Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
71454870 87736 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 444 6 0 5 6.3 Fc1ccc(-c2ccc(-c3nnc(CCCc4ccc5cccnc5n4)o3)cc2)cc1Cl 10.1016/j.bmcl.2011.04.091
CHEMBL2153587 87736 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 444 6 0 5 6.3 Fc1ccc(-c2ccc(-c3nnc(CCCc4ccc5cccnc5n4)o3)cc2)cc1Cl 10.1016/j.bmcl.2011.04.091
71460332 87708 4 None -9 3 Rat 7.0 pIC50 = 7 Functional
Antagonist activity at rat GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at rat GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 429 7 1 3 6.2 C[C@H](NC(=O)CCCc1ccc2cccnc2n1)c1ccc(-c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.04.091
CHEMBL2153446 87708 4 None -9 3 Rat 7.0 pIC50 = 7 Functional
Antagonist activity at rat GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at rat GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 429 7 1 3 6.2 C[C@H](NC(=O)CCCc1ccc2cccnc2n1)c1ccc(-c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.04.091
71460331 87700 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 381 7 1 3 4.9 O=C(CCCc1ccc2cccnc2n1)NCc1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2011.04.091
CHEMBL2153438 87700 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 381 7 1 3 4.9 O=C(CCCc1ccc2cccnc2n1)NCc1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2011.04.091
71449506 87709 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 411 8 1 4 4.9 COc1cccc(-c2ccc(CNC(=O)CCCc3ccc4cccnc4n3)cc2)c1 10.1016/j.bmcl.2011.04.091
CHEMBL2153447 87709 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 411 8 1 4 4.9 COc1cccc(-c2ccc(CNC(=O)CCCc3ccc4cccnc4n3)cc2)c1 10.1016/j.bmcl.2011.04.091
71449521 87733 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 459 7 1 6 4.5 O=C(CCCc1ccc2cccnc2n1)NCc1nnc(-c2ccc(F)c(C(F)(F)F)c2)o1 10.1016/j.bmcl.2011.04.091
CHEMBL2153584 87733 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 459 7 1 6 4.5 O=C(CCCc1ccc2cccnc2n1)NCc1nnc(-c2ccc(F)c(C(F)(F)F)c2)o1 10.1016/j.bmcl.2011.04.091
71458498 87740 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 443 6 1 4 6.1 Fc1ccc(-c2ccc(-c3nnc(CCCc4ccc5cccnc5n4)[nH]3)cc2)cc1Cl 10.1016/j.bmcl.2011.04.091
CHEMBL2153590 87740 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 443 6 1 4 6.1 Fc1ccc(-c2ccc(-c3nnc(CCCc4ccc5cccnc5n4)[nH]3)cc2)cc1Cl 10.1016/j.bmcl.2011.04.091
71460332 87708 4 None 9 3 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 429 7 1 3 6.2 C[C@H](NC(=O)CCCc1ccc2cccnc2n1)c1ccc(-c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.04.091
CHEMBL2153446 87708 4 None 9 3 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 429 7 1 3 6.2 C[C@H](NC(=O)CCCc1ccc2cccnc2n1)c1ccc(-c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.04.091
71462027 87702 0 None -2 3 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at rat GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 415 7 1 3 5.6 O=C(CCCc1ccc2cccnc2n1)NCc1ccc(-c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.04.091
CHEMBL2153440 87702 0 None -2 3 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at rat GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 415 7 1 3 5.6 O=C(CCCc1ccc2cccnc2n1)NCc1ccc(-c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.04.091
162670620 189746 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assayAntagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay
ChEMBL 380 6 2 3 4.3 O=C(O)C[C@H](NC(=O)c1cccc(-c2ccc(Cl)cc2)c1)c1cccnc1 10.1021/acs.jmedchem.0c01020
CHEMBL4793036 189746 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assayAntagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay
ChEMBL 380 6 2 3 4.3 O=C(O)C[C@H](NC(=O)c1cccc(-c2ccc(Cl)cc2)c1)c1cccnc1 10.1021/acs.jmedchem.0c01020
162646878 186336 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assayAntagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay
ChEMBL 383 5 2 2 5.0 O=C(O)Cc1ccccc1NC(=O)c1cccc(-c2ccc(Cl)cc2)c1F 10.1021/acs.jmedchem.0c01020
CHEMBL4741728 186336 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assayAntagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay
ChEMBL 383 5 2 2 5.0 O=C(O)Cc1ccccc1NC(=O)c1cccc(-c2ccc(Cl)cc2)c1F 10.1021/acs.jmedchem.0c01020
162664232 188858 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assayAntagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay
ChEMBL 365 5 2 2 4.9 O=C(O)Cc1ccccc1NC(=O)c1cccc(-c2ccc(Cl)cc2)c1 10.1021/acs.jmedchem.0c01020
CHEMBL4781545 188858 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assayAntagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay
ChEMBL 365 5 2 2 4.9 O=C(O)Cc1ccccc1NC(=O)c1cccc(-c2ccc(Cl)cc2)c1 10.1021/acs.jmedchem.0c01020
53358901 7909 9 None -3 2 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at rat GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 458 7 1 5 5.1 O=C(NCc1onc(c1)c1ccc(c(c1)C(F)(F)F)F)CCCc1ccc2c(n1)nccc2 10.1016/j.bmcl.2011.04.091
5514 7909 9 None -3 2 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at rat GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 458 7 1 5 5.1 O=C(NCc1onc(c1)c1ccc(c(c1)C(F)(F)F)F)CCCc1ccc2c(n1)nccc2 10.1016/j.bmcl.2011.04.091
CHEMBL2153581 7909 9 None -3 2 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at rat GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 458 7 1 5 5.1 O=C(NCc1onc(c1)c1ccc(c(c1)C(F)(F)F)F)CCCc1ccc2c(n1)nccc2 10.1016/j.bmcl.2011.04.091
71453124 87718 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 557 6 1 3 8.3 C[C@H](NC(=O)C(C)(C)c1ccc(-c2ccc3cccnc3n2)cc1)c1ccc(-c2ccc(F)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.04.091
CHEMBL2153465 87718 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 557 6 1 3 8.3 C[C@H](NC(=O)C(C)(C)c1ccc(-c2ccc3cccnc3n2)cc1)c1ccc(-c2ccc(F)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.04.091
162648855 186627 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assayAntagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay
ChEMBL 464 7 3 4 5.0 O=C(O)Cc1ccccc1NC(=O)c1cccc(-c2ccc(Cl)c(OC3CCNCC3)c2)c1 10.1021/acs.jmedchem.0c01020
CHEMBL4745252 186627 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assayAntagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay
ChEMBL 464 7 3 4 5.0 O=C(O)Cc1ccccc1NC(=O)c1cccc(-c2ccc(Cl)c(OC3CCNCC3)c2)c1 10.1021/acs.jmedchem.0c01020
162665674 189012 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assayAntagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay
ChEMBL 450 7 3 4 4.6 O=C(O)Cc1ccccc1NC(=O)c1cccc(-c2ccc(Cl)c(OC3CCNC3)c2)c1 10.1021/acs.jmedchem.0c01020
CHEMBL4783334 189012 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assayAntagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay
ChEMBL 450 7 3 4 4.6 O=C(O)Cc1ccccc1NC(=O)c1cccc(-c2ccc(Cl)c(OC3CCNC3)c2)c1 10.1021/acs.jmedchem.0c01020
162671190 189632 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assayAntagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay
ChEMBL 436 7 3 4 4.2 O=C(O)Cc1ccccc1NC(=O)c1cccc(-c2ccc(Cl)c(OC3CNC3)c2)c1 10.1021/acs.jmedchem.0c01020
CHEMBL4791540 189632 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assayAntagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay
ChEMBL 436 7 3 4 4.2 O=C(O)Cc1ccccc1NC(=O)c1cccc(-c2ccc(Cl)c(OC3CNC3)c2)c1 10.1021/acs.jmedchem.0c01020
71453121 87707 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 463 7 1 3 6.5 CC(NC(=O)CCCc1ccc2cccnc2n1)c1ccc(-c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.04.091
CHEMBL2153445 87707 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 463 7 1 3 6.5 CC(NC(=O)CCCc1ccc2cccnc2n1)c1ccc(-c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.04.091
71460333 87721 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 613 6 2 4 7.7 C[C@H](NC(=O)C(O)(c1ccc(-c2ccc3cccnc3n2)cc1)C(F)(F)F)c1ccc(-c2ccc(F)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.04.091
CHEMBL2153468 87721 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 613 6 2 4 7.7 C[C@H](NC(=O)C(O)(c1ccc(-c2ccc3cccnc3n2)cc1)C(F)(F)F)c1ccc(-c2ccc(F)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.04.091
71451318 87745 0 None 2 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 432 6 0 5 5.9 FC(F)(F)c1cc(-c2nnc(CCCCc3ccc4cccnc4n3)o2)ccc1Cl 10.1016/j.bmcl.2011.04.091
CHEMBL2153596 87745 0 None 2 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 432 6 0 5 5.9 FC(F)(F)c1cc(-c2nnc(CCCCc3ccc4cccnc4n3)o2)ccc1Cl 10.1016/j.bmcl.2011.04.091
71458486 87715 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 543 6 1 3 7.7 CC(C)(C(=O)NCc1ccc(-c2ccc(F)c(C(F)(F)F)c2)cc1)c1ccc(-c2ccc3cccnc3n2)cc1 10.1016/j.bmcl.2011.04.091
CHEMBL2153462 87715 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 543 6 1 3 7.7 CC(C)(C(=O)NCc1ccc(-c2ccc(F)c(C(F)(F)F)c2)cc1)c1ccc(-c2ccc3cccnc3n2)cc1 10.1016/j.bmcl.2011.04.091
71456642 87743 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 466 6 0 5 6.3 FC(F)(F)c1ccc(-c2nnc(CCCCc3ccc4cccnc4n3)o2)cc1C(F)(F)F 10.1016/j.bmcl.2011.04.091
CHEMBL2153594 87743 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 466 6 0 5 6.3 FC(F)(F)c1ccc(-c2nnc(CCCCc3ccc4cccnc4n3)o2)cc1C(F)(F)F 10.1016/j.bmcl.2011.04.091
71462032 87720 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 545 6 2 4 7.0 C[C@H](NC(=O)C(O)c1ccc(-c2ccc3cccnc3n2)cc1)c1ccc(-c2ccc(F)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.04.091
CHEMBL2153467 87720 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 545 6 2 4 7.0 C[C@H](NC(=O)C(O)c1ccc(-c2ccc3cccnc3n2)cc1)c1ccc(-c2ccc(F)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.04.091
71449523 87744 1 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 448 7 0 6 5.8 FC(F)(F)Oc1ccc(-c2nnc(CCCCc3ccc4cccnc4n3)o2)cc1Cl 10.1016/j.bmcl.2011.04.091
CHEMBL2153595 87744 1 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 448 7 0 6 5.8 FC(F)(F)Oc1ccc(-c2nnc(CCCCc3ccc4cccnc4n3)o2)cc1Cl 10.1016/j.bmcl.2011.04.091
71449508 87719 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 565 6 1 3 8.1 C[C@H](NC(=O)C(F)(F)c1ccc(-c2ccc3cccnc3n2)cc1)c1ccc(-c2ccc(F)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.04.091
CHEMBL2153466 87719 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 565 6 1 3 8.1 C[C@H](NC(=O)C(F)(F)c1ccc(-c2ccc3cccnc3n2)cc1)c1ccc(-c2ccc(F)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.04.091
162656033 187465 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assayAntagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay
ChEMBL 482 7 3 4 5.2 O=C(O)Cc1ccccc1NC(=O)c1cccc(-c2ccc(Cl)c(O[C@@H]3CCCNC3)c2)c1F 10.1021/acs.jmedchem.0c01020
CHEMBL4755411 187465 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assayAntagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay
ChEMBL 482 7 3 4 5.2 O=C(O)Cc1ccccc1NC(=O)c1cccc(-c2ccc(Cl)c(O[C@@H]3CCCNC3)c2)c1F 10.1021/acs.jmedchem.0c01020
71451310 87724 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 469 7 1 5 4.9 O=C(CCCc1ccc2cccnc2n1)NCc1ncc(-c2ccc(F)c(C(F)(F)F)c2)cn1 10.1016/j.bmcl.2011.04.091
CHEMBL2153470 87724 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 469 7 1 5 4.9 O=C(CCCc1ccc2cccnc2n1)NCc1ncc(-c2ccc(F)c(C(F)(F)F)c2)cn1 10.1016/j.bmcl.2011.04.091
71458497 87737 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 460 6 0 5 6.5 FC(F)(F)c1cccc(-c2ccc(-c3nnc(CCCc4ccc5cccnc5n4)o3)cc2)c1 10.1016/j.bmcl.2011.04.091
CHEMBL2153588 87737 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 460 6 0 5 6.5 FC(F)(F)c1cccc(-c2ccc(-c3nnc(CCCc4ccc5cccnc5n4)o3)cc2)c1 10.1016/j.bmcl.2011.04.091
71449524 87746 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 416 6 0 5 5.4 Fc1ccc(-c2nnc(CCCCc3ccc4cccnc4n3)o2)cc1C(F)(F)F 10.1016/j.bmcl.2011.04.091
CHEMBL2153597 87746 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 416 6 0 5 5.4 Fc1ccc(-c2nnc(CCCCc3ccc4cccnc4n3)o2)cc1C(F)(F)F 10.1016/j.bmcl.2011.04.091
71462034 87726 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 457 7 1 5 4.6 O=C(CCCc1ccc2cccnc2n1)NCc1cnn(-c2ccc(F)c(C(F)(F)F)c2)c1 10.1016/j.bmcl.2011.04.091
CHEMBL2153472 87726 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 457 7 1 5 4.6 O=C(CCCc1ccc2cccnc2n1)NCc1cnn(-c2ccc(F)c(C(F)(F)F)c2)c1 10.1016/j.bmcl.2011.04.091
71451308 87703 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 467 7 1 3 6.1 O=C(CCCc1ccc2cccnc2n1)NCc1ccc(-c2ccc(F)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.04.091
CHEMBL2153441 87703 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 467 7 1 3 6.1 O=C(CCCc1ccc2cccnc2n1)NCc1ccc(-c2ccc(F)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.04.091
162644696 186200 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assayAntagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay
ChEMBL 351 4 2 2 5.0 O=C(Nc1ccccc1C(=O)O)c1cccc(-c2ccc(Cl)cc2)c1 10.1021/acs.jmedchem.0c01020
CHEMBL4740249 186200 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assayAntagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay
ChEMBL 351 4 2 2 5.0 O=C(Nc1ccccc1C(=O)O)c1cccc(-c2ccc(Cl)cc2)c1 10.1021/acs.jmedchem.0c01020
10519 9589 23 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assayAntagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay
ChEMBL 443 7 2 4 4.0 CN1CCN(CC1)Cc1ccc(cc1)c1cccc(c1)C(=O)Nc1ccccc1CC(=O)O 10.1021/acs.jmedchem.0c01020
138811017 9589 23 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assayAntagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay
ChEMBL 443 7 2 4 4.0 CN1CCN(CC1)Cc1ccc(cc1)c1cccc(c1)C(=O)Nc1ccccc1CC(=O)O 10.1021/acs.jmedchem.0c01020
CHEMBL4790324 9589 23 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assayAntagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay
ChEMBL 443 7 2 4 4.0 CN1CCN(CC1)Cc1ccc(cc1)c1cccc(c1)C(=O)Nc1ccccc1CC(=O)O 10.1021/acs.jmedchem.0c01020
71458496 87734 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 475 7 1 6 4.9 O=C(CCCc1ccc2cccnc2n1)NCc1nnc(-c2ccc(F)c(C(F)(F)F)c2)s1 10.1016/j.bmcl.2011.04.091
CHEMBL2153585 87734 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 475 7 1 6 4.9 O=C(CCCc1ccc2cccnc2n1)NCc1nnc(-c2ccc(F)c(C(F)(F)F)c2)s1 10.1016/j.bmcl.2011.04.091
162664841 188883 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assayAntagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay
ChEMBL 424 8 3 4 4.2 NCCOc1cc(-c2cccc(C(=O)Nc3ccccc3CC(=O)O)c2)ccc1Cl 10.1021/acs.jmedchem.0c01020
CHEMBL4781889 188883 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assayAntagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay
ChEMBL 424 8 3 4 4.2 NCCOc1cc(-c2cccc(C(=O)Nc3ccccc3CC(=O)O)c2)ccc1Cl 10.1021/acs.jmedchem.0c01020
90480064 179136 1 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assayAntagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay
ChEMBL 360 6 3 3 3.7 NCc1cccc(-c2cccc(C(=O)Nc3ccccc3CC(=O)O)c2)c1 10.1021/acs.jmedchem.0c01020
CHEMBL4475961 179136 1 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assayAntagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay
ChEMBL 360 6 3 3 3.7 NCc1cccc(-c2cccc(C(=O)Nc3ccccc3CC(=O)O)c2)c1 10.1021/acs.jmedchem.0c01020
53358900 87701 1 None -4 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 395 7 1 3 5.2 Cc1cccc(-c2ccc(CNC(=O)CCCc3ccc4cccnc4n3)cc2)c1 10.1016/j.bmcl.2011.04.091
CHEMBL2153439 87701 1 None -4 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 395 7 1 3 5.2 Cc1cccc(-c2ccc(CNC(=O)CCCc3ccc4cccnc4n3)cc2)c1 10.1016/j.bmcl.2011.04.091
71456626 87711 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 429 7 1 3 5.9 Cc1cc(-c2ccc(CNC(=O)CCCc3ccc4cccnc4n3)cc2)ccc1Cl 10.1016/j.bmcl.2011.04.091
CHEMBL2153457 87711 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 429 7 1 3 5.9 Cc1cc(-c2ccc(CNC(=O)CCCc3ccc4cccnc4n3)cc2)ccc1Cl 10.1016/j.bmcl.2011.04.091
71453139 87732 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 422 7 1 5 5.0 O=C(CCCc1ccc2cccnc2n1)NCc1nc(-c2cccc(Cl)c2)cs1 10.1016/j.bmcl.2011.04.091
CHEMBL2153583 87732 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 422 7 1 5 5.0 O=C(CCCc1ccc2cccnc2n1)NCc1nc(-c2cccc(Cl)c2)cs1 10.1016/j.bmcl.2011.04.091
162646617 186448 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assayAntagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay
ChEMBL 394 6 3 3 4.3 NCc1cc(-c2cccc(C(=O)Nc3ccccc3CC(=O)O)c2)ccc1Cl 10.1021/acs.jmedchem.0c01020
CHEMBL4743401 186448 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assayAntagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay
ChEMBL 394 6 3 3 4.3 NCc1cc(-c2cccc(C(=O)Nc3ccccc3CC(=O)O)c2)ccc1Cl 10.1021/acs.jmedchem.0c01020
71449522 87738 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 442 6 0 5 6.6 Clc1cccc(-c2ccc(-c3nnc(CCCc4ccc5cccnc5n4)s3)cc2)c1 10.1016/j.bmcl.2011.04.091
CHEMBL2153589 87738 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 442 6 0 5 6.6 Clc1cccc(-c2ccc(-c3nnc(CCCc4ccc5cccnc5n4)s3)cc2)c1 10.1016/j.bmcl.2011.04.091
71451316 87741 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 398 6 0 5 5.3 FC(F)(F)c1ccc(-c2nnc(CCCCc3ccc4cccnc4n3)o2)cc1 10.1016/j.bmcl.2011.04.091
CHEMBL2153591 87741 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 398 6 0 5 5.3 FC(F)(F)c1ccc(-c2nnc(CCCCc3ccc4cccnc4n3)o2)cc1 10.1016/j.bmcl.2011.04.091
71454871 87742 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 414 7 0 6 5.1 FC(F)(F)Oc1ccc(-c2nnc(CCCCc3ccc4cccnc4n3)o2)cc1 10.1016/j.bmcl.2011.04.091
CHEMBL2153592 87742 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 414 7 0 6 5.1 FC(F)(F)Oc1ccc(-c2nnc(CCCCc3ccc4cccnc4n3)o2)cc1 10.1016/j.bmcl.2011.04.091
71456627 87712 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 481 6 1 3 6.6 O=C(Cc1ccc(-c2ccc3cccnc3n2)cc1)NCc1ccc(-c2ccc(F)c(Cl)c2)cc1 10.1016/j.bmcl.2011.04.091
CHEMBL2153459 87712 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 481 6 1 3 6.6 O=C(Cc1ccc(-c2ccc3cccnc3n2)cc1)NCc1ccc(-c2ccc(F)c(Cl)c2)cc1 10.1016/j.bmcl.2011.04.091
162665135 188974 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assayAntagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay
ChEMBL 380 6 2 3 4.3 O=C(O)CC(NC(=O)c1cccc(-c2ccc(Cl)cc2)c1)c1cccnc1 10.1021/acs.jmedchem.0c01020
CHEMBL4782840 188974 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assayAntagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay
ChEMBL 380 6 2 3 4.3 O=C(O)CC(NC(=O)c1cccc(-c2ccc(Cl)cc2)c1)c1cccnc1 10.1021/acs.jmedchem.0c01020
71456629 87717 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 530 6 2 4 6.4 NC(C(=O)NCc1ccc(-c2ccc(F)c(C(F)(F)F)c2)cc1)c1ccc(-c2ccc3cccnc3n2)cc1 10.1016/j.bmcl.2011.04.091
CHEMBL2153464 87717 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 530 6 2 4 6.4 NC(C(=O)NCc1ccc(-c2ccc(F)c(C(F)(F)F)c2)cc1)c1ccc(-c2ccc3cccnc3n2)cc1 10.1016/j.bmcl.2011.04.091
71456628 87716 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 599 6 2 4 7.2 O=C(NCc1ccc(-c2ccc(F)c(C(F)(F)F)c2)cc1)C(O)(c1ccc(-c2ccc3cccnc3n2)cc1)C(F)(F)F 10.1016/j.bmcl.2011.04.091
CHEMBL2153463 87716 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 599 6 2 4 7.2 O=C(NCc1ccc(-c2ccc(F)c(C(F)(F)F)c2)cc1)C(O)(c1ccc(-c2ccc3cccnc3n2)cc1)C(F)(F)F 10.1016/j.bmcl.2011.04.091
53358901 7909 9 None 3 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 458 7 1 5 5.1 O=C(NCc1onc(c1)c1ccc(c(c1)C(F)(F)F)F)CCCc1ccc2c(n1)nccc2 10.1016/j.bmcl.2011.04.091
5514 7909 9 None 3 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 458 7 1 5 5.1 O=C(NCc1onc(c1)c1ccc(c(c1)C(F)(F)F)F)CCCc1ccc2c(n1)nccc2 10.1016/j.bmcl.2011.04.091
CHEMBL2153581 7909 9 None 3 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 458 7 1 5 5.1 O=C(NCc1onc(c1)c1ccc(c(c1)C(F)(F)F)F)CCCc1ccc2c(n1)nccc2 10.1016/j.bmcl.2011.04.091
71462028 87704 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 433 7 1 3 5.7 O=C(CCCc1ccc2cccnc2n1)NCc1ccc(-c2ccc(F)c(Cl)c2)cc1 10.1016/j.bmcl.2011.04.091
CHEMBL2153442 87704 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 433 7 1 3 5.7 O=C(CCCc1ccc2cccnc2n1)NCc1ccc(-c2ccc(F)c(Cl)c2)cc1 10.1016/j.bmcl.2011.04.091
71462027 87702 0 None 2 3 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 415 7 1 3 5.6 O=C(CCCc1ccc2cccnc2n1)NCc1ccc(-c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.04.091
CHEMBL2153440 87702 0 None 2 3 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 415 7 1 3 5.6 O=C(CCCc1ccc2cccnc2n1)NCc1ccc(-c2cccc(Cl)c2)cc1 10.1016/j.bmcl.2011.04.091
71456641 87735 0 None 1 3 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 426 6 0 5 6.2 Clc1cccc(-c2ccc(-c3nnc(CCCc4ccc5cccnc5n4)o3)cc2)c1 10.1016/j.bmcl.2011.04.091
CHEMBL2153586 87735 0 None 1 3 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 426 6 0 5 6.2 Clc1cccc(-c2ccc(-c3nnc(CCCc4ccc5cccnc5n4)o3)cc2)c1 10.1016/j.bmcl.2011.04.091
71456643 87747 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 432 7 0 6 5.3 Fc1ccc(-c2nnc(CCCCc3ccc4cccnc4n3)o2)cc1OC(F)(F)F 10.1016/j.bmcl.2011.04.091
CHEMBL2153598 87747 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 432 7 0 6 5.3 Fc1ccc(-c2nnc(CCCCc3ccc4cccnc4n3)o2)cc1OC(F)(F)F 10.1016/j.bmcl.2011.04.091
71451309 87705 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 467 7 1 3 6.1 O=C(CCCc1ccc2cccnc2n1)NCc1ccc(-c2cccc(C(F)(F)F)c2)cc1F 10.1016/j.bmcl.2011.04.091
CHEMBL2153443 87705 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 467 7 1 3 6.1 O=C(CCCc1ccc2cccnc2n1)NCc1ccc(-c2cccc(C(F)(F)F)c2)cc1F 10.1016/j.bmcl.2011.04.091
71451318 87745 0 None -2 2 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity at rat GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at rat GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 432 6 0 5 5.9 FC(F)(F)c1cc(-c2nnc(CCCCc3ccc4cccnc4n3)o2)ccc1Cl 10.1016/j.bmcl.2011.04.091
CHEMBL2153596 87745 0 None -2 2 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity at rat GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at rat GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 432 6 0 5 5.9 FC(F)(F)c1cc(-c2nnc(CCCCc3ccc4cccnc4n3)o2)ccc1Cl 10.1016/j.bmcl.2011.04.091
71462033 87722 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 469 7 1 5 4.9 O=C(CCCc1ccc2cccnc2n1)NCc1cnc(-c2ccc(F)c(C(F)(F)F)c2)nc1 10.1016/j.bmcl.2011.04.091
CHEMBL2153469 87722 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 469 7 1 5 4.9 O=C(CCCc1ccc2cccnc2n1)NCc1cnc(-c2ccc(F)c(C(F)(F)F)c2)nc1 10.1016/j.bmcl.2011.04.091
71454858 87710 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 465 8 1 4 5.8 O=C(CCCc1ccc2cccnc2n1)NCc1ccc(-c2cccc(OC(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.04.091
CHEMBL2153448 87710 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 465 8 1 4 5.8 O=C(CCCc1ccc2cccnc2n1)NCc1ccc(-c2cccc(OC(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.04.091
162658251 187798 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assayAntagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay
ChEMBL 464 7 3 4 5.0 O=C(O)Cc1ccccc1NC(=O)c1cccc(-c2ccc(Cl)c(OC3CCCNC3)c2)c1 10.1021/acs.jmedchem.0c01020
CHEMBL4759141 187798 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assayAntagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay
ChEMBL 464 7 3 4 5.0 O=C(O)Cc1ccccc1NC(=O)c1cccc(-c2ccc(Cl)c(OC3CCCNC3)c2)c1 10.1021/acs.jmedchem.0c01020
71454857 87706 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 409 8 1 3 5.5 CCc1cccc(-c2ccc(CNC(=O)CCCc3ccc4cccnc4n3)cc2)c1 10.1016/j.bmcl.2011.04.091
CHEMBL2153444 87706 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 409 8 1 3 5.5 CCc1cccc(-c2ccc(CNC(=O)CCCc3ccc4cccnc4n3)cc2)c1 10.1016/j.bmcl.2011.04.091
71449520 87728 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 406 7 1 5 4.6 O=C(CCCc1ccc2cccnc2n1)NCc1cc(-c2cccc(Cl)c2)no1 10.1016/j.bmcl.2011.04.091
CHEMBL2153579 87728 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 406 7 1 5 4.6 O=C(CCCc1ccc2cccnc2n1)NCc1cc(-c2cccc(Cl)c2)no1 10.1016/j.bmcl.2011.04.091
71456641 87735 0 None -1 3 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at rat GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at rat GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 426 6 0 5 6.2 Clc1cccc(-c2ccc(-c3nnc(CCCc4ccc5cccnc5n4)o3)cc2)c1 10.1016/j.bmcl.2011.04.091
CHEMBL2153586 87735 0 None -1 3 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at rat GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at rat GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 426 6 0 5 6.2 Clc1cccc(-c2ccc(-c3nnc(CCCc4ccc5cccnc5n4)o3)cc2)c1 10.1016/j.bmcl.2011.04.091
53358775 87714 22 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 529 6 1 3 7.5 C[C@H](NC(=O)Cc1ccc(-c2ccc3cccnc3n2)cc1)c1ccc(-c2ccc(F)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.04.091
CHEMBL2153461 87714 22 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 529 6 1 3 7.5 C[C@H](NC(=O)Cc1ccc(-c2ccc3cccnc3n2)cc1)c1ccc(-c2ccc(F)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.04.091
53358900 87701 1 None 4 2 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity at rat GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at rat GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 395 7 1 3 5.2 Cc1cccc(-c2ccc(CNC(=O)CCCc3ccc4cccnc4n3)cc2)c1 10.1016/j.bmcl.2011.04.091
CHEMBL2153439 87701 1 None 4 2 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity at rat GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at rat GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 395 7 1 3 5.2 Cc1cccc(-c2ccc(CNC(=O)CCCc3ccc4cccnc4n3)cc2)c1 10.1016/j.bmcl.2011.04.091
71454869 87731 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 422 7 1 5 5.0 O=C(CCCc1ccc2cccnc2n1)NCc1csc(-c2cccc(Cl)c2)n1 10.1016/j.bmcl.2011.04.091
CHEMBL2153582 87731 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 422 7 1 5 5.0 O=C(CCCc1ccc2cccnc2n1)NCc1csc(-c2cccc(Cl)c2)n1 10.1016/j.bmcl.2011.04.091
71453125 87725 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 469 7 1 5 4.9 O=C(CCCc1ccc2cccnc2n1)NCc1ccc(-c2ccc(F)c(C(F)(F)F)c2)nn1 10.1016/j.bmcl.2011.04.091
CHEMBL2153471 87725 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 469 7 1 5 4.9 O=C(CCCc1ccc2cccnc2n1)NCc1ccc(-c2ccc(F)c(C(F)(F)F)c2)nn1 10.1016/j.bmcl.2011.04.091
71462031 87713 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 515 6 1 3 7.0 O=C(Cc1ccc(-c2ccc3cccnc3n2)cc1)NCc1ccc(-c2ccc(F)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.04.091
CHEMBL2153460 87713 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 515 6 1 3 7.0 O=C(Cc1ccc(-c2ccc3cccnc3n2)cc1)NCc1ccc(-c2ccc(F)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.04.091
162659507 188154 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assayAntagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay
ChEMBL 482 7 3 4 5.2 O=C(O)Cc1ccccc1NC(=O)c1cccc(-c2ccc(Cl)c(O[C@@H]3CCCNC3)c2F)c1 10.1021/acs.jmedchem.0c01020
CHEMBL4763307 188154 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assayAntagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay
ChEMBL 482 7 3 4 5.2 O=C(O)Cc1ccccc1NC(=O)c1cccc(-c2ccc(Cl)c(O[C@@H]3CCCNC3)c2F)c1 10.1021/acs.jmedchem.0c01020
71449505 87699 0 None 3 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 475 8 1 5 5.0 COC(=O)c1c(F)cccc1-c1ccc(CNC(=O)CCCc2ccc3cccnc3n2)c(F)c1 10.1016/j.bmcl.2011.04.091
CHEMBL2153436 87699 0 None 3 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 475 8 1 5 5.0 COC(=O)c1c(F)cccc1-c1ccc(CNC(=O)CCCc2ccc3cccnc3n2)c(F)c1 10.1016/j.bmcl.2011.04.091
154585554 187138 5 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assayAntagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay
ChEMBL 518 7 3 4 5.4 O=C(O)Cc1cc(F)ccc1NC(=O)c1cccc(-c2cc(O[C@@H]3CCCNC3)c(Cl)cc2F)c1F 10.1021/acs.jmedchem.0c01020
CHEMBL4751488 187138 5 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assayAntagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay
ChEMBL 518 7 3 4 5.4 O=C(O)Cc1cc(F)ccc1NC(=O)c1cccc(-c2cc(O[C@@H]3CCCNC3)c(Cl)cc2F)c1F 10.1021/acs.jmedchem.0c01020
71453138 87730 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 424 7 1 5 4.7 O=C(CCCc1ccc2cccnc2n1)NCc1cc(-c2ccc(F)c(Cl)c2)no1 10.1016/j.bmcl.2011.04.091
CHEMBL2153580 87730 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assayAntagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
ChEMBL 424 7 1 5 4.7 O=C(CCCc1ccc2cccnc2n1)NCc1cc(-c2ccc(F)c(Cl)c2)no1 10.1016/j.bmcl.2011.04.091
162657186 187624 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assayAntagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay
ChEMBL 500 7 3 4 5.3 O=C(O)Cc1cc(F)ccc1NC(=O)c1cccc(-c2cc(O[C@@H]3CCCNC3)c(Cl)cc2F)c1 10.1021/acs.jmedchem.0c01020
CHEMBL4757124 187624 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assayAntagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay
ChEMBL 500 7 3 4 5.3 O=C(O)Cc1cc(F)ccc1NC(=O)c1cccc(-c2cc(O[C@@H]3CCCNC3)c(Cl)cc2F)c1 10.1021/acs.jmedchem.0c01020
162652581 187243 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assayAntagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay
ChEMBL 500 7 3 4 5.3 O=C(O)Cc1cc(F)ccc1NC(=O)c1cccc(-c2ccc(Cl)c(O[C@@H]3CCCNC3)c2F)c1 10.1021/acs.jmedchem.0c01020
CHEMBL4752851 187243 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assayAntagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay
ChEMBL 500 7 3 4 5.3 O=C(O)Cc1cc(F)ccc1NC(=O)c1cccc(-c2ccc(Cl)c(O[C@@H]3CCCNC3)c2F)c1 10.1021/acs.jmedchem.0c01020
1110 10470 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 118 3 2 2 -0.1 OC(=O)CCC(=O)O None
21952380 10470 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 118 3 2 2 -0.1 OC(=O)CCC(=O)O None
2487 10470 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 118 3 2 2 -0.1 OC(=O)CCC(=O)O None
3637 10470 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 118 3 2 2 -0.1 OC(=O)CCC(=O)O None
CHEMBL576 10470 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 118 3 2 2 -0.1 OC(=O)CCC(=O)O None
DB00139 10470 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 118 3 2 2 -0.1 OC(=O)CCC(=O)O None
10296 7854 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
IP<sub>3</sub> accumulation, E<sub>max</sub>=61%IP<sub>3</sub> accumulation, E<sub>max</sub>=61%
Guide to Pharmacology 396 7 1 7 -0.4 [O-]C(=O)C[C@@H](C(=O)[O-])NC(=O)c1cccc(n1)c1ccc(cc1)OC(F)(F)F 29968758
137553167 7854 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
IP<sub>3</sub> accumulation, E<sub>max</sub>=61%IP<sub>3</sub> accumulation, E<sub>max</sub>=61%
Guide to Pharmacology 396 7 1 7 -0.4 [O-]C(=O)C[C@@H](C(=O)[O-])NC(=O)c1cccc(n1)c1ccc(cc1)OC(F)(F)F 29968758
10294 7769 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
IP<sub>3</sub> accumulation, E<sub>max</sub>=75%IP<sub>3</sub> accumulation, E<sub>max</sub>=75%
Guide to Pharmacology 321 6 3 4 1.7 O=C(c1ccc(o1)c1ccc(cc1)F)N[C@H](C(=O)O)CC(=O)O 29157600
41023370 7769 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
IP<sub>3</sub> accumulation, E<sub>max</sub>=75%IP<sub>3</sub> accumulation, E<sub>max</sub>=75%
Guide to Pharmacology 321 6 3 4 1.7 O=C(c1ccc(o1)c1ccc(cc1)F)N[C@H](C(=O)O)CC(=O)O 29157600
2734802 8765 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
IP<sub>3</sub> accumulation, E<sub>max</sub>=93%IP<sub>3</sub> accumulation, E<sub>max</sub>=93%
Guide to Pharmacology 132 2 2 3 -1.1 OC(=O)[C@@H]1O[C@@H]1C(=O)O 29157600
9631 8765 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
IP<sub>3</sub> accumulation, E<sub>max</sub>=93%IP<sub>3</sub> accumulation, E<sub>max</sub>=93%
Guide to Pharmacology 132 2 2 3 -1.1 OC(=O)[C@@H]1O[C@@H]1C(=O)O 29157600
CHEMBL1741775 8765 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
IP<sub>3</sub> accumulation, E<sub>max</sub>=93%IP<sub>3</sub> accumulation, E<sub>max</sub>=93%
Guide to Pharmacology 132 2 2 3 -1.1 OC(=O)[C@@H]1O[C@@H]1C(=O)O 29157600
487 9290 0 None - 1 Human 3.6 pEC50 = 3.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 118 2 2 2 -0.2 CC(C(=O)O)C(=O)O 15141213
9633 9290 0 None - 1 Human 3.6 pEC50 = 3.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 118 2 2 2 -0.2 CC(C(=O)O)C(=O)O 15141213
CHEMBL1232416 9290 0 None - 1 Human 3.6 pEC50 = 3.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 118 2 2 2 -0.2 CC(C(=O)O)C(=O)O 15141213
DB04183 9290 0 None - 1 Human 3.6 pEC50 = 3.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 118 2 2 2 -0.2 CC(C(=O)O)C(=O)O 15141213
487 9290 0 None - 1 Human 3.8 pEC50 = 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 118 2 2 2 -0.2 CC(C(=O)O)C(=O)O 28160606
9633 9290 0 None - 1 Human 3.8 pEC50 = 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 118 2 2 2 -0.2 CC(C(=O)O)C(=O)O 28160606
CHEMBL1232416 9290 0 None - 1 Human 3.8 pEC50 = 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 118 2 2 2 -0.2 CC(C(=O)O)C(=O)O 28160606
DB04183 9290 0 None - 1 Human 3.8 pEC50 = 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 118 2 2 2 -0.2 CC(C(=O)O)C(=O)O 28160606
1110 10470 0 None - 1 Human 3.9 pEC50 = 3.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 118 3 2 2 -0.1 OC(=O)CCC(=O)O 15141213
1110 10470 0 None - 1 Human 3.9 pEC50 = 3.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 118 3 2 2 -0.1 OC(=O)CCC(=O)O 23396314
21952380 10470 0 None - 1 Human 3.9 pEC50 = 3.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 118 3 2 2 -0.1 OC(=O)CCC(=O)O 15141213
21952380 10470 0 None - 1 Human 3.9 pEC50 = 3.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 118 3 2 2 -0.1 OC(=O)CCC(=O)O 23396314
2487 10470 0 None - 1 Human 3.9 pEC50 = 3.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 118 3 2 2 -0.1 OC(=O)CCC(=O)O 15141213
2487 10470 0 None - 1 Human 3.9 pEC50 = 3.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 118 3 2 2 -0.1 OC(=O)CCC(=O)O 23396314
3637 10470 0 None - 1 Human 3.9 pEC50 = 3.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 118 3 2 2 -0.1 OC(=O)CCC(=O)O 15141213
3637 10470 0 None - 1 Human 3.9 pEC50 = 3.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 118 3 2 2 -0.1 OC(=O)CCC(=O)O 23396314
CHEMBL576 10470 0 None - 1 Human 3.9 pEC50 = 3.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 118 3 2 2 -0.1 OC(=O)CCC(=O)O 15141213
CHEMBL576 10470 0 None - 1 Human 3.9 pEC50 = 3.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 118 3 2 2 -0.1 OC(=O)CCC(=O)O 23396314
DB00139 10470 0 None - 1 Human 3.9 pEC50 = 3.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 118 3 2 2 -0.1 OC(=O)CCC(=O)O 15141213
DB00139 10470 0 None - 1 Human 3.9 pEC50 = 3.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 118 3 2 2 -0.1 OC(=O)CCC(=O)O 23396314
444266 9233 72 None -2818 2 Human 4.1 pEC50 = 4.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 116 2 2 2 -0.3 OC(=O)/C=C\C(=O)O 15141213
444266 9233 72 None -2818 2 Human 4.1 pEC50 = 4.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 116 2 2 2 -0.3 OC(=O)/C=C\C(=O)O 26386312
444266 9233 72 None -2818 2 Human 4.1 pEC50 = 4.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 116 2 2 2 -0.3 OC(=O)/C=C\C(=O)O 28160606
9630 9233 72 None -2818 2 Human 4.1 pEC50 = 4.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 116 2 2 2 -0.3 OC(=O)/C=C\C(=O)O 15141213
9630 9233 72 None -2818 2 Human 4.1 pEC50 = 4.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 116 2 2 2 -0.3 OC(=O)/C=C\C(=O)O 26386312
9630 9233 72 None -2818 2 Human 4.1 pEC50 = 4.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 116 2 2 2 -0.3 OC(=O)/C=C\C(=O)O 28160606
CHEMBL539648 9233 72 None -2818 2 Human 4.1 pEC50 = 4.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 116 2 2 2 -0.3 OC(=O)/C=C\C(=O)O 15141213
CHEMBL539648 9233 72 None -2818 2 Human 4.1 pEC50 = 4.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 116 2 2 2 -0.3 OC(=O)/C=C\C(=O)O 26386312
CHEMBL539648 9233 72 None -2818 2 Human 4.1 pEC50 = 4.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 116 2 2 2 -0.3 OC(=O)/C=C\C(=O)O 28160606
DB04299 9233 72 None -2818 2 Human 4.1 pEC50 = 4.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 116 2 2 2 -0.3 OC(=O)/C=C\C(=O)O 15141213
DB04299 9233 72 None -2818 2 Human 4.1 pEC50 = 4.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 116 2 2 2 -0.3 OC(=O)/C=C\C(=O)O 26386312
DB04299 9233 72 None -2818 2 Human 4.1 pEC50 = 4.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 116 2 2 2 -0.3 OC(=O)/C=C\C(=O)O 28160606
9634 10333 0 None - 1 Human 4.1 pEC50 = 4.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 152 3 2 2 0.2 OC(=O)C[C@@H](C(=O)O)Cl 28160606
9793861 10333 0 None - 1 Human 4.1 pEC50 = 4.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 152 3 2 2 0.2 OC(=O)C[C@@H](C(=O)O)Cl 28160606
726455 8764 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 130 2 2 2 -0.2 OC(=O)[C@@H]1C[C@@H]1C(=O)O 28160606
9632 8764 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 130 2 2 2 -0.2 OC(=O)[C@@H]1C[C@@H]1C(=O)O 28160606
2734802 8765 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
cAMP inhibition, E<sub>max</sub>=100%cAMP inhibition, E<sub>max</sub>=100%
Guide to Pharmacology 132 2 2 3 -1.1 OC(=O)[C@@H]1O[C@@H]1C(=O)O 28160606
9631 8765 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
cAMP inhibition, E<sub>max</sub>=100%cAMP inhibition, E<sub>max</sub>=100%
Guide to Pharmacology 132 2 2 3 -1.1 OC(=O)[C@@H]1O[C@@H]1C(=O)O 28160606
CHEMBL1741775 8765 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
cAMP inhibition, E<sub>max</sub>=100%cAMP inhibition, E<sub>max</sub>=100%
Guide to Pharmacology 132 2 2 3 -1.1 OC(=O)[C@@H]1O[C@@H]1C(=O)O 28160606
5515 7921 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 533 11 1 7 5.7 O=C(NCCCCc1nnc(o1)c1ccc(c(c1)Cl)OC(F)(F)F)CCCc1ccc2c(n1)nccc2 21571530
73755126 7921 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 533 11 1 7 5.7 O=C(NCCCCc1nnc(o1)c1ccc(c(c1)Cl)OC(F)(F)F)CCCc1ccc2c(n1)nccc2 21571530
53358901 7909 9 None -3 2 Rat 6.9 pIC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 458 7 1 5 5.1 O=C(NCc1onc(c1)c1ccc(c(c1)C(F)(F)F)F)CCCc1ccc2c(n1)nccc2 21571530
5514 7909 9 None -3 2 Rat 6.9 pIC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 458 7 1 5 5.1 O=C(NCc1onc(c1)c1ccc(c(c1)C(F)(F)F)F)CCCc1ccc2c(n1)nccc2 21571530
CHEMBL2153581 7909 9 None -3 2 Rat 6.9 pIC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 458 7 1 5 5.1 O=C(NCc1onc(c1)c1ccc(c(c1)C(F)(F)F)F)CCCc1ccc2c(n1)nccc2 21571530
53358901 7909 9 None 3 2 Human 7.5 pIC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 458 7 1 5 5.1 O=C(NCc1onc(c1)c1ccc(c(c1)C(F)(F)F)F)CCCc1ccc2c(n1)nccc2 21571530
5514 7909 9 None 3 2 Human 7.5 pIC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 458 7 1 5 5.1 O=C(NCc1onc(c1)c1ccc(c(c1)C(F)(F)F)F)CCCc1ccc2c(n1)nccc2 21571530
CHEMBL2153581 7909 9 None 3 2 Human 7.5 pIC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 458 7 1 5 5.1 O=C(NCc1onc(c1)c1ccc(c(c1)C(F)(F)F)F)CCCc1ccc2c(n1)nccc2 21571530




Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Affinity)
# tested GPCRs
(Affinity)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
10519 9589 23 None - 1 Human 7.5 pKd = 7.5 Binding
Dissociation constant for [<sup>3</sup>H]-labelled NF-56-EJ40 binding to human SUCNR1 determined in a radioligand binding assay.Dissociation constant for [<sup>3</sup>H]-labelled NF-56-EJ40 binding to human SUCNR1 determined in a radioligand binding assay.
Guide to Pharmacology 443 7 2 4 4.0 CN1CCN(CC1)Cc1ccc(cc1)c1cccc(c1)C(=O)Nc1ccccc1CC(=O)O 31645725
138811017 9589 23 None - 1 Human 7.5 pKd = 7.5 Binding
Dissociation constant for [<sup>3</sup>H]-labelled NF-56-EJ40 binding to human SUCNR1 determined in a radioligand binding assay.Dissociation constant for [<sup>3</sup>H]-labelled NF-56-EJ40 binding to human SUCNR1 determined in a radioligand binding assay.
Guide to Pharmacology 443 7 2 4 4.0 CN1CCN(CC1)Cc1ccc(cc1)c1cccc(c1)C(=O)Nc1ccccc1CC(=O)O 31645725
CHEMBL4790324 9589 23 None - 1 Human 7.5 pKd = 7.5 Binding
Dissociation constant for [<sup>3</sup>H]-labelled NF-56-EJ40 binding to human SUCNR1 determined in a radioligand binding assay.Dissociation constant for [<sup>3</sup>H]-labelled NF-56-EJ40 binding to human SUCNR1 determined in a radioligand binding assay.
Guide to Pharmacology 443 7 2 4 4.0 CN1CCN(CC1)Cc1ccc(cc1)c1cccc(c1)C(=O)Nc1ccccc1CC(=O)O 31645725
10519 9589 23 None - 1 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 443 7 2 4 4.0 CN1CCN(CC1)Cc1ccc(cc1)c1cccc(c1)C(=O)Nc1ccccc1CC(=O)O 31645725
138811017 9589 23 None - 1 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 443 7 2 4 4.0 CN1CCN(CC1)Cc1ccc(cc1)c1cccc(c1)C(=O)Nc1ccccc1CC(=O)O 31645725
CHEMBL4790324 9589 23 None - 1 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 443 7 2 4 4.0 CN1CCN(CC1)Cc1ccc(cc1)c1cccc(c1)C(=O)Nc1ccccc1CC(=O)O 31645725