Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

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weight		 Rot
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 DOI
2733504 1434 None 13 Human Functional pEC50 = 6 6.0 -3 3
Agonist activity at FLAG/GFP-tagged GPR3 (unknown origin)-mediated cAMP signaling in HEK293 cells using d2-cAMP as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by HTRF assayAgonist activity at FLAG/GFP-tagged GPR3 (unknown origin)-mediated cAMP signaling in HEK293 cells using d2-cAMP as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by HTRF assay
ChEMBL 314 0 0 0 -3.2 c1ccc2c(c1)[I+]c1c2cccc1.[Cl-] 10.1021/acs.jmedchem.3c01707
7802 1434 None 13 Human Functional pEC50 = 6 6.0 -3 3
Agonist activity at FLAG/GFP-tagged GPR3 (unknown origin)-mediated cAMP signaling in HEK293 cells using d2-cAMP as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by HTRF assayAgonist activity at FLAG/GFP-tagged GPR3 (unknown origin)-mediated cAMP signaling in HEK293 cells using d2-cAMP as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by HTRF assay
ChEMBL 314 0 0 0 -3.2 c1ccc2c(c1)[I+]c1c2cccc1.[Cl-] 10.1021/acs.jmedchem.3c01707
CHEMBL365739 1434 None 13 Human Functional pEC50 = 6 6.0 -3 3
Agonist activity at FLAG/GFP-tagged GPR3 (unknown origin)-mediated cAMP signaling in HEK293 cells using d2-cAMP as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by HTRF assayAgonist activity at FLAG/GFP-tagged GPR3 (unknown origin)-mediated cAMP signaling in HEK293 cells using d2-cAMP as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by HTRF assay
ChEMBL 314 0 0 0 -3.2 c1ccc2c(c1)[I+]c1c2cccc1.[Cl-] 10.1021/acs.jmedchem.3c01707
CHEMBL397686 1434 None 13 Human Functional pEC50 = 6 6.0 -3 3
Agonist activity at FLAG/GFP-tagged GPR3 (unknown origin)-mediated cAMP signaling in HEK293 cells using d2-cAMP as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by HTRF assayAgonist activity at FLAG/GFP-tagged GPR3 (unknown origin)-mediated cAMP signaling in HEK293 cells using d2-cAMP as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by HTRF assay
ChEMBL 314 0 0 0 -3.2 c1ccc2c(c1)[I+]c1c2cccc1.[Cl-] 10.1021/acs.jmedchem.3c01707
172462474 196829 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 377 2 0 1 0.7 FC(F)(F)COc1ccc2c(c1)[I+]c1ccccc1-2 10.1016/j.bmcl.2023.129427
CHEMBL5432982 196829 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 377 2 0 1 0.7 FC(F)(F)COc1ccc2c(c1)[I+]c1ccccc1-2 10.1016/j.bmcl.2023.129427
134817096 167633 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 297 0 0 0 -0.1 Fc1ccc2c(c1)[I+]c1ccccc1-2 10.1016/j.bmcl.2023.129427
CHEMBL4300174 167633 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 297 0 0 0 -0.1 Fc1ccc2c(c1)[I+]c1ccccc1-2 10.1016/j.bmcl.2023.129427
4086473 196335 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 324 1 0 2 -0.3 O=[N+]([O-])c1ccc2c(c1)[I+]c1ccccc1-2 10.1016/j.bmcl.2023.129427
CHEMBL5421637 196335 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 324 1 0 2 -0.3 O=[N+]([O-])c1ccc2c(c1)[I+]c1ccccc1-2 10.1016/j.bmcl.2023.129427
172453881 196008 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 381 1 0 1 0.8 Fc1ccc2c(c1)[I+]c1cc(OC(F)(F)F)ccc1-2 10.1016/j.bmcl.2023.129427
CHEMBL5415054 196008 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 381 1 0 1 0.8 Fc1ccc2c(c1)[I+]c1cc(OC(F)(F)F)ccc1-2 10.1016/j.bmcl.2023.129427
172462319 196735 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 363 5 0 0 1.9 CCCCCCc1ccc2c(c1)[I+]c1ccccc1-2 10.1016/j.bmcl.2023.129427
CHEMBL5431176 196735 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 363 5 0 0 1.9 CCCCCCc1ccc2c(c1)[I+]c1ccccc1-2 10.1016/j.bmcl.2023.129427
71543612 167846 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 309 1 0 1 -0.2 COc1ccc2c(c1)[I+]c1ccccc1-2 10.1016/j.bmcl.2023.129427
CHEMBL4302860 167846 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 309 1 0 1 -0.2 COc1ccc2c(c1)[I+]c1ccccc1-2 10.1016/j.bmcl.2023.129427
172445328 195073 None 0 Human Functional pEC50 = 4.7 4.7 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 359 0 0 2 0.1 FC1(F)Oc2cc3c(cc2O1)-c1ccccc1[I+]3 10.1016/j.bmcl.2023.129427
CHEMBL5396263 195073 None 0 Human Functional pEC50 = 4.7 4.7 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 359 0 0 2 0.1 FC1(F)Oc2cc3c(cc2O1)-c1ccccc1[I+]3 10.1016/j.bmcl.2023.129427
265040 194995 None 13 Human Functional pEC50 = 4.7 4.7 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 209 1 0 1 3.3 CN(C)C1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2023.129427
CHEMBL5394629 194995 None 13 Human Functional pEC50 = 4.7 4.7 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 209 1 0 1 3.3 CN(C)C1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2023.129427
172460988 196521 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 399 1 0 1 1.0 Fc1cc2c(cc1F)-c1ccc(OC(F)(F)F)cc1[I+]2 10.1016/j.bmcl.2023.129427
CHEMBL5425788 196521 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 399 1 0 1 1.0 Fc1cc2c(cc1F)-c1ccc(OC(F)(F)F)cc1[I+]2 10.1016/j.bmcl.2023.129427
169450677 195267 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 363 1 0 1 0.7 FC(F)(F)Oc1ccc2c(c1)[I+]c1ccccc1-2 10.1016/j.bmcl.2023.129427
CHEMBL5399736 195267 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 363 1 0 1 0.7 FC(F)(F)Oc1ccc2c(c1)[I+]c1ccccc1-2 10.1016/j.bmcl.2023.129427
172464243 196781 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 447 2 0 2 1.6 FC(F)(F)Oc1ccc2c(c1)[I+]c1cc(OC(F)(F)F)ccc1-2 10.1016/j.bmcl.2023.129427
CHEMBL5432166 196781 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 447 2 0 2 1.6 FC(F)(F)Oc1ccc2c(c1)[I+]c1cc(OC(F)(F)F)ccc1-2 10.1016/j.bmcl.2023.129427
9190 57430 None 48 Human Functional pEC50 = 4.5 4.5 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 180 0 0 2 2.8 c1ccc2c(c1)nnc1ccccc12 10.1016/j.bmcl.2023.129427
CHEMBL1652414 57430 None 48 Human Functional pEC50 = 4.5 4.5 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 180 0 0 2 2.8 c1ccc2c(c1)nnc1ccccc12 10.1016/j.bmcl.2023.129427
172468235 196887 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 311 0 0 0 0.2 Cc1cc2c(cc1F)-c1ccccc1[I+]2 10.1016/j.bmcl.2023.129427
CHEMBL5434234 196887 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 311 0 0 0 0.2 Cc1cc2c(cc1F)-c1ccccc1[I+]2 10.1016/j.bmcl.2023.129427
2733504 1434 None 13 Human Functional pEC50 = 5.4 5.4 -3 3
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 314 0 0 0 -3.2 c1ccc2c(c1)[I+]c1c2cccc1.[Cl-] 10.1016/j.bmcl.2023.129427
7802 1434 None 13 Human Functional pEC50 = 5.4 5.4 -3 3
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 314 0 0 0 -3.2 c1ccc2c(c1)[I+]c1c2cccc1.[Cl-] 10.1016/j.bmcl.2023.129427
CHEMBL365739 1434 None 13 Human Functional pEC50 = 5.4 5.4 -3 3
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 314 0 0 0 -3.2 c1ccc2c(c1)[I+]c1c2cccc1.[Cl-] 10.1016/j.bmcl.2023.129427
CHEMBL397686 1434 None 13 Human Functional pEC50 = 5.4 5.4 -3 3
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 314 0 0 0 -3.2 c1ccc2c(c1)[I+]c1c2cccc1.[Cl-] 10.1016/j.bmcl.2023.129427
15142 67792 None 58 Human Functional pEC50 = 4.4 4.4 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 181 0 0 1 3.3 Cn1c2ccccc2c2ccccc21 10.1016/j.bmcl.2023.129427
CHEMBL1908211 67792 None 58 Human Functional pEC50 = 4.4 4.4 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 181 0 0 1 3.3 Cn1c2ccccc2c2ccccc21 10.1016/j.bmcl.2023.129427
1853 173344 None 66 Human Functional pEC50 = 4.4 4.4 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 195 0 1 1 2.7 O=c1[nH]c2ccccc2c2ccccc12 10.1016/j.bmcl.2023.129427
CHEMBL45245 173344 None 66 Human Functional pEC50 = 4.4 4.4 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 195 0 1 1 2.7 O=c1[nH]c2ccccc2c2ccccc12 10.1016/j.bmcl.2023.129427
172449189 195690 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 377 1 0 1 1.0 Cc1ccc2c(c1)[I+]c1cc(OC(F)(F)F)ccc1-2 10.1016/j.bmcl.2023.129427
CHEMBL5409202 195690 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 377 1 0 1 1.0 Cc1ccc2c(c1)[I+]c1cc(OC(F)(F)F)ccc1-2 10.1016/j.bmcl.2023.129427
13908 195535 None 54 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 216 0 0 2 2.5 O=S1(=O)c2ccccc2-c2ccccc21 10.1016/j.bmcl.2023.129427
CHEMBL5405489 195535 None 54 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 216 0 0 2 2.5 O=S1(=O)c2ccccc2-c2ccccc21 10.1016/j.bmcl.2023.129427
2733504 1434 None 13 Human Functional pEC50 = 5.3 5.3 -3 3
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 314 0 0 0 -3.2 c1ccc2c(c1)[I+]c1c2cccc1.[Cl-] 10.1016/j.bmcl.2023.129427
7802 1434 None 13 Human Functional pEC50 = 5.3 5.3 -3 3
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 314 0 0 0 -3.2 c1ccc2c(c1)[I+]c1c2cccc1.[Cl-] 10.1016/j.bmcl.2023.129427
CHEMBL365739 1434 None 13 Human Functional pEC50 = 5.3 5.3 -3 3
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 314 0 0 0 -3.2 c1ccc2c(c1)[I+]c1c2cccc1.[Cl-] 10.1016/j.bmcl.2023.129427
CHEMBL397686 1434 None 13 Human Functional pEC50 = 5.3 5.3 -3 3
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 314 0 0 0 -3.2 c1ccc2c(c1)[I+]c1c2cccc1.[Cl-] 10.1016/j.bmcl.2023.129427
242966 59667 None 2 Human Functional pEC50 = 4.2 4.2 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 209 0 0 1 3.9 CC1c2ccccc2-c2ccccc2N1C 10.1016/j.bmcl.2023.129427
CHEMBL1721150 59667 None 2 Human Functional pEC50 = 4.2 4.2 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 209 0 0 1 3.9 CC1c2ccccc2-c2ccccc2N1C 10.1016/j.bmcl.2023.129427
85743780 167687 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 293 0 0 0 0.1 Cc1ccc2c(c1)[I+]c1ccccc1-2 10.1016/j.bmcl.2023.129427
CHEMBL4173205 167687 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 293 0 0 0 0.1 Cc1ccc2c(c1)[I+]c1ccccc1-2 10.1016/j.bmcl.2023.129427
CHEMBL4300787 167687 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 293 0 0 0 0.1 Cc1ccc2c(c1)[I+]c1ccccc1-2 10.1016/j.bmcl.2023.129427
172445558 195458 None 0 Human Functional pEC50 = 4.2 4.2 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 283 1 0 2 4.0 CC(C)(C)[S+]([O-])N=C1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2023.129427
CHEMBL5404192 195458 None 0 Human Functional pEC50 = 4.2 4.2 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 283 1 0 2 4.0 CC(C)(C)[S+]([O-])N=C1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2023.129427
9189 188840 None 51 Human Functional pEC50 = 4.2 4.2 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 179 0 0 1 3.4 c1ccc2c(c1)cnc1ccccc12 10.1016/j.bmcl.2023.129427
CHEMBL504941 188840 None 51 Human Functional pEC50 = 4.2 4.2 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 179 0 0 1 3.4 c1ccc2c(c1)cnc1ccccc12 10.1016/j.bmcl.2023.129427
6854 92668 None 57 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 167 0 1 0 3.3 c1ccc2c(c1)[nH]c1ccccc12 10.1016/j.bmcl.2023.129427
CHEMBL243580 92668 None 57 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 167 0 1 0 3.3 c1ccc2c(c1)[nH]c1ccccc12 10.1016/j.bmcl.2023.129427
3023 83475 None 71 Human Functional pEC50 = 4.1 4.1 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 184 0 0 1 4.1 c1ccc2c(c1)sc1ccccc12 10.1016/j.bmcl.2023.129427
CHEMBL219828 83475 None 71 Human Functional pEC50 = 4.1 4.1 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 184 0 0 1 4.1 c1ccc2c(c1)sc1ccccc12 10.1016/j.bmcl.2023.129427
172464481 196594 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 365 0 0 0 1.0 Fc1cc2c(cc1C(F)(F)F)[I+]c1ccccc1-2 10.1016/j.bmcl.2023.129427
CHEMBL5427433 196594 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 365 0 0 0 1.0 Fc1cc2c(cc1C(F)(F)F)[I+]c1ccccc1-2 10.1016/j.bmcl.2023.129427
317988 195746 None 18 Human Functional pEC50 = 4.1 4.1 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 193 0 0 1 3.7 Cc1nc2ccccc2c2ccccc12 10.1016/j.bmcl.2023.129427
CHEMBL5410016 195746 None 18 Human Functional pEC50 = 4.1 4.1 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 193 0 0 1 3.7 Cc1nc2ccccc2c2ccccc12 10.1016/j.bmcl.2023.129427
134817130 167806 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 313 0 0 0 0.4 Clc1ccc2c(c1)[I+]c1ccccc1-2 10.1016/j.bmcl.2023.129427
CHEMBL4302437 167806 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 313 0 0 0 0.4 Clc1ccc2c(c1)[I+]c1ccccc1-2 10.1016/j.bmcl.2023.129427
172462478 196836 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 315 0 0 0 0.1 Fc1cc2c(cc1F)-c1ccccc1[I+]2 10.1016/j.bmcl.2023.129427
CHEMBL5433034 196836 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 315 0 0 0 0.1 Fc1cc2c(cc1F)-c1ccccc1[I+]2 10.1016/j.bmcl.2023.129427
172449198 195691 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 347 0 0 0 0.8 FC(F)(F)c1ccc2c(c1)[I+]c1ccccc1-2 10.1016/j.bmcl.2023.129427
CHEMBL5409214 195691 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 347 0 0 0 0.8 FC(F)(F)c1ccc2c(c1)[I+]c1ccccc1-2 10.1016/j.bmcl.2023.129427
2733504 1434 None 13 Human Functional pEC50 = 6 6.0 -3 3
UnclassifiedUnclassified
Guide to Pharmacology 314 0 0 0 -3.2 c1ccc2c(c1)[I+]c1c2cccc1.[Cl-] 24633425
7802 1434 None 13 Human Functional pEC50 = 6 6.0 -3 3
UnclassifiedUnclassified
Guide to Pharmacology 314 0 0 0 -3.2 c1ccc2c(c1)[I+]c1c2cccc1.[Cl-] 24633425
CHEMBL365739 1434 None 13 Human Functional pEC50 = 6 6.0 -3 3
UnclassifiedUnclassified
Guide to Pharmacology 314 0 0 0 -3.2 c1ccc2c(c1)[I+]c1c2cccc1.[Cl-] 24633425
CHEMBL397686 1434 None 13 Human Functional pEC50 = 6 6.0 -3 3
UnclassifiedUnclassified
Guide to Pharmacology 314 0 0 0 -3.2 c1ccc2c(c1)[I+]c1c2cccc1.[Cl-] 24633425
10883396 3649 None 30 Human Functional pEC50 None 7.4 7.4 -30 15
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 12220620
5283560 3649 None 30 Human Functional pEC50 None 7.4 7.4 -30 15
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 12220620
911 3649 None 30 Human Functional pEC50 None 7.4 7.4 -30 15
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 12220620
CHEMBL225155 3649 None 30 Human Functional pEC50 None 7.4 7.4 -30 15
UnclassifiedUnclassified
Guide to Pharmacology 379 17 4 4 4.0 CCCCCCCCCCCCC/C=C/[C@H]([C@H](COP(=O)(O)O)N)O 12220620


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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
Sel. page Common
name		 GPCRdb
ID		 Reference
ligand		 Vendors

 Species

 Assay
Type		 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
172447166 195003 None 0 Human Binding pEC50 = 5.0 5.0 - 0
Total binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assayTotal binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assay
ChEMBL 920 19 2 12 9.6 CC(C)Oc1cc(Cl)ccc1CNc1cc(-c2ccc(OCCCCCCNC(=O)c3ccc(-c4c5ccc(N(C)C)cc5[o+]c5cc(N(C)C)ccc45)c(C(=O)[O-])c3)cc2)nc2ncnn12 10.1021/acs.jmedchem.3c01707
CHEMBL5394725 195003 None 0 Human Binding pEC50 = 5.0 5.0 - 0
Total binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assayTotal binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assay
ChEMBL 920 19 2 12 9.6 CC(C)Oc1cc(Cl)ccc1CNc1cc(-c2ccc(OCCCCCCNC(=O)c3ccc(-c4c5ccc(N(C)C)cc5[o+]c5cc(N(C)C)ccc45)c(C(=O)[O-])c3)cc2)nc2ncnn12 10.1021/acs.jmedchem.3c01707
172452129 195773 None 0 Human Binding pEC50 = 5.9 5.9 -7 2
Modulation of N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate at 1 uM measured for 3 hrs in presence of DPI by NanoBRET assayModulation of N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate at 1 uM measured for 3 hrs in presence of DPI by NanoBRET assay
ChEMBL 920 19 2 12 9.6 CC(C)Oc1cc(Cl)ccc1CNc1cc(-c2ccccc2OCCCCCCNC(=O)c2ccc(-c3c4ccc(N(C)C)cc4[o+]c4cc(N(C)C)ccc34)c(C(=O)[O-])c2)nc2ncnn12 10.1021/acs.jmedchem.3c01707
CHEMBL5410506 195773 None 0 Human Binding pEC50 = 5.9 5.9 -7 2
Modulation of N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate at 1 uM measured for 3 hrs in presence of DPI by NanoBRET assayModulation of N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate at 1 uM measured for 3 hrs in presence of DPI by NanoBRET assay
ChEMBL 920 19 2 12 9.6 CC(C)Oc1cc(Cl)ccc1CNc1cc(-c2ccccc2OCCCCCCNC(=O)c2ccc(-c3c4ccc(N(C)C)cc4[o+]c4cc(N(C)C)ccc34)c(C(=O)[O-])c2)nc2ncnn12 10.1021/acs.jmedchem.3c01707
172442960 195543 None 0 Human Binding pEC50 = 5.5 5.5 - 0
Total binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assayTotal binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assay
ChEMBL 996 24 2 15 8.0 CC(C)Oc1cc(Cl)ccc1CNc1cc(-c2ccccc2OCCOCCOCCOCCNC(=O)c2ccc(-c3c4ccc(N(C)C)cc4[o+]c4cc(N(C)C)ccc34)c(C(=O)[O-])c2)nc2ncnn12 10.1021/acs.jmedchem.3c01707
CHEMBL5405597 195543 None 0 Human Binding pEC50 = 5.5 5.5 - 0
Total binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assayTotal binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assay
ChEMBL 996 24 2 15 8.0 CC(C)Oc1cc(Cl)ccc1CNc1cc(-c2ccccc2OCCOCCOCCOCCNC(=O)c2ccc(-c3c4ccc(N(C)C)cc4[o+]c4cc(N(C)C)ccc34)c(C(=O)[O-])c2)nc2ncnn12 10.1021/acs.jmedchem.3c01707
172445374 195171 None 0 Human Binding pEC50 = 5.4 5.4 - 0
Total binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assayTotal binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assay
ChEMBL 1084 30 2 17 8.1 CC(C)Oc1cc(Cl)ccc1CNc1cc(-c2ccccc2OCCOCCOCCOCCOCCOCCNC(=O)c2ccc(-c3c4ccc(N(C)C)cc4[o+]c4cc(N(C)C)ccc34)c(C(=O)[O-])c2)nc2ncnn12 10.1021/acs.jmedchem.3c01707
CHEMBL5398023 195171 None 0 Human Binding pEC50 = 5.4 5.4 - 0
Total binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assayTotal binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assay
ChEMBL 1084 30 2 17 8.1 CC(C)Oc1cc(Cl)ccc1CNc1cc(-c2ccccc2OCCOCCOCCOCCOCCOCCNC(=O)c2ccc(-c3c4ccc(N(C)C)cc4[o+]c4cc(N(C)C)ccc34)c(C(=O)[O-])c2)nc2ncnn12 10.1021/acs.jmedchem.3c01707
172458638 196423 None 0 Human Binding pEC50 = 5.4 5.4 - 0
Total binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assayTotal binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assay
ChEMBL 920 19 2 12 9.6 CC(C)Oc1cc(Cl)ccc1CNc1cc(-c2cccc(OCCCCCCNC(=O)c3ccc(-c4c5ccc(N(C)C)cc5[o+]c5cc(N(C)C)ccc45)c(C(=O)[O-])c3)c2)nc2ncnn12 10.1021/acs.jmedchem.3c01707
CHEMBL5423734 196423 None 0 Human Binding pEC50 = 5.4 5.4 - 0
Total binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assayTotal binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assay
ChEMBL 920 19 2 12 9.6 CC(C)Oc1cc(Cl)ccc1CNc1cc(-c2cccc(OCCCCCCNC(=O)c3ccc(-c4c5ccc(N(C)C)cc5[o+]c5cc(N(C)C)ccc45)c(C(=O)[O-])c3)c2)nc2ncnn12 10.1021/acs.jmedchem.3c01707
172452129 195773 None 0 Human Binding pEC50 = 6.1 6.1 -7 2
Total binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assayTotal binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assay
ChEMBL 920 19 2 12 9.6 CC(C)Oc1cc(Cl)ccc1CNc1cc(-c2ccccc2OCCCCCCNC(=O)c2ccc(-c3c4ccc(N(C)C)cc4[o+]c4cc(N(C)C)ccc34)c(C(=O)[O-])c2)nc2ncnn12 10.1021/acs.jmedchem.3c01707
CHEMBL5410506 195773 None 0 Human Binding pEC50 = 6.1 6.1 -7 2
Total binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assayTotal binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assay
ChEMBL 920 19 2 12 9.6 CC(C)Oc1cc(Cl)ccc1CNc1cc(-c2ccccc2OCCCCCCNC(=O)c2ccc(-c3c4ccc(N(C)C)cc4[o+]c4cc(N(C)C)ccc34)c(C(=O)[O-])c2)nc2ncnn12 10.1021/acs.jmedchem.3c01707
172452129 195773 None 0 Human Binding pIC50 = 5.9 5.9 -7 2
Competitive total binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate at 1 uM measured for 3 hrs in presence of AF64394 by NanoBRET assayCompetitive total binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate at 1 uM measured for 3 hrs in presence of AF64394 by NanoBRET assay
ChEMBL 920 19 2 12 9.6 CC(C)Oc1cc(Cl)ccc1CNc1cc(-c2ccccc2OCCCCCCNC(=O)c2ccc(-c3c4ccc(N(C)C)cc4[o+]c4cc(N(C)C)ccc34)c(C(=O)[O-])c2)nc2ncnn12 10.1021/acs.jmedchem.3c01707
CHEMBL5410506 195773 None 0 Human Binding pIC50 = 5.9 5.9 -7 2
Competitive total binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate at 1 uM measured for 3 hrs in presence of AF64394 by NanoBRET assayCompetitive total binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate at 1 uM measured for 3 hrs in presence of AF64394 by NanoBRET assay
ChEMBL 920 19 2 12 9.6 CC(C)Oc1cc(Cl)ccc1CNc1cc(-c2ccccc2OCCCCCCNC(=O)c2ccc(-c3c4ccc(N(C)C)cc4[o+]c4cc(N(C)C)ccc34)c(C(=O)[O-])c2)nc2ncnn12 10.1021/acs.jmedchem.3c01707
172452129 195773 None 0 Human Binding pKd = 7.0 7.0 -7 2
Binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using vivazine as substrate measured for 180 mins by time-course saturation based NanoBRET assayBinding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using vivazine as substrate measured for 180 mins by time-course saturation based NanoBRET assay
ChEMBL 920 19 2 12 9.6 CC(C)Oc1cc(Cl)ccc1CNc1cc(-c2ccccc2OCCCCCCNC(=O)c2ccc(-c3c4ccc(N(C)C)cc4[o+]c4cc(N(C)C)ccc34)c(C(=O)[O-])c2)nc2ncnn12 10.1021/acs.jmedchem.3c01707
CHEMBL5410506 195773 None 0 Human Binding pKd = 7.0 7.0 -7 2
Binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using vivazine as substrate measured for 180 mins by time-course saturation based NanoBRET assayBinding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using vivazine as substrate measured for 180 mins by time-course saturation based NanoBRET assay
ChEMBL 920 19 2 12 9.6 CC(C)Oc1cc(Cl)ccc1CNc1cc(-c2ccccc2OCCCCCCNC(=O)c2ccc(-c3c4ccc(N(C)C)cc4[o+]c4cc(N(C)C)ccc34)c(C(=O)[O-])c2)nc2ncnn12 10.1021/acs.jmedchem.3c01707
172452129 195773 None 0 Human Binding pKd = 6.5 6.5 -7 2
Specific binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assaySpecific binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assay
ChEMBL 920 19 2 12 9.6 CC(C)Oc1cc(Cl)ccc1CNc1cc(-c2ccccc2OCCCCCCNC(=O)c2ccc(-c3c4ccc(N(C)C)cc4[o+]c4cc(N(C)C)ccc34)c(C(=O)[O-])c2)nc2ncnn12 10.1021/acs.jmedchem.3c01707
CHEMBL5410506 195773 None 0 Human Binding pKd = 6.5 6.5 -7 2
Specific binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assaySpecific binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assay
ChEMBL 920 19 2 12 9.6 CC(C)Oc1cc(Cl)ccc1CNc1cc(-c2ccccc2OCCCCCCNC(=O)c2ccc(-c3c4ccc(N(C)C)cc4[o+]c4cc(N(C)C)ccc34)c(C(=O)[O-])c2)nc2ncnn12 10.1021/acs.jmedchem.3c01707
172452129 195773 None 0 Human Binding pKi = 6.5 6.5 -7 2
Competitive total binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate at 1 uM measured for 3 hrs in presence of AF64394 by NanoBRET assayCompetitive total binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate at 1 uM measured for 3 hrs in presence of AF64394 by NanoBRET assay
ChEMBL 920 19 2 12 9.6 CC(C)Oc1cc(Cl)ccc1CNc1cc(-c2ccccc2OCCCCCCNC(=O)c2ccc(-c3c4ccc(N(C)C)cc4[o+]c4cc(N(C)C)ccc34)c(C(=O)[O-])c2)nc2ncnn12 10.1021/acs.jmedchem.3c01707
CHEMBL5410506 195773 None 0 Human Binding pKi = 6.5 6.5 -7 2
Competitive total binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate at 1 uM measured for 3 hrs in presence of AF64394 by NanoBRET assayCompetitive total binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate at 1 uM measured for 3 hrs in presence of AF64394 by NanoBRET assay
ChEMBL 920 19 2 12 9.6 CC(C)Oc1cc(Cl)ccc1CNc1cc(-c2ccccc2OCCCCCCNC(=O)c2ccc(-c3c4ccc(N(C)C)cc4[o+]c4cc(N(C)C)ccc34)c(C(=O)[O-])c2)nc2ncnn12 10.1021/acs.jmedchem.3c01707
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