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	184276	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	184276	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	141225	1	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	226	1	2	5	1.7	Nc1nc2ccc(O)nc2n1-c1ccccc1	nan
	CHEMBL3717589	141225	1	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	226	1	2	5	1.7	Nc1nc2ccc(O)nc2n1-c1ccccc1	nan
	156019324	184753	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	184753	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	172222	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	172222	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	183816	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	183816	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	141538	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	141538	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	140421	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140421	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140435	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140435	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140436	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140436	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140443	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140443	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140459	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140459	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140462	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140462	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140476	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140476	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140482	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140482	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140501	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140501	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140524	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140524	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140532	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140532	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140544	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140544	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140571	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140571	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140572	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140572	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140580	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140580	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140601	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140601	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140616	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140616	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140624	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140624	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140628	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140628	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140630	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140630	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140636	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140636	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140638	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140638	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140641	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140641	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140644	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140644	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140659	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140659	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140687	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140687	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140698	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140698	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140705	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140705	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140709	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140709	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140724	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140724	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140725	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140725	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140733	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140733	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140734	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140734	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140738	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140738	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140744	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140744	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140768	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140768	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140770	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140770	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140783	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140783	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140794	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140794	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140813	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140813	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140833	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140833	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140834	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140834	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140838	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140838	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140841	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140841	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140846	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140846	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140849	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140849	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140853	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140853	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140869	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140869	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140874	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140874	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140892	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140892	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140901	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140901	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140905	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140905	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140907	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140907	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140908	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140908	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140923	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140923	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140940	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140940	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140945	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140945	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140950	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140950	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140957	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140957	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140959	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	140959	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141011	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141011	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141029	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141029	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141036	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141036	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141052	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141052	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141053	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141053	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141055	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141055	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141081	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141081	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141084	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141084	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141101	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141101	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141125	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141125	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141140	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141140	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141154	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141154	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141172	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141172	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141173	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141173	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141180	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141180	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141187	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141187	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141189	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141189	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141194	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141194	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141200	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141200	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141212	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141212	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141218	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141218	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141223	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141223	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141225	1	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	226	1	2	5	1.7	Nc1nc2ccc(O)nc2n1-c1ccccc1	nan
	CHEMBL3717589	141225	1	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	226	1	2	5	1.7	Nc1nc2ccc(O)nc2n1-c1ccccc1	nan
	58345680	141233	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141233	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141235	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141235	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141240	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141240	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141256	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141256	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141258	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141258	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141263	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141263	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141273	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141273	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141277	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141277	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141288	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141288	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141296	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141296	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141297	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141297	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141302	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141302	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141318	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141318	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141341	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141341	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141356	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141356	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141366	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141366	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141381	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141381	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141387	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141387	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141393	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141393	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141394	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141394	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141407	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141407	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141409	5	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	217	1	1	4	2.6	Oc1ccc2ncn(C3CCCCC3)c2n1	nan
	CHEMBL3718239	141409	5	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	217	1	1	4	2.6	Oc1ccc2ncn(C3CCCCC3)c2n1	nan
	58345649	141410	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141410	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141420	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141420	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141439	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141439	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141445	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141445	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141451	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141451	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141455	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141455	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141459	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141459	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141461	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141461	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141472	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141472	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141478	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141478	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141507	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141507	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141524	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141524	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141530	10	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	211	1	1	4	2.1	Oc1ccc2ncn(-c3ccccc3)c2n1	nan
	CHEMBL3718619	141530	10	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	211	1	1	4	2.1	Oc1ccc2ncn(-c3ccccc3)c2n1	nan
	58345755	141532	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141532	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141533	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141533	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141537	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141537	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141540	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141540	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141577	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141577	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141590	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141590	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141596	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141596	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141619	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141619	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141624	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141624	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141644	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141644	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141652	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141652	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141654	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141654	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141680	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141680	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141694	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141694	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141699	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141699	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141705	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141705	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141712	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141712	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141717	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141717	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141742	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141742	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141755	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	141755	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	184126	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	184126	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	184994	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	184994	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	87260	102	None	-2	4	Human	4.8	pEC50	=	4.8	Functional	Agonist activity at human recombinant GPR81 transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR81 transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assay	ChEMBL	172	1	2	2	1.7	O=C(O)c1cc(O)cc(Cl)c1	10.1021/ml3000676
	CHEMBL2146910	87260	102	None	-2	4	Human	4.8	pEC50	=	4.8	Functional	Agonist activity at human recombinant GPR81 transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR81 transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assay	ChEMBL	172	1	2	2	1.7	O=C(O)c1cc(O)cc(Cl)c1	10.1021/ml3000676
	156009546	183929	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	183929	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	184411	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	184411	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	184427	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	184427	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	184946	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	184946	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	183971	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	183971	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	184320	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	184320	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	87260	102	None	-3	4	Mouse	4.7	pEC50	=	4.7	Functional	Agonist activity at mouse GPR81Agonist activity at mouse GPR81	ChEMBL	172	1	2	2	1.7	O=C(O)c1cc(O)cc(Cl)c1	10.1021/ml3000676
	CHEMBL2146910	87260	102	None	-3	4	Mouse	4.7	pEC50	=	4.7	Functional	Agonist activity at mouse GPR81Agonist activity at mouse GPR81	ChEMBL	172	1	2	2	1.7	O=C(O)c1cc(O)cc(Cl)c1	10.1021/ml3000676
	57422810	184440	4	None	-2	3	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production	ChEMBL	602	7	2	10	4.4	CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)C4CCN(C)CC4)cc3s2)cc1-n1cccn1	10.1016/j.bmcl.2020.126953
	CHEMBL4641579	184440	4	None	-2	3	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production	ChEMBL	602	7	2	10	4.4	CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)C4CCN(C)CC4)cc3s2)cc1-n1cccn1	10.1016/j.bmcl.2020.126953
	58345743	140421	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140421	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140435	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140435	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140436	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140436	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140443	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140443	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140459	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140459	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140462	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140462	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140476	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140476	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140482	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140482	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140501	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140501	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140524	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140524	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140532	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140532	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140544	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140544	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140571	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140571	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140572	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140572	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140578	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140578	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140580	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140580	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140601	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140601	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140616	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140616	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140624	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140624	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140628	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140628	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140630	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140630	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140636	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140636	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140638	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140638	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140641	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140641	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140644	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140644	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140659	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140659	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140687	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140687	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140698	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140698	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140705	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140705	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140709	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140709	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140724	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140724	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140725	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140725	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140733	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140733	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140734	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140734	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140738	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140738	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140744	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140744	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140768	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140768	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140770	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140770	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140783	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140783	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140794	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140794	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140809	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140809	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140813	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140813	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140833	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140833	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140834	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140834	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140838	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140838	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140841	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140841	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140846	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140846	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140849	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140849	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140853	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140853	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140869	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140869	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140874	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140874	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140892	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140892	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140901	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140901	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140905	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140905	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140907	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140907	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140908	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140908	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140923	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140923	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140940	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140940	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140945	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140945	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140950	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140950	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140957	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140957	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140959	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	140959	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141011	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141011	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141029	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141029	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141036	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141036	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141052	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141052	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141053	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141053	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141055	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141055	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141081	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141081	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141084	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141084	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141125	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141125	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141140	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141140	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141154	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141154	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141172	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141172	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141173	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141173	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141180	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141180	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141187	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141187	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141189	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141189	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141194	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141194	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141200	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141200	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141218	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141218	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141223	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141223	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141233	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141233	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141235	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141235	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141240	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141240	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141256	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141256	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141258	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141258	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141263	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141263	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141273	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141273	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141277	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141277	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141288	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141288	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141296	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141296	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141297	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141297	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141302	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141302	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141318	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141318	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141341	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141341	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141356	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141356	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141366	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141366	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141381	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141381	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141387	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141387	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141393	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141393	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141394	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141394	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141407	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141407	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141409	5	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	217	1	1	4	2.6	Oc1ccc2ncn(C3CCCCC3)c2n1	nan
	CHEMBL3718239	141409	5	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	217	1	1	4	2.6	Oc1ccc2ncn(C3CCCCC3)c2n1	nan
	58345649	141410	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141410	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141420	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141420	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141439	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141439	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141445	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141445	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141451	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141451	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141455	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141455	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141459	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141459	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141461	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141461	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141472	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141472	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141478	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141478	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141507	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141507	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141524	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141524	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141530	10	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	211	1	1	4	2.1	Oc1ccc2ncn(-c3ccccc3)c2n1	nan
	CHEMBL3718619	141530	10	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	211	1	1	4	2.1	Oc1ccc2ncn(-c3ccccc3)c2n1	nan
	58345755	141532	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141532	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141533	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141533	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141537	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141537	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141538	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141538	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141540	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141540	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141577	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141577	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141590	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141590	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141596	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141596	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141624	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141624	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141644	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141644	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141652	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141652	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141654	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141654	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141680	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141680	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141694	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141694	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141699	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141699	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141705	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141705	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141712	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141712	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141717	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141717	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141732	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141732	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141742	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141742	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141755	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141755	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	141101	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	141101	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	184703	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	184703	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	184426	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	184426	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	184434	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	184434	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	141619	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	141619	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	184076	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	184076	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	140809	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	140809	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	184972	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	184972	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	141212	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	141212	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	184016	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	184016	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	184129	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	184129	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	87262	85	None	-	1	Human	4.4	pEC50	=	4.4	Functional	Agonist activity at human recombinant GPR81 transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR81 transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assay	ChEMBL	156	1	2	2	1.2	O=C(O)c1cc(O)cc(F)c1	10.1021/ml3000676
	CHEMBL2146989	87262	85	None	-	1	Human	4.4	pEC50	=	4.4	Functional	Agonist activity at human recombinant GPR81 transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR81 transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assay	ChEMBL	156	1	2	2	1.2	O=C(O)c1cc(O)cc(F)c1	10.1021/ml3000676
	156016789	184488	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	184488	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	87259	102	None	-	1	Human	4.4	pEC50	=	4.4	Functional	Agonist activity at human recombinant GPR81 transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR81 transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assay	ChEMBL	152	1	2	2	1.4	Cc1cc(O)cc(C(=O)O)c1	10.1021/ml3000676
	CHEMBL2146905	87259	102	None	-	1	Human	4.4	pEC50	=	4.4	Functional	Agonist activity at human recombinant GPR81 transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR81 transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assay	ChEMBL	152	1	2	2	1.4	Cc1cc(O)cc(C(=O)O)c1	10.1021/ml3000676
	156018460	184656	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	184656	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	184477	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	184477	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	184089	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	184089	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	184091	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	184091	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	183897	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	183897	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	184781	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	184781	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	87260	102	None	-9	4	Dog	4.2	pEC50	=	4.2	Functional	Agonist activity at dog GPR81Agonist activity at dog GPR81	ChEMBL	172	1	2	2	1.7	O=C(O)c1cc(O)cc(Cl)c1	10.1021/ml3000676
	CHEMBL2146910	87260	102	None	-9	4	Dog	4.2	pEC50	=	4.2	Functional	Agonist activity at dog GPR81Agonist activity at dog GPR81	ChEMBL	172	1	2	2	1.7	O=C(O)c1cc(O)cc(Cl)c1	10.1021/ml3000676
	57422696	120255	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	120255	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	87260	102	None	2	4	Rat	5.2	pEC50	=	5.2	Functional	Agonist activity at rat GPR81Agonist activity at rat GPR81	ChEMBL	172	1	2	2	1.7	O=C(O)c1cc(O)cc(Cl)c1	10.1021/ml3000676
	CHEMBL2146910	87260	102	None	2	4	Rat	5.2	pEC50	=	5.2	Functional	Agonist activity at rat GPR81Agonist activity at rat GPR81	ChEMBL	172	1	2	2	1.7	O=C(O)c1cc(O)cc(Cl)c1	10.1021/ml3000676
	156011543	184218	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	184218	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	7852	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	7852	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	7852	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	184212	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	184212	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	184423	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	184423	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	184177	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	184177	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	140578	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	140578	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	183919	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	183919	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	141732	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	141732	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	184579	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	184579	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	8543	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	8543	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	8543	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	8543	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	9116	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	9116	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	9116	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	9116	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	9116	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	9116	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	9116	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	9116	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	9116	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	9116	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	9116	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	9116	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	9116	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	9116	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	9116	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	9116	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	9116	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	9116	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	9116	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	9116	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	9116	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	9116	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	9116	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	9116	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	8224	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	8224	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	8224	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	8224	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	6882	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	6882	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	6882	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	6882	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	6882	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	6882	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	7852	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	7852	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	7852	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	7852	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	7852	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	7852	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	7849	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	7849	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	172274	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	172274	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	172594	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	172594	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	172222	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	172222	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)