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	176923	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	176923	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	133924	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	226	1	2	5	1.7	Nc1nc2ccc(O)nc2n1-c1ccccc1	nan
	CHEMBL3717589	133924	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	226	1	2	5	1.7	Nc1nc2ccc(O)nc2n1-c1ccccc1	nan
	156019324	177400	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	177400	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	164891	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	164891	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	176463	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	176463	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	134237	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	134237	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	133120	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133120	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133134	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133134	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133135	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133135	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133142	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133142	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133158	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133158	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133161	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133161	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133175	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133175	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133181	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133181	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133200	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133200	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133223	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133223	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133231	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133231	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133243	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133243	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133270	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133270	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133271	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133271	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133279	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133279	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133300	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133300	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133315	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133315	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133323	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133323	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133327	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	284	1	2	5	2.6	Nc1nc2ccc(O)nc2n1C12CC3CC(CC(C3)C1)C2	nan
	CHEMBL3715572	133327	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	284	1	2	5	2.6	Nc1nc2ccc(O)nc2n1C12CC3CC(CC(C3)C1)C2	nan
	46830068	133329	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133329	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133335	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133335	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133337	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133337	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133340	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133340	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133343	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133343	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133358	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133358	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133386	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133386	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133397	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133397	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133404	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133404	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133408	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133408	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133423	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133423	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133424	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	256	2	1	6	2.0	O=[N+]([O-])c1ccccc1-n1cnc2ccc(O)nc21	nan
	CHEMBL3715890	133424	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	256	2	1	6	2.0	O=[N+]([O-])c1ccccc1-n1cnc2ccc(O)nc21	nan
	58345672	133432	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133432	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133433	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133433	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133437	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133437	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133443	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133443	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133467	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133467	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133469	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	239	2	1	4	2.7	CCc1ccccc1-n1cnc2ccc(O)nc21	nan
	CHEMBL3716041	133469	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	239	2	1	4	2.7	CCc1ccccc1-n1cnc2ccc(O)nc21	nan
	58345733	133482	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133482	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133493	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133493	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133512	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133512	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133532	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	241	2	1	5	2.1	COc1ccc(-n2cnc3ccc(O)nc32)cc1	nan
	CHEMBL3716252	133532	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	241	2	1	5	2.1	COc1ccc(-n2cnc3ccc(O)nc32)cc1	nan
	58345723	133533	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133533	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133537	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133537	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133540	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133540	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133545	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133545	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133548	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133548	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133552	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133552	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133568	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133568	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133573	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133573	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133591	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	261	1	1	4	3.3	Oc1ccc2ncn(-c3cccc4ccccc34)c2n1	nan
	CHEMBL3716441	133591	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	261	1	1	4	3.3	Oc1ccc2ncn(-c3cccc4ccccc34)c2n1	nan
	58345634	133600	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133600	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133604	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133604	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133606	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133606	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133607	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133607	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133622	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133622	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133639	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133639	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133644	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133644	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133649	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133649	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133656	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133656	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133658	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	225	1	1	4	2.4	Cc1ccc(-n2cnc3ccc(O)nc32)cc1	nan
	CHEMBL3716686	133658	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	225	1	1	4	2.4	Cc1ccc(-n2cnc3ccc(O)nc32)cc1	nan
	58345761	133710	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133710	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133728	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133728	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133735	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133735	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133751	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133751	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133752	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133752	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133754	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	243	1	1	4	2.6	Cc1nc2ccc(O)nc2n1-c1ccccc1F	nan
	CHEMBL3716997	133754	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	243	1	1	4	2.6	Cc1nc2ccc(O)nc2n1-c1ccccc1F	nan
	58345740	133780	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133780	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133783	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133783	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133800	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133800	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133824	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133824	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133839	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133839	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133853	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133853	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133871	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133871	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133872	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133872	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133879	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133879	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133886	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	297	1	1	4	3.3	Oc1ccc2ncn(-c3cccc(F)c3C(F)(F)F)c2n1	nan
	CHEMBL3717464	133886	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	297	1	1	4	3.3	Oc1ccc2ncn(-c3cccc(F)c3C(F)(F)F)c2n1	nan
	58345689	133888	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133888	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133893	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133893	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133899	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133899	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133911	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	231	1	1	4	3.0	Oc1ccc2ncn(C3CCCCCC3)c2n1	nan
	CHEMBL3717555	133911	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	231	1	1	4	3.0	Oc1ccc2ncn(C3CCCCCC3)c2n1	nan
	58345748	133917	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133917	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133922	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133922	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133924	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133924	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133932	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133932	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133934	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133934	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133939	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133939	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133955	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	357	1	1	4	3.9	Oc1ccc2ncn(-c3ccc(Br)cc3C(F)(F)F)c2n1	nan
	CHEMBL3717689	133955	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	357	1	1	4	3.9	Oc1ccc2ncn(-c3ccc(Br)cc3C(F)(F)F)c2n1	nan
	58345766	133957	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133957	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133962	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133962	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133972	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133972	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133976	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133976	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133987	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133987	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133995	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133995	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133996	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	133996	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134001	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134001	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134017	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134017	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134040	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134040	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134055	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	259	1	1	4	3.1	Cc1ccccc1-n1c(Cl)nc2ccc(O)nc21	nan
	CHEMBL3718055	134055	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	259	1	1	4	3.1	Cc1ccccc1-n1c(Cl)nc2ccc(O)nc21	nan
	58345664	134065	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134065	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134080	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	357	1	1	4	3.9	Oc1ccc2ncn(-c3cccc(Br)c3C(F)(F)F)c2n1	nan
	CHEMBL3718131	134080	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	357	1	1	4	3.9	Oc1ccc2ncn(-c3cccc(Br)c3C(F)(F)F)c2n1	nan
	58345641	134086	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134086	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134092	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134092	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134093	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	240	1	2	5	2.0	Cc1ccccc1-n1c(N)nc2ccc(O)nc21	nan
	CHEMBL3718177	134093	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	240	1	2	5	2.0	Cc1ccccc1-n1c(N)nc2ccc(O)nc21	nan
	58345673	134106	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	263	1	1	4	2.9	Oc1ccc2nc(Cl)n(-c3ccccc3F)c2n1	nan
	CHEMBL3718227	134106	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	263	1	1	4	2.9	Oc1ccc2nc(Cl)n(-c3ccccc3F)c2n1	nan
	58345754	134108	6	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	217	1	1	4	2.6	Oc1ccc2ncn(C3CCCCC3)c2n1	nan
	CHEMBL3718239	134108	6	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	217	1	1	4	2.6	Oc1ccc2ncn(C3CCCCC3)c2n1	nan
	58345649	134109	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134109	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134119	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134119	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134138	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134138	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134144	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134144	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134150	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134150	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134154	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134154	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134158	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	279	1	1	4	3.1	Oc1ccc2ncn(-c3ccccc3C(F)(F)F)c2n1	nan
	CHEMBL3718371	134158	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	279	1	1	4	3.1	Oc1ccc2ncn(-c3ccccc3C(F)(F)F)c2n1	nan
	58345669	134160	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134160	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134171	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134171	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134177	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134177	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134206	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134206	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134223	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	262	1	2	5	2.0	Nc1nc2ccc(O)nc2n1-c1cccc(F)c1F	nan
	CHEMBL3718610	134223	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	262	1	2	5	2.0	Nc1nc2ccc(O)nc2n1-c1cccc(F)c1F	nan
	58345732	134229	9	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	211	1	1	4	2.1	Oc1ccc2ncn(-c3ccccc3)c2n1	nan
	CHEMBL3718619	134229	9	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	211	1	1	4	2.1	Oc1ccc2ncn(-c3ccccc3)c2n1	nan
	58345755	134231	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134231	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134232	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134232	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134236	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134236	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134239	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134239	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134276	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	303	1	1	4	3.2	Cc1nc2ccc(O)nc2n1-c1ccc(Br)cc1	nan
	CHEMBL3718747	134276	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	303	1	1	4	3.2	Cc1nc2ccc(O)nc2n1-c1ccc(Br)cc1	nan
	58345721	134289	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134289	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134295	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134295	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134318	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134318	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134323	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	231	1	1	4	2.9	CC1CCCCC1n1cnc2ccc(O)nc21	nan
	CHEMBL3718877	134323	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	231	1	1	4	2.9	CC1CCCCC1n1cnc2ccc(O)nc21	nan
	58345652	134343	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134343	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134351	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134351	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134353	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134353	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134379	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134379	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134393	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134393	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134398	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	225	1	1	4	2.4	Cc1nc2ccc(O)nc2n1-c1ccccc1	nan
	CHEMBL3719178	134398	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	225	1	1	4	2.4	Cc1nc2ccc(O)nc2n1-c1ccccc1	nan
	58345642	134404	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134404	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134411	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	337	1	1	4	3.9	Cc1cc(Br)c(Cl)cc1-n1cnc2ccc(O)nc21	nan
	CHEMBL3719226	134411	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	337	1	1	4	3.9	Cc1cc(Br)c(Cl)cc1-n1cnc2ccc(O)nc21	nan
	58345703	134416	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	279	1	1	4	3.4	Oc1ccc2ncn(-c3ccc(Cl)cc3Cl)c2n1	nan
	CHEMBL3719235	134416	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	279	1	1	4	3.4	Oc1ccc2ncn(-c3ccc(Cl)cc3Cl)c2n1	nan
	58345730	134441	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	266	1	2	5	2.2	Nc1nc2ccc(O)nc2n1-c1cccc2c1CCC2	nan
	CHEMBL3719308	134441	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay	ChEMBL	266	1	2	5	2.2	Nc1nc2ccc(O)nc2n1-c1cccc2c1CCC2	nan
	58345715	134454	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	134454	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 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	176773	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	176773	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	177641	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	177641	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	80074	94	None	-2	4	Human	4.8	pEC50	=	4.8	Functional	Agonist activity at human recombinant GPR81 transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR81 transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assay	ChEMBL	172	1	2	2	1.7	O=C(O)c1cc(O)cc(Cl)c1	10.1021/ml3000676
	CHEMBL2146910	80074	94	None	-2	4	Human	4.8	pEC50	=	4.8	Functional	Agonist activity at human recombinant GPR81 transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR81 transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assay	ChEMBL	172	1	2	2	1.7	O=C(O)c1cc(O)cc(Cl)c1	10.1021/ml3000676
	156009546	176576	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	176576	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	177058	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	177058	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	177074	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	177074	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	177593	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	177593	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	176618	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	176618	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	176967	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	176967	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	80074	94	None	-3	4	Mouse	4.7	pEC50	=	4.7	Functional	Agonist activity at mouse GPR81Agonist activity at mouse GPR81	ChEMBL	172	1	2	2	1.7	O=C(O)c1cc(O)cc(Cl)c1	10.1021/ml3000676
	CHEMBL2146910	80074	94	None	-3	4	Mouse	4.7	pEC50	=	4.7	Functional	Agonist activity at mouse GPR81Agonist activity at mouse GPR81	ChEMBL	172	1	2	2	1.7	O=C(O)c1cc(O)cc(Cl)c1	10.1021/ml3000676
	57422810	177087	2	None	-2	3	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production	ChEMBL	602	7	2	10	4.4	CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)C4CCN(C)CC4)cc3s2)cc1-n1cccn1	10.1016/j.bmcl.2020.126953
	CHEMBL4641579	177087	2	None	-2	3	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production	ChEMBL	602	7	2	10	4.4	CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)C4CCN(C)CC4)cc3s2)cc1-n1cccn1	10.1016/j.bmcl.2020.126953
	58345743	133120	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133120	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133134	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133134	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133135	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133135	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133142	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133142	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133158	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133158	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133161	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133161	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133175	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133175	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133181	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133181	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133200	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133200	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133223	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133223	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133231	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133231	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133243	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133243	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133270	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133270	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133271	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133271	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133277	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133277	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133279	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133279	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133300	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133300	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133315	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133315	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133323	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133323	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133327	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	284	1	2	5	2.6	Nc1nc2ccc(O)nc2n1C12CC3CC(CC(C3)C1)C2	nan
	CHEMBL3715572	133327	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	284	1	2	5	2.6	Nc1nc2ccc(O)nc2n1C12CC3CC(CC(C3)C1)C2	nan
	46830068	133329	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133329	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133335	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133335	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133337	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133337	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133340	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133340	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133343	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133343	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133358	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133358	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133386	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133386	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133397	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133397	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133404	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133404	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133408	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133408	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133423	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133423	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133424	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	256	2	1	6	2.0	O=[N+]([O-])c1ccccc1-n1cnc2ccc(O)nc21	nan
	CHEMBL3715890	133424	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	256	2	1	6	2.0	O=[N+]([O-])c1ccccc1-n1cnc2ccc(O)nc21	nan
	58345672	133432	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133432	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133433	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133433	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133437	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133437	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133443	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133443	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133467	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133467	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133469	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	239	2	1	4	2.7	CCc1ccccc1-n1cnc2ccc(O)nc21	nan
	CHEMBL3716041	133469	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	239	2	1	4	2.7	CCc1ccccc1-n1cnc2ccc(O)nc21	nan
	58345733	133482	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133482	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133493	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133493	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133508	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133508	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133512	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133512	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133532	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	241	2	1	5	2.1	COc1ccc(-n2cnc3ccc(O)nc32)cc1	nan
	CHEMBL3716252	133532	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	241	2	1	5	2.1	COc1ccc(-n2cnc3ccc(O)nc32)cc1	nan
	58345723	133533	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133533	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133537	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133537	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133540	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133540	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133545	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133545	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133548	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133548	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133552	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133552	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133568	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133568	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133573	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133573	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133591	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	261	1	1	4	3.3	Oc1ccc2ncn(-c3cccc4ccccc34)c2n1	nan
	CHEMBL3716441	133591	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	261	1	1	4	3.3	Oc1ccc2ncn(-c3cccc4ccccc34)c2n1	nan
	58345634	133600	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133600	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133604	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133604	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133606	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133606	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133607	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133607	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133622	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133622	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133639	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133639	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133644	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133644	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133649	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133649	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133656	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133656	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133658	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	225	1	1	4	2.4	Cc1ccc(-n2cnc3ccc(O)nc32)cc1	nan
	CHEMBL3716686	133658	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	225	1	1	4	2.4	Cc1ccc(-n2cnc3ccc(O)nc32)cc1	nan
	58345761	133710	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133710	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133728	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133728	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133735	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133735	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133751	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133751	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133752	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133752	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133754	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	243	1	1	4	2.6	Cc1nc2ccc(O)nc2n1-c1ccccc1F	nan
	CHEMBL3716997	133754	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	243	1	1	4	2.6	Cc1nc2ccc(O)nc2n1-c1ccccc1F	nan
	58345740	133780	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133780	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133783	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133783	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133824	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133824	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133839	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133839	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133853	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133853	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133871	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133871	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133872	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133872	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133879	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133879	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133886	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	297	1	1	4	3.3	Oc1ccc2ncn(-c3cccc(F)c3C(F)(F)F)c2n1	nan
	CHEMBL3717464	133886	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	297	1	1	4	3.3	Oc1ccc2ncn(-c3cccc(F)c3C(F)(F)F)c2n1	nan
	58345689	133888	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133888	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133893	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133893	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133899	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133899	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133917	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133917	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133922	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133922	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133932	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133932	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133934	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133934	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133939	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133939	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133955	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	357	1	1	4	3.9	Oc1ccc2ncn(-c3ccc(Br)cc3C(F)(F)F)c2n1	nan
	CHEMBL3717689	133955	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	357	1	1	4	3.9	Oc1ccc2ncn(-c3ccc(Br)cc3C(F)(F)F)c2n1	nan
	58345766	133957	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133957	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133962	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133962	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133972	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133972	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133976	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133976	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133987	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133987	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133995	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133995	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133996	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133996	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134001	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134001	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134017	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134017	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134040	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134040	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134055	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	259	1	1	4	3.1	Cc1ccccc1-n1c(Cl)nc2ccc(O)nc21	nan
	CHEMBL3718055	134055	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	259	1	1	4	3.1	Cc1ccccc1-n1c(Cl)nc2ccc(O)nc21	nan
	58345664	134065	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134065	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134080	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	357	1	1	4	3.9	Oc1ccc2ncn(-c3cccc(Br)c3C(F)(F)F)c2n1	nan
	CHEMBL3718131	134080	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	357	1	1	4	3.9	Oc1ccc2ncn(-c3cccc(Br)c3C(F)(F)F)c2n1	nan
	58345641	134086	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134086	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134092	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134092	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134093	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	240	1	2	5	2.0	Cc1ccccc1-n1c(N)nc2ccc(O)nc21	nan
	CHEMBL3718177	134093	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	240	1	2	5	2.0	Cc1ccccc1-n1c(N)nc2ccc(O)nc21	nan
	58345673	134106	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	263	1	1	4	2.9	Oc1ccc2nc(Cl)n(-c3ccccc3F)c2n1	nan
	CHEMBL3718227	134106	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	263	1	1	4	2.9	Oc1ccc2nc(Cl)n(-c3ccccc3F)c2n1	nan
	58345754	134108	6	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	217	1	1	4	2.6	Oc1ccc2ncn(C3CCCCC3)c2n1	nan
	CHEMBL3718239	134108	6	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	217	1	1	4	2.6	Oc1ccc2ncn(C3CCCCC3)c2n1	nan
	58345649	134109	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134109	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134119	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134119	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134138	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134138	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134144	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134144	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134150	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134150	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134154	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134154	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134158	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	279	1	1	4	3.1	Oc1ccc2ncn(-c3ccccc3C(F)(F)F)c2n1	nan
	CHEMBL3718371	134158	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	279	1	1	4	3.1	Oc1ccc2ncn(-c3ccccc3C(F)(F)F)c2n1	nan
	58345669	134160	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134160	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134171	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134171	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134177	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134177	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134206	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134206	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134223	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	262	1	2	5	2.0	Nc1nc2ccc(O)nc2n1-c1cccc(F)c1F	nan
	CHEMBL3718610	134223	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	262	1	2	5	2.0	Nc1nc2ccc(O)nc2n1-c1cccc(F)c1F	nan
	58345732	134229	9	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	211	1	1	4	2.1	Oc1ccc2ncn(-c3ccccc3)c2n1	nan
	CHEMBL3718619	134229	9	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	211	1	1	4	2.1	Oc1ccc2ncn(-c3ccccc3)c2n1	nan
	58345755	134231	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134231	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134232	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134232	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134236	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134236	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134237	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134237	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134239	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134239	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134276	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	303	1	1	4	3.2	Cc1nc2ccc(O)nc2n1-c1ccc(Br)cc1	nan
	CHEMBL3718747	134276	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	303	1	1	4	3.2	Cc1nc2ccc(O)nc2n1-c1ccc(Br)cc1	nan
	58345721	134289	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134289	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134295	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134295	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134323	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134323	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134343	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134343	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134351	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134351	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134353	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134353	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134379	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134379	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134393	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134393	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134398	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	225	1	1	4	2.4	Cc1nc2ccc(O)nc2n1-c1ccccc1	nan
	CHEMBL3719178	134398	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	225	1	1	4	2.4	Cc1nc2ccc(O)nc2n1-c1ccccc1	nan
	58345642	134404	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134404	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134411	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	337	1	1	4	3.9	Cc1cc(Br)c(Cl)cc1-n1cnc2ccc(O)nc21	nan
	CHEMBL3719226	134411	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	337	1	1	4	3.9	Cc1cc(Br)c(Cl)cc1-n1cnc2ccc(O)nc21	nan
	58345703	134416	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	279	1	1	4	3.4	Oc1ccc2ncn(-c3ccc(Cl)cc3Cl)c2n1	nan
	CHEMBL3719235	134416	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	279	1	1	4	3.4	Oc1ccc2ncn(-c3ccc(Cl)cc3Cl)c2n1	nan
	58345687	134431	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134431	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134441	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	266	1	2	5	2.2	Nc1nc2ccc(O)nc2n1-c1cccc2c1CCC2	nan
	CHEMBL3719308	134441	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay	ChEMBL	266	1	2	5	2.2	Nc1nc2ccc(O)nc2n1-c1cccc2c1CCC2	nan
	58345715	134454	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	134454	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity 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	133800	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	133800	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	177350	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	177350	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	177073	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	177073	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	177081	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	177081	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	134318	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	134318	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	176723	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	176723	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	133508	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	133508	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	177619	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	177619	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	133911	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	133911	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	176663	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	176663	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	176776	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	176776	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	80076	75	None	-	1	Human	4.4	pEC50	=	4.4	Functional	Agonist activity at human recombinant GPR81 transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR81 transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assay	ChEMBL	156	1	2	2	1.2	O=C(O)c1cc(O)cc(F)c1	10.1021/ml3000676
	CHEMBL2146989	80076	75	None	-	1	Human	4.4	pEC50	=	4.4	Functional	Agonist activity at human recombinant GPR81 transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR81 transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assay	ChEMBL	156	1	2	2	1.2	O=C(O)c1cc(O)cc(F)c1	10.1021/ml3000676
	156016789	177135	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	177135	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	80073	98	None	-	1	Human	4.4	pEC50	=	4.4	Functional	Agonist activity at human recombinant GPR81 transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR81 transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assay	ChEMBL	152	1	2	2	1.4	Cc1cc(O)cc(C(=O)O)c1	10.1021/ml3000676
	CHEMBL2146905	80073	98	None	-	1	Human	4.4	pEC50	=	4.4	Functional	Agonist activity at human recombinant GPR81 transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant GPR81 transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assay	ChEMBL	152	1	2	2	1.4	Cc1cc(O)cc(C(=O)O)c1	10.1021/ml3000676
	156018460	177303	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	177303	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	177124	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	177124	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	176736	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	176736	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	176738	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	176738	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	176544	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	176544	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	177428	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	177428	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	80074	94	None	-9	4	Dog	4.2	pEC50	=	4.2	Functional	Agonist activity at dog GPR81Agonist activity at dog GPR81	ChEMBL	172	1	2	2	1.7	O=C(O)c1cc(O)cc(Cl)c1	10.1021/ml3000676
	CHEMBL2146910	80074	94	None	-9	4	Dog	4.2	pEC50	=	4.2	Functional	Agonist activity at dog GPR81Agonist activity at dog GPR81	ChEMBL	172	1	2	2	1.7	O=C(O)c1cc(O)cc(Cl)c1	10.1021/ml3000676
	57422696	112979	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	112979	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	80074	94	None	2	4	Rat	5.2	pEC50	=	5.2	Functional	Agonist activity at rat GPR81Agonist activity at rat GPR81	ChEMBL	172	1	2	2	1.7	O=C(O)c1cc(O)cc(Cl)c1	10.1021/ml3000676
	CHEMBL2146910	80074	94	None	2	4	Rat	5.2	pEC50	=	5.2	Functional	Agonist activity at rat GPR81Agonist activity at rat GPR81	ChEMBL	172	1	2	2	1.7	O=C(O)c1cc(O)cc(Cl)c1	10.1021/ml3000676
	156011543	176865	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	176865	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	1049	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	1049	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	1049	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	176859	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	176859	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	177070	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	177070	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	176824	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	176824	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	133277	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	133277	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	176566	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	176566	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	134431	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	134431	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	177226	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	177226	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	1732	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	1732	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	1732	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	1732	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	2305	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	2305	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	2305	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	2305	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	2305	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	2305	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	2305	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	2305	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	2305	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	2305	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	2305	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	2305	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	2305	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	2305	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	2305	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	2305	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	2305	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	2305	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	2305	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	2305	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	2305	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	2305	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	2305	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	2305	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	1414	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	1414	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	1414	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	1414	0	None	-	1	Human	2.5	pEC50	=	2.5	Functional	UnclassifiedUnclassified	Guide to Pharmacology	90	1	2	2	-0.5	OC(=O)[C@H](O)C	18952058
	5783	94	0	None	-1	2	Human	3.7	pEC50	=	3.7	Functional	UnclassifiedUnclassified	Guide to Pharmacology	154	1	3	3	0.8	Oc1cc(O)cc(c1)C(=O)O	22434674
	7424	94	0	None	-1	2	Human	3.7	pEC50	=	3.7	Functional	UnclassifiedUnclassified	Guide to Pharmacology	154	1	3	3	0.8	Oc1cc(O)cc(c1)C(=O)O	22434674
	CHEMBL95308	94	0	None	-1	2	Human	3.7	pEC50	=	3.7	Functional	UnclassifiedUnclassified	Guide to Pharmacology	154	1	3	3	0.8	Oc1cc(O)cc(c1)C(=O)O	22434674
	5783	94	0	None	1	2	Mouse	3.8	pEC50	=	3.8	Functional	UnclassifiedUnclassified	Guide to Pharmacology	154	1	3	3	0.8	Oc1cc(O)cc(c1)C(=O)O	22434674
	7424	94	0	None	1	2	Mouse	3.8	pEC50	=	3.8	Functional	UnclassifiedUnclassified	Guide to Pharmacology	154	1	3	3	0.8	Oc1cc(O)cc(c1)C(=O)O	22434674
	CHEMBL95308	94	0	None	1	2	Mouse	3.8	pEC50	=	3.8	Functional	UnclassifiedUnclassified	Guide to Pharmacology	154	1	3	3	0.8	Oc1cc(O)cc(c1)C(=O)O	22434674
	11197	1049	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	1049	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	1049	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	1049	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	1049	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	1049	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	1046	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	1046	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	164943	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	164943	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	165262	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	165262	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	164891	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	164891	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)