Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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ID		 #Vendors

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ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 AssayType

 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
156013464 177497 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 486 6 2 7 4.7 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2ncc(-c3ccccc3)s2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4639430 177497 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 486 6 2 7 4.7 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2ncc(-c3ccccc3)s2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
58345681 134447 1 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 226 1 2 5 1.7 Nc1nc2ccc(O)nc2n1-c1ccccc1 nan
CHEMBL3717589 134447 1 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 226 1 2 5 1.7 Nc1nc2ccc(O)nc2n1-c1ccccc1 nan
156019324 177974 0 None 14 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 530 7 1 8 4.9 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(OC4CCN(C)CC4)cc3s2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4646005 177974 0 None 14 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 530 7 1 8 4.9 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(OC4CCN(C)CC4)cc3s2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
145985690 165443 0 None 1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 464 5 2 7 3.9 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3c(s2)CCCC3)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4239086 165443 0 None 1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 464 5 2 7 3.9 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3c(s2)CCCC3)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
156009938 177037 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 556 7 2 8 4.7 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(CN4CCN(C)CC4)cc3s2)cc1N1CCCC1 10.1016/j.bmcl.2020.126953
CHEMBL4632482 177037 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 556 7 2 8 4.7 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(CN4CCN(C)CC4)cc3s2)cc1N1CCCC1 10.1016/j.bmcl.2020.126953
58345670 134760 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 313 1 1 4 3.8 Oc1ccc2ncn(-c3ccc(Cl)cc3C(F)(F)F)c2n1 nan
CHEMBL3718634 134760 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 313 1 1 4 3.8 Oc1ccc2ncn(-c3ccc(Cl)cc3C(F)(F)F)c2n1 nan
58345743 133643 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 328 1 2 5 3.7 Nc1nc2ccc(O)nc2n1-c1ccc(Cl)c(Cl)c1Cl nan
CHEMBL3714817 133643 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 328 1 2 5 3.7 Nc1nc2ccc(O)nc2n1-c1ccc(Cl)c(Cl)c1Cl nan
58345768 133657 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 285 2 1 4 3.7 Oc1ccc2nc(C3CC3)n(-c3ccccc3Cl)c2n1 nan
CHEMBL3714879 133657 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 285 2 1 4 3.7 Oc1ccc2nc(C3CC3)n(-c3ccccc3Cl)c2n1 nan
58345668 133658 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 304 1 2 5 2.5 Nc1nc2ccc(O)nc2n1-c1ccc(Br)cc1 nan
CHEMBL3714885 133658 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 304 1 2 5 2.5 Nc1nc2ccc(O)nc2n1-c1ccc(Br)cc1 nan
58345728 133665 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 347 1 1 4 4.2 Oc1ccc2ncn(-c3ccc(C(F)(F)F)cc3C(F)(F)F)c2n1 nan
CHEMBL3714909 133665 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 347 1 1 4 4.2 Oc1ccc2ncn(-c3ccc(C(F)(F)F)cc3C(F)(F)F)c2n1 nan
58345725 133681 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 367 1 1 4 3.7 Oc1ccc2nc(Br)n(-c3ccccc3Br)c2n1 nan
CHEMBL3714960 133681 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 367 1 1 4 3.7 Oc1ccc2nc(Br)n(-c3ccccc3Br)c2n1 nan
58345654 133684 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 243 1 1 4 2.6 Cc1cc(F)ccc1-n1cnc2ccc(O)nc21 nan
CHEMBL3714970 133684 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 243 1 1 4 2.6 Cc1cc(F)ccc1-n1cnc2ccc(O)nc21 nan
58345758 133698 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 278 1 2 5 2.5 Nc1nc2ccc(O)nc2n1-c1cccc(F)c1Cl nan
CHEMBL3715004 133698 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 278 1 2 5 2.5 Nc1nc2ccc(O)nc2n1-c1cccc(F)c1Cl nan
58345741 133704 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 239 1 1 4 2.7 Cc1ccc(-n2c(C)nc3ccc(O)nc32)cc1 nan
CHEMBL3715017 133704 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 239 1 1 4 2.7 Cc1ccc(-n2c(C)nc3ccc(O)nc32)cc1 nan
58345706 133723 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 253 3 1 4 3.1 CCCc1nc2ccc(O)nc2n1-c1ccccc1 nan
CHEMBL3715077 133723 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 253 3 1 4 3.1 CCCc1nc2ccc(O)nc2n1-c1ccccc1 nan
58345750 133746 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 255 1 1 6 1.9 Oc1ccc2ncn(-c3ccc4c(c3)OCO4)c2n1 nan
CHEMBL3715155 133746 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 255 1 1 6 1.9 Oc1ccc2ncn(-c3ccc4c(c3)OCO4)c2n1 nan
58345653 133754 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 303 1 1 4 3.2 Cc1nc2ccc(O)nc2n1-c1ccccc1Br nan
CHEMBL3715174 133754 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 303 1 1 4 3.2 Cc1nc2ccc(O)nc2n1-c1ccccc1Br nan
58345739 133766 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 247 1 1 4 2.4 Oc1ccc2ncn(-c3cccc(F)c3F)c2n1 nan
CHEMBL3715218 133766 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 247 1 1 4 2.4 Oc1ccc2ncn(-c3cccc(F)c3F)c2n1 nan
58345704 133793 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 245 1 1 4 3.4 Oc1ccc2ncn(C3CCCCCCC3)c2n1 nan
CHEMBL3715359 133793 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 245 1 1 4 3.4 Oc1ccc2ncn(C3CCCCCCC3)c2n1 nan
58345713 133794 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 328 1 2 5 3.7 Nc1nc2ccc(O)nc2n1-c1cc(Cl)c(Cl)cc1Cl nan
CHEMBL3715361 133794 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 328 1 2 5 3.7 Nc1nc2ccc(O)nc2n1-c1cc(Cl)c(Cl)cc1Cl nan
58345751 133802 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 244 1 2 5 1.8 Nc1nc2ccc(O)nc2n1-c1ccccc1F nan
CHEMBL3715394 133802 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 244 1 2 5 1.8 Nc1nc2ccc(O)nc2n1-c1ccccc1F nan
58345683 133823 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 295 2 1 5 3.0 Oc1ccc2ncn(-c3ccccc3OC(F)(F)F)c2n1 nan
CHEMBL3715478 133823 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 295 2 1 5 3.0 Oc1ccc2ncn(-c3ccccc3OC(F)(F)F)c2n1 nan
58345724 133838 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 253 1 1 4 3.1 Cc1cccc(-n2c(C)nc3ccc(O)nc32)c1C nan
CHEMBL3715536 133838 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 253 1 1 4 3.1 Cc1cccc(-n2c(C)nc3ccc(O)nc32)c1C nan
58345682 133846 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 275 1 1 4 3.6 Cc1nc2ccc(O)nc2n1-c1cccc2ccccc12 nan
CHEMBL3715558 133846 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 275 1 1 4 3.6 Cc1nc2ccc(O)nc2n1-c1cccc2ccccc12 nan
58345677 133850 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 284 1 2 5 2.6 Nc1nc2ccc(O)nc2n1C12CC3CC(CC(C3)C1)C2 nan
CHEMBL3715572 133850 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 284 1 2 5 2.6 Nc1nc2ccc(O)nc2n1C12CC3CC(CC(C3)C1)C2 nan
46830068 133852 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 245 1 1 4 2.8 Oc1ccc2ncn(-c3ccccc3Cl)c2n1 nan
CHEMBL3715577 133852 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 245 1 1 4 2.8 Oc1ccc2ncn(-c3ccccc3Cl)c2n1 nan
58345738 133858 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 233 1 2 5 1.6 Oc1ccc2ncn(C3CCCCC3O)c2n1 nan
CHEMBL3715599 133858 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 233 1 2 5 1.6 Oc1ccc2ncn(C3CCCCC3O)c2n1 nan
58345667 133860 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 265 1 1 4 3.5 CC1CCCCC1n1c(Cl)nc2ccc(O)nc21 nan
CHEMBL3715601 133860 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 265 1 1 4 3.5 CC1CCCCC1n1c(Cl)nc2ccc(O)nc21 nan
58345753 133863 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 247 1 2 5 2.0 Oc1ccc2ncn(C3CCCCCC3O)c2n1 nan
CHEMBL3715611 133863 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 247 1 2 5 2.0 Oc1ccc2ncn(C3CCCCCC3O)c2n1 nan
58345771 133866 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 231 1 1 4 2.8 CC1(n2cnc3ccc(O)nc32)CCCCC1 nan
CHEMBL3715620 133866 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 231 1 1 4 2.8 CC1(n2cnc3ccc(O)nc32)CCCCC1 nan
58345698 133881 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 235 1 1 5 2.2 Oc1ccc2ncn(C3CCSCC3)c2n1 nan
CHEMBL3715673 133881 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 235 1 1 5 2.2 Oc1ccc2ncn(C3CCSCC3)c2n1 nan
67312894 133909 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 289 1 1 4 3.9 Cc1ccc2ccccc2c1-n1c(C)nc2ccc(O)nc21 nan
CHEMBL3715748 133909 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 289 1 1 4 3.9 Cc1ccc2ccccc2c1-n1c(C)nc2ccc(O)nc21 nan
58345684 133920 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 295 1 1 4 3.9 Oc1ccc2ncn(-c3ccc(Cl)c4ccccc34)c2n1 nan
CHEMBL3715778 133920 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 295 1 1 4 3.9 Oc1ccc2ncn(-c3ccc(Cl)c4ccccc34)c2n1 nan
58345752 133927 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 245 1 1 4 3.1 Cc1nc2ccc(O)nc2n1C1(C)CCCCC1 nan
CHEMBL3715818 133927 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 245 1 1 4 3.1 Cc1nc2ccc(O)nc2n1C1(C)CCCCC1 nan
58345726 133931 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 253 2 1 4 3.0 CCc1ccc(-n2c(C)nc3ccc(O)nc32)cc1 nan
CHEMBL3715837 133931 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 253 2 1 4 3.0 CCc1ccc(-n2c(C)nc3ccc(O)nc32)cc1 nan
58345765 133946 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 325 2 1 5 4.0 Cc1nc2ccc(O)nc2n1-c1ccccc1SC(F)(F)F nan
CHEMBL3715889 133946 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 325 2 1 5 4.0 Cc1nc2ccc(O)nc2n1-c1ccccc1SC(F)(F)F nan
58345697 133947 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 256 2 1 6 2.0 O=[N+]([O-])c1ccccc1-n1cnc2ccc(O)nc21 nan
CHEMBL3715890 133947 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 256 2 1 6 2.0 O=[N+]([O-])c1ccccc1-n1cnc2ccc(O)nc21 nan
58345672 133955 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 239 1 1 4 2.7 Cc1cc(C)cc(-n2cnc3ccc(O)nc32)c1 nan
CHEMBL3715915 133955 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 239 1 1 4 2.7 Cc1cc(C)cc(-n2cnc3ccc(O)nc32)c1 nan
58345731 133956 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 329 2 1 5 3.7 Oc1ccc2nc(Cl)n(-c3ccccc3OC(F)(F)F)c2n1 nan
CHEMBL3715916 133956 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 329 2 1 5 3.7 Oc1ccc2nc(Cl)n(-c3ccccc3OC(F)(F)F)c2n1 nan
58345656 133960 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 345 2 1 5 4.4 Oc1ccc2nc(Cl)n(-c3ccccc3SC(F)(F)F)c2n1 nan
CHEMBL3715927 133960 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 345 2 1 5 4.4 Oc1ccc2nc(Cl)n(-c3ccccc3SC(F)(F)F)c2n1 nan
58345659 133966 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 251 1 1 4 2.6 Oc1ccc2ncn(-c3ccc4c(c3)CCC4)c2n1 nan
CHEMBL3715949 133966 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 251 1 1 4 2.6 Oc1ccc2ncn(-c3ccc4c(c3)CCC4)c2n1 nan
58345692 133990 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 274 1 2 5 2.7 Cc1c(Cl)cccc1-n1c(N)nc2ccc(O)nc21 nan
CHEMBL3716036 133990 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 274 1 2 5 2.7 Cc1c(Cl)cccc1-n1c(N)nc2ccc(O)nc21 nan
58345694 133992 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 239 2 1 4 2.7 CCc1ccccc1-n1cnc2ccc(O)nc21 nan
CHEMBL3716041 133992 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 239 2 1 4 2.7 CCc1ccccc1-n1cnc2ccc(O)nc21 nan
58345733 134005 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 317 1 1 4 3.5 Cc1cccc(-n2c(C)nc3ccc(O)nc32)c1Br nan
CHEMBL3716083 134005 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 317 1 1 4 3.5 Cc1cccc(-n2c(C)nc3ccc(O)nc32)c1Br nan
86655263 134016 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 383 3 1 7 2.2 CS(=O)(=O)Oc1ccc2nc(O)n(-c3ccccc3Br)c2n1 nan
CHEMBL3716136 134016 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 383 3 1 7 2.2 CS(=O)(=O)Oc1ccc2nc(O)n(-c3ccccc3Br)c2n1 nan
58345650 134035 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 287 2 1 4 3.8 Oc1ccc2nc(-c3ccccc3)n(-c3ccccc3)c2n1 nan
CHEMBL3716180 134035 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 287 2 1 4 3.8 Oc1ccc2nc(-c3ccccc3)n(-c3ccccc3)c2n1 nan
58345686 134055 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 241 2 1 5 2.1 COc1ccc(-n2cnc3ccc(O)nc32)cc1 nan
CHEMBL3716252 134055 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 241 2 1 5 2.1 COc1ccc(-n2cnc3ccc(O)nc32)cc1 nan
58345723 134056 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 231 1 1 4 3.0 Cc1nc2ccc(O)nc2n1C1CCCCC1 nan
CHEMBL3716253 134056 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 231 1 1 4 3.0 Cc1nc2ccc(O)nc2n1C1CCCCC1 nan
58345735 134060 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 297 1 1 4 3.3 Oc1ccc2ncn(-c3ccc(F)cc3C(F)(F)F)c2n1 nan
CHEMBL3716263 134060 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 297 1 1 4 3.3 Oc1ccc2ncn(-c3ccc(F)cc3C(F)(F)F)c2n1 nan
58345707 134063 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 219 1 1 5 1.5 Oc1ccc2ncn(C3CCOCC3)c2n1 nan
CHEMBL3716273 134063 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 219 1 1 5 1.5 Oc1ccc2ncn(C3CCOCC3)c2n1 nan
58345635 134068 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 239 1 1 4 2.7 Cc1ccc(C)c(-n2cnc3ccc(O)nc32)c1 nan
CHEMBL3716281 134068 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 239 1 1 4 2.7 Cc1ccc(C)c(-n2cnc3ccc(O)nc32)c1 nan
58345663 134071 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 253 2 1 4 3.3 CC(C)c1ccccc1-n1cnc2ccc(O)nc21 nan
CHEMBL3716287 134071 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 253 2 1 4 3.3 CC(C)c1ccccc1-n1cnc2ccc(O)nc21 nan
58345691 134075 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 251 2 1 4 3.0 Oc1ccc2ncn(-c3ccccc3C3CC3)c2n1 nan
CHEMBL3716302 134075 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 251 2 1 4 3.0 Oc1ccc2ncn(-c3ccccc3C3CC3)c2n1 nan
58345708 134091 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 279 1 1 4 3.4 Oc1ccc2nc(Cl)n(-c3ccccc3Cl)c2n1 nan
CHEMBL3716351 134091 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 279 1 1 4 3.4 Oc1ccc2nc(Cl)n(-c3ccccc3Cl)c2n1 nan
58345763 134096 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 267 1 1 4 3.3 Oc1ccc2ncn(C3CCCCCC3(F)F)c2n1 nan
CHEMBL3716370 134096 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 267 1 1 4 3.3 Oc1ccc2ncn(C3CCCCCC3(F)F)c2n1 nan
58345693 134114 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 261 1 1 4 3.3 Oc1ccc2ncn(-c3cccc4ccccc34)c2n1 nan
CHEMBL3716441 134114 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 261 1 1 4 3.3 Oc1ccc2ncn(-c3cccc4ccccc34)c2n1 nan
58345634 134123 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 246 1 2 5 2.6 Nc1nc2ccc(O)nc2n1C1CCCCCC1 nan
CHEMBL3716479 134123 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 246 1 2 5 2.6 Nc1nc2ccc(O)nc2n1C1CCCCCC1 nan
58345729 134127 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 231 1 1 5 1.8 O=C1CCCCC1n1cnc2ccc(O)nc21 nan
CHEMBL3716494 134127 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 231 1 1 5 1.8 O=C1CCCCC1n1cnc2ccc(O)nc21 nan
58345695 134129 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 297 1 1 4 3.3 Oc1ccc2ncn(-c3cccc(C(F)(F)F)c3F)c2n1 nan
CHEMBL3716500 134129 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 297 1 1 4 3.3 Oc1ccc2ncn(-c3cccc(C(F)(F)F)c3F)c2n1 nan
58345655 134130 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 254 2 2 5 2.3 CCc1ccc(-n2c(N)nc3ccc(O)nc32)cc1 nan
CHEMBL3716501 134130 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 254 2 2 5 2.3 CCc1ccc(-n2c(N)nc3ccc(O)nc32)cc1 nan
58345665 134145 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 239 1 1 4 2.7 Cc1ccc(-n2cnc3ccc(O)nc32)cc1C nan
CHEMBL3716553 134145 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 239 1 1 4 2.7 Cc1ccc(-n2cnc3ccc(O)nc32)cc1C nan
58345646 134162 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 335 3 1 5 3.9 Oc1ccc2nc(C3CC3)n(-c3ccccc3OC(F)(F)F)c2n1 nan
CHEMBL3716607 134162 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 335 3 1 5 3.9 Oc1ccc2nc(C3CC3)n(-c3ccccc3OC(F)(F)F)c2n1 nan
58345770 134167 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 229 1 1 4 2.3 Oc1ccc2ncn(-c3ccc(F)cc3)c2n1 nan
CHEMBL3716628 134167 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 229 1 1 4 2.3 Oc1ccc2ncn(-c3ccc(F)cc3)c2n1 nan
58345647 134172 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 229 1 1 4 2.5 Oc1ccc2ncn(C3CC4CCC3C4)c2n1 nan
CHEMBL3716637 134172 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 229 1 1 4 2.5 Oc1ccc2ncn(C3CC4CCC3C4)c2n1 nan
58345757 134179 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 259 2 1 4 3.5 CCC1(n2c(C)nc3ccc(O)nc32)CCCCC1 nan
CHEMBL3716678 134179 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 259 2 1 4 3.5 CCC1(n2c(C)nc3ccc(O)nc32)CCCCC1 nan
58345645 134181 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 225 1 1 4 2.4 Cc1ccc(-n2cnc3ccc(O)nc32)cc1 nan
CHEMBL3716686 134181 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 225 1 1 4 2.4 Cc1ccc(-n2cnc3ccc(O)nc32)cc1 nan
58345761 134233 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 245 1 1 5 2.2 O=C1CCCCCC1n1cnc2ccc(O)nc21 nan
CHEMBL3716863 134233 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 245 1 1 5 2.2 O=C1CCCCCC1n1cnc2ccc(O)nc21 nan
58345737 134251 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 263 1 1 4 2.9 Oc1ccc2ncn(-c3cccc(F)c3Cl)c2n1 nan
CHEMBL3716914 134251 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 263 1 1 4 2.9 Oc1ccc2ncn(-c3cccc(F)c3Cl)c2n1 nan
58345709 134258 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 233 1 2 5 1.6 Oc1ccc2ncn(C3CCC(O)CC3)c2n1 nan
CHEMBL3716940 134258 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 233 1 2 5 1.6 Oc1ccc2ncn(C3CCC(O)CC3)c2n1 nan
58345722 134274 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 259 1 1 4 3.1 Cc1c(Cl)cccc1-n1cnc2ccc(O)nc21 nan
CHEMBL3716993 134274 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 259 1 1 4 3.1 Cc1c(Cl)cccc1-n1cnc2ccc(O)nc21 nan
58345643 134275 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 327 1 1 4 4.4 Cc1nc2ccc(O)nc2n1-c1ccc(Cl)c(Cl)c1Cl nan
CHEMBL3716994 134275 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 327 1 1 4 4.4 Cc1nc2ccc(O)nc2n1-c1ccc(Cl)c(Cl)c1Cl nan
58345712 134277 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 243 1 1 4 2.6 Cc1nc2ccc(O)nc2n1-c1ccccc1F nan
CHEMBL3716997 134277 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 243 1 1 4 2.6 Cc1nc2ccc(O)nc2n1-c1ccccc1F nan
58345740 134303 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 276 1 2 5 2.9 Nc1nc2ccc(O)nc2n1-c1cccc2ccccc12 nan
CHEMBL3717084 134303 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 276 1 2 5 2.9 Nc1nc2ccc(O)nc2n1-c1cccc2ccccc12 nan
58345660 134306 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 303 1 1 4 3.2 Cc1cc(Br)ccc1-n1cnc2ccc(O)nc21 nan
CHEMBL3717091 134306 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 303 1 1 4 3.2 Cc1cc(Br)ccc1-n1cnc2ccc(O)nc21 nan
58345720 134323 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 258 1 2 5 2.2 Cc1c(F)cccc1-n1c(N)nc2ccc(O)nc21 nan
CHEMBL3717145 134323 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 258 1 2 5 2.2 Cc1c(F)cccc1-n1c(N)nc2ccc(O)nc21 nan
58345648 134347 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 271 2 1 5 3.2 CSc1ccccc1-n1c(C)nc2ccc(O)nc21 nan
CHEMBL3717252 134347 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 271 2 1 5 3.2 CSc1ccccc1-n1c(C)nc2ccc(O)nc21 nan
127024263 134362 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 258 1 2 5 2.2 Cc1cccc(-n2c(N)nc3ccc(O)nc32)c1F nan
CHEMBL3717311 134362 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 258 1 2 5 2.2 Cc1cccc(-n2c(N)nc3ccc(O)nc32)c1F nan
58345666 134376 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 279 1 1 4 3.4 Oc1ccc2ncn(-c3cccc(Cl)c3Cl)c2n1 nan
CHEMBL3717347 134376 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 279 1 1 4 3.4 Oc1ccc2ncn(-c3cccc(Cl)c3Cl)c2n1 nan
58345661 134394 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 307 1 1 4 3.0 Oc1ccc2nc(Br)n(-c3ccccc3F)c2n1 nan
CHEMBL3717420 134394 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 307 1 1 4 3.0 Oc1ccc2nc(Br)n(-c3ccccc3F)c2n1 nan
58345756 134395 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 239 1 1 4 2.7 Cc1cccc(C)c1-n1cnc2ccc(O)nc21 nan
CHEMBL3717421 134395 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 239 1 1 4 2.7 Cc1cccc(C)c1-n1cnc2ccc(O)nc21 nan
58345637 134402 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 326 2 2 6 3.3 Nc1nc2ccc(O)nc2n1-c1ccccc1SC(F)(F)F nan
CHEMBL3717447 134402 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 326 2 2 6 3.3 Nc1nc2ccc(O)nc2n1-c1ccccc1SC(F)(F)F nan
58345747 134409 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 297 1 1 4 3.3 Oc1ccc2ncn(-c3cccc(F)c3C(F)(F)F)c2n1 nan
CHEMBL3717464 134409 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 297 1 1 4 3.3 Oc1ccc2ncn(-c3cccc(F)c3C(F)(F)F)c2n1 nan
58345689 134411 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 279 1 1 4 3.4 Oc1ccc2ncn(-c3c(Cl)cccc3Cl)c2n1 nan
CHEMBL3717469 134411 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 279 1 1 4 3.4 Oc1ccc2ncn(-c3c(Cl)cccc3Cl)c2n1 nan
58345640 134416 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 332 1 1 6 3.1 CC(C)(C)OC(=O)N1CCCC(n2cnc3ccc(O)nc32)CC1 nan
CHEMBL3717482 134416 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 332 1 1 6 3.1 CC(C)(C)OC(=O)N1CCCC(n2cnc3ccc(O)nc32)CC1 nan
58345675 134422 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 229 1 1 4 2.3 Oc1ccc2ncn(-c3ccccc3F)c2n1 nan
CHEMBL3717503 134422 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 229 1 1 4 2.3 Oc1ccc2ncn(-c3ccccc3F)c2n1 nan
58345651 134434 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 231 1 1 4 3.0 Oc1ccc2ncn(C3CCCCCC3)c2n1 nan
CHEMBL3717555 134434 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 231 1 1 4 3.0 Oc1ccc2ncn(C3CCCCCC3)c2n1 nan
58345748 134440 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 239 1 1 4 2.7 Cc1cccc(-n2cnc3ccc(O)nc32)c1C nan
CHEMBL3717573 134440 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 239 1 1 4 2.7 Cc1cccc(-n2cnc3ccc(O)nc32)c1C nan
58345745 134445 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 287 2 1 4 3.8 Oc1ccc2ncn(-c3ccccc3-c3ccccc3)c2n1 nan
CHEMBL3717582 134445 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 287 2 1 4 3.8 Oc1ccc2ncn(-c3ccccc3-c3ccccc3)c2n1 nan
58345681 134447 1 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 226 1 2 5 1.7 Nc1nc2ccc(O)nc2n1-c1ccccc1 nan
CHEMBL3717589 134447 1 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 226 1 2 5 1.7 Nc1nc2ccc(O)nc2n1-c1ccccc1 nan
58345680 134455 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 245 1 1 4 2.8 Oc1ccc2ncn(-c3cccc(Cl)c3)c2n1 nan
CHEMBL3717604 134455 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 245 1 1 4 2.8 Oc1ccc2ncn(-c3cccc(Cl)c3)c2n1 nan
58345696 134457 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 293 1 1 4 3.5 Cc1nc2ccc(O)nc2n1-c1ccccc1C(F)(F)F nan
CHEMBL3717608 134457 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 293 1 1 4 3.5 Cc1nc2ccc(O)nc2n1-c1ccccc1C(F)(F)F nan
58345685 134462 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 323 1 1 4 3.5 Oc1ccc2nc(Br)n(-c3ccccc3Cl)c2n1 nan
CHEMBL3717636 134462 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 323 1 1 4 3.5 Oc1ccc2nc(Br)n(-c3ccccc3Cl)c2n1 nan
58345678 134478 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 357 1 1 4 3.9 Oc1ccc2ncn(-c3ccc(Br)cc3C(F)(F)F)c2n1 nan
CHEMBL3717689 134478 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 357 1 1 4 3.9 Oc1ccc2ncn(-c3ccc(Br)cc3C(F)(F)F)c2n1 nan
58345766 134480 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 313 1 1 4 4.1 Oc1ccc2ncn(-c3cc(Cl)c(Cl)cc3Cl)c2n1 nan
CHEMBL3717694 134480 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 313 1 1 4 4.1 Oc1ccc2ncn(-c3cc(Cl)c(Cl)cc3Cl)c2n1 nan
58345714 134485 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 309 1 1 4 4.2 Cc1nc2ccc(O)nc2n1-c1ccc(Cl)c2ccccc12 nan
CHEMBL3717710 134485 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 309 1 1 4 4.2 Cc1nc2ccc(O)nc2n1-c1ccc(Cl)c2ccccc12 nan
58345701 134495 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 239 1 1 4 2.7 Cc1ccc(-n2cnc3ccc(O)nc32)c(C)c1 nan
CHEMBL3717752 134495 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 239 1 1 4 2.7 Cc1ccc(-n2cnc3ccc(O)nc32)c(C)c1 nan
58345759 134499 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 310 1 2 5 3.5 Nc1nc2ccc(O)nc2n1-c1ccc(Cl)c2ccccc12 nan
CHEMBL3717773 134499 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 310 1 2 5 3.5 Nc1nc2ccc(O)nc2n1-c1ccc(Cl)c2ccccc12 nan
58345700 134510 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 289 1 1 4 2.9 Oc1ccc2ncn(-c3ccccc3Br)c2n1 nan
CHEMBL3717797 134510 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 289 1 1 4 2.9 Oc1ccc2ncn(-c3ccccc3Br)c2n1 nan
58345702 134518 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 313 1 1 4 3.8 Oc1ccc2nc(Cl)n(-c3ccccc3C(F)(F)F)c2n1 nan
CHEMBL3717818 134518 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 313 1 1 4 3.8 Oc1ccc2nc(Cl)n(-c3ccccc3C(F)(F)F)c2n1 nan
58345746 134519 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 301 3 1 4 3.7 Oc1ccc2ncn(-c3ccc(Cc4ccccc4)cc3)c2n1 nan
CHEMBL3717820 134519 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 301 3 1 4 3.7 Oc1ccc2ncn(-c3ccc(Cc4ccccc4)cc3)c2n1 nan
58345638 134524 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 309 2 1 5 3.3 Cc1nc2ccc(O)nc2n1-c1ccccc1OC(F)(F)F nan
CHEMBL3717852 134524 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 309 2 1 5 3.3 Cc1nc2ccc(O)nc2n1-c1ccccc1OC(F)(F)F nan
58345688 134540 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 245 1 1 4 3.3 Cc1nc2ccc(O)nc2n1C1CCCCCC1 nan
CHEMBL3717920 134540 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 245 1 1 4 3.3 Cc1nc2ccc(O)nc2n1C1CCCCCC1 nan
58345710 134563 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 294 1 2 5 2.7 Nc1nc2ccc(O)nc2n1-c1ccccc1C(F)(F)F nan
CHEMBL3717985 134563 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 294 1 2 5 2.7 Nc1nc2ccc(O)nc2n1-c1ccccc1C(F)(F)F nan
58345734 134578 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 259 1 1 4 3.1 Cc1ccccc1-n1c(Cl)nc2ccc(O)nc21 nan
CHEMBL3718055 134578 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 259 1 1 4 3.1 Cc1ccccc1-n1c(Cl)nc2ccc(O)nc21 nan
58345664 134588 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 310 2 2 6 2.6 Nc1nc2ccc(O)nc2n1-c1ccccc1OC(F)(F)F nan
CHEMBL3718085 134588 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 310 2 2 6 2.6 Nc1nc2ccc(O)nc2n1-c1ccccc1OC(F)(F)F nan
58345657 134603 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 357 1 1 4 3.9 Oc1ccc2ncn(-c3cccc(Br)c3C(F)(F)F)c2n1 nan
CHEMBL3718131 134603 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 357 1 1 4 3.9 Oc1ccc2ncn(-c3cccc(Br)c3C(F)(F)F)c2n1 nan
58345641 134609 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 217 1 1 5 2.2 Oc1ccc2ncn(-c3ccsc3)c2n1 nan
CHEMBL3718159 134609 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 217 1 1 5 2.2 Oc1ccc2ncn(-c3ccsc3)c2n1 nan
58345676 134615 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 243 1 1 4 2.6 Cc1c(F)cccc1-n1cnc2ccc(O)nc21 nan
CHEMBL3718175 134615 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 243 1 1 4 2.6 Cc1c(F)cccc1-n1cnc2ccc(O)nc21 nan
58345705 134616 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 240 1 2 5 2.0 Cc1ccccc1-n1c(N)nc2ccc(O)nc21 nan
CHEMBL3718177 134616 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 240 1 2 5 2.0 Cc1ccccc1-n1c(N)nc2ccc(O)nc21 nan
58345673 134629 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 263 1 1 4 2.9 Oc1ccc2nc(Cl)n(-c3ccccc3F)c2n1 nan
CHEMBL3718227 134629 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 263 1 1 4 2.9 Oc1ccc2nc(Cl)n(-c3ccccc3F)c2n1 nan
58345754 134631 5 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 217 1 1 4 2.6 Oc1ccc2ncn(C3CCCCC3)c2n1 nan
CHEMBL3718239 134631 5 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 217 1 1 4 2.6 Oc1ccc2ncn(C3CCCCC3)c2n1 nan
58345649 134632 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 246 1 1 5 2.2 Oc1ccc2ncn(-c3ccncc3Cl)c2n1 nan
CHEMBL3718240 134632 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 246 1 1 5 2.2 Oc1ccc2ncn(-c3ccncc3Cl)c2n1 nan
58345674 134642 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 240 1 2 5 2.0 Cc1ccc(-n2c(N)nc3ccc(O)nc32)cc1 nan
CHEMBL3718264 134642 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 240 1 2 5 2.0 Cc1ccc(-n2c(N)nc3ccc(O)nc32)cc1 nan
58345769 134661 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 275 1 1 4 3.6 Cc1ccc2ccccc2c1-n1cnc2ccc(O)nc21 nan
CHEMBL3718300 134661 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 275 1 1 4 3.6 Cc1ccc2ccccc2c1-n1cnc2ccc(O)nc21 nan
58345764 134667 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 290 1 2 5 3.2 Cc1ccc2ccccc2c1-n1c(N)nc2ccc(O)nc21 nan
CHEMBL3718324 134667 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 290 1 2 5 3.2 Cc1ccc2ccccc2c1-n1c(N)nc2ccc(O)nc21 nan
58345690 134673 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 259 1 1 4 3.1 Cc1nc2ccc(O)nc2n1-c1ccccc1Cl nan
CHEMBL3718342 134673 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 259 1 1 4 3.1 Cc1nc2ccc(O)nc2n1-c1ccccc1Cl nan
58345679 134677 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 241 2 1 5 2.1 COc1ccccc1-n1cnc2ccc(O)nc21 nan
CHEMBL3718354 134677 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 241 2 1 5 2.1 COc1ccccc1-n1cnc2ccc(O)nc21 nan
58345639 134681 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 279 1 1 4 3.1 Oc1ccc2ncn(-c3ccccc3C(F)(F)F)c2n1 nan
CHEMBL3718371 134681 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 279 1 1 4 3.1 Oc1ccc2ncn(-c3ccccc3C(F)(F)F)c2n1 nan
58345669 134683 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 313 1 1 4 4.1 Oc1ccc2ncn(-c3ccc(Cl)c(Cl)c3Cl)c2n1 nan
CHEMBL3718374 134683 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 313 1 1 4 4.1 Oc1ccc2ncn(-c3ccc(Cl)c(Cl)c3Cl)c2n1 nan
58345727 134694 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 225 1 1 4 2.4 Cc1ccccc1-n1cnc2ccc(O)nc21 nan
CHEMBL3718416 134694 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 225 1 1 4 2.4 Cc1ccccc1-n1cnc2ccc(O)nc21 nan
86655261 134700 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 311 3 1 7 2.0 CS(=O)(=O)Oc1ccc2nc(O)n(C3CCCCC3)c2n1 nan
CHEMBL3718427 134700 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 311 3 1 7 2.0 CS(=O)(=O)Oc1ccc2nc(O)n(C3CCCCC3)c2n1 nan
58345762 134729 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 245 1 1 4 2.8 Oc1ccc2nc(Cl)n(-c3ccccc3)c2n1 nan
CHEMBL3718549 134729 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 245 1 1 4 2.8 Oc1ccc2nc(Cl)n(-c3ccccc3)c2n1 nan
58345760 134746 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 262 1 2 5 2.0 Nc1nc2ccc(O)nc2n1-c1cccc(F)c1F nan
CHEMBL3718610 134746 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 262 1 2 5 2.0 Nc1nc2ccc(O)nc2n1-c1cccc(F)c1F nan
58345732 134752 10 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 211 1 1 4 2.1 Oc1ccc2ncn(-c3ccccc3)c2n1 nan
CHEMBL3718619 134752 10 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 211 1 1 4 2.1 Oc1ccc2ncn(-c3ccccc3)c2n1 nan
58345755 134754 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 327 1 1 4 4.4 Cc1nc2ccc(O)nc2n1-c1cc(Cl)c(Cl)cc1Cl nan
CHEMBL3718623 134754 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 327 1 1 4 4.4 Cc1nc2ccc(O)nc2n1-c1cc(Cl)c(Cl)cc1Cl nan
58345662 134755 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 203 1 1 4 2.3 Oc1ccc2ncn(C3CCCC3)c2n1 nan
CHEMBL3718624 134755 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 203 1 1 4 2.3 Oc1ccc2ncn(C3CCCC3)c2n1 nan
58345736 134759 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 263 1 1 4 3.2 Oc1ccc2nc(Cl)n(C3CC4CCC3C4)c2n1 nan
CHEMBL3718632 134759 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 263 1 1 4 3.2 Oc1ccc2nc(Cl)n(C3CC4CCC3C4)c2n1 nan
58345671 134762 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 251 1 1 4 2.6 Oc1ccc2ncn(-c3cccc4c3CCC4)c2n1 nan
CHEMBL3718637 134762 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 251 1 1 4 2.6 Oc1ccc2ncn(-c3cccc4c3CCC4)c2n1 nan
58345699 134799 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 303 1 1 4 3.2 Cc1nc2ccc(O)nc2n1-c1ccc(Br)cc1 nan
CHEMBL3718747 134799 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 303 1 1 4 3.2 Cc1nc2ccc(O)nc2n1-c1ccc(Br)cc1 nan
58345721 134812 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 303 1 1 4 3.2 Cc1cccc(-n2cnc3ccc(O)nc32)c1Br nan
CHEMBL3718790 134812 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 303 1 1 4 3.2 Cc1cccc(-n2cnc3ccc(O)nc32)c1Br nan
58345742 134818 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 283 1 1 4 3.4 Cc1nc2ccc(O)nc2n1C12CC3CC(CC(C3)C1)C2 nan
CHEMBL3718804 134818 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 283 1 1 4 3.4 Cc1nc2ccc(O)nc2n1C12CC3CC(CC(C3)C1)C2 nan
58345749 134841 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 263 1 1 4 2.9 Oc1ccc2ncn(-c3cccc(Cl)c3F)c2n1 nan
CHEMBL3718861 134841 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 263 1 1 4 2.9 Oc1ccc2ncn(-c3cccc(Cl)c3F)c2n1 nan
58345717 134846 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 231 1 1 4 2.9 CC1CCCCC1n1cnc2ccc(O)nc21 nan
CHEMBL3718877 134846 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 231 1 1 4 2.9 CC1CCCCC1n1cnc2ccc(O)nc21 nan
58345652 134866 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 260 1 2 5 2.4 Nc1nc2ccc(O)nc2n1-c1ccccc1Cl nan
CHEMBL3718998 134866 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 260 1 2 5 2.4 Nc1nc2ccc(O)nc2n1-c1ccccc1Cl nan
58345767 134874 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 311 2 1 5 3.7 Oc1ccc2ncn(-c3ccccc3SC(F)(F)F)c2n1 nan
CHEMBL3719017 134874 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 311 2 1 5 3.7 Oc1ccc2ncn(-c3ccccc3SC(F)(F)F)c2n1 nan
58345744 134876 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 189 1 1 4 1.9 Oc1ccc2ncn(C3CCC3)c2n1 nan
CHEMBL3719026 134876 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 189 1 1 4 1.9 Oc1ccc2ncn(C3CCC3)c2n1 nan
58345658 134902 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 259 1 1 4 3.1 Cc1ccc(Cl)cc1-n1cnc2ccc(O)nc21 nan
CHEMBL3719094 134902 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 259 1 1 4 3.1 Cc1ccc(Cl)cc1-n1cnc2ccc(O)nc21 nan
58345716 134916 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 323 1 1 4 3.5 Oc1ccc2nc(Cl)n(-c3ccccc3Br)c2n1 nan
CHEMBL3719152 134916 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 323 1 1 4 3.5 Oc1ccc2nc(Cl)n(-c3ccccc3Br)c2n1 nan
58345718 134921 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 225 1 1 4 2.4 Cc1nc2ccc(O)nc2n1-c1ccccc1 nan
CHEMBL3719178 134921 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 225 1 1 4 2.4 Cc1nc2ccc(O)nc2n1-c1ccccc1 nan
58345642 134927 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 303 1 1 4 3.2 Cc1ccccc1-n1c(Br)nc2ccc(O)nc21 nan
CHEMBL3719204 134927 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 303 1 1 4 3.2 Cc1ccccc1-n1c(Br)nc2ccc(O)nc21 nan
58345711 134934 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 337 1 1 4 3.9 Cc1cc(Br)c(Cl)cc1-n1cnc2ccc(O)nc21 nan
CHEMBL3719226 134934 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 337 1 1 4 3.9 Cc1cc(Br)c(Cl)cc1-n1cnc2ccc(O)nc21 nan
58345703 134939 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 279 1 1 4 3.4 Oc1ccc2ncn(-c3ccc(Cl)cc3Cl)c2n1 nan
CHEMBL3719235 134939 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 279 1 1 4 3.4 Oc1ccc2ncn(-c3ccc(Cl)cc3Cl)c2n1 nan
58345730 134964 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 266 1 2 5 2.2 Nc1nc2ccc(O)nc2n1-c1cccc2c1CCC2 nan
CHEMBL3719308 134964 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 266 1 2 5 2.2 Nc1nc2ccc(O)nc2n1-c1cccc2c1CCC2 nan
58345715 134977 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 257 2 1 5 2.8 CSc1nc2ccc(O)nc2n1-c1ccccc1 nan
CHEMBL3719363 134977 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 257 2 1 5 2.8 CSc1nc2ccc(O)nc2n1-c1ccccc1 nan
156012564 177347 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 606 7 2 9 4.3 CCOc1cc(C(F)(F)F)c(C(=O)NC(=O)Nc2nc3ccc(CN4CCN(C)CC4)cc3s2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4637486 177347 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 606 7 2 9 4.3 CCOc1cc(C(F)(F)F)c(C(=O)NC(=O)Nc2nc3ccc(CN4CCN(C)CC4)cc3s2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
156021885 178215 0 None 8 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 635 10 1 10 4.2 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1N1CCO[C@H](C)C1 10.1016/j.bmcl.2020.126953
CHEMBL4649741 178215 0 None 8 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 635 10 1 10 4.2 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1N1CCO[C@H](C)C1 10.1016/j.bmcl.2020.126953
13071646 80485 102 None -2 4 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant GPR81 transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR81 transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assay
ChEMBL 172 1 2 2 1.7 O=C(O)c1cc(O)cc(Cl)c1 10.1021/ml3000676
CHEMBL2146910 80485 102 None -2 4 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant GPR81 transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR81 transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assay
ChEMBL 172 1 2 2 1.7 O=C(O)c1cc(O)cc(Cl)c1 10.1021/ml3000676
156009546 177150 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 621 7 2 10 4.0 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)C4CCN(C)CC4)cc3s2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4634029 177150 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 621 7 2 10 4.0 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)C4CCN(C)CC4)cc3s2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
156017002 177632 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 553 7 2 9 4.2 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(CN4CCN(C)CC4)cc3s2)cc1-n1cccn1 10.1016/j.bmcl.2020.126953
CHEMBL4641219 177632 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 553 7 2 9 4.2 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(CN4CCN(C)CC4)cc3s2)cc1-n1cccn1 10.1016/j.bmcl.2020.126953
156017170 177648 0 None 6 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 417 5 1 6 4.4 CCOc1cc(Cl)c(C(=O)Nc2nc3ccccc3s2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4641449 177648 0 None 6 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 417 5 1 6 4.4 CCOc1cc(Cl)c(C(=O)Nc2nc3ccccc3s2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
156021336 178167 0 None 29 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 467 5 1 6 5.2 CCOc1cc(Cl)c(-c2ccc(-c3nc4ccccc4s3)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4649089 178167 0 None 29 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 467 5 1 6 5.2 CCOc1cc(Cl)c(-c2ccc(-c3nc4ccccc4s3)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
156014693 177192 0 None 41 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 530 6 2 8 2.9 CCOc1cc(Cl)c(-c2ccc(-c3nc4c(s3)CN(C(=O)CO)CC4)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4635089 177192 0 None 41 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 530 6 2 8 2.9 CCOc1cc(Cl)c(-c2ccc(-c3nc4c(s3)CN(C(=O)CO)CC4)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
156015181 177541 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 552 7 2 8 4.8 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(CN4CCN(C)CC4)cc3s2)cc1-n1cccc1 10.1016/j.bmcl.2020.126953
CHEMBL4640189 177541 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 552 7 2 8 4.8 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(CN4CCN(C)CC4)cc3s2)cc1-n1cccc1 10.1016/j.bmcl.2020.126953
13071646 80485 102 None -3 4 Mouse 4.7 pEC50 = 4.7 Functional
Agonist activity at mouse GPR81Agonist activity at mouse GPR81
ChEMBL 172 1 2 2 1.7 O=C(O)c1cc(O)cc(Cl)c1 10.1021/ml3000676
CHEMBL2146910 80485 102 None -3 4 Mouse 4.7 pEC50 = 4.7 Functional
Agonist activity at mouse GPR81Agonist activity at mouse GPR81
ChEMBL 172 1 2 2 1.7 O=C(O)c1cc(O)cc(Cl)c1 10.1021/ml3000676
57422810 177661 4 None -2 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 602 7 2 10 4.4 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)C4CCN(C)CC4)cc3s2)cc1-n1cccn1 10.1016/j.bmcl.2020.126953
CHEMBL4641579 177661 4 None -2 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 602 7 2 10 4.4 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)C4CCN(C)CC4)cc3s2)cc1-n1cccn1 10.1016/j.bmcl.2020.126953
58345743 133643 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 328 1 2 5 3.7 Nc1nc2ccc(O)nc2n1-c1ccc(Cl)c(Cl)c1Cl nan
CHEMBL3714817 133643 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 328 1 2 5 3.7 Nc1nc2ccc(O)nc2n1-c1ccc(Cl)c(Cl)c1Cl nan
58345768 133657 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 285 2 1 4 3.7 Oc1ccc2nc(C3CC3)n(-c3ccccc3Cl)c2n1 nan
CHEMBL3714879 133657 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 285 2 1 4 3.7 Oc1ccc2nc(C3CC3)n(-c3ccccc3Cl)c2n1 nan
58345668 133658 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 304 1 2 5 2.5 Nc1nc2ccc(O)nc2n1-c1ccc(Br)cc1 nan
CHEMBL3714885 133658 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 304 1 2 5 2.5 Nc1nc2ccc(O)nc2n1-c1ccc(Br)cc1 nan
58345728 133665 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 347 1 1 4 4.2 Oc1ccc2ncn(-c3ccc(C(F)(F)F)cc3C(F)(F)F)c2n1 nan
CHEMBL3714909 133665 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 347 1 1 4 4.2 Oc1ccc2ncn(-c3ccc(C(F)(F)F)cc3C(F)(F)F)c2n1 nan
58345725 133681 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 367 1 1 4 3.7 Oc1ccc2nc(Br)n(-c3ccccc3Br)c2n1 nan
CHEMBL3714960 133681 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 367 1 1 4 3.7 Oc1ccc2nc(Br)n(-c3ccccc3Br)c2n1 nan
58345654 133684 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 243 1 1 4 2.6 Cc1cc(F)ccc1-n1cnc2ccc(O)nc21 nan
CHEMBL3714970 133684 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 243 1 1 4 2.6 Cc1cc(F)ccc1-n1cnc2ccc(O)nc21 nan
58345758 133698 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 278 1 2 5 2.5 Nc1nc2ccc(O)nc2n1-c1cccc(F)c1Cl nan
CHEMBL3715004 133698 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 278 1 2 5 2.5 Nc1nc2ccc(O)nc2n1-c1cccc(F)c1Cl nan
58345741 133704 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 239 1 1 4 2.7 Cc1ccc(-n2c(C)nc3ccc(O)nc32)cc1 nan
CHEMBL3715017 133704 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 239 1 1 4 2.7 Cc1ccc(-n2c(C)nc3ccc(O)nc32)cc1 nan
58345706 133723 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 253 3 1 4 3.1 CCCc1nc2ccc(O)nc2n1-c1ccccc1 nan
CHEMBL3715077 133723 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 253 3 1 4 3.1 CCCc1nc2ccc(O)nc2n1-c1ccccc1 nan
58345750 133746 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 255 1 1 6 1.9 Oc1ccc2ncn(-c3ccc4c(c3)OCO4)c2n1 nan
CHEMBL3715155 133746 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 255 1 1 6 1.9 Oc1ccc2ncn(-c3ccc4c(c3)OCO4)c2n1 nan
58345653 133754 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 303 1 1 4 3.2 Cc1nc2ccc(O)nc2n1-c1ccccc1Br nan
CHEMBL3715174 133754 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 303 1 1 4 3.2 Cc1nc2ccc(O)nc2n1-c1ccccc1Br nan
58345739 133766 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 247 1 1 4 2.4 Oc1ccc2ncn(-c3cccc(F)c3F)c2n1 nan
CHEMBL3715218 133766 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 247 1 1 4 2.4 Oc1ccc2ncn(-c3cccc(F)c3F)c2n1 nan
58345704 133793 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 245 1 1 4 3.4 Oc1ccc2ncn(C3CCCCCCC3)c2n1 nan
CHEMBL3715359 133793 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 245 1 1 4 3.4 Oc1ccc2ncn(C3CCCCCCC3)c2n1 nan
58345713 133794 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 328 1 2 5 3.7 Nc1nc2ccc(O)nc2n1-c1cc(Cl)c(Cl)cc1Cl nan
CHEMBL3715361 133794 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 328 1 2 5 3.7 Nc1nc2ccc(O)nc2n1-c1cc(Cl)c(Cl)cc1Cl nan
58345644 133800 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 251 1 1 4 3.3 Oc1ccc2nc(Cl)n(C3CCCCC3)c2n1 nan
CHEMBL3715375 133800 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 251 1 1 4 3.3 Oc1ccc2nc(Cl)n(C3CCCCC3)c2n1 nan
58345751 133802 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 244 1 2 5 1.8 Nc1nc2ccc(O)nc2n1-c1ccccc1F nan
CHEMBL3715394 133802 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 244 1 2 5 1.8 Nc1nc2ccc(O)nc2n1-c1ccccc1F nan
58345683 133823 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 295 2 1 5 3.0 Oc1ccc2ncn(-c3ccccc3OC(F)(F)F)c2n1 nan
CHEMBL3715478 133823 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 295 2 1 5 3.0 Oc1ccc2ncn(-c3ccccc3OC(F)(F)F)c2n1 nan
58345724 133838 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 253 1 1 4 3.1 Cc1cccc(-n2c(C)nc3ccc(O)nc32)c1C nan
CHEMBL3715536 133838 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 253 1 1 4 3.1 Cc1cccc(-n2c(C)nc3ccc(O)nc32)c1C nan
58345682 133846 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 275 1 1 4 3.6 Cc1nc2ccc(O)nc2n1-c1cccc2ccccc12 nan
CHEMBL3715558 133846 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 275 1 1 4 3.6 Cc1nc2ccc(O)nc2n1-c1cccc2ccccc12 nan
58345677 133850 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 284 1 2 5 2.6 Nc1nc2ccc(O)nc2n1C12CC3CC(CC(C3)C1)C2 nan
CHEMBL3715572 133850 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 284 1 2 5 2.6 Nc1nc2ccc(O)nc2n1C12CC3CC(CC(C3)C1)C2 nan
46830068 133852 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 245 1 1 4 2.8 Oc1ccc2ncn(-c3ccccc3Cl)c2n1 nan
CHEMBL3715577 133852 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 245 1 1 4 2.8 Oc1ccc2ncn(-c3ccccc3Cl)c2n1 nan
58345738 133858 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 233 1 2 5 1.6 Oc1ccc2ncn(C3CCCCC3O)c2n1 nan
CHEMBL3715599 133858 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 233 1 2 5 1.6 Oc1ccc2ncn(C3CCCCC3O)c2n1 nan
58345667 133860 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 265 1 1 4 3.5 CC1CCCCC1n1c(Cl)nc2ccc(O)nc21 nan
CHEMBL3715601 133860 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 265 1 1 4 3.5 CC1CCCCC1n1c(Cl)nc2ccc(O)nc21 nan
58345753 133863 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 247 1 2 5 2.0 Oc1ccc2ncn(C3CCCCCC3O)c2n1 nan
CHEMBL3715611 133863 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 247 1 2 5 2.0 Oc1ccc2ncn(C3CCCCCC3O)c2n1 nan
58345771 133866 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 231 1 1 4 2.8 CC1(n2cnc3ccc(O)nc32)CCCCC1 nan
CHEMBL3715620 133866 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 231 1 1 4 2.8 CC1(n2cnc3ccc(O)nc32)CCCCC1 nan
58345698 133881 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 235 1 1 5 2.2 Oc1ccc2ncn(C3CCSCC3)c2n1 nan
CHEMBL3715673 133881 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 235 1 1 5 2.2 Oc1ccc2ncn(C3CCSCC3)c2n1 nan
67312894 133909 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 289 1 1 4 3.9 Cc1ccc2ccccc2c1-n1c(C)nc2ccc(O)nc21 nan
CHEMBL3715748 133909 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 289 1 1 4 3.9 Cc1ccc2ccccc2c1-n1c(C)nc2ccc(O)nc21 nan
58345684 133920 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 295 1 1 4 3.9 Oc1ccc2ncn(-c3ccc(Cl)c4ccccc34)c2n1 nan
CHEMBL3715778 133920 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 295 1 1 4 3.9 Oc1ccc2ncn(-c3ccc(Cl)c4ccccc34)c2n1 nan
58345752 133927 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 245 1 1 4 3.1 Cc1nc2ccc(O)nc2n1C1(C)CCCCC1 nan
CHEMBL3715818 133927 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 245 1 1 4 3.1 Cc1nc2ccc(O)nc2n1C1(C)CCCCC1 nan
58345726 133931 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 253 2 1 4 3.0 CCc1ccc(-n2c(C)nc3ccc(O)nc32)cc1 nan
CHEMBL3715837 133931 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 253 2 1 4 3.0 CCc1ccc(-n2c(C)nc3ccc(O)nc32)cc1 nan
58345765 133946 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 325 2 1 5 4.0 Cc1nc2ccc(O)nc2n1-c1ccccc1SC(F)(F)F nan
CHEMBL3715889 133946 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 325 2 1 5 4.0 Cc1nc2ccc(O)nc2n1-c1ccccc1SC(F)(F)F nan
58345697 133947 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 256 2 1 6 2.0 O=[N+]([O-])c1ccccc1-n1cnc2ccc(O)nc21 nan
CHEMBL3715890 133947 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 256 2 1 6 2.0 O=[N+]([O-])c1ccccc1-n1cnc2ccc(O)nc21 nan
58345672 133955 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 239 1 1 4 2.7 Cc1cc(C)cc(-n2cnc3ccc(O)nc32)c1 nan
CHEMBL3715915 133955 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 239 1 1 4 2.7 Cc1cc(C)cc(-n2cnc3ccc(O)nc32)c1 nan
58345731 133956 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 329 2 1 5 3.7 Oc1ccc2nc(Cl)n(-c3ccccc3OC(F)(F)F)c2n1 nan
CHEMBL3715916 133956 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 329 2 1 5 3.7 Oc1ccc2nc(Cl)n(-c3ccccc3OC(F)(F)F)c2n1 nan
58345656 133960 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 345 2 1 5 4.4 Oc1ccc2nc(Cl)n(-c3ccccc3SC(F)(F)F)c2n1 nan
CHEMBL3715927 133960 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 345 2 1 5 4.4 Oc1ccc2nc(Cl)n(-c3ccccc3SC(F)(F)F)c2n1 nan
58345659 133966 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 251 1 1 4 2.6 Oc1ccc2ncn(-c3ccc4c(c3)CCC4)c2n1 nan
CHEMBL3715949 133966 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 251 1 1 4 2.6 Oc1ccc2ncn(-c3ccc4c(c3)CCC4)c2n1 nan
58345692 133990 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 274 1 2 5 2.7 Cc1c(Cl)cccc1-n1c(N)nc2ccc(O)nc21 nan
CHEMBL3716036 133990 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 274 1 2 5 2.7 Cc1c(Cl)cccc1-n1c(N)nc2ccc(O)nc21 nan
58345694 133992 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 239 2 1 4 2.7 CCc1ccccc1-n1cnc2ccc(O)nc21 nan
CHEMBL3716041 133992 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 239 2 1 4 2.7 CCc1ccccc1-n1cnc2ccc(O)nc21 nan
58345733 134005 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 317 1 1 4 3.5 Cc1cccc(-n2c(C)nc3ccc(O)nc32)c1Br nan
CHEMBL3716083 134005 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 317 1 1 4 3.5 Cc1cccc(-n2c(C)nc3ccc(O)nc32)c1Br nan
86655263 134016 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 383 3 1 7 2.2 CS(=O)(=O)Oc1ccc2nc(O)n(-c3ccccc3Br)c2n1 nan
CHEMBL3716136 134016 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 383 3 1 7 2.2 CS(=O)(=O)Oc1ccc2nc(O)n(-c3ccccc3Br)c2n1 nan
58345719 134031 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 269 1 1 4 3.1 Oc1ccc2ncn(C34CC5CC(CC(C5)C3)C4)c2n1 nan
CHEMBL3716171 134031 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 269 1 1 4 3.1 Oc1ccc2ncn(C34CC5CC(CC(C5)C3)C4)c2n1 nan
58345650 134035 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 287 2 1 4 3.8 Oc1ccc2nc(-c3ccccc3)n(-c3ccccc3)c2n1 nan
CHEMBL3716180 134035 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 287 2 1 4 3.8 Oc1ccc2nc(-c3ccccc3)n(-c3ccccc3)c2n1 nan
58345686 134055 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 241 2 1 5 2.1 COc1ccc(-n2cnc3ccc(O)nc32)cc1 nan
CHEMBL3716252 134055 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 241 2 1 5 2.1 COc1ccc(-n2cnc3ccc(O)nc32)cc1 nan
58345723 134056 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 231 1 1 4 3.0 Cc1nc2ccc(O)nc2n1C1CCCCC1 nan
CHEMBL3716253 134056 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 231 1 1 4 3.0 Cc1nc2ccc(O)nc2n1C1CCCCC1 nan
58345735 134060 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 297 1 1 4 3.3 Oc1ccc2ncn(-c3ccc(F)cc3C(F)(F)F)c2n1 nan
CHEMBL3716263 134060 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 297 1 1 4 3.3 Oc1ccc2ncn(-c3ccc(F)cc3C(F)(F)F)c2n1 nan
58345707 134063 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 219 1 1 5 1.5 Oc1ccc2ncn(C3CCOCC3)c2n1 nan
CHEMBL3716273 134063 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 219 1 1 5 1.5 Oc1ccc2ncn(C3CCOCC3)c2n1 nan
58345635 134068 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 239 1 1 4 2.7 Cc1ccc(C)c(-n2cnc3ccc(O)nc32)c1 nan
CHEMBL3716281 134068 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 239 1 1 4 2.7 Cc1ccc(C)c(-n2cnc3ccc(O)nc32)c1 nan
58345663 134071 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 253 2 1 4 3.3 CC(C)c1ccccc1-n1cnc2ccc(O)nc21 nan
CHEMBL3716287 134071 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 253 2 1 4 3.3 CC(C)c1ccccc1-n1cnc2ccc(O)nc21 nan
58345691 134075 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 251 2 1 4 3.0 Oc1ccc2ncn(-c3ccccc3C3CC3)c2n1 nan
CHEMBL3716302 134075 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 251 2 1 4 3.0 Oc1ccc2ncn(-c3ccccc3C3CC3)c2n1 nan
58345708 134091 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 279 1 1 4 3.4 Oc1ccc2nc(Cl)n(-c3ccccc3Cl)c2n1 nan
CHEMBL3716351 134091 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 279 1 1 4 3.4 Oc1ccc2nc(Cl)n(-c3ccccc3Cl)c2n1 nan
58345763 134096 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 267 1 1 4 3.3 Oc1ccc2ncn(C3CCCCCC3(F)F)c2n1 nan
CHEMBL3716370 134096 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 267 1 1 4 3.3 Oc1ccc2ncn(C3CCCCCC3(F)F)c2n1 nan
58345693 134114 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 261 1 1 4 3.3 Oc1ccc2ncn(-c3cccc4ccccc34)c2n1 nan
CHEMBL3716441 134114 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 261 1 1 4 3.3 Oc1ccc2ncn(-c3cccc4ccccc34)c2n1 nan
58345634 134123 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 246 1 2 5 2.6 Nc1nc2ccc(O)nc2n1C1CCCCCC1 nan
CHEMBL3716479 134123 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 246 1 2 5 2.6 Nc1nc2ccc(O)nc2n1C1CCCCCC1 nan
58345729 134127 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 231 1 1 5 1.8 O=C1CCCCC1n1cnc2ccc(O)nc21 nan
CHEMBL3716494 134127 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 231 1 1 5 1.8 O=C1CCCCC1n1cnc2ccc(O)nc21 nan
58345695 134129 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 297 1 1 4 3.3 Oc1ccc2ncn(-c3cccc(C(F)(F)F)c3F)c2n1 nan
CHEMBL3716500 134129 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 297 1 1 4 3.3 Oc1ccc2ncn(-c3cccc(C(F)(F)F)c3F)c2n1 nan
58345655 134130 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 254 2 2 5 2.3 CCc1ccc(-n2c(N)nc3ccc(O)nc32)cc1 nan
CHEMBL3716501 134130 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 254 2 2 5 2.3 CCc1ccc(-n2c(N)nc3ccc(O)nc32)cc1 nan
58345665 134145 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 239 1 1 4 2.7 Cc1ccc(-n2cnc3ccc(O)nc32)cc1C nan
CHEMBL3716553 134145 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 239 1 1 4 2.7 Cc1ccc(-n2cnc3ccc(O)nc32)cc1C nan
58345646 134162 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 335 3 1 5 3.9 Oc1ccc2nc(C3CC3)n(-c3ccccc3OC(F)(F)F)c2n1 nan
CHEMBL3716607 134162 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 335 3 1 5 3.9 Oc1ccc2nc(C3CC3)n(-c3ccccc3OC(F)(F)F)c2n1 nan
58345770 134167 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 229 1 1 4 2.3 Oc1ccc2ncn(-c3ccc(F)cc3)c2n1 nan
CHEMBL3716628 134167 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 229 1 1 4 2.3 Oc1ccc2ncn(-c3ccc(F)cc3)c2n1 nan
58345647 134172 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 229 1 1 4 2.5 Oc1ccc2ncn(C3CC4CCC3C4)c2n1 nan
CHEMBL3716637 134172 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 229 1 1 4 2.5 Oc1ccc2ncn(C3CC4CCC3C4)c2n1 nan
58345757 134179 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 259 2 1 4 3.5 CCC1(n2c(C)nc3ccc(O)nc32)CCCCC1 nan
CHEMBL3716678 134179 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 259 2 1 4 3.5 CCC1(n2c(C)nc3ccc(O)nc32)CCCCC1 nan
58345645 134181 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 225 1 1 4 2.4 Cc1ccc(-n2cnc3ccc(O)nc32)cc1 nan
CHEMBL3716686 134181 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 225 1 1 4 2.4 Cc1ccc(-n2cnc3ccc(O)nc32)cc1 nan
58345761 134233 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 245 1 1 5 2.2 O=C1CCCCCC1n1cnc2ccc(O)nc21 nan
CHEMBL3716863 134233 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 245 1 1 5 2.2 O=C1CCCCCC1n1cnc2ccc(O)nc21 nan
58345737 134251 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 263 1 1 4 2.9 Oc1ccc2ncn(-c3cccc(F)c3Cl)c2n1 nan
CHEMBL3716914 134251 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 263 1 1 4 2.9 Oc1ccc2ncn(-c3cccc(F)c3Cl)c2n1 nan
58345709 134258 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 233 1 2 5 1.6 Oc1ccc2ncn(C3CCC(O)CC3)c2n1 nan
CHEMBL3716940 134258 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 233 1 2 5 1.6 Oc1ccc2ncn(C3CCC(O)CC3)c2n1 nan
58345722 134274 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 259 1 1 4 3.1 Cc1c(Cl)cccc1-n1cnc2ccc(O)nc21 nan
CHEMBL3716993 134274 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 259 1 1 4 3.1 Cc1c(Cl)cccc1-n1cnc2ccc(O)nc21 nan
58345643 134275 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 327 1 1 4 4.4 Cc1nc2ccc(O)nc2n1-c1ccc(Cl)c(Cl)c1Cl nan
CHEMBL3716994 134275 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 327 1 1 4 4.4 Cc1nc2ccc(O)nc2n1-c1ccc(Cl)c(Cl)c1Cl nan
58345712 134277 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 243 1 1 4 2.6 Cc1nc2ccc(O)nc2n1-c1ccccc1F nan
CHEMBL3716997 134277 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 243 1 1 4 2.6 Cc1nc2ccc(O)nc2n1-c1ccccc1F nan
58345740 134303 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 276 1 2 5 2.9 Nc1nc2ccc(O)nc2n1-c1cccc2ccccc12 nan
CHEMBL3717084 134303 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 276 1 2 5 2.9 Nc1nc2ccc(O)nc2n1-c1cccc2ccccc12 nan
58345660 134306 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 303 1 1 4 3.2 Cc1cc(Br)ccc1-n1cnc2ccc(O)nc21 nan
CHEMBL3717091 134306 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 303 1 1 4 3.2 Cc1cc(Br)ccc1-n1cnc2ccc(O)nc21 nan
58345648 134347 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 271 2 1 5 3.2 CSc1ccccc1-n1c(C)nc2ccc(O)nc21 nan
CHEMBL3717252 134347 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 271 2 1 5 3.2 CSc1ccccc1-n1c(C)nc2ccc(O)nc21 nan
127024263 134362 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 258 1 2 5 2.2 Cc1cccc(-n2c(N)nc3ccc(O)nc32)c1F nan
CHEMBL3717311 134362 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 258 1 2 5 2.2 Cc1cccc(-n2c(N)nc3ccc(O)nc32)c1F nan
58345666 134376 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 279 1 1 4 3.4 Oc1ccc2ncn(-c3cccc(Cl)c3Cl)c2n1 nan
CHEMBL3717347 134376 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 279 1 1 4 3.4 Oc1ccc2ncn(-c3cccc(Cl)c3Cl)c2n1 nan
58345661 134394 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 307 1 1 4 3.0 Oc1ccc2nc(Br)n(-c3ccccc3F)c2n1 nan
CHEMBL3717420 134394 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 307 1 1 4 3.0 Oc1ccc2nc(Br)n(-c3ccccc3F)c2n1 nan
58345756 134395 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 239 1 1 4 2.7 Cc1cccc(C)c1-n1cnc2ccc(O)nc21 nan
CHEMBL3717421 134395 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 239 1 1 4 2.7 Cc1cccc(C)c1-n1cnc2ccc(O)nc21 nan
58345637 134402 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 326 2 2 6 3.3 Nc1nc2ccc(O)nc2n1-c1ccccc1SC(F)(F)F nan
CHEMBL3717447 134402 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 326 2 2 6 3.3 Nc1nc2ccc(O)nc2n1-c1ccccc1SC(F)(F)F nan
58345747 134409 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 297 1 1 4 3.3 Oc1ccc2ncn(-c3cccc(F)c3C(F)(F)F)c2n1 nan
CHEMBL3717464 134409 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 297 1 1 4 3.3 Oc1ccc2ncn(-c3cccc(F)c3C(F)(F)F)c2n1 nan
58345689 134411 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 279 1 1 4 3.4 Oc1ccc2ncn(-c3c(Cl)cccc3Cl)c2n1 nan
CHEMBL3717469 134411 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 279 1 1 4 3.4 Oc1ccc2ncn(-c3c(Cl)cccc3Cl)c2n1 nan
58345640 134416 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 332 1 1 6 3.1 CC(C)(C)OC(=O)N1CCCC(n2cnc3ccc(O)nc32)CC1 nan
CHEMBL3717482 134416 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 332 1 1 6 3.1 CC(C)(C)OC(=O)N1CCCC(n2cnc3ccc(O)nc32)CC1 nan
58345675 134422 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 229 1 1 4 2.3 Oc1ccc2ncn(-c3ccccc3F)c2n1 nan
CHEMBL3717503 134422 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 229 1 1 4 2.3 Oc1ccc2ncn(-c3ccccc3F)c2n1 nan
58345748 134440 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 239 1 1 4 2.7 Cc1cccc(-n2cnc3ccc(O)nc32)c1C nan
CHEMBL3717573 134440 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 239 1 1 4 2.7 Cc1cccc(-n2cnc3ccc(O)nc32)c1C nan
58345745 134445 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 287 2 1 4 3.8 Oc1ccc2ncn(-c3ccccc3-c3ccccc3)c2n1 nan
CHEMBL3717582 134445 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 287 2 1 4 3.8 Oc1ccc2ncn(-c3ccccc3-c3ccccc3)c2n1 nan
58345680 134455 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 245 1 1 4 2.8 Oc1ccc2ncn(-c3cccc(Cl)c3)c2n1 nan
CHEMBL3717604 134455 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 245 1 1 4 2.8 Oc1ccc2ncn(-c3cccc(Cl)c3)c2n1 nan
58345696 134457 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 293 1 1 4 3.5 Cc1nc2ccc(O)nc2n1-c1ccccc1C(F)(F)F nan
CHEMBL3717608 134457 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 293 1 1 4 3.5 Cc1nc2ccc(O)nc2n1-c1ccccc1C(F)(F)F nan
58345685 134462 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 323 1 1 4 3.5 Oc1ccc2nc(Br)n(-c3ccccc3Cl)c2n1 nan
CHEMBL3717636 134462 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 323 1 1 4 3.5 Oc1ccc2nc(Br)n(-c3ccccc3Cl)c2n1 nan
58345678 134478 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 357 1 1 4 3.9 Oc1ccc2ncn(-c3ccc(Br)cc3C(F)(F)F)c2n1 nan
CHEMBL3717689 134478 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 357 1 1 4 3.9 Oc1ccc2ncn(-c3ccc(Br)cc3C(F)(F)F)c2n1 nan
58345766 134480 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 313 1 1 4 4.1 Oc1ccc2ncn(-c3cc(Cl)c(Cl)cc3Cl)c2n1 nan
CHEMBL3717694 134480 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 313 1 1 4 4.1 Oc1ccc2ncn(-c3cc(Cl)c(Cl)cc3Cl)c2n1 nan
58345714 134485 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 309 1 1 4 4.2 Cc1nc2ccc(O)nc2n1-c1ccc(Cl)c2ccccc12 nan
CHEMBL3717710 134485 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 309 1 1 4 4.2 Cc1nc2ccc(O)nc2n1-c1ccc(Cl)c2ccccc12 nan
58345701 134495 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 239 1 1 4 2.7 Cc1ccc(-n2cnc3ccc(O)nc32)c(C)c1 nan
CHEMBL3717752 134495 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 239 1 1 4 2.7 Cc1ccc(-n2cnc3ccc(O)nc32)c(C)c1 nan
58345759 134499 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 310 1 2 5 3.5 Nc1nc2ccc(O)nc2n1-c1ccc(Cl)c2ccccc12 nan
CHEMBL3717773 134499 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 310 1 2 5 3.5 Nc1nc2ccc(O)nc2n1-c1ccc(Cl)c2ccccc12 nan
58345700 134510 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 289 1 1 4 2.9 Oc1ccc2ncn(-c3ccccc3Br)c2n1 nan
CHEMBL3717797 134510 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 289 1 1 4 2.9 Oc1ccc2ncn(-c3ccccc3Br)c2n1 nan
58345702 134518 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 313 1 1 4 3.8 Oc1ccc2nc(Cl)n(-c3ccccc3C(F)(F)F)c2n1 nan
CHEMBL3717818 134518 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 313 1 1 4 3.8 Oc1ccc2nc(Cl)n(-c3ccccc3C(F)(F)F)c2n1 nan
58345746 134519 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 301 3 1 4 3.7 Oc1ccc2ncn(-c3ccc(Cc4ccccc4)cc3)c2n1 nan
CHEMBL3717820 134519 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 301 3 1 4 3.7 Oc1ccc2ncn(-c3ccc(Cc4ccccc4)cc3)c2n1 nan
58345638 134524 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 309 2 1 5 3.3 Cc1nc2ccc(O)nc2n1-c1ccccc1OC(F)(F)F nan
CHEMBL3717852 134524 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 309 2 1 5 3.3 Cc1nc2ccc(O)nc2n1-c1ccccc1OC(F)(F)F nan
58345688 134540 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 245 1 1 4 3.3 Cc1nc2ccc(O)nc2n1C1CCCCCC1 nan
CHEMBL3717920 134540 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 245 1 1 4 3.3 Cc1nc2ccc(O)nc2n1C1CCCCCC1 nan
58345710 134563 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 294 1 2 5 2.7 Nc1nc2ccc(O)nc2n1-c1ccccc1C(F)(F)F nan
CHEMBL3717985 134563 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 294 1 2 5 2.7 Nc1nc2ccc(O)nc2n1-c1ccccc1C(F)(F)F nan
58345734 134578 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 259 1 1 4 3.1 Cc1ccccc1-n1c(Cl)nc2ccc(O)nc21 nan
CHEMBL3718055 134578 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 259 1 1 4 3.1 Cc1ccccc1-n1c(Cl)nc2ccc(O)nc21 nan
58345664 134588 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 310 2 2 6 2.6 Nc1nc2ccc(O)nc2n1-c1ccccc1OC(F)(F)F nan
CHEMBL3718085 134588 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 310 2 2 6 2.6 Nc1nc2ccc(O)nc2n1-c1ccccc1OC(F)(F)F nan
58345657 134603 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 357 1 1 4 3.9 Oc1ccc2ncn(-c3cccc(Br)c3C(F)(F)F)c2n1 nan
CHEMBL3718131 134603 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 357 1 1 4 3.9 Oc1ccc2ncn(-c3cccc(Br)c3C(F)(F)F)c2n1 nan
58345641 134609 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 217 1 1 5 2.2 Oc1ccc2ncn(-c3ccsc3)c2n1 nan
CHEMBL3718159 134609 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 217 1 1 5 2.2 Oc1ccc2ncn(-c3ccsc3)c2n1 nan
58345676 134615 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 243 1 1 4 2.6 Cc1c(F)cccc1-n1cnc2ccc(O)nc21 nan
CHEMBL3718175 134615 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 243 1 1 4 2.6 Cc1c(F)cccc1-n1cnc2ccc(O)nc21 nan
58345705 134616 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 240 1 2 5 2.0 Cc1ccccc1-n1c(N)nc2ccc(O)nc21 nan
CHEMBL3718177 134616 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 240 1 2 5 2.0 Cc1ccccc1-n1c(N)nc2ccc(O)nc21 nan
58345673 134629 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 263 1 1 4 2.9 Oc1ccc2nc(Cl)n(-c3ccccc3F)c2n1 nan
CHEMBL3718227 134629 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 263 1 1 4 2.9 Oc1ccc2nc(Cl)n(-c3ccccc3F)c2n1 nan
58345754 134631 5 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 217 1 1 4 2.6 Oc1ccc2ncn(C3CCCCC3)c2n1 nan
CHEMBL3718239 134631 5 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 217 1 1 4 2.6 Oc1ccc2ncn(C3CCCCC3)c2n1 nan
58345649 134632 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 246 1 1 5 2.2 Oc1ccc2ncn(-c3ccncc3Cl)c2n1 nan
CHEMBL3718240 134632 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 246 1 1 5 2.2 Oc1ccc2ncn(-c3ccncc3Cl)c2n1 nan
58345674 134642 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 240 1 2 5 2.0 Cc1ccc(-n2c(N)nc3ccc(O)nc32)cc1 nan
CHEMBL3718264 134642 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 240 1 2 5 2.0 Cc1ccc(-n2c(N)nc3ccc(O)nc32)cc1 nan
58345769 134661 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 275 1 1 4 3.6 Cc1ccc2ccccc2c1-n1cnc2ccc(O)nc21 nan
CHEMBL3718300 134661 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 275 1 1 4 3.6 Cc1ccc2ccccc2c1-n1cnc2ccc(O)nc21 nan
58345764 134667 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 290 1 2 5 3.2 Cc1ccc2ccccc2c1-n1c(N)nc2ccc(O)nc21 nan
CHEMBL3718324 134667 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 290 1 2 5 3.2 Cc1ccc2ccccc2c1-n1c(N)nc2ccc(O)nc21 nan
58345690 134673 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 259 1 1 4 3.1 Cc1nc2ccc(O)nc2n1-c1ccccc1Cl nan
CHEMBL3718342 134673 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 259 1 1 4 3.1 Cc1nc2ccc(O)nc2n1-c1ccccc1Cl nan
58345679 134677 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 241 2 1 5 2.1 COc1ccccc1-n1cnc2ccc(O)nc21 nan
CHEMBL3718354 134677 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 241 2 1 5 2.1 COc1ccccc1-n1cnc2ccc(O)nc21 nan
58345639 134681 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 279 1 1 4 3.1 Oc1ccc2ncn(-c3ccccc3C(F)(F)F)c2n1 nan
CHEMBL3718371 134681 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 279 1 1 4 3.1 Oc1ccc2ncn(-c3ccccc3C(F)(F)F)c2n1 nan
58345669 134683 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 313 1 1 4 4.1 Oc1ccc2ncn(-c3ccc(Cl)c(Cl)c3Cl)c2n1 nan
CHEMBL3718374 134683 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 313 1 1 4 4.1 Oc1ccc2ncn(-c3ccc(Cl)c(Cl)c3Cl)c2n1 nan
58345727 134694 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 225 1 1 4 2.4 Cc1ccccc1-n1cnc2ccc(O)nc21 nan
CHEMBL3718416 134694 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 225 1 1 4 2.4 Cc1ccccc1-n1cnc2ccc(O)nc21 nan
86655261 134700 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 311 3 1 7 2.0 CS(=O)(=O)Oc1ccc2nc(O)n(C3CCCCC3)c2n1 nan
CHEMBL3718427 134700 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 311 3 1 7 2.0 CS(=O)(=O)Oc1ccc2nc(O)n(C3CCCCC3)c2n1 nan
58345762 134729 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 245 1 1 4 2.8 Oc1ccc2nc(Cl)n(-c3ccccc3)c2n1 nan
CHEMBL3718549 134729 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 245 1 1 4 2.8 Oc1ccc2nc(Cl)n(-c3ccccc3)c2n1 nan
58345760 134746 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 262 1 2 5 2.0 Nc1nc2ccc(O)nc2n1-c1cccc(F)c1F nan
CHEMBL3718610 134746 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 262 1 2 5 2.0 Nc1nc2ccc(O)nc2n1-c1cccc(F)c1F nan
58345732 134752 10 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 211 1 1 4 2.1 Oc1ccc2ncn(-c3ccccc3)c2n1 nan
CHEMBL3718619 134752 10 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 211 1 1 4 2.1 Oc1ccc2ncn(-c3ccccc3)c2n1 nan
58345755 134754 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 327 1 1 4 4.4 Cc1nc2ccc(O)nc2n1-c1cc(Cl)c(Cl)cc1Cl nan
CHEMBL3718623 134754 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 327 1 1 4 4.4 Cc1nc2ccc(O)nc2n1-c1cc(Cl)c(Cl)cc1Cl nan
58345662 134755 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 203 1 1 4 2.3 Oc1ccc2ncn(C3CCCC3)c2n1 nan
CHEMBL3718624 134755 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 203 1 1 4 2.3 Oc1ccc2ncn(C3CCCC3)c2n1 nan
58345736 134759 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 263 1 1 4 3.2 Oc1ccc2nc(Cl)n(C3CC4CCC3C4)c2n1 nan
CHEMBL3718632 134759 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 263 1 1 4 3.2 Oc1ccc2nc(Cl)n(C3CC4CCC3C4)c2n1 nan
58345670 134760 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 313 1 1 4 3.8 Oc1ccc2ncn(-c3ccc(Cl)cc3C(F)(F)F)c2n1 nan
CHEMBL3718634 134760 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 313 1 1 4 3.8 Oc1ccc2ncn(-c3ccc(Cl)cc3C(F)(F)F)c2n1 nan
58345671 134762 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 251 1 1 4 2.6 Oc1ccc2ncn(-c3cccc4c3CCC4)c2n1 nan
CHEMBL3718637 134762 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 251 1 1 4 2.6 Oc1ccc2ncn(-c3cccc4c3CCC4)c2n1 nan
58345699 134799 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 303 1 1 4 3.2 Cc1nc2ccc(O)nc2n1-c1ccc(Br)cc1 nan
CHEMBL3718747 134799 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 303 1 1 4 3.2 Cc1nc2ccc(O)nc2n1-c1ccc(Br)cc1 nan
58345721 134812 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 303 1 1 4 3.2 Cc1cccc(-n2cnc3ccc(O)nc32)c1Br nan
CHEMBL3718790 134812 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 303 1 1 4 3.2 Cc1cccc(-n2cnc3ccc(O)nc32)c1Br nan
58345742 134818 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 283 1 1 4 3.4 Cc1nc2ccc(O)nc2n1C12CC3CC(CC(C3)C1)C2 nan
CHEMBL3718804 134818 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 283 1 1 4 3.4 Cc1nc2ccc(O)nc2n1C12CC3CC(CC(C3)C1)C2 nan
58345717 134846 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 231 1 1 4 2.9 CC1CCCCC1n1cnc2ccc(O)nc21 nan
CHEMBL3718877 134846 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 231 1 1 4 2.9 CC1CCCCC1n1cnc2ccc(O)nc21 nan
58345652 134866 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 260 1 2 5 2.4 Nc1nc2ccc(O)nc2n1-c1ccccc1Cl nan
CHEMBL3718998 134866 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 260 1 2 5 2.4 Nc1nc2ccc(O)nc2n1-c1ccccc1Cl nan
58345767 134874 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 311 2 1 5 3.7 Oc1ccc2ncn(-c3ccccc3SC(F)(F)F)c2n1 nan
CHEMBL3719017 134874 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 311 2 1 5 3.7 Oc1ccc2ncn(-c3ccccc3SC(F)(F)F)c2n1 nan
58345744 134876 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 189 1 1 4 1.9 Oc1ccc2ncn(C3CCC3)c2n1 nan
CHEMBL3719026 134876 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 189 1 1 4 1.9 Oc1ccc2ncn(C3CCC3)c2n1 nan
58345658 134902 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 259 1 1 4 3.1 Cc1ccc(Cl)cc1-n1cnc2ccc(O)nc21 nan
CHEMBL3719094 134902 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 259 1 1 4 3.1 Cc1ccc(Cl)cc1-n1cnc2ccc(O)nc21 nan
58345716 134916 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 323 1 1 4 3.5 Oc1ccc2nc(Cl)n(-c3ccccc3Br)c2n1 nan
CHEMBL3719152 134916 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 323 1 1 4 3.5 Oc1ccc2nc(Cl)n(-c3ccccc3Br)c2n1 nan
58345718 134921 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 225 1 1 4 2.4 Cc1nc2ccc(O)nc2n1-c1ccccc1 nan
CHEMBL3719178 134921 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 225 1 1 4 2.4 Cc1nc2ccc(O)nc2n1-c1ccccc1 nan
58345642 134927 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 303 1 1 4 3.2 Cc1ccccc1-n1c(Br)nc2ccc(O)nc21 nan
CHEMBL3719204 134927 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 303 1 1 4 3.2 Cc1ccccc1-n1c(Br)nc2ccc(O)nc21 nan
58345711 134934 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 337 1 1 4 3.9 Cc1cc(Br)c(Cl)cc1-n1cnc2ccc(O)nc21 nan
CHEMBL3719226 134934 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 337 1 1 4 3.9 Cc1cc(Br)c(Cl)cc1-n1cnc2ccc(O)nc21 nan
58345703 134939 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 279 1 1 4 3.4 Oc1ccc2ncn(-c3ccc(Cl)cc3Cl)c2n1 nan
CHEMBL3719235 134939 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 279 1 1 4 3.4 Oc1ccc2ncn(-c3ccc(Cl)cc3Cl)c2n1 nan
58345687 134954 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 285 2 1 4 3.7 Oc1ccc2nc(Cl)n(-c3ccccc3C3CC3)c2n1 nan
CHEMBL3719273 134954 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 285 2 1 4 3.7 Oc1ccc2nc(Cl)n(-c3ccccc3C3CC3)c2n1 nan
58345730 134964 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 266 1 2 5 2.2 Nc1nc2ccc(O)nc2n1-c1cccc2c1CCC2 nan
CHEMBL3719308 134964 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 266 1 2 5 2.2 Nc1nc2ccc(O)nc2n1-c1cccc2c1CCC2 nan
58345715 134977 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 257 2 1 5 2.8 CSc1nc2ccc(O)nc2n1-c1ccccc1 nan
CHEMBL3719363 134977 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 257 2 1 5 2.8 CSc1nc2ccc(O)nc2n1-c1ccccc1 nan
58345720 134323 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 258 1 2 5 2.2 Cc1c(F)cccc1-n1c(N)nc2ccc(O)nc21 nan
CHEMBL3717145 134323 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 258 1 2 5 2.2 Cc1c(F)cccc1-n1c(N)nc2ccc(O)nc21 nan
156018500 177924 0 None 6 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 629 7 1 10 4.5 CCOc1cc(Cl)c(-c2ncc(-c3nc4ccc(S(=O)(=O)C5CCN(C)CC5)cc4s3)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4645314 177924 0 None 6 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 629 7 1 10 4.5 CCOc1cc(Cl)c(-c2ncc(-c3nc4ccc(S(=O)(=O)C5CCN(C)CC5)cc4s3)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
156016504 177647 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 459 5 2 6 4.8 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2cc3ccccc3s2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4641428 177647 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 459 5 2 6 4.8 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2cc3ccccc3s2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
156016073 177655 0 None 11 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 649 10 1 10 4.6 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1N1C[C@H](C)O[C@@H](C)C1 10.1016/j.bmcl.2020.126953
CHEMBL4641503 177655 0 None 11 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 649 10 1 10 4.6 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1N1C[C@H](C)O[C@@H](C)C1 10.1016/j.bmcl.2020.126953
58345749 134841 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 263 1 1 4 2.9 Oc1ccc2ncn(-c3cccc(Cl)c3F)c2n1 nan
CHEMBL3718861 134841 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 263 1 1 4 2.9 Oc1ccc2ncn(-c3cccc(Cl)c3F)c2n1 nan
156012845 177297 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 460 5 2 7 4.1 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3ccccc3s2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4636565 177297 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 460 5 2 7 4.1 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3ccccc3s2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
58345719 134031 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 269 1 1 4 3.1 Oc1ccc2ncn(C34CC5CC(CC(C5)C3)C4)c2n1 nan
CHEMBL3716171 134031 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 269 1 1 4 3.1 Oc1ccc2ncn(C34CC5CC(CC(C5)C3)C4)c2n1 nan
156022271 178193 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 586 7 2 9 4.3 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(CN4CCN(C)CC4)cc3s2)cc1N1CCO[C@H](C)C1 10.1016/j.bmcl.2020.126953
CHEMBL4649373 178193 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 586 7 2 9 4.3 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(CN4CCN(C)CC4)cc3s2)cc1N1CCO[C@H](C)C1 10.1016/j.bmcl.2020.126953
58345651 134434 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 231 1 1 4 3.0 Oc1ccc2ncn(C3CCCCCC3)c2n1 nan
CHEMBL3717555 134434 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay
ChEMBL 231 1 1 4 3.0 Oc1ccc2ncn(C3CCCCCC3)c2n1 nan
156013623 177237 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 553 7 3 8 4.4 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(CN4CCN(C)CC4)cc3s2)cc1-c1ccn[nH]1 10.1016/j.bmcl.2020.126953
CHEMBL4635725 177237 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 553 7 3 8 4.4 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(CN4CCN(C)CC4)cc3s2)cc1-c1ccn[nH]1 10.1016/j.bmcl.2020.126953
57422804 177350 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 576 5 2 9 4.1 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(-n5cccn5)c(F)cc4Cl)sc3c2)CC1 10.1016/j.bmcl.2020.126953
CHEMBL4637505 177350 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 576 5 2 9 4.1 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(-n5cccn5)c(F)cc4Cl)sc3c2)CC1 10.1016/j.bmcl.2020.126953
11228924 80487 85 None - 1 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human recombinant GPR81 transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR81 transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assay
ChEMBL 156 1 2 2 1.2 O=C(O)c1cc(O)cc(F)c1 10.1021/ml3000676
CHEMBL2146989 80487 85 None - 1 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human recombinant GPR81 transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR81 transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assay
ChEMBL 156 1 2 2 1.2 O=C(O)c1cc(O)cc(F)c1 10.1021/ml3000676
156016789 177709 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 529 7 1 8 4.2 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(CN4CCN(C)CC4)cc3s2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4642179 177709 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 529 7 1 8 4.2 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(CN4CCN(C)CC4)cc3s2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
231756 80484 102 None - 1 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human recombinant GPR81 transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR81 transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assay
ChEMBL 152 1 2 2 1.4 Cc1cc(O)cc(C(=O)O)c1 10.1021/ml3000676
CHEMBL2146905 80484 102 None - 1 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human recombinant GPR81 transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR81 transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assay
ChEMBL 152 1 2 2 1.4 Cc1cc(O)cc(C(=O)O)c1 10.1021/ml3000676
156018460 177877 0 None 10 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 468 5 1 7 4.6 CCOc1cc(Cl)c(-c2ncc(-c3nc4ccccc4s3)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4644587 177877 0 None 10 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 468 5 1 7 4.6 CCOc1cc(Cl)c(-c2ncc(-c3nc4ccccc4s3)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
156016110 177698 0 None 7 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 628 7 1 9 5.1 CCOc1cc(Cl)c(-c2ccc(-c3nc4ccc(S(=O)(=O)C5CCN(C)CC5)cc4s3)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4642043 177698 0 None 7 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 628 7 1 9 5.1 CCOc1cc(Cl)c(-c2ccc(-c3nc4ccc(S(=O)(=O)C5CCN(C)CC5)cc4s3)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
156012428 177310 0 None 12 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 649 10 1 10 4.6 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1N1C[C@H](C)O[C@H](C)C1 10.1016/j.bmcl.2020.126953
CHEMBL4636832 177310 0 None 12 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 649 10 1 10 4.6 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1N1C[C@H](C)O[C@H](C)C1 10.1016/j.bmcl.2020.126953
156012757 177312 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 487 6 2 7 4.1 CCOc1ccc(C(=O)NC(=O)Nc2nc3ccc(CN4CCN(C)CC4)cc3s2)c(Cl)c1 10.1016/j.bmcl.2020.126953
CHEMBL4636849 177312 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 487 6 2 7 4.1 CCOc1ccc(C(=O)NC(=O)Nc2nc3ccc(CN4CCN(C)CC4)cc3s2)c(Cl)c1 10.1016/j.bmcl.2020.126953
156010748 177118 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 621 10 1 10 3.8 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4633635 177118 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 621 10 1 10 3.8 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
57422809 178002 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 572 5 2 9 4.3 Cc1cc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)C4CCN(C)CC4)cc3s2)cc1-n1cccn1 10.1016/j.bmcl.2020.126953
CHEMBL4646399 178002 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 572 5 2 9 4.3 Cc1cc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)C4CCN(C)CC4)cc3s2)cc1-n1cccn1 10.1016/j.bmcl.2020.126953
13071646 80485 102 None -9 4 Dog 4.2 pEC50 = 4.2 Functional
Agonist activity at dog GPR81Agonist activity at dog GPR81
ChEMBL 172 1 2 2 1.7 O=C(O)c1cc(O)cc(Cl)c1 10.1021/ml3000676
CHEMBL2146910 80485 102 None -9 4 Dog 4.2 pEC50 = 4.2 Functional
Agonist activity at dog GPR81Agonist activity at dog GPR81
ChEMBL 172 1 2 2 1.7 O=C(O)c1cc(O)cc(Cl)c1 10.1021/ml3000676
57422696 113478 0 None -457 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 558 5 2 9 4.0 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(-n5cccn5)ccc4Cl)sc3c2)CC1 10.1016/j.bmcl.2020.126953
CHEMBL3319403 113478 0 None -457 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 558 5 2 9 4.0 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(-n5cccn5)ccc4Cl)sc3c2)CC1 10.1016/j.bmcl.2020.126953
13071646 80485 102 None 2 4 Rat 5.2 pEC50 = 5.2 Functional
Agonist activity at rat GPR81Agonist activity at rat GPR81
ChEMBL 172 1 2 2 1.7 O=C(O)c1cc(O)cc(Cl)c1 10.1021/ml3000676
CHEMBL2146910 80485 102 None 2 4 Rat 5.2 pEC50 = 5.2 Functional
Agonist activity at rat GPR81Agonist activity at rat GPR81
ChEMBL 172 1 2 2 1.7 O=C(O)c1cc(O)cc(Cl)c1 10.1021/ml3000676
156011543 177439 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 507 5 2 8 2.9 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3c(s2)CN(C(C)=O)CC3)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4638731 177439 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 507 5 2 8 2.9 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3c(s2)CN(C(C)=O)CC3)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
11197 1066 0 None 12 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 572 7 2 9 3.9 CCOc1cc(Cl)c(cc1N1CCOCC1)C(=O)NC(=O)Nc1nc2c(s1)cc(cc2)CN1CCN(CC1)C 10.1016/j.bmcl.2020.126953
154699458 1066 0 None 12 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 572 7 2 9 3.9 CCOc1cc(Cl)c(cc1N1CCOCC1)C(=O)NC(=O)Nc1nc2c(s1)cc(cc2)CN1CCN(CC1)C 10.1016/j.bmcl.2020.126953
CHEMBL4632411 1066 0 None 12 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 572 7 2 9 3.9 CCOc1cc(Cl)c(cc1N1CCOCC1)C(=O)NC(=O)Nc1nc2c(s1)cc(cc2)CN1CCN(CC1)C 10.1016/j.bmcl.2020.126953
156012724 177433 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 578 7 1 9 4.3 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(S(=O)(=O)C4CCN(C)CC4)cc3s2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4638676 177433 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 578 7 1 9 4.3 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(S(=O)(=O)C4CCN(C)CC4)cc3s2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
156016380 177644 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 538 7 2 9 3.2 CCOc1ccc(C(=O)NC(=O)Nc2nc3ccc(CN4CCN(C)CC4)cc3s2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4641372 177644 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 538 7 2 9 3.2 CCOc1ccc(C(=O)NC(=O)Nc2nc3ccc(CN4CCN(C)CC4)cc3s2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
156011618 177398 0 None 25 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 544 7 1 8 3.6 CCOc1cc(Cl)c(-c2ccc(-c3nc4c(s3)CN(C(=O)COC)CC4)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4638263 177398 0 None 25 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 544 7 1 8 3.6 CCOc1cc(Cl)c(-c2ccc(-c3nc4c(s3)CN(C(=O)COC)CC4)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
58345644 133800 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 251 1 1 4 3.3 Oc1ccc2nc(Cl)n(C3CCCCC3)c2n1 nan
CHEMBL3715375 133800 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 251 1 1 4 3.3 Oc1ccc2nc(Cl)n(C3CCCCC3)c2n1 nan
156010684 177140 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 424 5 2 7 3.3 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2ncc(C)s2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4633947 177140 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 424 5 2 7 3.3 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2ncc(C)s2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
58345687 134954 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 285 2 1 4 3.7 Oc1ccc2nc(Cl)n(-c3ccccc3C3CC3)c2n1 nan
CHEMBL3719273 134954 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay
ChEMBL 285 2 1 4 3.7 Oc1ccc2nc(Cl)n(-c3ccccc3C3CC3)c2n1 nan
156017705 177800 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 523 6 3 9 1.9 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3c(s2)CN(C(=O)CO)CC3)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4643496 177800 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 523 6 3 9 1.9 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3c(s2)CN(C(=O)CO)CC3)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
10413 1762 0 None - 1 Human 1.8 pEC50 = 1.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 104 3 2 2 -0.2 OCCCC(=O)O 19047060
4711 1762 0 None - 1 Human 1.8 pEC50 = 1.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 104 3 2 2 -0.2 OCCCC(=O)O 19047060
CHEMBL1342 1762 0 None - 1 Human 1.8 pEC50 = 1.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 104 3 2 2 -0.2 OCCCC(=O)O 19047060
DB01440 1762 0 None - 1 Human 1.8 pEC50 = 1.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 104 3 2 2 -0.2 OCCCC(=O)O 19047060
107689 2336 0 None -2 2 Human 2.1 pEC50 = 2.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 90 1 2 2 -0.5 OC(=O)[C@@H](O)C 18952058
107689 2336 0 None -2 2 Human 2.1 pEC50 = 2.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 90 1 2 2 -0.5 OC(=O)[C@@H](O)C 19047060
107689 2336 0 None -2 2 Human 2.1 pEC50 = 2.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 90 1 2 2 -0.5 OC(=O)[C@@H](O)C 20374963
107689 2336 0 None -2 2 Human 2.1 pEC50 = 2.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 90 1 2 2 -0.5 OC(=O)[C@@H](O)C 23396314
2932 2336 0 None -2 2 Human 2.1 pEC50 = 2.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 90 1 2 2 -0.5 OC(=O)[C@@H](O)C 18952058
2932 2336 0 None -2 2 Human 2.1 pEC50 = 2.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 90 1 2 2 -0.5 OC(=O)[C@@H](O)C 19047060
2932 2336 0 None -2 2 Human 2.1 pEC50 = 2.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 90 1 2 2 -0.5 OC(=O)[C@@H](O)C 20374963
2932 2336 0 None -2 2 Human 2.1 pEC50 = 2.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 90 1 2 2 -0.5 OC(=O)[C@@H](O)C 23396314
CHEMBL330546 2336 0 None -2 2 Human 2.1 pEC50 = 2.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 90 1 2 2 -0.5 OC(=O)[C@@H](O)C 18952058
CHEMBL330546 2336 0 None -2 2 Human 2.1 pEC50 = 2.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 90 1 2 2 -0.5 OC(=O)[C@@H](O)C 19047060
CHEMBL330546 2336 0 None -2 2 Human 2.1 pEC50 = 2.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 90 1 2 2 -0.5 OC(=O)[C@@H](O)C 20374963
CHEMBL330546 2336 0 None -2 2 Human 2.1 pEC50 = 2.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 90 1 2 2 -0.5 OC(=O)[C@@H](O)C 23396314
DB14475 2336 0 None -2 2 Human 2.1 pEC50 = 2.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 90 1 2 2 -0.5 OC(=O)[C@@H](O)C 18952058
DB14475 2336 0 None -2 2 Human 2.1 pEC50 = 2.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 90 1 2 2 -0.5 OC(=O)[C@@H](O)C 19047060
DB14475 2336 0 None -2 2 Human 2.1 pEC50 = 2.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 90 1 2 2 -0.5 OC(=O)[C@@H](O)C 20374963
DB14475 2336 0 None -2 2 Human 2.1 pEC50 = 2.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 90 1 2 2 -0.5 OC(=O)[C@@H](O)C 23396314
107689 2336 0 None 2 2 Mouse 2.5 pEC50 = 2.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 90 1 2 2 -0.5 OC(=O)[C@@H](O)C 19047060
107689 2336 0 None 2 2 Mouse 2.5 pEC50 = 2.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 90 1 2 2 -0.5 OC(=O)[C@@H](O)C 20374963
2932 2336 0 None 2 2 Mouse 2.5 pEC50 = 2.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 90 1 2 2 -0.5 OC(=O)[C@@H](O)C 19047060
2932 2336 0 None 2 2 Mouse 2.5 pEC50 = 2.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 90 1 2 2 -0.5 OC(=O)[C@@H](O)C 20374963
CHEMBL330546 2336 0 None 2 2 Mouse 2.5 pEC50 = 2.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 90 1 2 2 -0.5 OC(=O)[C@@H](O)C 19047060
CHEMBL330546 2336 0 None 2 2 Mouse 2.5 pEC50 = 2.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 90 1 2 2 -0.5 OC(=O)[C@@H](O)C 20374963
DB14475 2336 0 None 2 2 Mouse 2.5 pEC50 = 2.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 90 1 2 2 -0.5 OC(=O)[C@@H](O)C 19047060
DB14475 2336 0 None 2 2 Mouse 2.5 pEC50 = 2.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 90 1 2 2 -0.5 OC(=O)[C@@H](O)C 20374963
2934 1442 0 None - 1 Human 2.5 pEC50 = 2.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 90 1 2 2 -0.5 OC(=O)[C@H](O)C 18952058
61503 1442 0 None - 1 Human 2.5 pEC50 = 2.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 90 1 2 2 -0.5 OC(=O)[C@H](O)C 18952058
CHEMBL358850 1442 0 None - 1 Human 2.5 pEC50 = 2.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 90 1 2 2 -0.5 OC(=O)[C@H](O)C 18952058
DB03066 1442 0 None - 1 Human 2.5 pEC50 = 2.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 90 1 2 2 -0.5 OC(=O)[C@H](O)C 18952058
5783 94 0 None -1 2 Human 3.7 pEC50 = 3.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 154 1 3 3 0.8 Oc1cc(O)cc(c1)C(=O)O 22434674
7424 94 0 None -1 2 Human 3.7 pEC50 = 3.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 154 1 3 3 0.8 Oc1cc(O)cc(c1)C(=O)O 22434674
CHEMBL95308 94 0 None -1 2 Human 3.7 pEC50 = 3.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 154 1 3 3 0.8 Oc1cc(O)cc(c1)C(=O)O 22434674
5783 94 0 None 1 2 Mouse 3.8 pEC50 = 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 154 1 3 3 0.8 Oc1cc(O)cc(c1)C(=O)O 22434674
7424 94 0 None 1 2 Mouse 3.8 pEC50 = 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 154 1 3 3 0.8 Oc1cc(O)cc(c1)C(=O)O 22434674
CHEMBL95308 94 0 None 1 2 Mouse 3.8 pEC50 = 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 154 1 3 3 0.8 Oc1cc(O)cc(c1)C(=O)O 22434674
11197 1066 0 None 12 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 572 7 2 9 3.9 CCOc1cc(Cl)c(cc1N1CCOCC1)C(=O)NC(=O)Nc1nc2c(s1)cc(cc2)CN1CCN(CC1)C 28978803
11197 1066 0 None 12 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 572 7 2 9 3.9 CCOc1cc(Cl)c(cc1N1CCOCC1)C(=O)NC(=O)Nc1nc2c(s1)cc(cc2)CN1CCN(CC1)C 31932225
154699458 1066 0 None 12 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 572 7 2 9 3.9 CCOc1cc(Cl)c(cc1N1CCOCC1)C(=O)NC(=O)Nc1nc2c(s1)cc(cc2)CN1CCN(CC1)C 28978803
154699458 1066 0 None 12 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 572 7 2 9 3.9 CCOc1cc(Cl)c(cc1N1CCOCC1)C(=O)NC(=O)Nc1nc2c(s1)cc(cc2)CN1CCN(CC1)C 31932225
CHEMBL4632411 1066 0 None 12 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 572 7 2 9 3.9 CCOc1cc(Cl)c(cc1N1CCOCC1)C(=O)NC(=O)Nc1nc2c(s1)cc(cc2)CN1CCN(CC1)C 28978803
CHEMBL4632411 1066 0 None 12 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 572 7 2 9 3.9 CCOc1cc(Cl)c(cc1N1CCOCC1)C(=O)NC(=O)Nc1nc2c(s1)cc(cc2)CN1CCN(CC1)C 31932225
8467 1063 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 446 5 1 6 4.0 C[C@@H]1CC[C@H](CC1)C(=O)Nc1nc(c(s1)CC(=O)N1CCN(CC1)C)c1cccs1 24486398
86279608 1063 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 446 5 1 6 4.0 C[C@@H]1CC[C@H](CC1)C(=O)Nc1nc(c(s1)CC(=O)N1CCN(CC1)C)c1cccs1 24486398


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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
Sel. page Similar-
ity		 Common
name		 GPCRdb
ID		 #Vendors

 Reference
ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 Assay
Type		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
145984458 165495 0 None - 0 Rat 6.0 pEC50 = 6 Binding
Agonist activity at rat GPR81 expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assayAgonist activity at rat GPR81 expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assay
ChEMBL 600 7 2 8 4.6 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3c(s2)C[Si](C)(c2ccc(OC)cc2)CC3)cc1N1CCOCC1 10.1021/acs.jmedchem.7b00718
CHEMBL4240407 165495 0 None - 0 Rat 6.0 pEC50 = 6 Binding
Agonist activity at rat GPR81 expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assayAgonist activity at rat GPR81 expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assay
ChEMBL 600 7 2 8 4.6 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3c(s2)C[Si](C)(c2ccc(OC)cc2)CC3)cc1N1CCOCC1 10.1021/acs.jmedchem.7b00718
145984088 165815 0 None - 0 Rat 5.9 pEC50 = 5.9 Binding
Agonist activity at rat GPR81 expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assayAgonist activity at rat GPR81 expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assay
ChEMBL 630 8 2 9 4.6 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3c(s2)C[Si](C)(c2c(OC)cccc2OC)CC3)cc1N1CCOCC1 10.1021/acs.jmedchem.7b00718
CHEMBL4248415 165815 0 None - 0 Rat 5.9 pEC50 = 5.9 Binding
Agonist activity at rat GPR81 expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assayAgonist activity at rat GPR81 expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assay
ChEMBL 630 8 2 9 4.6 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3c(s2)C[Si](C)(c2c(OC)cccc2OC)CC3)cc1N1CCOCC1 10.1021/acs.jmedchem.7b00718
145985690 165443 0 None - 0 Rat 6.6 pEC50 = 6.6 Binding
Agonist activity at rat GPR81 expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assayAgonist activity at rat GPR81 expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assay
ChEMBL 464 5 2 7 3.9 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3c(s2)CCCC3)cc1N1CCOCC1 10.1021/acs.jmedchem.7b00718
CHEMBL4239086 165443 0 None - 0 Rat 6.6 pEC50 = 6.6 Binding
Agonist activity at rat GPR81 expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assayAgonist activity at rat GPR81 expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assay
ChEMBL 464 5 2 7 3.9 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3c(s2)CCCC3)cc1N1CCOCC1 10.1021/acs.jmedchem.7b00718