GPCRdb

Ligand source activities (1 row/activity)

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Ligands					Receptor			Assay information							Chemical information
Sel. page	Common name	GPCRdb ID	#Vendors	Reference ligand	Fold selectivity (Potency)	# tested GPCRs (Potency)	Species	p-value (-log)	Type	Activity Relation	Activity Value	Assay Type	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI
	156013464	176913	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	176913	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	133911	0	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	133911	0	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	177390	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	177390	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	164880	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	164880	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	176453	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	176453	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	134224	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	134224	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	133107	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133107	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133121	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133121	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133122	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133122	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133129	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133129	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133145	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133145	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133148	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133148	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133162	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133162	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133168	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133168	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133187	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133187	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133210	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133210	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133218	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133218	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133230	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133230	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133257	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133257	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133258	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133258	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133266	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133266	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133287	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133287	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133302	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133302	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133310	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133310	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133314	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133314	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133316	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133316	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133322	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133322	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133324	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133324	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133327	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133327	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133330	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133330	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133345	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133345	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133373	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133373	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133384	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133384	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133391	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133391	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133395	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133395	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133410	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133410	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133411	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133411	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133419	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133419	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133420	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133420	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133424	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133424	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133430	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133430	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133454	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133454	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133456	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133456	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133469	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133469	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133480	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133480	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133499	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133499	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133519	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133519	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133520	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133520	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133524	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133524	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133527	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133527	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133532	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133532	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133535	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133535	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133539	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133539	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133555	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133555	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133560	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133560	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133578	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133578	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133587	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133587	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133591	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133591	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133593	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133593	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133594	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133594	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133609	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133609	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133626	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133626	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133631	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133631	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133636	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133636	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	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	259	2	1	4	3.5	CCC1(n2c(C)nc3ccc(O)nc32)CCCCC1	nan
	CHEMBL3716678	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	259	2	1	4	3.5	CCC1(n2c(C)nc3ccc(O)nc32)CCCCC1	nan
	58345645	133645	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133645	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133697	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133697	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133715	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133715	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133722	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133722	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133738	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133738	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133739	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133739	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133741	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133741	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133767	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133767	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133770	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133770	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133787	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133787	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133811	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133811	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133826	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133826	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133840	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133840	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	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	307	1	1	4	3.0	Oc1ccc2nc(Br)n(-c3ccccc3F)c2n1	nan
	CHEMBL3717420	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	307	1	1	4	3.0	Oc1ccc2nc(Br)n(-c3ccccc3F)c2n1	nan
	58345756	133859	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133859	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	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	326	2	2	6	3.3	Nc1nc2ccc(O)nc2n1-c1ccccc1SC(F)(F)F	nan
	CHEMBL3717447	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	326	2	2	6	3.3	Nc1nc2ccc(O)nc2n1-c1ccccc1SC(F)(F)F	nan
	58345747	133873	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133873	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133875	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133875	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133880	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133880	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133886	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133886	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133898	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133898	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133904	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133904	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	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	287	2	1	4	3.8	Oc1ccc2ncn(-c3ccccc3-c3ccccc3)c2n1	nan
	CHEMBL3717582	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	287	2	1	4	3.8	Oc1ccc2ncn(-c3ccccc3-c3ccccc3)c2n1	nan
	58345681	133911	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133911	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133919	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133919	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133921	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133921	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133926	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133926	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133942	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133942	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133944	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133944	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133949	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133949	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133959	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133959	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133963	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133963	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133974	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133974	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133982	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133982	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133983	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133983	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133988	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133988	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134004	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134004	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134027	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134027	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134042	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134042	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134052	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134052	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134067	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134067	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134073	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134073	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134079	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134079	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134080	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134080	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134093	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134093	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134095	6	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134095	6	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	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	246	1	1	5	2.2	Oc1ccc2ncn(-c3ccncc3Cl)c2n1	nan
	CHEMBL3718240	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	246	1	1	5	2.2	Oc1ccc2ncn(-c3ccncc3Cl)c2n1	nan
	58345674	134106	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134106	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134125	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134125	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134131	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134131	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134137	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134137	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134141	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134141	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	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	279	1	1	4	3.1	Oc1ccc2ncn(-c3ccccc3C(F)(F)F)c2n1	nan
	CHEMBL3718371	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	279	1	1	4	3.1	Oc1ccc2ncn(-c3ccccc3C(F)(F)F)c2n1	nan
	58345669	134147	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134147	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134158	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134158	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134164	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134164	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134193	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134193	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134210	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134210	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134216	9	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134216	9	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134218	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134218	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134219	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134219	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134223	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134223	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134226	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134226	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134263	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134263	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134276	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134276	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134282	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134282	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134305	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134305	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134310	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134310	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134330	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134330	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134338	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134338	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134340	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134340	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134366	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134366	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134380	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134380	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134385	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134385	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134391	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134391	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134398	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134398	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134403	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134403	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134428	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134428	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134441	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134441	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	176763	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	176763	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	177631	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	177631	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	80059	94	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	80059	94	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	176566	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	176566	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	177048	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	177048	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	177064	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	177064	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	177583	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	177583	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	176608	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	176608	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	176957	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	176957	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	80059	94	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	80059	94	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	177077	2	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	177077	2	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	133107	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133107	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133121	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133121	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133122	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133122	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133129	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133129	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133145	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133145	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133148	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133148	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133162	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133162	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133168	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133168	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133187	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133187	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133210	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133210	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133218	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133218	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133230	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133230	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133257	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133257	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133258	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133258	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133264	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133264	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133266	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133266	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133287	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133287	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133302	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133302	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133310	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133310	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133314	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133314	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133316	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133316	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133322	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133322	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133324	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133324	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133327	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133327	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133330	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133330	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133345	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133345	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133373	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133373	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133384	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133384	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133391	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133391	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133395	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133395	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133410	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133410	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133411	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133411	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133419	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133419	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133420	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133420	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133424	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133424	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133430	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133430	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133454	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133454	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133456	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133456	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133469	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133469	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133480	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133480	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133495	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133495	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133499	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133499	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133519	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133519	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133520	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133520	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133524	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133524	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133527	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133527	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133532	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133532	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133535	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133535	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133539	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133539	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133555	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133555	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133560	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133560	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133578	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133578	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133587	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133587	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133591	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133591	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133593	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133593	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133594	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133594	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133609	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133609	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133626	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133626	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133631	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133631	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133636	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133636	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	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	259	2	1	4	3.5	CCC1(n2c(C)nc3ccc(O)nc32)CCCCC1	nan
	CHEMBL3716678	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	259	2	1	4	3.5	CCC1(n2c(C)nc3ccc(O)nc32)CCCCC1	nan
	58345645	133645	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133645	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133697	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133697	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133715	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133715	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133722	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133722	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133738	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133738	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133739	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133739	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133741	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133741	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133767	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133767	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133770	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133770	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133811	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133811	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133826	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133826	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133840	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133840	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	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	307	1	1	4	3.0	Oc1ccc2nc(Br)n(-c3ccccc3F)c2n1	nan
	CHEMBL3717420	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	307	1	1	4	3.0	Oc1ccc2nc(Br)n(-c3ccccc3F)c2n1	nan
	58345756	133859	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133859	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	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	326	2	2	6	3.3	Nc1nc2ccc(O)nc2n1-c1ccccc1SC(F)(F)F	nan
	CHEMBL3717447	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	326	2	2	6	3.3	Nc1nc2ccc(O)nc2n1-c1ccccc1SC(F)(F)F	nan
	58345747	133873	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133873	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133875	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133875	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133880	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133880	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133886	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133886	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133904	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133904	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	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	287	2	1	4	3.8	Oc1ccc2ncn(-c3ccccc3-c3ccccc3)c2n1	nan
	CHEMBL3717582	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	287	2	1	4	3.8	Oc1ccc2ncn(-c3ccccc3-c3ccccc3)c2n1	nan
	58345680	133919	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133919	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133921	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133921	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133926	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133926	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133942	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133942	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133944	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133944	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133949	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133949	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133959	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133959	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133963	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133963	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133974	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133974	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133982	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133982	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133983	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133983	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133988	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133988	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134004	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134004	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134027	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134027	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134042	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134042	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134052	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134052	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134067	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134067	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134073	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134073	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134079	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134079	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134080	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134080	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134093	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134093	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134095	6	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134095	6	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	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	246	1	1	5	2.2	Oc1ccc2ncn(-c3ccncc3Cl)c2n1	nan
	CHEMBL3718240	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	246	1	1	5	2.2	Oc1ccc2ncn(-c3ccncc3Cl)c2n1	nan
	58345674	134106	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134106	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134125	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134125	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134131	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134131	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134137	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134137	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134141	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134141	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	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	279	1	1	4	3.1	Oc1ccc2ncn(-c3ccccc3C(F)(F)F)c2n1	nan
	CHEMBL3718371	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	279	1	1	4	3.1	Oc1ccc2ncn(-c3ccccc3C(F)(F)F)c2n1	nan
	58345669	134147	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134147	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134158	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134158	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134164	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134164	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134193	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134193	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134210	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134210	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134216	9	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134216	9	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134218	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134218	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134219	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134219	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134223	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134223	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134224	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134224	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134226	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134226	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134263	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134263	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134276	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134276	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134282	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134282	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134310	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134310	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134330	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134330	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134338	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134338	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134340	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134340	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134366	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134366	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134380	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134380	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134385	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134385	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134391	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134391	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134398	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134398	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134403	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134403	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134418	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134418	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134428	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134428	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134441	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134441	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133787	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	133787	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	177340	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	177340	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	177063	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	177063	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	177071	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	177071	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	134305	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	134305	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	176713	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	176713	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	133495	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	133495	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	177609	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	177609	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	133898	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	133898	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	176653	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	176653	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	176766	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	176766	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	80061	75	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	80061	75	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	177125	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	177125	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	80058	98	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	80058	98	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	177293	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	177293	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	177114	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	177114	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	176726	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	176726	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	176728	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	176728	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	176534	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	176534	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	177418	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	177418	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	80059	94	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	80059	94	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	112966	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	112966	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	80059	94	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	80059	94	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	176855	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	176855	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	1046	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	1046	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	1046	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	176849	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	176849	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	177060	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	177060	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	176814	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	176814	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	133264	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	133264	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	176556	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	176556	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	134418	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	134418	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	177216	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	177216	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	1724	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	1724	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	1724	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	1724	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	2295	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	2295	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	2295	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	2295	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	2295	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	2295	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	2295	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	2295	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	2295	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	2295	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	2295	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	2295	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	2295	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	2295	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	2295	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	2295	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	2295	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	2295	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	2295	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	2295	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	2295	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	2295	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	2295	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	2295	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	1409	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	1409	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	1409	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	1409	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	1046	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	1046	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	1046	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	1046	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	1046	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	1046	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	1043	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	1043	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					Receptor			Assay information							Chemical information
Sel. page	Common name	GPCRdb ID	#Vendors	Reference ligand	Fold selectivity (Affinity)	# tested GPCRs (Affinity)	Species	p-value (-log)	Type	Activity Relation	Activity Value	Assay Type	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI
	145984458	164932	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	164932	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	165251	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	165251	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	164880	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	164880	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

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Main reference

Ligand source activities (1 row/activity)