136086824 6845 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 453 7 3 8 2.7 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CC(c2ccc(F)nc2)CC1 10.1016/j.bmcl.2010.04.001
CHEMBL1084031 6845 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cellsDisplacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
ChEMBL 453 7 3 8 2.7 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CC(c2ccc(F)nc2)CC1 10.1016/j.bmcl.2010.04.001
12003788 196265 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 278 2 2 2 2.7 O=C(O)c1n[nH]c2c1CC(c1cc(F)ccc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL1237148 196265 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 278 2 2 2 2.7 O=C(O)c1n[nH]c2c1CC(c1cc(F)ccc1F)CC2 10.1016/j.bmcl.2009.06.054
CHEMBL542000 196265 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serumDisplacement of [3H]niacin from human niacin receptor expressed in CKO-K1 cells in absence of 5% human serum
ChEMBL 278 2 2 2 2.7 O=C(O)c1n[nH]c2c1CC(c1cc(F)ccc1F)CC2 10.1016/j.bmcl.2009.06.054
12003597 14984 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 234 2 2 3 2.1 O=C(O)c1n[nH]c2c1CC(c1ccsc1)C2 10.1016/j.bmcl.2010.06.041
CHEMBL1208925 14984 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]nicotinic acid from human GPR10a receptorDisplacement of [3H]nicotinic acid from human GPR10a receptor
ChEMBL 234 2 2 3 2.1 O=C(O)c1n[nH]c2c1CC(c1ccsc1)C2 10.1016/j.bmcl.2010.06.041
12002525 192452 None 0 Mouse Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 288 2 2 4 1.8 Fc1cccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1F 10.1016/j.bmcl.2009.03.014
CHEMBL520676 192452 None 0 Mouse Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 288 2 2 4 1.8 Fc1cccc(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)c1F 10.1016/j.bmcl.2009.03.014
11299550 192116 None 0 Mouse Binding pIC50 = 5.1 5.1 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 244 2 2 4 1.5 C1CCC(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)C1 10.1016/j.bmcl.2009.03.014
CHEMBL520159 192116 None 0 Mouse Binding pIC50 = 5.1 5.1 - 0
Displacement of [3H]nicotinic acid from mouse GPR109a receptorDisplacement of [3H]nicotinic acid from mouse GPR109a receptor
ChEMBL 244 2 2 4 1.5 C1CCC(C2Cc3[nH]nc(-c4nnn[nH]4)c3C2)C1 10.1016/j.bmcl.2009.03.014
122181107 121885 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 379 6 3 3 4.5 O=C(CCc1ccc(-c2ccc(O)c(F)c2)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
CHEMBL3589793 121885 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 379 6 3 3 4.5 O=C(CCc1ccc(-c2ccc(O)c(F)c2)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
46890199 7160 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 380 6 3 6 2.8 Cc1c(CC(C)C(=O)Nc2ccccc2C(=O)O)cnn1-c1ccc(O)cn1 10.1016/j.bmcl.2010.04.013
CHEMBL1085401 7160 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]niacin from GRP109A receptorDisplacement of [3H]niacin from GRP109A receptor
ChEMBL 380 6 3 6 2.8 Cc1c(CC(C)C(=O)Nc2ccccc2C(=O)O)cnn1-c1ccc(O)cn1 10.1016/j.bmcl.2010.04.013
135899280 16141 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 308 5 2 4 1.6 O=C(CCc1ccccc1)NCc1nc2ncccc2c(=O)[nH]1 10.1016/j.bmcl.2010.07.108
CHEMBL1223958 16141 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of radioligand from human GPR109ADisplacement of radioligand from human GPR109A
ChEMBL 308 5 2 4 1.6 O=C(CCc1ccccc1)NCc1nc2ncccc2c(=O)[nH]1 10.1016/j.bmcl.2010.07.108
11625092 6686 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 379 6 2 2 5.3 O=C(CCc1ccc(-c2ccccc2Cl)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
CHEMBL1083473 6686 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 379 6 2 2 5.3 O=C(CCc1ccc(-c2ccccc2Cl)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
11617151 88673 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 345 6 2 2 4.6 O=C(CCc1ccc(-c2ccccc2)cc1)Nc1ccccc1C(=O)O 10.1021/jm700942d
CHEMBL235741 88673 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]niacin from human GPR109ADisplacement of [3H]niacin from human GPR109A
ChEMBL 345 6 2 2 4.6 O=C(CCc1ccc(-c2ccccc2)cc1)Nc1ccccc1C(=O)O 10.1021/jm700942d
11631886 121878 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 361 6 3 3 4.3 O=C(CCc1ccc(-c2cccc(O)c2)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
CHEMBL3589786 121878 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysisDisplacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
ChEMBL 361 6 3 3 4.3 O=C(CCc1ccc(-c2cccc(O)c2)cc1)Nc1ccccc1C(=O)O 10.1016/j.bmc.2015.02.018
136375465 177238 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 357 6 3 8 1.4 Cn1cc(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
CHEMBL4633857 177238 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysisDisplacement of [3H]nicotinic acid from GRP109A receptor (unknown origin) expressed in 293-EBNA cell membranes by liquid scintillation analysis
ChEMBL 357 6 3 8 1.4 Cn1cc(NC(=O)CCc2nc(-c3ccc(O)cn3)no2)c(C(=O)O)c1 10.1016/j.bmcl.2020.127105
49862073 14979 None 1 Mouse Binding pIC50 = 6 6.0 - 0
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 194 2 2 2 1.5 CC(C)C1Cc2[nH]nc(C(=O)O)c2C1 10.1016/j.bmcl.2010.06.041
CHEMBL1208920 14979 None 1 Mouse Binding pIC50 = 6 6.0 - 0
Displacement of [3H]nicotinic acid from mouse GPR10a receptorDisplacement of [3H]nicotinic acid from mouse GPR10a receptor
ChEMBL 194 2 2 2 1.5 CC(C)C1Cc2[nH]nc(C(=O)O)c2C1 10.1016/j.bmcl.2010.06.041
135887290 6989 None 0 Human Binding pKi = 8.9 8.9 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 430 6 3 7 2.6 O=C(O)C1=C(NC(=O)C(F)(F)C(F)(F)c2nc(-c3ccc(O)cn3)no2)CCCC1 10.1021/jm100022r
CHEMBL1084657 6989 None 0 Human Binding pKi = 8.9 8.9 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 430 6 3 7 2.6 O=C(O)C1=C(NC(=O)C(F)(F)C(F)(F)c2nc(-c3ccc(O)cn3)no2)CCCC1 10.1021/jm100022r
6436431 61721 None 3 Human Binding pKi = 6 6.0 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 158 4 1 3 0.6 CCCOC(=O)/C=C/C(=O)O 10.1016/j.bmcl.2010.11.091
CHEMBL1771638 61721 None 3 Human Binding pKi = 6 6.0 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 158 4 1 3 0.6 CCCOC(=O)/C=C/C(=O)O 10.1016/j.bmcl.2010.11.091
54580649 61767 None 0 Human Binding pKi = 5 5.0 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 220 5 1 3 1.4 O=C(O)/C=C/C(=O)OCCc1ccccc1 10.1016/j.bmcl.2010.11.091
CHEMBL1771739 61767 None 0 Human Binding pKi = 5 5.0 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 220 5 1 3 1.4 O=C(O)/C=C/C(=O)OCCc1ccccc1 10.1016/j.bmcl.2010.11.091
117629482 2823 None 82 Human Binding pKi = 7.0 7.0 -3 2
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm100022r
1588 2823 None 82 Human Binding pKi = 7.0 7.0 -3 2
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm100022r
1594 2823 None 82 Human Binding pKi = 7.0 7.0 -3 2
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm100022r
2835 2823 None 82 Human Binding pKi = 7.0 7.0 -3 2
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm100022r
938 2823 None 82 Human Binding pKi = 7.0 7.0 -3 2
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm100022r
CHEMBL573 2823 None 82 Human Binding pKi = 7.0 7.0 -3 2
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm100022r
DB00627 2823 None 82 Human Binding pKi = 7.0 7.0 -3 2
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm100022r
135887288 7618 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 398 6 3 7 2.6 O=C(O)C1=C(NC(=O)C2(Cc3nc(-c4ccc(O)cn4)no3)CCC2)CCCC1 10.1021/jm100022r
CHEMBL1088074 7618 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 398 6 3 7 2.6 O=C(O)C1=C(NC(=O)C2(Cc3nc(-c4ccc(O)cn4)no3)CCC2)CCCC1 10.1021/jm100022r
135887285 7440 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 384 6 3 7 2.2 O=C(O)C1=C(NC(=O)C2(Cc3nc(-c4ccc(O)cn4)no3)CC2)CCCC1 10.1021/jm100022r
CHEMBL1086658 7440 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 384 6 3 7 2.2 O=C(O)C1=C(NC(=O)C2(Cc3nc(-c4ccc(O)cn4)no3)CC2)CCCC1 10.1021/jm100022r
135416391 6922 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 372 6 3 7 2.4 CC(CC(=O)NC1=C(C(=O)O)CCCC1)c1nc(-c2ccc(O)cn2)no1 10.1021/jm100022r
CHEMBL1084393 6922 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 372 6 3 7 2.4 CC(CC(=O)NC1=C(C(=O)O)CCCC1)c1nc(-c2ccc(O)cn2)no1 10.1021/jm100022r
135800194 89525 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 354 6 3 7 2.1 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1ccccc1C(=O)O 10.1021/jm100022r
CHEMBL237248 89525 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 354 6 3 7 2.1 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1ccccc1C(=O)O 10.1021/jm100022r
11041813 93804 None 21 Rat Binding pKi = 5.9 5.9 - 1
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 202 3 2 2 1.7 O=C(O)c1cc(Cc2ccccc2)n[nH]1 10.1021/jm030888c
CHEMBL247317 93804 None 21 Rat Binding pKi = 5.9 5.9 - 1
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 202 3 2 2 1.7 O=C(O)c1cc(Cc2ccccc2)n[nH]1 10.1021/jm030888c
135887289 6923 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 386 6 3 7 2.5 CC(C)(CC(=O)NC1=C(C(=O)O)CCCC1)c1nc(-c2ccc(O)cn2)no1 10.1021/jm100022r
CHEMBL1084394 6923 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 386 6 3 7 2.5 CC(C)(CC(=O)NC1=C(C(=O)O)CCCC1)c1nc(-c2ccc(O)cn2)no1 10.1021/jm100022r
5787 3005 None 68 Human Binding pKi = 4.9 4.9 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 164 2 2 2 1.5 OC(=O)/C=C/c1ccc(cc1)O 10.1016/j.bmcl.2010.11.091
637542 3005 None 68 Human Binding pKi = 4.9 4.9 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 164 2 2 2 1.5 OC(=O)/C=C/c1ccc(cc1)O 10.1016/j.bmcl.2010.11.091
CHEMBL66879 3005 None 68 Human Binding pKi = 4.9 4.9 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 164 2 2 2 1.5 OC(=O)/C=C/c1ccc(cc1)O 10.1016/j.bmcl.2010.11.091
DB04066 3005 None 68 Human Binding pKi = 4.9 4.9 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 164 2 2 2 1.5 OC(=O)/C=C/c1ccc(cc1)O 10.1016/j.bmcl.2010.11.091
643403 101647 None 49 Human Binding pKi = 4.9 4.9 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 138 2 1 2 1.4 O=C(O)/C=C/c1ccoc1 10.1016/j.bmcl.2010.11.091
CHEMBL298683 101647 None 49 Human Binding pKi = 4.9 4.9 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 138 2 1 2 1.4 O=C(O)/C=C/c1ccoc1 10.1016/j.bmcl.2010.11.091
676464 89910 None 48 Rat Binding pKi = 6.8 6.8 - 1
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 154 3 2 2 1.1 CCCc1cc(C(=O)O)n[nH]1 10.1021/jm030888c
CHEMBL237788 89910 None 48 Rat Binding pKi = 6.8 6.8 - 1
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 154 3 2 2 1.1 CCCc1cc(C(=O)O)n[nH]1 10.1021/jm030888c
135416388 7526 None 0 Human Binding pKi = 6.8 6.8 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 358 6 3 7 1.8 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CCCC1 10.1021/jm100022r
CHEMBL1087302 7526 None 0 Human Binding pKi = 6.8 6.8 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 358 6 3 7 1.8 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CCCC1 10.1021/jm100022r
776416 18945 None 63 Human Binding pKi = 6.8 6.8 1 2
Binding affinity at GPR109aBinding affinity at GPR109a
ChEMBL 152 1 2 2 0.6 O=C(O)c1n[nH]c2c1CCC2 10.1021/jm800896z
CHEMBL128604 18945 None 63 Human Binding pKi = 6.8 6.8 1 2
Binding affinity at GPR109aBinding affinity at GPR109a
ChEMBL 152 1 2 2 0.6 O=C(O)c1n[nH]c2c1CCC2 10.1021/jm800896z
776416 18945 None 63 Rat Binding pKi = 6.8 6.8 -1 2
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 152 1 2 2 0.6 O=C(O)c1n[nH]c2c1CCC2 10.1021/jm030888c
CHEMBL128604 18945 None 63 Rat Binding pKi = 6.8 6.8 -1 2
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 152 1 2 2 0.6 O=C(O)c1n[nH]c2c1CCC2 10.1021/jm030888c
11830866 19416 None 25 Rat Binding pKi = 5.8 5.8 - 1
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 216 4 2 2 1.9 O=C(O)c1cc(CCc2ccccc2)[nH]n1 10.1021/jm030888c
CHEMBL129385 19416 None 25 Rat Binding pKi = 5.8 5.8 - 1
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 216 4 2 2 1.9 O=C(O)c1cc(CCc2ccccc2)[nH]n1 10.1021/jm030888c
5369209 2591 None 55 Human Binding pKi = 6.8 6.8 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 130 2 1 3 -0.2 COC(=O)/C=C/C(=O)O 10.1016/j.bmcl.2010.11.091
5786 2591 None 55 Human Binding pKi = 6.8 6.8 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 130 2 1 3 -0.2 COC(=O)/C=C/C(=O)O 10.1016/j.bmcl.2010.11.091
CHEMBL589586 2591 None 55 Human Binding pKi = 6.8 6.8 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 130 2 1 3 -0.2 COC(=O)/C=C/C(=O)O 10.1016/j.bmcl.2010.11.091
DB14219 2591 None 55 Human Binding pKi = 6.8 6.8 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 130 2 1 3 -0.2 COC(=O)/C=C/C(=O)O 10.1016/j.bmcl.2010.11.091
10878560 19154 None 0 Rat Binding pKi = 4.7 4.7 - 1
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 216 3 2 2 2.0 Cc1ccc(Cc2cc(C(=O)O)[nH]n2)cc1 10.1021/jm030888c
CHEMBL128949 19154 None 0 Rat Binding pKi = 4.7 4.7 - 1
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 216 3 2 2 2.0 Cc1ccc(Cc2cc(C(=O)O)[nH]n2)cc1 10.1021/jm030888c
13169286 18847 None 0 Rat Binding pKi = 4.7 4.7 - 1
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 266 11 2 2 4.2 CCCCCCCCCCCc1cc(C(=O)O)[nH]n1 10.1021/jm030888c
CHEMBL128077 18847 None 0 Rat Binding pKi = 4.7 4.7 - 1
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 266 11 2 2 4.2 CCCCCCCCCCCc1cc(C(=O)O)[nH]n1 10.1021/jm030888c
135416393 7631 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 374 6 4 8 0.8 O=C(O)C1=C(NC(=O)C(O)Cc2nc(-c3ccc(O)cn3)no2)CCCC1 10.1021/jm100022r
CHEMBL1088213 7631 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 374 6 4 8 0.8 O=C(O)C1=C(NC(=O)C(O)Cc2nc(-c3ccc(O)cn3)no2)CCCC1 10.1021/jm100022r
135416392 7439 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 372 6 3 7 2.0 CC(Cc1nc(-c2ccc(O)cn2)no1)C(=O)NC1=C(C(=O)O)CCCC1 10.1021/jm100022r
CHEMBL1086656 7439 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 372 6 3 7 2.0 CC(Cc1nc(-c2ccc(O)cn2)no1)C(=O)NC1=C(C(=O)O)CCCC1 10.1021/jm100022r
135416392 7439 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 372 6 3 7 2.0 CC(Cc1nc(-c2ccc(O)cn2)no1)C(=O)NC1=C(C(=O)O)CCCC1 10.1021/jm100022r
CHEMBL1086656 7439 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 372 6 3 7 2.0 CC(Cc1nc(-c2ccc(O)cn2)no1)C(=O)NC1=C(C(=O)O)CCCC1 10.1021/jm100022r
54582649 61770 None 0 Human Binding pKi = 5.6 5.6 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 224 4 1 3 1.5 O=C(O)/C=C/C(=O)OCc1cccc(F)c1 10.1016/j.bmcl.2010.11.091
CHEMBL1771745 61770 None 0 Human Binding pKi = 5.6 5.6 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 224 4 1 3 1.5 O=C(O)/C=C/C(=O)OCc1cccc(F)c1 10.1016/j.bmcl.2010.11.091
135887289 6923 None 0 Human Binding pKi = 4.6 4.6 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 386 6 3 7 2.5 CC(C)(CC(=O)NC1=C(C(=O)O)CCCC1)c1nc(-c2ccc(O)cn2)no1 10.1021/jm100022r
CHEMBL1084394 6923 None 0 Human Binding pKi = 4.6 4.6 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 386 6 3 7 2.5 CC(C)(CC(=O)NC1=C(C(=O)O)CCCC1)c1nc(-c2ccc(O)cn2)no1 10.1021/jm100022r
5816396 61725 None 2 Human Binding pKi = 5.6 5.6 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 200 7 1 3 1.8 CCCCCCOC(=O)/C=C/C(=O)O 10.1016/j.bmcl.2010.11.091
CHEMBL1771642 61725 None 2 Human Binding pKi = 5.6 5.6 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 200 7 1 3 1.8 CCCCCCOC(=O)/C=C/C(=O)O 10.1016/j.bmcl.2010.11.091
135416391 6922 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 372 6 3 7 2.4 CC(CC(=O)NC1=C(C(=O)O)CCCC1)c1nc(-c2ccc(O)cn2)no1 10.1021/jm100022r
CHEMBL1084393 6922 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 372 6 3 7 2.4 CC(CC(=O)NC1=C(C(=O)O)CCCC1)c1nc(-c2ccc(O)cn2)no1 10.1021/jm100022r
135416388 7526 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 358 6 3 7 1.8 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CCCC1 10.1021/jm100022r
CHEMBL1087302 7526 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 358 6 3 7 1.8 O=C(CCc1nc(-c2ccc(O)cn2)no1)NC1=C(C(=O)O)CCCC1 10.1021/jm100022r
117629482 2823 None 82 Rat Binding pKi = 7.5 7.5 3 2
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm030888c
1588 2823 None 82 Rat Binding pKi = 7.5 7.5 3 2
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm030888c
1594 2823 None 82 Rat Binding pKi = 7.5 7.5 3 2
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm030888c
2835 2823 None 82 Rat Binding pKi = 7.5 7.5 3 2
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm030888c
938 2823 None 82 Rat Binding pKi = 7.5 7.5 3 2
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm030888c
CHEMBL573 2823 None 82 Rat Binding pKi = 7.5 7.5 3 2
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm030888c
DB00627 2823 None 82 Rat Binding pKi = 7.5 7.5 3 2
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm030888c
648852 116974 None 55 Human Binding pKi = 5.5 5.5 1 2
Binding affinity at GPR109aBinding affinity at GPR109a
ChEMBL 166 1 2 2 1.0 O=C(O)c1n[nH]c2c1CCCC2 10.1021/jm800896z
CHEMBL338405 116974 None 55 Human Binding pKi = 5.5 5.5 1 2
Binding affinity at GPR109aBinding affinity at GPR109a
ChEMBL 166 1 2 2 1.0 O=C(O)c1n[nH]c2c1CCCC2 10.1021/jm800896z
6437229 61765 None 8 Human Binding pKi = 5.5 5.5 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 206 4 1 3 1.4 O=C(O)/C=C/C(=O)OCc1ccccc1 10.1016/j.bmcl.2010.11.091
CHEMBL1771737 61765 None 8 Human Binding pKi = 5.5 5.5 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 206 4 1 3 1.4 O=C(O)/C=C/C(=O)OCc1ccccc1 10.1016/j.bmcl.2010.11.091
648852 116974 None 55 Rat Binding pKi = 5.5 5.5 -1 2
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 166 1 2 2 1.0 O=C(O)c1n[nH]c2c1CCCC2 10.1021/jm030888c
CHEMBL338405 116974 None 55 Rat Binding pKi = 5.5 5.5 -1 2
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 166 1 2 2 1.0 O=C(O)c1n[nH]c2c1CCCC2 10.1021/jm030888c
135887288 7618 None 0 Human Binding pKi = 6.4 6.4 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 398 6 3 7 2.6 O=C(O)C1=C(NC(=O)C2(Cc3nc(-c4ccc(O)cn4)no3)CCC2)CCCC1 10.1021/jm100022r
CHEMBL1088074 7618 None 0 Human Binding pKi = 6.4 6.4 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 398 6 3 7 2.6 O=C(O)C1=C(NC(=O)C2(Cc3nc(-c4ccc(O)cn4)no3)CCC2)CCCC1 10.1021/jm100022r
10857469 118621 None 1 Rat Binding pKi = 5.4 5.4 - 1
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 236 3 2 2 2.4 O=C(O)c1cc(Cc2ccc(Cl)cc2)[nH]n1 10.1021/jm030888c
CHEMBL341520 118621 None 1 Rat Binding pKi = 5.4 5.4 - 1
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 236 3 2 2 2.4 O=C(O)c1cc(Cc2ccc(Cl)cc2)[nH]n1 10.1021/jm030888c
818267 118516 None 50 Rat Binding pKi = 4.4 4.4 - 1
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 202 2 2 2 2.1 Cc1ccc(-c2cc(C(=O)O)[nH]n2)cc1 10.1021/jm030888c
CHEMBL341154 118516 None 50 Rat Binding pKi = 4.4 4.4 - 1
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 202 2 2 2 2.1 Cc1ccc(-c2cc(C(=O)O)[nH]n2)cc1 10.1021/jm030888c
135416394 2560 None 43 Human Binding pKi = 8.4 8.4 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 10.1021/jm100022r
5788 2560 None 43 Human Binding pKi = 8.4 8.4 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 10.1021/jm100022r
73755154 2560 None 43 Human Binding pKi = 8.4 8.4 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 10.1021/jm100022r
CHEMBL1086657 2560 None 43 Human Binding pKi = 8.4 8.4 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 10.1021/jm100022r
135416392 7439 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 372 6 3 7 2.0 CC(Cc1nc(-c2ccc(O)cn2)no1)C(=O)NC1=C(C(=O)O)CCCC1 10.1021/jm100022r
CHEMBL1086656 7439 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 372 6 3 7 2.0 CC(Cc1nc(-c2ccc(O)cn2)no1)C(=O)NC1=C(C(=O)O)CCCC1 10.1021/jm100022r
135800194 89525 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 354 6 3 7 2.1 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1ccccc1C(=O)O 10.1021/jm100022r
CHEMBL237248 89525 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 354 6 3 7 2.1 O=C(CCc1nc(-c2ccc(O)cn2)no1)Nc1ccccc1C(=O)O 10.1021/jm100022r
5358902 61720 None 53 Human Binding pKi = 6.4 6.4 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 144 3 1 3 0.2 CCOC(=O)/C=C/C(=O)O 10.1016/j.bmcl.2010.11.091
CHEMBL1771637 61720 None 53 Human Binding pKi = 6.4 6.4 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 144 3 1 3 0.2 CCOC(=O)/C=C/C(=O)O 10.1016/j.bmcl.2010.11.091
6057891 61722 None 31 Human Binding pKi = 5.4 5.4 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 158 3 1 3 0.6 CC(C)OC(=O)/C=C/C(=O)O 10.1016/j.bmcl.2010.11.091
CHEMBL1771639 61722 None 31 Human Binding pKi = 5.4 5.4 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 158 3 1 3 0.6 CC(C)OC(=O)/C=C/C(=O)O 10.1016/j.bmcl.2010.11.091
3203 939 None 65 Human Binding pKi = 5.3 5.3 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 148 2 1 1 1.8 OC(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2010.11.091
444539 939 None 65 Human Binding pKi = 5.3 5.3 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 148 2 1 1 1.8 OC(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2010.11.091
CHEMBL27246 939 None 65 Human Binding pKi = 5.3 5.3 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 148 2 1 1 1.8 OC(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2010.11.091
117629482 2823 None 82 Human Binding pKi = 7.3 7.3 -3 2
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm800258p
1588 2823 None 82 Human Binding pKi = 7.3 7.3 -3 2
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm800258p
1594 2823 None 82 Human Binding pKi = 7.3 7.3 -3 2
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm800258p
2835 2823 None 82 Human Binding pKi = 7.3 7.3 -3 2
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm800258p
938 2823 None 82 Human Binding pKi = 7.3 7.3 -3 2
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm800258p
CHEMBL573 2823 None 82 Human Binding pKi = 7.3 7.3 -3 2
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm800258p
DB00627 2823 None 82 Human Binding pKi = 7.3 7.3 -3 2
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cells
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm800258p
11776293 149345 None 4 Rat Binding pKi = 6.3 6.3 - 1
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 236 3 2 2 2.4 O=C(O)c1cc(Cc2cccc(Cl)c2)n[nH]1 10.1021/jm030888c
CHEMBL394441 149345 None 4 Rat Binding pKi = 6.3 6.3 - 1
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 236 3 2 2 2.4 O=C(O)c1cc(Cc2cccc(Cl)c2)n[nH]1 10.1021/jm030888c
11159621 2548 None 38 Human Binding pKi = 6.3 6.3 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cells
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
5784 2548 None 38 Human Binding pKi = 6.3 6.3 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cells
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
CHEMBL456145 2548 None 38 Human Binding pKi = 6.3 6.3 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cells
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
DB05939 2548 None 38 Human Binding pKi = 6.3 6.3 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cells
ChEMBL 176 1 2 4 0.1 n1[nH]nc(n1)c1n[nH]c2c1CCC2 10.1021/jm800258p
735981 61772 None 59 Human Binding pKi = 5.3 5.3 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 154 2 1 2 1.8 O=C(O)/C=C/c1cccs1 10.1016/j.bmcl.2010.11.091
CHEMBL1771765 61772 None 59 Human Binding pKi = 5.3 5.3 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 154 2 1 2 1.8 O=C(O)/C=C/c1cccs1 10.1016/j.bmcl.2010.11.091
14112183 61766 None 0 Human Binding pKi = 5.2 5.2 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 220 4 1 3 1.9 CC(OC(=O)/C=C/C(=O)O)c1ccccc1 10.1016/j.bmcl.2010.11.091
CHEMBL1771738 61766 None 0 Human Binding pKi = 5.2 5.2 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 220 4 1 3 1.9 CC(OC(=O)/C=C/C(=O)O)c1ccccc1 10.1016/j.bmcl.2010.11.091
574310 18963 None 77 Rat Binding pKi = 6.2 6.2 - 1
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 112 1 2 2 0.1 O=C(O)c1cc[nH]n1 10.1021/jm030888c
CHEMBL128679 18963 None 77 Rat Binding pKi = 6.2 6.2 - 1
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 112 1 2 2 0.1 O=C(O)c1cc[nH]n1 10.1021/jm030888c
135416394 2560 None 43 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 10.1021/jm100022r
5788 2560 None 43 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 10.1021/jm100022r
73755154 2560 None 43 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 10.1021/jm100022r
CHEMBL1086657 2560 None 43 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 10.1021/jm100022r
11746440 19410 None 0 Rat Binding pKi = 5.2 5.2 - 1
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 230 5 2 2 2.3 O=C(O)c1cc(CCCc2ccccc2)[nH]n1 10.1021/jm030888c
CHEMBL129326 19410 None 0 Rat Binding pKi = 5.2 5.2 - 1
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 230 5 2 2 2.3 O=C(O)c1cc(CCCc2ccccc2)[nH]n1 10.1021/jm030888c
4430637 116901 None 53 Rat Binding pKi = 4.2 4.2 - 1
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 222 2 2 2 2.4 O=C(O)c1cc(-c2cccc(Cl)c2)[nH]n1 10.1021/jm030888c
CHEMBL338017 116901 None 53 Rat Binding pKi = 4.2 4.2 - 1
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 222 2 2 2 2.4 O=C(O)c1cc(-c2cccc(Cl)c2)[nH]n1 10.1021/jm030888c
135416393 7631 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 374 6 4 8 0.8 O=C(O)C1=C(NC(=O)C(O)Cc2nc(-c3ccc(O)cn3)no2)CCCC1 10.1021/jm100022r
CHEMBL1088213 7631 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 374 6 4 8 0.8 O=C(O)C1=C(NC(=O)C(O)Cc2nc(-c3ccc(O)cn3)no2)CCCC1 10.1021/jm100022r
10922388 18523 None 0 Rat Binding pKi = 4.2 4.2 - 1
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 232 4 2 3 1.7 COc1ccc(Cc2cc(C(=O)O)[nH]n2)cc1 10.1021/jm030888c
CHEMBL127387 18523 None 0 Rat Binding pKi = 4.2 4.2 - 1
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 232 4 2 3 1.7 COc1ccc(Cc2cc(C(=O)O)[nH]n2)cc1 10.1021/jm030888c
776421 89962 None 65 Rat Binding pKi = 6.2 6.2 - 1
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 154 2 2 2 1.2 CC(C)c1cc(C(=O)O)n[nH]1 10.1021/jm030888c
CHEMBL238002 89962 None 65 Rat Binding pKi = 6.2 6.2 - 1
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 154 2 2 2 1.2 CC(C)c1cc(C(=O)O)n[nH]1 10.1021/jm030888c
10103897 61724 None 1 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 186 6 1 3 1.4 CCCCCOC(=O)/C=C/C(=O)O 10.1016/j.bmcl.2010.11.091
CHEMBL1771641 61724 None 1 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 186 6 1 3 1.4 CCCCCOC(=O)/C=C/C(=O)O 10.1016/j.bmcl.2010.11.091
13153555 93916 None 26 Human Binding pKi = 7.1 7.1 - 1
Binding affinity at GPR109aBinding affinity at GPR109a
ChEMBL 182 5 2 2 1.8 CCCCCc1cc(C(=O)O)[nH]n1 10.1021/jm800896z
CHEMBL247921 93916 None 26 Human Binding pKi = 7.1 7.1 - 1
Binding affinity at GPR109aBinding affinity at GPR109a
ChEMBL 182 5 2 2 1.8 CCCCCc1cc(C(=O)O)[nH]n1 10.1021/jm800896z
1591 131 None 45 Rat Binding pKi = 7.1 7.1 - 1
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 168 4 2 2 1.5 CCCCc1cc(n[nH]1)C(=O)O 10.1021/jm030888c
6485181 131 None 45 Rat Binding pKi = 7.1 7.1 - 1
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 168 4 2 2 1.5 CCCCc1cc(n[nH]1)C(=O)O 10.1021/jm030888c
CHEMBL428730 131 None 45 Rat Binding pKi = 7.1 7.1 - 1
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
ChEMBL 168 4 2 2 1.5 CCCCc1cc(n[nH]1)C(=O)O 10.1021/jm030888c
5475335 61723 None 21 Human Binding pKi = 6.1 6.1 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 172 5 1 3 1.0 CCCCOC(=O)/C=C/C(=O)O 10.1016/j.bmcl.2010.11.091
CHEMBL1771640 61723 None 21 Human Binding pKi = 6.1 6.1 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 172 5 1 3 1.0 CCCCOC(=O)/C=C/C(=O)O 10.1016/j.bmcl.2010.11.091
135416392 7439 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 372 6 3 7 2.0 CC(Cc1nc(-c2ccc(O)cn2)no1)C(=O)NC1=C(C(=O)O)CCCC1 10.1021/jm100022r
CHEMBL1086656 7439 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 372 6 3 7 2.0 CC(Cc1nc(-c2ccc(O)cn2)no1)C(=O)NC1=C(C(=O)O)CCCC1 10.1021/jm100022r
643402 61771 None 62 Human Binding pKi = 5.1 5.1 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 138 2 1 2 1.4 O=C(O)/C=C/c1ccco1 10.1016/j.bmcl.2010.11.091
CHEMBL1771761 61771 None 62 Human Binding pKi = 5.1 5.1 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 138 2 1 2 1.4 O=C(O)/C=C/c1ccco1 10.1016/j.bmcl.2010.11.091
117629482 2823 None 82 Human Binding pKi = 7.1 7.1 -3 2
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm100022r
1588 2823 None 82 Human Binding pKi = 7.1 7.1 -3 2
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm100022r
1594 2823 None 82 Human Binding pKi = 7.1 7.1 -3 2
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm100022r
2835 2823 None 82 Human Binding pKi = 7.1 7.1 -3 2
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm100022r
938 2823 None 82 Human Binding pKi = 7.1 7.1 -3 2
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm100022r
CHEMBL573 2823 None 82 Human Binding pKi = 7.1 7.1 -3 2
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm100022r
DB00627 2823 None 82 Human Binding pKi = 7.1 7.1 -3 2
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometryDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
ChEMBL 123 1 1 2 0.8 OC(=O)c1cccnc1 10.1021/jm100022r
135887290 6989 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 430 6 3 7 2.6 O=C(O)C1=C(NC(=O)C(F)(F)C(F)(F)c2nc(-c3ccc(O)cn3)no2)CCCC1 10.1021/jm100022r
CHEMBL1084657 6989 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 430 6 3 7 2.6 O=C(O)C1=C(NC(=O)C(F)(F)C(F)(F)c2nc(-c3ccc(O)cn3)no2)CCCC1 10.1021/jm100022r
54583606 61769 None 0 Human Binding pKi = 5.1 5.1 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 240 4 1 3 2.0 O=C(O)/C=C/C(=O)OCc1cccc(Cl)c1 10.1016/j.bmcl.2010.11.091
CHEMBL1771744 61769 None 0 Human Binding pKi = 5.1 5.1 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 240 4 1 3 2.0 O=C(O)/C=C/C(=O)OCc1cccc(Cl)c1 10.1016/j.bmcl.2010.11.091
135887285 7440 None 0 Human Binding pKi = 5.0 5.0 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 384 6 3 7 2.2 O=C(O)C1=C(NC(=O)C2(Cc3nc(-c4ccc(O)cn4)no3)CC2)CCCC1 10.1021/jm100022r
CHEMBL1086658 7440 None 0 Human Binding pKi = 5.0 5.0 - 1
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albuminDisplacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry in presence of 4% human serum albumin
ChEMBL 384 6 3 7 2.2 O=C(O)C1=C(NC(=O)C2(Cc3nc(-c4ccc(O)cn4)no3)CC2)CCCC1 10.1021/jm100022r
54582648 61768 None 0 Human Binding pKi = 5.0 5.0 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 284 4 1 3 2.1 O=C(O)/C=C/C(=O)OCc1cccc(Br)c1 10.1016/j.bmcl.2010.11.091
CHEMBL1771743 61768 None 0 Human Binding pKi = 5.0 5.0 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
ChEMBL 284 4 1 3 2.1 O=C(O)/C=C/C(=O)OCc1cccc(Br)c1 10.1016/j.bmcl.2010.11.091
117629482 2823 None 82 Mouse Binding pIC50 = 8.2 8.2 - 2
Displacement of [3H]niacin from mouse GPR109ADisplacement of [3H]niacin from mouse GPR109A
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
1588 2823 None 82 Mouse Binding pIC50 = 8.2 8.2 - 2
Displacement of [3H]niacin from mouse GPR109ADisplacement of [3H]niacin from mouse GPR109A
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
1594 2823 None 82 Mouse Binding pIC50 = 8.2 8.2 - 2
Displacement of [3H]niacin from mouse GPR109ADisplacement of [3H]niacin from mouse GPR109A
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
2835 2823 None 82 Mouse Binding pIC50 = 8.2 8.2 - 2
Displacement of [3H]niacin from mouse GPR109ADisplacement of [3H]niacin from mouse GPR109A
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
938 2823 None 82 Mouse Binding pIC50 = 8.2 8.2 - 2
Displacement of [3H]niacin from mouse GPR109ADisplacement of [3H]niacin from mouse GPR109A
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
CHEMBL573 2823 None 82 Mouse Binding pIC50 = 8.2 8.2 - 2
Displacement of [3H]niacin from mouse GPR109ADisplacement of [3H]niacin from mouse GPR109A
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
DB00627 2823 None 82 Mouse Binding pIC50 = 8.2 8.2 - 2
Displacement of [3H]niacin from mouse GPR109ADisplacement of [3H]niacin from mouse GPR109A
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
117629482 2823 None 82 Human Binding pKd = 7.2 7.2 -3 2
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12522134
117629482 2823 None 82 Human Binding pKd = 7.2 7.2 -3 2
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12563315
117629482 2823 None 82 Human Binding pKd = 7.2 7.2 -3 2
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12646212
1588 2823 None 82 Human Binding pKd = 7.2 7.2 -3 2
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12522134
1588 2823 None 82 Human Binding pKd = 7.2 7.2 -3 2
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12563315
1588 2823 None 82 Human Binding pKd = 7.2 7.2 -3 2
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12646212
1594 2823 None 82 Human Binding pKd = 7.2 7.2 -3 2
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12522134
1594 2823 None 82 Human Binding pKd = 7.2 7.2 -3 2
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12563315
1594 2823 None 82 Human Binding pKd = 7.2 7.2 -3 2
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12646212
2835 2823 None 82 Human Binding pKd = 7.2 7.2 -3 2
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12522134
2835 2823 None 82 Human Binding pKd = 7.2 7.2 -3 2
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12563315
2835 2823 None 82 Human Binding pKd = 7.2 7.2 -3 2
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12646212
938 2823 None 82 Human Binding pKd = 7.2 7.2 -3 2
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12522134
938 2823 None 82 Human Binding pKd = 7.2 7.2 -3 2
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12563315
938 2823 None 82 Human Binding pKd = 7.2 7.2 -3 2
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12646212
CHEMBL573 2823 None 82 Human Binding pKd = 7.2 7.2 -3 2
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12522134
CHEMBL573 2823 None 82 Human Binding pKd = 7.2 7.2 -3 2
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12563315
CHEMBL573 2823 None 82 Human Binding pKd = 7.2 7.2 -3 2
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12646212
DB00627 2823 None 82 Human Binding pKd = 7.2 7.2 -3 2
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12522134
DB00627 2823 None 82 Human Binding pKd = 7.2 7.2 -3 2
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12563315
DB00627 2823 None 82 Human Binding pKd = 7.2 7.2 -3 2
UnclassifiedUnclassified
Guide to Pharmacology 123 1 1 2 0.8 OC(=O)c1cccnc1 12646212
637568 78312 None 61 Human Binding pKi = 8.2 8.2 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
Drug Central 144 2 0 4 -0.1 COC(=O)/C=C/C(=O)OC None
CHEMBL2107333 78312 None 61 Human Binding pKi = 8.2 8.2 - 1
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation countingDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in human HEK293T cells by liquid scintillation counting
Drug Central 144 2 0 4 -0.1 COC(=O)/C=C/C(=O)OC None
117629482 2823 None 82 Human Binding pKi = 8.1 8.1 -3 2
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cells
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
1588 2823 None 82 Human Binding pKi = 8.1 8.1 -3 2
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cells
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
1594 2823 None 82 Human Binding pKi = 8.1 8.1 -3 2
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cells
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
2835 2823 None 82 Human Binding pKi = 8.1 8.1 -3 2
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cells
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
938 2823 None 82 Human Binding pKi = 8.1 8.1 -3 2
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cells
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
CHEMBL573 2823 None 82 Human Binding pKi = 8.1 8.1 -3 2
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cells
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
DB00627 2823 None 82 Human Binding pKi = 8.1 8.1 -3 2
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cellsDisplacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cells
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
117629482 2823 None 82 Rat Binding pKi = 8.1 8.1 3 2
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
1588 2823 None 82 Rat Binding pKi = 8.1 8.1 3 2
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
1594 2823 None 82 Rat Binding pKi = 8.1 8.1 3 2
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
2835 2823 None 82 Rat Binding pKi = 8.1 8.1 3 2
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
938 2823 None 82 Rat Binding pKi = 8.1 8.1 3 2
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
CHEMBL573 2823 None 82 Rat Binding pKi = 8.1 8.1 3 2
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
DB00627 2823 None 82 Rat Binding pKi = 8.1 8.1 3 2
Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
Drug Central 123 1 1 2 0.8 OC(=O)c1cccnc1 None
5369209 2591 None 55 Human Binding pKi = 6.7 6.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 130 2 1 3 -0.2 COC(=O)/C=C/C(=O)O 21167710
5786 2591 None 55 Human Binding pKi = 6.7 6.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 130 2 1 3 -0.2 COC(=O)/C=C/C(=O)O 21167710
CHEMBL589586 2591 None 55 Human Binding pKi = 6.7 6.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 130 2 1 3 -0.2 COC(=O)/C=C/C(=O)O 21167710
DB14219 2591 None 55 Human Binding pKi = 6.7 6.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 130 2 1 3 -0.2 COC(=O)/C=C/C(=O)O 21167710
135416394 2560 None 43 Human Binding pKi = 8.4 8.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 20184326
5788 2560 None 43 Human Binding pKi = 8.4 8.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 20184326
73755154 2560 None 43 Human Binding pKi = 8.4 8.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 20184326
CHEMBL1086657 2560 None 43 Human Binding pKi = 8.4 8.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 386 6 3 7 2.4 Oc1ccc(nc1)c1noc(n1)CC(C(=O)NC1=C(CCCC1)C(=O)O)(C)C 20184326
1591 131 None 45 Rat Binding pKi None 7.1 7.1 - 1
UnclassifiedUnclassified
Guide to Pharmacology 168 4 2 2 1.5 CCCCc1cc(n[nH]1)C(=O)O 12930155
6485181 131 None 45 Rat Binding pKi None 7.1 7.1 - 1
UnclassifiedUnclassified
Guide to Pharmacology 168 4 2 2 1.5 CCCCc1cc(n[nH]1)C(=O)O 12930155
CHEMBL428730 131 None 45 Rat Binding pKi None 7.1 7.1 - 1
UnclassifiedUnclassified
Guide to Pharmacology 168 4 2 2 1.5 CCCCc1cc(n[nH]1)C(=O)O 12930155
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