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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
	164611580	183944	0	None	2454	2	Human	10.7	pEC50	=	10.7	Functional	Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis	ChEMBL	395	3	1	6	2.1	O=C(NC12CCC(CC1)CC2)c1nn(-c2c[n+]([O-])ccn2)c2c1CC1CCC2O1	10.1021/acsmedchemlett.1c00331
	CHEMBL4847866	183944	0	None	2454	2	Human	10.7	pEC50	=	10.7	Functional	Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis	ChEMBL	395	3	1	6	2.1	O=C(NC12CCC(CC1)CC2)c1nn(-c2c[n+]([O-])ccn2)c2c1CC1CCC2O1	10.1021/acsmedchemlett.1c00331
	164625379	185644	0	None	831	2	Human	10.7	pEC50	=	10.7	Functional	Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis	ChEMBL	391	3	1	6	2.7	O=C(NC12CC3CC(CC1C3)C2)c1nn(-c2cnccn2)c2c1CC1CCC2O1	10.1021/acsmedchemlett.1c00331
	CHEMBL4873473	185644	0	None	831	2	Human	10.7	pEC50	=	10.7	Functional	Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis	ChEMBL	391	3	1	6	2.7	O=C(NC12CC3CC(CC1C3)C2)c1nn(-c2cnccn2)c2c1CC1CCC2O1	10.1021/acsmedchemlett.1c00331
	138491556	162046	0	None	15	2	Human	10.5	pEC50	=	10.5	Functional	Agonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assayAgonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assay	ChEMBL	383	15	1	2	6.0	CC/C=C\C/C=C\C/C=C\CC1OC1C/C=C\C/C=C\CCC(=O)NC1CC1	10.1021/acs.jmedchem.8b00243
	CHEMBL4169198	162046	0	None	15	2	Human	10.5	pEC50	=	10.5	Functional	Agonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assayAgonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assay	ChEMBL	383	15	1	2	6.0	CC/C=C\C/C=C\C/C=C\CC1OC1C/C=C\C/C=C\CCC(=O)NC1CC1	10.1021/acs.jmedchem.8b00243
	15614389	167440	0	None	2	2	Rat	10.5	pEC50	=	10.5	Functional	Effective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptorEffective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptor	ChEMBL	386	7	2	3	6.2	CCCCCCC(C)(C)c1cc(O)c2c(c1)OC(C)(C)[C@@H]1CC=C(CO)CC21	10.1021/jm970126f
	CHEMBL432107	167440	0	None	2	2	Rat	10.5	pEC50	=	10.5	Functional	Effective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptorEffective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptor	ChEMBL	386	7	2	3	6.2	CCCCCCC(C)(C)c1cc(O)c2c(c1)OC(C)(C)[C@@H]1CC=C(CO)CC21	10.1021/jm970126f
	156248679	184899	0	None	14454	2	Human	10.4	pEC50	=	10.4	Functional	Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis	ChEMBL	393	3	1	6	2.7	O=C(NC1(C(F)(F)F)CCC1)c1nn(-c2cnccn2)c2c1CC1CCC2O1	10.1021/acsmedchemlett.1c00331
	CHEMBL4862304	184899	0	None	14454	2	Human	10.4	pEC50	=	10.4	Functional	Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis	ChEMBL	393	3	1	6	2.7	O=C(NC1(C(F)(F)F)CCC1)c1nn(-c2cnccn2)c2c1CC1CCC2O1	10.1021/acsmedchemlett.1c00331
	156248933	185797	0	None	-	1	Human	10.4	pEC50	=	10.4	Functional	Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis	ChEMBL	366	4	0	8	3.2	CCC(C)(C)c1noc(-c2nn(-c3cnccn3)c3c2CC2CCC3O2)n1	10.1021/acsmedchemlett.1c00331
	CHEMBL4875720	185797	0	None	-	1	Human	10.4	pEC50	=	10.4	Functional	Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis	ChEMBL	366	4	0	8	3.2	CCC(C)(C)c1noc(-c2nn(-c3cnccn3)c3c2CC2CCC3O2)n1	10.1021/acsmedchemlett.1c00331
	164609298	183869	0	None	35481	2	Human	10.3	pEC50	=	10.3	Functional	Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis	ChEMBL	353	3	1	6	1.0	O=C(NC12CC(C1)C2)c1nn(-c2c[n+]([O-])ccn2)c2c1CC1CCC2O1	10.1021/acsmedchemlett.1c00331
	CHEMBL4846759	183869	0	None	35481	2	Human	10.3	pEC50	=	10.3	Functional	Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis	ChEMBL	353	3	1	6	1.0	O=C(NC12CC(C1)C2)c1nn(-c2c[n+]([O-])ccn2)c2c1CC1CCC2O1	10.1021/acsmedchemlett.1c00331
	10500128	9329	0	None	3	2	Rat	10.3	pEC50	=	10.3	Functional	Effective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptorEffective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptor	ChEMBL	382	7	2	3	6.4	CCCCCCC(C)(C)c1cc(O)c2c(c1)OC(C)(C)c1ccc(CO)cc1-2	10.1021/jm970126f
	CHEMBL111724	9329	0	None	3	2	Rat	10.3	pEC50	=	10.3	Functional	Effective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptorEffective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptor	ChEMBL	382	7	2	3	6.4	CCCCCCC(C)(C)c1cc(O)c2c(c1)OC(C)(C)c1ccc(CO)cc1-2	10.1021/jm970126f
	164621737	185092	0	None	2187	2	Human	10.2	pEC50	=	10.2	Functional	Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis	ChEMBL	384	2	0	8	2.5	CC(C)(C)c1nnc(-c2nn(-c3c[n+]([O-])ccn3)c3c2CC2CCC3O2)s1	10.1021/acsmedchemlett.1c00331
	CHEMBL4865162	185092	0	None	2187	2	Human	10.2	pEC50	=	10.2	Functional	Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis	ChEMBL	384	2	0	8	2.5	CC(C)(C)c1nnc(-c2nn(-c3c[n+]([O-])ccn3)c3c2CC2CCC3O2)s1	10.1021/acsmedchemlett.1c00331
	138491578	162538	0	None	1	2	Human	10.2	pEC50	=	10.2	Functional	Agonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assayAgonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assay	ChEMBL	401	16	2	3	5.2	CC/C=C\C/C=C\C/C=C\CC1OC1C/C=C\C/C=C\CCC(=O)NC(C)CO	10.1021/acs.jmedchem.8b00243
	CHEMBL4177060	162538	0	None	1	2	Human	10.2	pEC50	=	10.2	Functional	Agonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assayAgonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assay	ChEMBL	401	16	2	3	5.2	CC/C=C\C/C=C\C/C=C\CC1OC1C/C=C\C/C=C\CCC(=O)NC(C)CO	10.1021/acs.jmedchem.8b00243
	164619069	185590	0	None	8	2	Human	10.1	pEC50	=	10.1	Functional	Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis	ChEMBL	425	3	1	4	4.2	O=C(NC12CC3CC(CC1C3)C2)c1nn(-c2ccc(F)cc2F)c2c1CC1CCC2O1	10.1021/acsmedchemlett.1c00331
	CHEMBL4872695	185590	0	None	8	2	Human	10.1	pEC50	=	10.1	Functional	Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis	ChEMBL	425	3	1	4	4.2	O=C(NC12CC3CC(CC1C3)C2)c1nn(-c2ccc(F)cc2F)c2c1CC1CCC2O1	10.1021/acsmedchemlett.1c00331
	CHEMBL5091754	213540	0	None	4	2	Human	10.1	pEC50	=	10.1	Functional	Agonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assayAgonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assay	ChEMBL		None	None	None		CC(C)(CCCCCCC#N)c1cc(O)c2c(c1)OC(C)(C)[C@@H]1CC[C@@H](CO)C[C@@H]21	10.1021/acs.jmedchem.0c02053
	164620714	185492	0	None	4677	2	Human	10.1	pEC50	=	10.1	Functional	Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis	ChEMBL	371	4	2	7	1.6	CC(C)(C)[C@@H](CO)NC(=O)c1nn(-c2cnccn2)c2c1C[C@H]1CC[C@@H]2O1	10.1021/acsmedchemlett.1c00331
	CHEMBL4871491	185492	0	None	4677	2	Human	10.1	pEC50	=	10.1	Functional	Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis	ChEMBL	371	4	2	7	1.6	CC(C)(C)[C@@H](CO)NC(=O)c1nn(-c2cnccn2)c2c1C[C@H]1CC[C@@H]2O1	10.1021/acsmedchemlett.1c00331
	CHEMBL5081770	212984	0	None	7	2	Human	10.0	pEC50	=	10.0	Functional	Agonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assayAgonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assay	ChEMBL		None	None	None		CC(C)(CCCCCCN=[N+]=[N-])c1cc(O)c2c(c1)OC(C)(C)[C@@H]1CC[C@@H](CO)C[C@@H]21	10.1021/acs.jmedchem.0c02053
	104850	3266	93	None	1	6	Human	10.0	pEC50	=	10.0	Functional	Inverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 minsInverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 mins	ChEMBL	462	4	1	4	5.9	Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1	10.1016/j.ejmech.2009.12.018
	4150	3266	93	None	1	6	Human	10.0	pEC50	=	10.0	Functional	Inverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 minsInverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 mins	ChEMBL	462	4	1	4	5.9	Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1	10.1016/j.ejmech.2009.12.018
	743	3266	93	None	1	6	Human	10.0	pEC50	=	10.0	Functional	Inverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 minsInverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 mins	ChEMBL	462	4	1	4	5.9	Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1	10.1016/j.ejmech.2009.12.018
	CHEMBL111	3266	93	None	1	6	Human	10.0	pEC50	=	10.0	Functional	Inverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 minsInverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 mins	ChEMBL	462	4	1	4	5.9	Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1	10.1016/j.ejmech.2009.12.018
	DB06155	3266	93	None	1	6	Human	10.0	pEC50	=	10.0	Functional	Inverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 minsInverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 mins	ChEMBL	462	4	1	4	5.9	Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1	10.1016/j.ejmech.2009.12.018
	4412255	1156	26	None	7	5	Rat	9.9	pEC50	=	9.9	Functional	cAMP Activation Assay: The compound of Example 3 was tested for agonist activity at the rat CB1 (rCB1) and rCB2 receptors, at eight concentrations, in duplicate: 10, 3, 1, 0.3, 0.1, 0.03, 0.01 and 0.001 μM. Recombinant cells grown to mid-log phase in culture media without antibiotics were detached with PBS containing 5 mM EDTA, centrifuged and resuspended in assay buffer at a concentration of 16.6×105 cells/ml. The test was performed in 96 well plates. For testing, 12 μl of cells (2×103 cells/well) were mixed with 12 μl of agonist at increasing concentrations.cAMP Activation Assay: The compound of Example 3 was tested for agonist activity at the rat CB1 (rCB1) and rCB2 receptors, at eight concentrations, in duplicate: 10, 3, 1, 0.3, 0.1, 0.03, 0.01 and 0.001 μM. Recombinant cells grown to mid-log phase in culture media without antibiotics were detached with PBS containing 5 mM EDTA, centrifuged and resuspended in assay buffer at a concentration of 16.6×105 cells/ml. The test was performed in 96 well plates. For testing, 12 μl of cells (2×103 cells/well) were mixed with 12 μl of agonist at increasing concentrations.	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)C1CC(O)CCC1CCCO)(C)C	nan
	5570	1156	26	None	7	5	Rat	9.9	pEC50	=	9.9	Functional	cAMP Activation Assay: The compound of Example 3 was tested for agonist activity at the rat CB1 (rCB1) and rCB2 receptors, at eight concentrations, in duplicate: 10, 3, 1, 0.3, 0.1, 0.03, 0.01 and 0.001 μM. Recombinant cells grown to mid-log phase in culture media without antibiotics were detached with PBS containing 5 mM EDTA, centrifuged and resuspended in assay buffer at a concentration of 16.6×105 cells/ml. The test was performed in 96 well plates. For testing, 12 μl of cells (2×103 cells/well) were mixed with 12 μl of agonist at increasing concentrations.cAMP Activation Assay: The compound of Example 3 was tested for agonist activity at the rat CB1 (rCB1) and rCB2 receptors, at eight concentrations, in duplicate: 10, 3, 1, 0.3, 0.1, 0.03, 0.01 and 0.001 μM. Recombinant cells grown to mid-log phase in culture media without antibiotics were detached with PBS containing 5 mM EDTA, centrifuged and resuspended in assay buffer at a concentration of 16.6×105 cells/ml. The test was performed in 96 well plates. For testing, 12 μl of cells (2×103 cells/well) were mixed with 12 μl of agonist at increasing concentrations.	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)C1CC(O)CCC1CCCO)(C)C	nan
	CHEMBL77520	1156	26	None	7	5	Rat	9.9	pEC50	=	9.9	Functional	cAMP Activation Assay: The compound of Example 3 was tested for agonist activity at the rat CB1 (rCB1) and rCB2 receptors, at eight concentrations, in duplicate: 10, 3, 1, 0.3, 0.1, 0.03, 0.01 and 0.001 μM. Recombinant cells grown to mid-log phase in culture media without antibiotics were detached with PBS containing 5 mM EDTA, centrifuged and resuspended in assay buffer at a concentration of 16.6×105 cells/ml. The test was performed in 96 well plates. For testing, 12 μl of cells (2×103 cells/well) were mixed with 12 μl of agonist at increasing concentrations.cAMP Activation Assay: The compound of Example 3 was tested for agonist activity at the rat CB1 (rCB1) and rCB2 receptors, at eight concentrations, in duplicate: 10, 3, 1, 0.3, 0.1, 0.03, 0.01 and 0.001 μM. Recombinant cells grown to mid-log phase in culture media without antibiotics were detached with PBS containing 5 mM EDTA, centrifuged and resuspended in assay buffer at a concentration of 16.6×105 cells/ml. The test was performed in 96 well plates. For testing, 12 μl of cells (2×103 cells/well) were mixed with 12 μl of agonist at increasing concentrations.	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)C1CC(O)CCC1CCCO)(C)C	nan
	104895	1157	23	None	-22	9	Rat	9.8	pEC50	=	9.8	Functional	Agonist activity at rat recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP levelAgonist activity at rat recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP level	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1021/jm800463f
	730	1157	23	None	-22	9	Rat	9.8	pEC50	=	9.8	Functional	Agonist activity at rat recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP levelAgonist activity at rat recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP level	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1021/jm800463f
	734	1157	23	None	-22	9	Rat	9.8	pEC50	=	9.8	Functional	Agonist activity at rat recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP levelAgonist activity at rat recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP level	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1021/jm800463f
	CHEMBL559612	1157	23	None	-22	9	Rat	9.8	pEC50	=	9.8	Functional	Agonist activity at rat recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP levelAgonist activity at rat recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP level	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1021/jm800463f
	10618930	8381	0	None	4	2	Rat	9.7	pEC50	=	9.7	Functional	Effective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptorEffective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptor	ChEMBL	366	6	1	2	7.2	CCCCCCC(C)(C)c1cc(O)c2c(c1)OC(C)(C)c1ccc(C)cc1-2	10.1021/jm970126f
	CHEMBL109393	8381	0	None	4	2	Rat	9.7	pEC50	=	9.7	Functional	Effective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptorEffective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptor	ChEMBL	366	6	1	2	7.2	CCCCCCC(C)(C)c1cc(O)c2c(c1)OC(C)(C)c1ccc(C)cc1-2	10.1021/jm970126f
	138491579	162262	0	None	38	2	Human	9.7	pEC50	=	9.7	Functional	Agonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assayAgonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assay	ChEMBL	401	17	2	3	5.2	CC/C=C\C/C=C\C/C=C\CC1OC1C/C=C\C/C=C\CCC(=O)NCCCO	10.1021/acs.jmedchem.8b00243
	CHEMBL4172580	162262	0	None	38	2	Human	9.7	pEC50	=	9.7	Functional	Agonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assayAgonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assay	ChEMBL	401	17	2	3	5.2	CC/C=C\C/C=C\C/C=C\CC1OC1C/C=C\C/C=C\CCC(=O)NCCCO	10.1021/acs.jmedchem.8b00243
	104895	1157	23	None	-9	9	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at human recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP levelAgonist activity at human recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP level	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1021/jm800463f
	730	1157	23	None	-9	9	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at human recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP levelAgonist activity at human recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP level	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1021/jm800463f
	734	1157	23	None	-9	9	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at human recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP levelAgonist activity at human recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP level	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1021/jm800463f
	CHEMBL559612	1157	23	None	-9	9	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at human recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP levelAgonist activity at human recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP level	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1021/jm800463f
	104895	1157	23	None	-9	9	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as reversal of forskolin-evoked cAMP accumulationAgonist activity at human CB1 receptor expressed in HEK293 cells assessed as reversal of forskolin-evoked cAMP accumulation	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1021/jm070317a
	730	1157	23	None	-9	9	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as reversal of forskolin-evoked cAMP accumulationAgonist activity at human CB1 receptor expressed in HEK293 cells assessed as reversal of forskolin-evoked cAMP accumulation	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1021/jm070317a
	734	1157	23	None	-9	9	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as reversal of forskolin-evoked cAMP accumulationAgonist activity at human CB1 receptor expressed in HEK293 cells assessed as reversal of forskolin-evoked cAMP accumulation	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1021/jm070317a
	CHEMBL559612	1157	23	None	-9	9	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as reversal of forskolin-evoked cAMP accumulationAgonist activity at human CB1 receptor expressed in HEK293 cells assessed as reversal of forskolin-evoked cAMP accumulation	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1021/jm070317a
	118720555	115426	0	None	-1	2	Human	9.5	pEC50	=	9.5	Functional	Agonist activity at human recombinant CB1 receptor expressed in CHOK1 cells assessed as cAMP accumulation by HTRF methodAgonist activity at human recombinant CB1 receptor expressed in CHOK1 cells assessed as cAMP accumulation by HTRF method	ChEMBL	389	5	1	3	4.4	CC(C)(NC(=O)c1nn(Cc2ccc(F)cc2)c2c1C[C@H]1C[C@@H]21)c1ccccc1	10.1016/j.bmcl.2014.11.040
	CHEMBL3354941	115426	0	None	-1	2	Human	9.5	pEC50	=	9.5	Functional	Agonist activity at human recombinant CB1 receptor expressed in CHOK1 cells assessed as cAMP accumulation by HTRF methodAgonist activity at human recombinant CB1 receptor expressed in CHOK1 cells assessed as cAMP accumulation by HTRF method	ChEMBL	389	5	1	3	4.4	CC(C)(NC(=O)c1nn(Cc2ccc(F)cc2)c2c1C[C@H]1C[C@@H]21)c1ccccc1	10.1016/j.bmcl.2014.11.040
	145971834	164010	0	None	-	1	Rat	9.5	pEC50	=	9.5	Functional	Agonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 minsAgonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins	ChEMBL	357	15	1	1	6.7	CCCCC/C=C\[C@H](C)/C=C\C/C=C\C/C=C\CCCC(=O)NC1CC1	10.1021/acs.jmedchem.8b00611
	CHEMBL4215369	164010	0	None	-	1	Rat	9.5	pEC50	=	9.5	Functional	Agonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 minsAgonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins	ChEMBL	357	15	1	1	6.7	CCCCC/C=C\[C@H](C)/C=C\C/C=C\C/C=C\CCCC(=O)NC1CC1	10.1021/acs.jmedchem.8b00611
	24945480	186335	0	None	-	1	Human	9.5	pEC50	=	9.5	Functional	Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level	ChEMBL	426	4	0	3	3.6	CC(C(=O)N1CCN(S(=O)(=O)c2cc(Cl)cc(Cl)c2)CC1)c1ccccc1	10.1021/jm900063x
	CHEMBL490024	186335	0	None	-	1	Human	9.5	pEC50	=	9.5	Functional	Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level	ChEMBL	426	4	0	3	3.6	CC(C(=O)N1CCN(S(=O)(=O)c2cc(Cl)cc(Cl)c2)CC1)c1ccccc1	10.1021/jm900063x
	CHEMBL5071417	212477	0	None	3	2	Human	9.5	pEC50	=	9.5	Functional	Agonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assayAgonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assay	ChEMBL		None	None	None		CC1(C)Oc2cc(C3(CCCCCCC#N)CCCC3)cc(O)c2[C@@H]2C[C@H](CO)CC[C@H]21	10.1021/acs.jmedchem.0c02053
	162664878	181586	0	None	46	2	Human	9.4	pEC50	=	9.4	Functional	Antagonist activity at human CB1R expressed in CHO cell membranes preincubated for 30 mins followed by GTPgammaS addition and measured after 90 mins by [35S]GTPgammaS assayAntagonist activity at human CB1R expressed in CHO cell membranes preincubated for 30 mins followed by GTPgammaS addition and measured after 90 mins by [35S]GTPgammaS assay	ChEMBL	432	5	1	3	5.5	Cc1c(-c2ccccc2)cc(C(=O)NC2CCCCCC2)c(=O)n1Cc1ccc(F)cc1	10.1016/j.ejmech.2020.112858
	CHEMBL4782654	181586	0	None	46	2	Human	9.4	pEC50	=	9.4	Functional	Antagonist activity at human CB1R expressed in CHO cell membranes preincubated for 30 mins followed by GTPgammaS addition and measured after 90 mins by [35S]GTPgammaS assayAntagonist activity at human CB1R expressed in CHO cell membranes preincubated for 30 mins followed by GTPgammaS addition and measured after 90 mins by [35S]GTPgammaS assay	ChEMBL	432	5	1	3	5.5	Cc1c(-c2ccccc2)cc(C(=O)NC2CCCCCC2)c(=O)n1Cc1ccc(F)cc1	10.1016/j.ejmech.2020.112858
	76310146	104054	0	None	-	1	Rat	9.4	pEC50	=	9.4	Functional	Agonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 8 data points after 30 minsAgonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 8 data points after 30 mins	ChEMBL	398	5	1	4	5.8	CCCCOC(=O)C1(c2cc(O)c3c(c2)OC(C)(C)[C@@H]2CC=C(C)C[C@@H]32)CCC1	10.1021/jm501165d
	CHEMBL3104362	104054	0	None	-	1	Rat	9.4	pEC50	=	9.4	Functional	Agonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 8 data points after 30 minsAgonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 8 data points after 30 mins	ChEMBL	398	5	1	4	5.8	CCCCOC(=O)C1(c2cc(O)c3c(c2)OC(C)(C)[C@@H]2CC=C(C)C[C@@H]32)CCC1	10.1021/jm501165d
	76310146	104054	0	None	-	1	Rat	9.4	pEC50	=	9.4	Functional	Agonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 minsAgonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins	ChEMBL	398	5	1	4	5.8	CCCCOC(=O)C1(c2cc(O)c3c(c2)OC(C)(C)[C@@H]2CC=C(C)C[C@@H]32)CCC1	10.1021/jm4016075
	CHEMBL3104362	104054	0	None	-	1	Rat	9.4	pEC50	=	9.4	Functional	Agonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 minsAgonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins	ChEMBL	398	5	1	4	5.8	CCCCOC(=O)C1(c2cc(O)c3c(c2)OC(C)(C)[C@@H]2CC=C(C)C[C@@H]32)CCC1	10.1021/jm4016075
	145984226	164944	0	None	2	2	Rat	9.4	pEC50	=	9.4	Functional	Agonist activity at recombinant rat Cb1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP levelsAgonist activity at recombinant rat Cb1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP levels	ChEMBL	411	5	1	4	6.1	CC1=CC[C@H]2[C@H](C1)c1c(O)cc(/C(C)=N/OCCCC(F)(F)F)cc1OC2(C)C	10.1016/j.bmc.2018.08.003
	CHEMBL4240671	164944	0	None	2	2	Rat	9.4	pEC50	=	9.4	Functional	Agonist activity at recombinant rat Cb1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP levelsAgonist activity at recombinant rat Cb1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP levels	ChEMBL	411	5	1	4	6.1	CC1=CC[C@H]2[C@H](C1)c1c(O)cc(/C(C)=N/OCCCC(F)(F)F)cc1OC2(C)C	10.1016/j.bmc.2018.08.003
	CHEMBL5074603	212539	0	None	-1	2	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assayAgonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assay	ChEMBL		None	None	None		CC1(C)Oc2cc(C3(CCCCCCCN=C=S)CCCC3)cc(O)c2[C@@H]2C[C@H](CO)CC[C@H]21	10.1021/acs.jmedchem.0c02053
	145957967	161592	7	None	52	2	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assayAgonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assay	ChEMBL	387	16	2	3	4.8	CC/C=C\C/C=C\C/C=C\CC1OC1C/C=C\C/C=C\CCC(=O)NCCO	10.1021/acs.jmedchem.8b00243
	CHEMBL4161934	161592	7	None	52	2	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assayAgonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assay	ChEMBL	387	16	2	3	4.8	CC/C=C\C/C=C\C/C=C\CC1OC1C/C=C\C/C=C\CCC(=O)NCCO	10.1021/acs.jmedchem.8b00243
	86274158	192079	13	None	26	2	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at human CB1 receptor expressed in mouse AtT20 cells by FLIPR assayAgonist activity at human CB1 receptor expressed in mouse AtT20 cells by FLIPR assay	ChEMBL	367	8	1	3	4.8	CC(C)(NC(=O)c1nn(CCCCCF)c2ccccc12)c1ccccc1	10.1021/acs.jmedchem.2c00969
	CHEMBL5219235	192079	13	None	26	2	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at human CB1 receptor expressed in mouse AtT20 cells by FLIPR assayAgonist activity at human CB1 receptor expressed in mouse AtT20 cells by FLIPR assay	ChEMBL	367	8	1	3	4.8	CC(C)(NC(=O)c1nn(CCCCCF)c2ccccc12)c1ccccc1	10.1021/acs.jmedchem.2c00969
	104895	1157	23	None	-9	9	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at human CB1 receptor expressed in HEK cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human CB1 receptor expressed in HEK cells assessed as inhibition of forskolin-induced cAMP accumulation	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1021/acs.jmedchem.5b00579
	730	1157	23	None	-9	9	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at human CB1 receptor expressed in HEK cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human CB1 receptor expressed in HEK cells assessed as inhibition of forskolin-induced cAMP accumulation	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1021/acs.jmedchem.5b00579
	734	1157	23	None	-9	9	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at human CB1 receptor expressed in HEK cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human CB1 receptor expressed in HEK cells assessed as inhibition of forskolin-induced cAMP accumulation	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1021/acs.jmedchem.5b00579
	CHEMBL559612	1157	23	None	-9	9	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at human CB1 receptor expressed in HEK cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human CB1 receptor expressed in HEK cells assessed as inhibition of forskolin-induced cAMP accumulation	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1021/acs.jmedchem.5b00579
	76324747	104053	0	None	-	1	Rat	9.3	pEC50	=	9.3	Functional	Agonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 8 data points after 30 minsAgonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 8 data points after 30 mins	ChEMBL	386	5	1	4	5.6	CCCCOC(=O)C(C)(C)c1cc(O)c2c(c1)OC(C)(C)[C@@H]1CC=C(C)C[C@@H]21	10.1021/jm501165d
	CHEMBL3104360	104053	0	None	-	1	Rat	9.3	pEC50	=	9.3	Functional	Agonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 8 data points after 30 minsAgonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 8 data points after 30 mins	ChEMBL	386	5	1	4	5.6	CCCCOC(=O)C(C)(C)c1cc(O)c2c(c1)OC(C)(C)[C@@H]1CC=C(C)C[C@@H]21	10.1021/jm501165d
	76324747	104053	0	None	-	1	Rat	9.3	pEC50	=	9.3	Functional	Agonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 minsAgonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins	ChEMBL	386	5	1	4	5.6	CCCCOC(=O)C(C)(C)c1cc(O)c2c(c1)OC(C)(C)[C@@H]1CC=C(C)C[C@@H]21	10.1021/jm4016075
	CHEMBL3104360	104053	0	None	-	1	Rat	9.3	pEC50	=	9.3	Functional	Agonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 minsAgonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins	ChEMBL	386	5	1	4	5.6	CCCCOC(=O)C(C)(C)c1cc(O)c2c(c1)OC(C)(C)[C@@H]1CC=C(C)C[C@@H]21	10.1021/jm4016075
	46239964	117107	1	None	-12	2	Human	9.3	pEC50	=	9.3	Functional	Inhibition of human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsInhibition of human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins	ChEMBL	396	3	1	5	4.4	CC(C)(C)c1cc(NC(=O)[C@]2(C)CCCN2c2ccc(C(F)(F)F)cn2)no1	10.1016/j.bmcl.2014.12.033
	CHEMBL3400946	117107	1	None	-12	2	Human	9.3	pEC50	=	9.3	Functional	Inhibition of human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsInhibition of human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins	ChEMBL	396	3	1	5	4.4	CC(C)(C)c1cc(NC(=O)[C@]2(C)CCCN2c2ccc(C(F)(F)F)cn2)no1	10.1016/j.bmcl.2014.12.033
	24945636	186188	0	None	-	1	Human	9.3	pEC50	=	9.3	Functional	Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level	ChEMBL	494	5	0	3	4.5	O=C(CCc1ccc(C(F)(F)F)cc1)N1CCN(S(=O)(=O)c2cc(Cl)cc(Cl)c2)CC1	10.1021/jm900063x
	CHEMBL489031	186188	0	None	-	1	Human	9.3	pEC50	=	9.3	Functional	Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level	ChEMBL	494	5	0	3	4.5	O=C(CCc1ccc(C(F)(F)F)cc1)N1CCN(S(=O)(=O)c2cc(Cl)cc(Cl)c2)CC1	10.1021/jm900063x
	24944972	186249	0	None	-	1	Human	9.3	pEC50	=	9.3	Functional	Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level	ChEMBL	404	3	0	3	3.4	O=C(C1CCCCC1)N1CCN(S(=O)(=O)c2cc(Cl)cc(Cl)c2)CC1	10.1021/jm900063x
	CHEMBL489429	186249	0	None	-	1	Human	9.3	pEC50	=	9.3	Functional	Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level	ChEMBL	404	3	0	3	3.4	O=C(C1CCCCC1)N1CCN(S(=O)(=O)c2cc(Cl)cc(Cl)c2)CC1	10.1021/jm900063x
	24945479	188915	0	None	-	1	Human	9.3	pEC50	=	9.3	Functional	Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level	ChEMBL	480	4	0	3	4.1	O=C(Cc1ccc(C(F)(F)F)cc1)N1CCN(S(=O)(=O)c2cc(Cl)cc(Cl)c2)CC1	10.1021/jm900063x
	CHEMBL514068	188915	0	None	-	1	Human	9.3	pEC50	=	9.3	Functional	Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level	ChEMBL	480	4	0	3	4.1	O=C(Cc1ccc(C(F)(F)F)cc1)N1CCN(S(=O)(=O)c2cc(Cl)cc(Cl)c2)CC1	10.1021/jm900063x
	24945635	189119	0	None	-	1	Human	9.3	pEC50	=	9.3	Functional	Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level	ChEMBL	437	4	0	4	2.9	N#Cc1ccc(CC(=O)N2CCN(S(=O)(=O)c3cc(Cl)cc(Cl)c3)CC2)cc1	10.1021/jm900063x
	CHEMBL515641	189119	0	None	-	1	Human	9.3	pEC50	=	9.3	Functional	Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level	ChEMBL	437	4	0	4	2.9	N#Cc1ccc(CC(=O)N2CCN(S(=O)(=O)c3cc(Cl)cc(Cl)c3)CC2)cc1	10.1021/jm900063x
	CHEMBL5092703	213598	0	None	5	2	Human	9.3	pEC50	=	9.3	Functional	Agonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assayAgonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assay	ChEMBL		None	None	None		CC1(C)Oc2cc(C3(CCCCCCN=C=S)CCCC3)cc(O)c2[C@@H]2C[C@H](CO)CC[C@H]21	10.1021/acs.jmedchem.0c02053
	164620733	185495	0	None	-	1	Human	9.3	pEC50	=	9.3	Functional	Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis	ChEMBL	371	4	2	7	1.6	CC(C)(C)[C@@H](CO)NC(=O)c1nn(-c2cnccn2)c2c1C[C@@H]1CC[C@H]2O1	10.1021/acsmedchemlett.1c00331
	CHEMBL4871528	185495	0	None	-	1	Human	9.3	pEC50	=	9.3	Functional	Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis	ChEMBL	371	4	2	7	1.6	CC(C)(C)[C@@H](CO)NC(=O)c1nn(-c2cnccn2)c2c1C[C@@H]1CC[C@H]2O1	10.1021/acsmedchemlett.1c00331
	145984466	164956	0	None	15	2	Rat	9.2	pEC50	=	9.2	Functional	Agonist activity at recombinant rat Cb1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP levelsAgonist activity at recombinant rat Cb1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP levels	ChEMBL	357	5	1	4	5.5	CCCCO/N=C(\C)c1cc(O)c2c(c1)OC(C)(C)[C@H]1CC=C(C)C[C@H]21	10.1016/j.bmc.2018.08.003
	CHEMBL4240996	164956	0	None	15	2	Rat	9.2	pEC50	=	9.2	Functional	Agonist activity at recombinant rat Cb1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP levelsAgonist activity at recombinant rat Cb1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP levels	ChEMBL	357	5	1	4	5.5	CCCCO/N=C(\C)c1cc(O)c2c(c1)OC(C)(C)[C@H]1CC=C(C)C[C@H]21	10.1016/j.bmc.2018.08.003
	44339199	9226	0	None	1	2	Rat	9.2	pEC50	=	9.2	Functional	Effective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptorEffective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptor	ChEMBL	370	6	1	2	7.3	CCCCCCC(C)(C)c1cc(O)c2c(c1)OC(C)(C)[C@@H]1CCC(C)=CC21	10.1021/jm970126f
	CHEMBL111148	9226	0	None	1	2	Rat	9.2	pEC50	=	9.2	Functional	Effective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptorEffective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptor	ChEMBL	370	6	1	2	7.3	CCCCCCC(C)(C)c1cc(O)c2c(c1)OC(C)(C)[C@@H]1CCC(C)=CC21	10.1021/jm970126f
	107778	114702	30	None	-2	2	Human	9.2	pEC50	=	9.2	Functional	Activity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assayActivity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assay	ChEMBL	386	7	2	3	6.2	CCCCCCC(C)(C)c1cc(O)c2c(c1)OC(C)(C)[C@H]1CC=C(CO)C[C@H]21	10.1021/jm0503906
	CHEMBL334533	114702	30	None	-2	2	Human	9.2	pEC50	=	9.2	Functional	Activity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assayActivity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assay	ChEMBL	386	7	2	3	6.2	CCCCCCC(C)(C)c1cc(O)c2c(c1)OC(C)(C)[C@H]1CC=C(CO)C[C@H]21	10.1021/jm0503906
	145964903	163459	0	None	-	1	Rat	9.2	pEC50	=	9.2	Functional	Agonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 minsAgonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins	ChEMBL	375	16	2	2	5.9	CCCCC/C=C\[C@H](C)/C=C\C/C=C\C/C=C\CCCC(=O)N[C@H](C)CO	10.1021/acs.jmedchem.8b00611
	CHEMBL4208628	163459	0	None	-	1	Rat	9.2	pEC50	=	9.2	Functional	Agonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 minsAgonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins	ChEMBL	375	16	2	2	5.9	CCCCC/C=C\[C@H](C)/C=C\C/C=C\C/C=C\CCCC(=O)N[C@H](C)CO	10.1021/acs.jmedchem.8b00611
	24744027	189271	0	None	-4	2	Rat	9.2	pEC50	=	9.2	Functional	Agonist activity at rat recombinant CB1R expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP levelAgonist activity at rat recombinant CB1R expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP level	ChEMBL	520	5	0	3	4.7	O=C(Cc1ccc(C(F)(F)F)cc1)N1CCN(S(=O)(=O)c2cc(C3CC3)cc(C(F)(F)F)c2)CC1	10.1021/jm900063x
	CHEMBL516900	189271	0	None	-4	2	Rat	9.2	pEC50	=	9.2	Functional	Agonist activity at rat recombinant CB1R expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP levelAgonist activity at rat recombinant CB1R expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP level	ChEMBL	520	5	0	3	4.7	O=C(Cc1ccc(C(F)(F)F)cc1)N1CCN(S(=O)(=O)c2cc(C3CC3)cc(C(F)(F)F)c2)CC1	10.1021/jm900063x
	3868445	192553	1	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level	ChEMBL	386	3	0	3	3.3	O=C(C1CCCCC1)N1CCN(S(=O)(=O)c2cccc3ccccc23)CC1	10.1021/jm900063x
	CHEMBL523100	192553	1	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level	ChEMBL	386	3	0	3	3.3	O=C(C1CCCCC1)N1CCN(S(=O)(=O)c2cccc3ccccc23)CC1	10.1021/jm900063x
	24944801	192762	0	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level	ChEMBL	414	3	0	3	4.0	CC1(C)CN(S(=O)(=O)c2cccc3ccccc23)CCN1C(=O)C1CCCCC1	10.1021/jm900063x
	CHEMBL525204	192762	0	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level	ChEMBL	414	3	0	3	4.0	CC1(C)CN(S(=O)(=O)c2cccc3ccccc23)CCN1C(=O)C1CCCCC1	10.1021/jm900063x
	731	1908	22	None	-2	4	Human	9.2	pEC50	=	9.2	Functional	Potency at human CB1 receptor in a [35S]GTP-gamma-S functional assayPotency at human CB1 receptor in a [35S]GTP-gamma-S functional assay	ChEMBL	386	7	2	3	6.2	CCCCCCC(c1cc(O)c2c(c1)OC([C@H]1[C@H]2CC(=CC1)CO)(C)C)(C)C	10.1021/jm050484f
	9821569	1908	22	None	-2	4	Human	9.2	pEC50	=	9.2	Functional	Potency at human CB1 receptor in a [35S]GTP-gamma-S functional assayPotency at human CB1 receptor in a [35S]GTP-gamma-S functional assay	ChEMBL	386	7	2	3	6.2	CCCCCCC(c1cc(O)c2c(c1)OC([C@H]1[C@H]2CC(=CC1)CO)(C)C)(C)C	10.1021/jm050484f
	CHEMBL307696	1908	22	None	-2	4	Human	9.2	pEC50	=	9.2	Functional	Potency at human CB1 receptor in a [35S]GTP-gamma-S functional assayPotency at human CB1 receptor in a [35S]GTP-gamma-S functional assay	ChEMBL	386	7	2	3	6.2	CCCCCCC(c1cc(O)c2c(c1)OC([C@H]1[C@H]2CC(=CC1)CO)(C)C)(C)C	10.1021/jm050484f
	104895	1157	23	None	-9	9	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid releaseAgonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid release	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1016/j.ejmech.2011.08.021
	730	1157	23	None	-9	9	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid releaseAgonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid release	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1016/j.ejmech.2011.08.021
	734	1157	23	None	-9	9	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid releaseAgonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid release	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1016/j.ejmech.2011.08.021
	CHEMBL559612	1157	23	None	-9	9	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid releaseAgonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid release	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1016/j.ejmech.2011.08.021
	49855337	15819	0	None	-2	2	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release assayAgonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release assay	ChEMBL	395	6	1	2	5.9	CCCCCC1=NN(C(=O)N[C@H]2C[C@H]3CC[C@]2(C)C3(C)C)CC1c1ccccc1	10.1016/j.bmcl.2010.07.056
	CHEMBL1223588	15819	0	None	-2	2	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release assayAgonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release assay	ChEMBL	395	6	1	2	5.9	CCCCCC1=NN(C(=O)N[C@H]2C[C@H]3CC[C@]2(C)C3(C)C)CC1c1ccccc1	10.1016/j.bmcl.2010.07.056
	155907792	189300	2	None	-1	2	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assayAgonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assay	ChEMBL	330	6	2	4	2.5	CCCCn1nc(C(=O)N[C@H](C(N)=O)C(C)(C)C)c2ccccc21	10.1039/d1md00242b
	CHEMBL5169682	189300	2	None	-1	2	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assayAgonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assay	ChEMBL	330	6	2	4	2.5	CCCCn1nc(C(=O)N[C@H](C(N)=O)C(C)(C)C)c2ccccc21	10.1039/d1md00242b
	155907792	189300	2	None	-1	2	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assayAgonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assay	ChEMBL	330	6	2	4	2.5	CCCCn1nc(C(=O)N[C@H](C(N)=O)C(C)(C)C)c2ccccc21	10.1039/d1md00242b
	CHEMBL5169682	189300	2	None	-1	2	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assayAgonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assay	ChEMBL	330	6	2	4	2.5	CCCCn1nc(C(=O)N[C@H](C(N)=O)C(C)(C)C)c2ccccc21	10.1039/d1md00242b
	104895	1157	23	None	-9	9	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at human CB1 receptor transfected in CHO cell membranes by [35S]GTPgammaS binding assayAgonist activity at human CB1 receptor transfected in CHO cell membranes by [35S]GTPgammaS binding assay	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1016/j.ejmech.2012.09.035
	730	1157	23	None	-9	9	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at human CB1 receptor transfected in CHO cell membranes by [35S]GTPgammaS binding assayAgonist activity at human CB1 receptor transfected in CHO cell membranes by [35S]GTPgammaS binding assay	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1016/j.ejmech.2012.09.035
	734	1157	23	None	-9	9	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at human CB1 receptor transfected in CHO cell membranes by [35S]GTPgammaS binding assayAgonist activity at human CB1 receptor transfected in CHO cell membranes by [35S]GTPgammaS binding assay	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1016/j.ejmech.2012.09.035
	CHEMBL559612	1157	23	None	-9	9	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at human CB1 receptor transfected in CHO cell membranes by [35S]GTPgammaS binding assayAgonist activity at human CB1 receptor transfected in CHO cell membranes by [35S]GTPgammaS binding assay	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1016/j.ejmech.2012.09.035
	145985012	165043	0	None	-	1	Rat	9.2	pEC50	=	9.2	Functional	Agonist activity at recombinant rat Cb1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP levelsAgonist activity at recombinant rat Cb1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP levels	ChEMBL	375	6	1	4	5.5	CC1=CC[C@H]2[C@H](C1)c1c(O)cc(/C(C)=N/OCCCCF)cc1OC2(C)C	10.1016/j.bmc.2018.08.003
	CHEMBL4242964	165043	0	None	-	1	Rat	9.2	pEC50	=	9.2	Functional	Agonist activity at recombinant rat Cb1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP levelsAgonist activity at recombinant rat Cb1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP levels	ChEMBL	375	6	1	4	5.5	CC1=CC[C@H]2[C@H](C1)c1c(O)cc(/C(C)=N/OCCCCF)cc1OC2(C)C	10.1016/j.bmc.2018.08.003
	118733881	118060	0	None	-	1	Rat	9.1	pEC50	=	9.1	Functional	Agonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 60 minsAgonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 60 mins	ChEMBL	453	3	2	5	5.7	CC1(C)Oc2cc([C@]34CC5CC(C[C@@](CN=C=S)(C5)C3)C4)cc(O)c2[C@@H]2C[C@H](O)CC[C@H]21	10.1021/jm501960u
	CHEMBL3416128	118060	0	None	-	1	Rat	9.1	pEC50	=	9.1	Functional	Agonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 60 minsAgonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 60 mins	ChEMBL	453	3	2	5	5.7	CC1(C)Oc2cc([C@]34CC5CC(C[C@@](CN=C=S)(C5)C3)C4)cc(O)c2[C@@H]2C[C@H](O)CC[C@H]21	10.1021/jm501960u
	162662574	181312	0	None	-	1	Rat	9.1	pEC50	=	9.1	Functional	Agonist activity at rat brain CB1 receptor assessed as decrease in forskolin-stimulated cAMP level stimulated for 30 mins followed by Eu-cAMP tracer addition and measured after 60 minsAgonist activity at rat brain CB1 receptor assessed as decrease in forskolin-stimulated cAMP level stimulated for 30 mins followed by Eu-cAMP tracer addition and measured after 60 mins	ChEMBL	455	3	2	6	5.1	CC1(C)Oc2cc(C34CC5CC(CC(CN=C=S)(C5)O3)C4)cc(O)c2[C@@H]2C[C@H](O)CC[C@H]21	10.1016/j.bmcl.2021.127882
	CHEMBL4779296	181312	0	None	-	1	Rat	9.1	pEC50	=	9.1	Functional	Agonist activity at rat brain CB1 receptor assessed as decrease in forskolin-stimulated cAMP level stimulated for 30 mins followed by Eu-cAMP tracer addition and measured after 60 minsAgonist activity at rat brain CB1 receptor assessed as decrease in forskolin-stimulated cAMP level stimulated for 30 mins followed by Eu-cAMP tracer addition and measured after 60 mins	ChEMBL	455	3	2	6	5.1	CC1(C)Oc2cc(C34CC5CC(CC(CN=C=S)(C5)O3)C4)cc(O)c2[C@@H]2C[C@H](O)CC[C@H]21	10.1016/j.bmcl.2021.127882
	44177373	8348	0	None	-	1	Human	9.1	pEC50	=	9.1	Functional	Inverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 minsInverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 mins	ChEMBL	459	4	1	2	6.1	Cc1ccc(C(c2ccc(Cl)cc2Cl)N2CCN(C(=O)NC3CCCCC3)CC2)cc1	10.1016/j.ejmech.2009.12.018
	CHEMBL1093735	8348	0	None	-	1	Human	9.1	pEC50	=	9.1	Functional	Inverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 minsInverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 mins	ChEMBL	459	4	1	2	6.1	Cc1ccc(C(c2ccc(Cl)cc2Cl)N2CCN(C(=O)NC3CCCCC3)CC2)cc1	10.1016/j.ejmech.2009.12.018
	89994983	156286	0	None	-	1	Rat	9.1	pEC50	=	9.1	Functional	Agonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 8 data points after 30 minsAgonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 8 data points after 30 mins	ChEMBL	397	5	1	5	5.1	CC1=CC[C@@H]2[C@@H](C1)c1c(O)cc(C(C)(C)C(=O)OCCCC#N)cc1OC2(C)C	10.1021/jm501165d
	CHEMBL4071389	156286	0	None	-	1	Rat	9.1	pEC50	=	9.1	Functional	Agonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 8 data points after 30 minsAgonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 8 data points after 30 mins	ChEMBL	397	5	1	5	5.1	CC1=CC[C@@H]2[C@@H](C1)c1c(O)cc(C(C)(C)C(=O)OCCCC#N)cc1OC2(C)C	10.1021/jm501165d
	104895	1157	23	None	-9	9	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assayAgonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assay	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1021/acs.jmedchem.8b00243
	730	1157	23	None	-9	9	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assayAgonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assay	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1021/acs.jmedchem.8b00243
	734	1157	23	None	-9	9	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assayAgonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assay	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1021/acs.jmedchem.8b00243
	CHEMBL559612	1157	23	None	-9	9	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assayAgonist activity at N-terminal FLAG-tagged human CB1 receptor transfected in human HTLA cells assessed as induction of beta-arrestin-recruitment after 8 to 14 hrs by bright-glo luminescence based assay	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1021/acs.jmedchem.8b00243
	162657901	180500	0	None	-	1	Rat	9.1	pEC50	=	9.1	Functional	Agonist activity at rat brain CB1 receptor assessed as decrease in forskolin-stimulated cAMP level stimulated for 30 mins followed by Eu-cAMP tracer addition and measured after 60 minsAgonist activity at rat brain CB1 receptor assessed as decrease in forskolin-stimulated cAMP level stimulated for 30 mins followed by Eu-cAMP tracer addition and measured after 60 mins	ChEMBL	469	4	2	6	5.3	CC1(C)Oc2cc(C34CC5CC(CC(CN=C=S)(C5)O3)C4)cc(O)c2[C@@H]2C[C@H](CO)CC[C@H]21	10.1016/j.bmcl.2021.127882
	CHEMBL4760082	180500	0	None	-	1	Rat	9.1	pEC50	=	9.1	Functional	Agonist activity at rat brain CB1 receptor assessed as decrease in forskolin-stimulated cAMP level stimulated for 30 mins followed by Eu-cAMP tracer addition and measured after 60 minsAgonist activity at rat brain CB1 receptor assessed as decrease in forskolin-stimulated cAMP level stimulated for 30 mins followed by Eu-cAMP tracer addition and measured after 60 mins	ChEMBL	469	4	2	6	5.3	CC1(C)Oc2cc(C34CC5CC(CC(CN=C=S)(C5)O3)C4)cc(O)c2[C@@H]2C[C@H](CO)CC[C@H]21	10.1016/j.bmcl.2021.127882
	162668251	181946	0	None	-	1	Rat	9.1	pEC50	=	9.1	Functional	Agonist activity at rat brain CB1 receptor assessed as decrease in forskolin-stimulated cAMP level stimulated for 30 mins followed by Eu-cAMP tracer addition and measured after 60 minsAgonist activity at rat brain CB1 receptor assessed as decrease in forskolin-stimulated cAMP level stimulated for 30 mins followed by Eu-cAMP tracer addition and measured after 60 mins	ChEMBL	453	4	2	5	5.5	CC1(C)Oc2cc(C34CC5CC(CC(CN=[N+]=[N-])(C5)O3)C4)cc(O)c2[C@@H]2C[C@H](CO)CC[C@H]21	10.1016/j.bmcl.2021.127882
	CHEMBL4787347	181946	0	None	-	1	Rat	9.1	pEC50	=	9.1	Functional	Agonist activity at rat brain CB1 receptor assessed as decrease in forskolin-stimulated cAMP level stimulated for 30 mins followed by Eu-cAMP tracer addition and measured after 60 minsAgonist activity at rat brain CB1 receptor assessed as decrease in forskolin-stimulated cAMP level stimulated for 30 mins followed by Eu-cAMP tracer addition and measured after 60 mins	ChEMBL	453	4	2	5	5.5	CC1(C)Oc2cc(C34CC5CC(CC(CN=[N+]=[N-])(C5)O3)C4)cc(O)c2[C@@H]2C[C@H](CO)CC[C@H]21	10.1016/j.bmcl.2021.127882
	145983146	165328	0	None	56	2	Rat	9.1	pEC50	=	9.1	Functional	Agonist activity at recombinant rat Cb1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP levelsAgonist activity at recombinant rat Cb1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP levels	ChEMBL	421	6	1	5	5.8	CC1=CC[C@H]2[C@H](C1)c1c(O)cc(/C(C)=N/OCCOc3ccccc3)cc1OC2(C)C	10.1016/j.bmc.2018.08.003
	CHEMBL4249729	165328	0	None	56	2	Rat	9.1	pEC50	=	9.1	Functional	Agonist activity at recombinant rat Cb1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP levelsAgonist activity at recombinant rat Cb1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP levels	ChEMBL	421	6	1	5	5.8	CC1=CC[C@H]2[C@H](C1)c1c(O)cc(/C(C)=N/OCCOc3ccccc3)cc1OC2(C)C	10.1016/j.bmc.2018.08.003
	45101490	195425	0	None	301	2	Human	9.1	pEC50	=	9.1	Functional	Inverse agonist activity at human CB1 receptor assessed as forskolin-induced cAMP level by adenylyl cyclase activation flash plate assayInverse agonist activity at human CB1 receptor assessed as forskolin-induced cAMP level by adenylyl cyclase activation flash plate assay	ChEMBL	514	8	2	4	6.3	C[C@H](NC(=O)C(C)(C)Nc1cc(C(F)(F)F)ccn1)[C@@H](Cc1ccc(Cl)cc1)c1cccc(C#N)c1	10.1016/j.bmcl.2009.07.046
	CHEMBL567679	195425	0	None	301	2	Human	9.1	pEC50	=	9.1	Functional	Inverse agonist activity at human CB1 receptor assessed as forskolin-induced cAMP level by adenylyl cyclase activation flash plate assayInverse agonist activity at human CB1 receptor assessed as forskolin-induced cAMP level by adenylyl cyclase activation flash plate assay	ChEMBL	514	8	2	4	6.3	C[C@H](NC(=O)C(C)(C)Nc1cc(C(F)(F)F)ccn1)[C@@H](Cc1ccc(Cl)cc1)c1cccc(C#N)c1	10.1016/j.bmcl.2009.07.046
	24768473	97400	0	None	2	3	Mouse	9.0	pEC50	=	9	Functional	Activity at mouse CB1 receptor in mouse N18TG2 cells assessed as forskolin-induced cAMP formationActivity at mouse CB1 receptor in mouse N18TG2 cells assessed as forskolin-induced cAMP formation	ChEMBL	416	4	1	4	5.3	Cc1c(C(=O)NC2CCCCC2)nn(-c2ccc(Cl)c(Cl)c2)c1-n1cccc1	10.1021/jm070566z
	CHEMBL272203	97400	0	None	2	3	Mouse	9.0	pEC50	=	9	Functional	Activity at mouse CB1 receptor in mouse N18TG2 cells assessed as forskolin-induced cAMP formationActivity at mouse CB1 receptor in mouse N18TG2 cells assessed as forskolin-induced cAMP formation	ChEMBL	416	4	1	4	5.3	Cc1c(C(=O)NC2CCCCC2)nn(-c2ccc(Cl)c(Cl)c2)c1-n1cccc1	10.1021/jm070566z
	89994988	155520	0	None	-	1	Rat	9.0	pEC50	=	9	Functional	Agonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 minsAgonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 mins	ChEMBL	411	6	1	5	5.5	CC1=CC[C@@H]2[C@@H](C1)c1c(O)cc(C(C)(C)C(=O)OCCCCC#N)cc1OC2(C)C	10.1021/jm501165d
	CHEMBL4062745	155520	0	None	-	1	Rat	9.0	pEC50	=	9	Functional	Agonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 minsAgonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 mins	ChEMBL	411	6	1	5	5.5	CC1=CC[C@@H]2[C@@H](C1)c1c(O)cc(C(C)(C)C(=O)OCCCCC#N)cc1OC2(C)C	10.1021/jm501165d
	89994947	155606	0	None	-	1	Rat	9.0	pEC50	=	9	Functional	Agonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 minsAgonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 mins	ChEMBL	423	6	1	5	5.7	CC1=CC[C@@H]2[C@@H](C1)c1c(O)cc(C3(C(=O)OCCCCC#N)CCC3)cc1OC2(C)C	10.1021/jm501165d
	CHEMBL4063822	155606	0	None	-	1	Rat	9.0	pEC50	=	9	Functional	Agonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 minsAgonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 mins	ChEMBL	423	6	1	5	5.7	CC1=CC[C@@H]2[C@@H](C1)c1c(O)cc(C3(C(=O)OCCCCC#N)CCC3)cc1OC2(C)C	10.1021/jm501165d
	89994978	156423	0	None	-	1	Rat	9.0	pEC50	=	9	Functional	Agonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 minsAgonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 mins	ChEMBL	358	3	1	4	4.8	CCOC(=O)C(C)(C)c1cc(O)c2c(c1)OC(C)(C)[C@@H]1CC=C(C)C[C@@H]21	10.1021/jm501165d
	CHEMBL4073011	156423	0	None	-	1	Rat	9.0	pEC50	=	9	Functional	Agonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 minsAgonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 mins	ChEMBL	358	3	1	4	4.8	CCOC(=O)C(C)(C)c1cc(O)c2c(c1)OC(C)(C)[C@@H]1CC=C(C)C[C@@H]21	10.1021/jm501165d
	89994961	157820	0	None	-	1	Rat	9.0	pEC50	=	9	Functional	Agonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 minsAgonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 mins	ChEMBL	399	6	2	3	5.6	CCCCCNC(=O)C(C)(C)c1cc(O)c2c(c1)OC(C)(C)[C@@H]1CC=C(C)C[C@@H]21	10.1021/jm501165d
	CHEMBL4089791	157820	0	None	-	1	Rat	9.0	pEC50	=	9	Functional	Agonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 minsAgonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 mins	ChEMBL	399	6	2	3	5.6	CCCCCNC(=O)C(C)(C)c1cc(O)c2c(c1)OC(C)(C)[C@@H]1CC=C(C)C[C@@H]21	10.1021/jm501165d
	89994985	158627	0	None	-	1	Rat	9.0	pEC50	=	9	Functional	Agonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 minsAgonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 mins	ChEMBL	438	6	1	6	5.1	CC1=CC[C@@H]2[C@@H](C1)c1c(O)cc(C(C)(C)C(=O)OCCCn3ccnc3)cc1OC2(C)C	10.1021/jm501165d
	CHEMBL4098428	158627	0	None	-	1	Rat	9.0	pEC50	=	9	Functional	Agonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 minsAgonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 mins	ChEMBL	438	6	1	6	5.1	CC1=CC[C@@H]2[C@@H](C1)c1c(O)cc(C(C)(C)C(=O)OCCCn3ccnc3)cc1OC2(C)C	10.1021/jm501165d
	42625791	180717	0	None	-	1	Human	9.0	pEC50	=	9	Functional	Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level	ChEMBL	548	4	0	3	4.8	O=C(Cc1ccc(C(F)(F)F)cc1)N1CCN(S(=O)(=O)c2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC1	10.1021/jm900063x
	CHEMBL476253	180717	0	None	-	1	Human	9.0	pEC50	=	9	Functional	Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level	ChEMBL	548	4	0	3	4.8	O=C(Cc1ccc(C(F)(F)F)cc1)N1CCN(S(=O)(=O)c2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC1	10.1021/jm900063x
	42625463	180718	0	None	-	1	Human	9.0	pEC50	=	9	Functional	Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level	ChEMBL	558	4	0	3	4.6	O=C(Cc1ccc(C(F)(F)F)cc1)N1CCN(S(=O)(=O)c2cc(Br)cc(C(F)(F)F)c2)CC1	10.1021/jm900063x
	CHEMBL476254	180718	0	None	-	1	Human	9.0	pEC50	=	9	Functional	Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level	ChEMBL	558	4	0	3	4.6	O=C(Cc1ccc(C(F)(F)F)cc1)N1CCN(S(=O)(=O)c2cc(Br)cc(C(F)(F)F)c2)CC1	10.1021/jm900063x
	24945235	181910	0	None	-	1	Human	9.0	pEC50	=	9	Functional	Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level	ChEMBL	538	5	0	5	3.6	COC(=O)c1cc(C(F)(F)F)cc(S(=O)(=O)N2CCN(C(=O)Cc3ccc(C(F)(F)F)cc3)CC2)c1	10.1021/jm900063x
	CHEMBL478696	181910	0	None	-	1	Human	9.0	pEC50	=	9	Functional	Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level	ChEMBL	538	5	0	5	3.6	COC(=O)c1cc(C(F)(F)F)cc(S(=O)(=O)N2CCN(C(=O)Cc3ccc(C(F)(F)F)cc3)CC2)c1	10.1021/jm900063x
	2729564	186247	6	None	-	1	Human	9.0	pEC50	=	9	Functional	Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level	ChEMBL	472	3	0	3	4.1	O=C(C1CCCCC1)N1CCN(S(=O)(=O)c2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC1	10.1021/jm900063x
	CHEMBL489425	186247	6	None	-	1	Human	9.0	pEC50	=	9	Functional	Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level	ChEMBL	472	3	0	3	4.1	O=C(C1CCCCC1)N1CCN(S(=O)(=O)c2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC1	10.1021/jm900063x
	24744027	189271	0	None	4	2	Human	9.0	pEC50	=	9	Functional	Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level	ChEMBL	520	5	0	3	4.7	O=C(Cc1ccc(C(F)(F)F)cc1)N1CCN(S(=O)(=O)c2cc(C3CC3)cc(C(F)(F)F)c2)CC1	10.1021/jm900063x
	CHEMBL516900	189271	0	None	4	2	Human	9.0	pEC50	=	9	Functional	Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level	ChEMBL	520	5	0	3	4.7	O=C(Cc1ccc(C(F)(F)F)cc1)N1CCN(S(=O)(=O)c2cc(C3CC3)cc(C(F)(F)F)c2)CC1	10.1021/jm900063x
	24744027	189271	0	None	4	2	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at human recombinant CB1R expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP levelAgonist activity at human recombinant CB1R expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP level	ChEMBL	520	5	0	3	4.7	O=C(Cc1ccc(C(F)(F)F)cc1)N1CCN(S(=O)(=O)c2cc(C3CC3)cc(C(F)(F)F)c2)CC1	10.1021/jm900063x
	CHEMBL516900	189271	0	None	4	2	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at human recombinant CB1R expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP levelAgonist activity at human recombinant CB1R expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP level	ChEMBL	520	5	0	3	4.7	O=C(Cc1ccc(C(F)(F)F)cc1)N1CCN(S(=O)(=O)c2cc(C3CC3)cc(C(F)(F)F)c2)CC1	10.1021/jm900063x
	24944970	192530	0	None	-	1	Human	9.0	pEC50	=	9.0	Functional	Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level	ChEMBL	364	3	0	3	2.7	Cc1cc(C)cc(S(=O)(=O)N2CCN(C(=O)C3CCCCC3)CC2)c1	10.1021/jm900063x
	CHEMBL522930	192530	0	None	-	1	Human	9.0	pEC50	=	9.0	Functional	Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level	ChEMBL	364	3	0	3	2.7	Cc1cc(C)cc(S(=O)(=O)N2CCN(C(=O)C3CCCCC3)CC2)c1	10.1021/jm900063x
	162665228	181514	0	None	2	2	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at human CB1R expressed in CHO cell membranes after 90 mins by [35S]GTPgammaS assayAgonist activity at human CB1R expressed in CHO cell membranes after 90 mins by [35S]GTPgammaS assay	ChEMBL	390	4	1	3	4.5	Cc1c(Cl)cc(C(=O)NC2CCCCCC2)c(=O)n1Cc1ccc(F)cc1	10.1016/j.ejmech.2020.112858
	CHEMBL4781952	181514	0	None	2	2	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at human CB1R expressed in CHO cell membranes after 90 mins by [35S]GTPgammaS assayAgonist activity at human CB1R expressed in CHO cell membranes after 90 mins by [35S]GTPgammaS assay	ChEMBL	390	4	1	3	4.5	Cc1c(Cl)cc(C(=O)NC2CCCCCC2)c(=O)n1Cc1ccc(F)cc1	10.1016/j.ejmech.2020.112858
	104895	1157	23	None	-9	9	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assayAgonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assay	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1021/acs.jmedchem.0c02053
	730	1157	23	None	-9	9	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assayAgonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assay	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1021/acs.jmedchem.0c02053
	734	1157	23	None	-9	9	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assayAgonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assay	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1021/acs.jmedchem.0c02053
	CHEMBL559612	1157	23	None	-9	9	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assayAgonist activity at 3xHA tagged human CB1 receptor expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP accumulation incubated for 30 mins by cAMP assay	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1021/acs.jmedchem.0c02053
	10024106	95709	0	None	-	1	Human	8.9	pEC50	=	8.9	Functional	Activity at human CB1R expressed in HEK293 cells assessed as intracellular cAMP levelActivity at human CB1R expressed in HEK293 cells assessed as intracellular cAMP level	ChEMBL	403	3	0	3	5.1	O=C(c1cc2c(cc1F)OC(c1ccccc1)(c1ccccc1)O2)N1CCCCC1	10.1021/jm701487t
	CHEMBL260625	95709	0	None	-	1	Human	8.9	pEC50	=	8.9	Functional	Activity at human CB1R expressed in HEK293 cells assessed as intracellular cAMP levelActivity at human CB1R expressed in HEK293 cells assessed as intracellular cAMP level	ChEMBL	403	3	0	3	5.1	O=C(c1cc2c(cc1F)OC(c1ccccc1)(c1ccccc1)O2)N1CCCCC1	10.1021/jm701487t
	156248392	183788	0	None	89	2	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis	ChEMBL	361	2	1	4	3.5	CC(C)(C)NC(=O)c1nn(-c2ccc(F)cc2F)c2c1CC1CCC2O1	10.1021/acsmedchemlett.1c00331
	CHEMBL4845707	183788	0	None	89	2	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis	ChEMBL	361	2	1	4	3.5	CC(C)(C)NC(=O)c1nn(-c2ccc(F)cc2F)c2c1CC1CCC2O1	10.1021/acsmedchemlett.1c00331
	162676369	182752	0	None	-	1	Human	8.9	pEC50	=	8.9	Functional	Negative allosteric modulator activity at CB1 receptor (unknown origin) expressed in HEK293 cell membrane assessed as reduction in CP55,940-induced [35S]GTPgammaS binding by measuring EC50 of CP55,940 at 3.2 uM incubated for 60 mins by liquid scintillation counting analysis (Rvb = 4.7 nM)Negative allosteric modulator activity at CB1 receptor (unknown origin) expressed in HEK293 cell membrane assessed as reduction in CP55,940-induced [35S]GTPgammaS binding by measuring EC50 of CP55,940 at 3.2 uM incubated for 60 mins by liquid scintillation counting analysis (Rvb = 4.7 nM)	ChEMBL	396	7	2	3	4.7	CN(C)c1ccc(CCNC(=O)c2[nH]c3ccc(Cl)cc3c2CN=[N+]=[N-])cc1	10.1016/j.ejmech.2016.05.044
	CHEMBL4797581	182752	0	None	-	1	Human	8.9	pEC50	=	8.9	Functional	Negative allosteric modulator activity at CB1 receptor (unknown origin) expressed in HEK293 cell membrane assessed as reduction in CP55,940-induced [35S]GTPgammaS binding by measuring EC50 of CP55,940 at 3.2 uM incubated for 60 mins by liquid scintillation counting analysis (Rvb = 4.7 nM)Negative allosteric modulator activity at CB1 receptor (unknown origin) expressed in HEK293 cell membrane assessed as reduction in CP55,940-induced [35S]GTPgammaS binding by measuring EC50 of CP55,940 at 3.2 uM incubated for 60 mins by liquid scintillation counting analysis (Rvb = 4.7 nM)	ChEMBL	396	7	2	3	4.7	CN(C)c1ccc(CCNC(=O)c2[nH]c3ccc(Cl)cc3c2CN=[N+]=[N-])cc1	10.1016/j.ejmech.2016.05.044
	104895	1157	23	None	-9	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release assayAgonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release assay	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1016/j.bmcl.2010.07.056
	730	1157	23	None	-9	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release assayAgonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release assay	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1016/j.bmcl.2010.07.056
	734	1157	23	None	-9	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release assayAgonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release assay	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1016/j.bmcl.2010.07.056
	CHEMBL559612	1157	23	None	-9	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release assayAgonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release assay	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1016/j.bmcl.2010.07.056
	71661716	87856	1	None	-	1	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human CB1 receptor transfected in HEK293 cells assessed as reduction in forskolin-stimulated cAMP accumulation after 30 minsAgonist activity at human CB1 receptor transfected in HEK293 cells assessed as reduction in forskolin-stimulated cAMP accumulation after 30 mins	ChEMBL	396	2	2	3	5.5	CC1(C)Oc2cc(C34CC5CC(CC(C5)C3)C4)cc(O)c2[C@@H]2C[C@H](CO)CC[C@H]21	10.1021/jm4000775
	CHEMBL2348462	87856	1	None	-	1	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human CB1 receptor transfected in HEK293 cells assessed as reduction in forskolin-stimulated cAMP accumulation after 30 minsAgonist activity at human CB1 receptor transfected in HEK293 cells assessed as reduction in forskolin-stimulated cAMP accumulation after 30 mins	ChEMBL	396	2	2	3	5.5	CC1(C)Oc2cc(C34CC5CC(CC(C5)C3)C4)cc(O)c2[C@@H]2C[C@H](CO)CC[C@H]21	10.1021/jm4000775
	42625862	192144	0	None	3	2	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human recombinant CB1R expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP levelAgonist activity at human recombinant CB1R expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP level	ChEMBL	506	4	0	3	4.7	O=C(c1ccc(C(F)(F)F)cc1)N1CCN(S(=O)(=O)c2cc(C3CC3)cc(C(F)(F)F)c2)CC1	10.1021/jm900063x
	CHEMBL522114	192144	0	None	3	2	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human recombinant CB1R expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP levelAgonist activity at human recombinant CB1R expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP level	ChEMBL	506	4	0	3	4.7	O=C(c1ccc(C(F)(F)F)cc1)N1CCN(S(=O)(=O)c2cc(C3CC3)cc(C(F)(F)F)c2)CC1	10.1021/jm900063x
	49781019	17972	0	None	20	2	Rat	8.9	pEC50	=	8.9	Functional	Antagonist activity at rat brain CB1 receptor assessed as inhibition of [35S]GTPgammaS bindingAntagonist activity at rat brain CB1 receptor assessed as inhibition of [35S]GTPgammaS binding	ChEMBL	1023	26	3	7	15.1	Cc1c(C(=O)NCCCCCCCCCNCCCCCCCCCNC(=O)c2nn(-c3ccc(Cl)cc3Cl)c(-c3ccc(Cl)cc3)c2C)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1	10.1021/jm1006676
	CHEMBL1269767	17972	0	None	20	2	Rat	8.9	pEC50	=	8.9	Functional	Antagonist activity at rat brain CB1 receptor assessed as inhibition of [35S]GTPgammaS bindingAntagonist activity at rat brain CB1 receptor assessed as inhibition of [35S]GTPgammaS binding	ChEMBL	1023	26	3	7	15.1	Cc1c(C(=O)NCCCCCCCCCNCCCCCCCCCNC(=O)c2nn(-c3ccc(Cl)cc3Cl)c(-c3ccc(Cl)cc3)c2C)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1	10.1021/jm1006676
	164887460	191533	1	None	2	2	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at N-terminal 3HA-tagged human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured for 30 mins by FRET assayAgonist activity at N-terminal 3HA-tagged human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured for 30 mins by FRET assay	ChEMBL	395	6	1	4	5.9	CC1(C)Oc2cc(C3(CCCCCC#N)CCC3)cc(O)c2[C@@H]2CC(=O)CC[C@H]21	10.1016/j.ejmech.2021.114027
	CHEMBL5203712	191533	1	None	2	2	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at N-terminal 3HA-tagged human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured for 30 mins by FRET assayAgonist activity at N-terminal 3HA-tagged human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured for 30 mins by FRET assay	ChEMBL	395	6	1	4	5.9	CC1(C)Oc2cc(C3(CCCCCC#N)CCC3)cc(O)c2[C@@H]2CC(=O)CC[C@H]21	10.1016/j.ejmech.2021.114027
	145959588	161784	0	None	-1	2	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human CB1 receptor expressed in CHO cell membranes after 90 mins by [35S]GTPgammaS binding assayAgonist activity at human CB1 receptor expressed in CHO cell membranes after 90 mins by [35S]GTPgammaS binding assay	ChEMBL	434	4	1	3	4.6	Cc1c(Br)cn(Cc2ccc(F)cc2)c(=O)c1C(=O)NC1CCCCCC1	10.1016/j.ejmech.2018.05.019
	CHEMBL4164954	161784	0	None	-1	2	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human CB1 receptor expressed in CHO cell membranes after 90 mins by [35S]GTPgammaS binding assayAgonist activity at human CB1 receptor expressed in CHO cell membranes after 90 mins by [35S]GTPgammaS binding assay	ChEMBL	434	4	1	3	4.6	Cc1c(Br)cn(Cc2ccc(F)cc2)c(=O)c1C(=O)NC1CCCCCC1	10.1016/j.ejmech.2018.05.019
	104895	1157	23	None	-9	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human CB1 receptor expressed in CHO cell membranes assessed as increase in G-protein coupling by measuring [35S]GTPgammaS binding after 90 mins in presence of [35S]GTPgammaS by liquid scintillation analysisAgonist activity at human CB1 receptor expressed in CHO cell membranes assessed as increase in G-protein coupling by measuring [35S]GTPgammaS binding after 90 mins in presence of [35S]GTPgammaS by liquid scintillation analysis	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1021/acs.jmedchem.9b01142
	730	1157	23	None	-9	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human CB1 receptor expressed in CHO cell membranes assessed as increase in G-protein coupling by measuring [35S]GTPgammaS binding after 90 mins in presence of [35S]GTPgammaS by liquid scintillation analysisAgonist activity at human CB1 receptor expressed in CHO cell membranes assessed as increase in G-protein coupling by measuring [35S]GTPgammaS binding after 90 mins in presence of [35S]GTPgammaS by liquid scintillation analysis	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1021/acs.jmedchem.9b01142
	734	1157	23	None	-9	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human CB1 receptor expressed in CHO cell membranes assessed as increase in G-protein coupling by measuring [35S]GTPgammaS binding after 90 mins in presence of [35S]GTPgammaS by liquid scintillation analysisAgonist activity at human CB1 receptor expressed in CHO cell membranes assessed as increase in G-protein coupling by measuring [35S]GTPgammaS binding after 90 mins in presence of [35S]GTPgammaS by liquid scintillation analysis	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1021/acs.jmedchem.9b01142
	CHEMBL559612	1157	23	None	-9	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human CB1 receptor expressed in CHO cell membranes assessed as increase in G-protein coupling by measuring [35S]GTPgammaS binding after 90 mins in presence of [35S]GTPgammaS by liquid scintillation analysisAgonist activity at human CB1 receptor expressed in CHO cell membranes assessed as increase in G-protein coupling by measuring [35S]GTPgammaS binding after 90 mins in presence of [35S]GTPgammaS by liquid scintillation analysis	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1021/acs.jmedchem.9b01142
	104895	1157	23	None	-9	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human recombinant CB1 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAgonist activity at human recombinant CB1 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1016/j.bmc.2014.07.006
	730	1157	23	None	-9	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human recombinant CB1 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAgonist activity at human recombinant CB1 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1016/j.bmc.2014.07.006
	734	1157	23	None	-9	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human recombinant CB1 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAgonist activity at human recombinant CB1 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1016/j.bmc.2014.07.006
	CHEMBL559612	1157	23	None	-9	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human recombinant CB1 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAgonist activity at human recombinant CB1 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1016/j.bmc.2014.07.006
	104895	1157	23	None	-9	9	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at N-terminal 3HA-tagged human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured for 30 mins by FRET assayAgonist activity at N-terminal 3HA-tagged human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured for 30 mins by FRET assay	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1016/j.ejmech.2021.114027
	730	1157	23	None	-9	9	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at N-terminal 3HA-tagged human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured for 30 mins by FRET assayAgonist activity at N-terminal 3HA-tagged human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured for 30 mins by FRET assay	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1016/j.ejmech.2021.114027
	734	1157	23	None	-9	9	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at N-terminal 3HA-tagged human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured for 30 mins by FRET assayAgonist activity at N-terminal 3HA-tagged human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured for 30 mins by FRET assay	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1016/j.ejmech.2021.114027
	CHEMBL559612	1157	23	None	-9	9	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at N-terminal 3HA-tagged human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured for 30 mins by FRET assayAgonist activity at N-terminal 3HA-tagged human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured for 30 mins by FRET assay	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1016/j.ejmech.2021.114027
	104850	3266	93	None	1	6	Human	8.8	pEC50	=	8.8	Functional	Antagonist activity at human CB1 receptor overexpressed in HEK cells assessed as [35S]GTPgamma binding after 1 hr by liquid scintillation counting analysisAntagonist activity at human CB1 receptor overexpressed in HEK cells assessed as [35S]GTPgamma binding after 1 hr by liquid scintillation counting analysis	ChEMBL	462	4	1	4	5.9	Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1	10.1021/jm4010708
	4150	3266	93	None	1	6	Human	8.8	pEC50	=	8.8	Functional	Antagonist activity at human CB1 receptor overexpressed in HEK cells assessed as [35S]GTPgamma binding after 1 hr by liquid scintillation counting analysisAntagonist activity at human CB1 receptor overexpressed in HEK cells assessed as [35S]GTPgamma binding after 1 hr by liquid scintillation counting analysis	ChEMBL	462	4	1	4	5.9	Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1	10.1021/jm4010708
	743	3266	93	None	1	6	Human	8.8	pEC50	=	8.8	Functional	Antagonist activity at human CB1 receptor overexpressed in HEK cells assessed as [35S]GTPgamma binding after 1 hr by liquid scintillation counting analysisAntagonist activity at human CB1 receptor overexpressed in HEK cells assessed as [35S]GTPgamma binding after 1 hr by liquid scintillation counting analysis	ChEMBL	462	4	1	4	5.9	Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1	10.1021/jm4010708
	CHEMBL111	3266	93	None	1	6	Human	8.8	pEC50	=	8.8	Functional	Antagonist activity at human CB1 receptor overexpressed in HEK cells assessed as [35S]GTPgamma binding after 1 hr by liquid scintillation counting analysisAntagonist activity at human CB1 receptor overexpressed in HEK cells assessed as [35S]GTPgamma binding after 1 hr by liquid scintillation counting analysis	ChEMBL	462	4	1	4	5.9	Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1	10.1021/jm4010708
	DB06155	3266	93	None	1	6	Human	8.8	pEC50	=	8.8	Functional	Antagonist activity at human CB1 receptor overexpressed in HEK cells assessed as [35S]GTPgamma binding after 1 hr by liquid scintillation counting analysisAntagonist activity at human CB1 receptor overexpressed in HEK cells assessed as [35S]GTPgamma binding after 1 hr by liquid scintillation counting analysis	ChEMBL	462	4	1	4	5.9	Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1	10.1021/jm4010708
	24945315	186250	0	None	-	1	Human	8.8	pEC50	=	8.8	Functional	Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level	ChEMBL	494	4	0	3	4.6	CC(C(=O)N1CCN(S(=O)(=O)c2cc(Cl)cc(Cl)c2)CC1)c1ccc(C(F)(F)F)cc1	10.1021/jm900063x
	CHEMBL489437	186250	0	None	-	1	Human	8.8	pEC50	=	8.8	Functional	Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level	ChEMBL	494	4	0	3	4.6	CC(C(=O)N1CCN(S(=O)(=O)c2cc(Cl)cc(Cl)c2)CC1)c1ccc(C(F)(F)F)cc1	10.1021/jm900063x
	104895	1157	23	None	-9	9	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding assayAgonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding assay	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1016/j.ejmech.2021.113354
	730	1157	23	None	-9	9	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding assayAgonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding assay	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1016/j.ejmech.2021.113354
	734	1157	23	None	-9	9	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding assayAgonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding assay	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1016/j.ejmech.2021.113354
	CHEMBL559612	1157	23	None	-9	9	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding assayAgonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding assay	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1016/j.ejmech.2021.113354
	162672230	182255	0	None	4	2	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	351	8	1	5	3.3	CCCCCn1nc(C(=O)N[C@@H](C(=O)OC)C(C)C)cc1C(C)(C)C	10.1021/acs.jmedchem.0c01023
	CHEMBL4791449	182255	0	None	4	2	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	351	8	1	5	3.3	CCCCCn1nc(C(=O)N[C@@H](C(=O)OC)C(C)C)cc1C(C)(C)C	10.1021/acs.jmedchem.0c01023
	118733874	118055	0	None	10	2	Rat	8.8	pEC50	=	8.8	Functional	Agonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 60 minsAgonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 60 mins	ChEMBL	455	2	3	5	4.8	COC(=O)N[C@]12CC3CC(C1)C[C@](c1cc(O)c4c(c1)OC(C)(C)[C@@H]1CC[C@@H](O)C[C@@H]41)(C3)C2	10.1021/jm501960u
	CHEMBL3416121	118055	0	None	10	2	Rat	8.8	pEC50	=	8.8	Functional	Agonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 60 minsAgonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 60 mins	ChEMBL	455	2	3	5	4.8	COC(=O)N[C@]12CC3CC(C1)C[C@](c1cc(O)c4c(c1)OC(C)(C)[C@@H]1CC[C@@H](O)C[C@@H]41)(C3)C2	10.1021/jm501960u
	104895	1157	23	None	-9	9	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human CB1 receptor expressed in CHO cell membrane assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assayAgonist activity at human CB1 receptor expressed in CHO cell membrane assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assay	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1016/j.bmc.2020.115513
	730	1157	23	None	-9	9	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human CB1 receptor expressed in CHO cell membrane assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assayAgonist activity at human CB1 receptor expressed in CHO cell membrane assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assay	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1016/j.bmc.2020.115513
	734	1157	23	None	-9	9	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human CB1 receptor expressed in CHO cell membrane assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assayAgonist activity at human CB1 receptor expressed in CHO cell membrane assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assay	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1016/j.bmc.2020.115513
	CHEMBL559612	1157	23	None	-9	9	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human CB1 receptor expressed in CHO cell membrane assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assayAgonist activity at human CB1 receptor expressed in CHO cell membrane assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assay	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1016/j.bmc.2020.115513
	155541870	172472	0	None	-2	2	Human	8.8	pEC50	=	8.8	Functional	Positive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced inhibition of forskolin-induced cAMP accumulation after 90 mins in presence of 100 nM CP55940 by hit-hunter cAMP assayPositive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced inhibition of forskolin-induced cAMP accumulation after 90 mins in presence of 100 nM CP55940 by hit-hunter cAMP assay	ChEMBL	396	5	1	2	5.7	O=[N+]([O-])CC(c1ccccc1F)c1c(-c2cccc(F)c2)[nH]c2c(F)cccc12	10.1021/acs.jmedchem.9b01142
	CHEMBL4519310	172472	0	None	-2	2	Human	8.8	pEC50	=	8.8	Functional	Positive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced inhibition of forskolin-induced cAMP accumulation after 90 mins in presence of 100 nM CP55940 by hit-hunter cAMP assayPositive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced inhibition of forskolin-induced cAMP accumulation after 90 mins in presence of 100 nM CP55940 by hit-hunter cAMP assay	ChEMBL	396	5	1	2	5.7	O=[N+]([O-])CC(c1ccccc1F)c1c(-c2cccc(F)c2)[nH]c2c(F)cccc12	10.1021/acs.jmedchem.9b01142
	49781021	17974	0	None	33	2	Rat	8.8	pEC50	=	8.8	Functional	Antagonist activity at rat brain CB1 receptor assessed as inhibition of [35S]GTPgammaS bindingAntagonist activity at rat brain CB1 receptor assessed as inhibition of [35S]GTPgammaS binding	ChEMBL	925	18	2	7	12.4	Cc1c(C(=O)NCCCCCN(C)CCCCCNC(=O)c2nn(-c3ccc(Cl)cc3Cl)c(-c3ccc(Cl)cc3)c2C)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1	10.1021/jm1006676
	CHEMBL1269769	17974	0	None	33	2	Rat	8.8	pEC50	=	8.8	Functional	Antagonist activity at rat brain CB1 receptor assessed as inhibition of [35S]GTPgammaS bindingAntagonist activity at rat brain CB1 receptor assessed as inhibition of [35S]GTPgammaS binding	ChEMBL	925	18	2	7	12.4	Cc1c(C(=O)NCCCCCN(C)CCCCCNC(=O)c2nn(-c3ccc(Cl)cc3Cl)c(-c3ccc(Cl)cc3)c2C)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1	10.1021/jm1006676
	57606063	74203	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma bindingAgonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma binding	ChEMBL	437	6	1	4	3.5	CCN(CC(=O)NC1CC1)C(=O)c1ccc2c(c1)c1c(n2C)CC[C@@H](C2CCOCC2)C1	10.1016/j.bmcl.2012.04.128
	CHEMBL2029727	74203	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma bindingAgonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma binding	ChEMBL	437	6	1	4	3.5	CCN(CC(=O)NC1CC1)C(=O)c1ccc2c(c1)c1c(n2C)CC[C@@H](C2CCOCC2)C1	10.1016/j.bmcl.2012.04.128
	145967019	163886	0	None	-	1	Rat	8.7	pEC50	=	8.7	Functional	Agonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 minsAgonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins	ChEMBL	398	17	1	2	6.9	C[C@H](/C=C\C/C=C\C/C=C\CCCC(=O)NC1CC1)/C=C\CCCCCN=[N+]=[N-]	10.1021/acs.jmedchem.8b00611
	CHEMBL4213900	163886	0	None	-	1	Rat	8.7	pEC50	=	8.7	Functional	Agonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 minsAgonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins	ChEMBL	398	17	1	2	6.9	C[C@H](/C=C\C/C=C\C/C=C\CCCC(=O)NC1CC1)/C=C\CCCCCN=[N+]=[N-]	10.1021/acs.jmedchem.8b00611
	45487312	196120	0	None	26	2	Human	8.7	pEC50	=	8.7	Functional	Inverse agonist activity at human CB1 receptor assessed as forskolin-induced cAMP level by adenylyl cyclase activation flash plate assayInverse agonist activity at human CB1 receptor assessed as forskolin-induced cAMP level by adenylyl cyclase activation flash plate assay	ChEMBL	496	8	2	4	6.5	C[C@H](NC(=O)C(C)(C)Nc1cc2ccccc2cn1)[C@@H](Cc1ccc(Cl)cc1)c1cccc(C#N)c1	10.1016/j.bmcl.2009.07.046
	CHEMBL572097	196120	0	None	26	2	Human	8.7	pEC50	=	8.7	Functional	Inverse agonist activity at human CB1 receptor assessed as forskolin-induced cAMP level by adenylyl cyclase activation flash plate assayInverse agonist activity at human CB1 receptor assessed as forskolin-induced cAMP level by adenylyl cyclase activation flash plate assay	ChEMBL	496	8	2	4	6.5	C[C@H](NC(=O)C(C)(C)Nc1cc2ccccc2cn1)[C@@H](Cc1ccc(Cl)cc1)c1cccc(C#N)c1	10.1016/j.bmcl.2009.07.046
	54580071	62757	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assayAgonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assay	ChEMBL	461	9	1	6	5.2	CCc1sc(-c2cn(CC3CCOCC3)c3c(Cl)cccc23)nc1CN(CC)CCO	10.1016/j.bmcl.2011.02.023
	CHEMBL1762814	62757	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assayAgonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assay	ChEMBL	461	9	1	6	5.2	CCc1sc(-c2cn(CC3CCOCC3)c3c(Cl)cccc23)nc1CN(CC)CCO	10.1016/j.bmcl.2011.02.023
	CHEMBL1789190	62757	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assayAgonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assay	ChEMBL	461	9	1	6	5.2	CCc1sc(-c2cn(CC3CCOCC3)c3c(Cl)cccc23)nc1CN(CC)CCO	10.1016/j.bmcl.2011.02.023
	104895	1157	23	None	-9	9	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human recombinant cannabinoid CB1 receptor expressed in HEK cells transfected with CNG assessed as decrease in cAMP level measured up to 1 hr by ACTOne membrane potential dye based assayAgonist activity at human recombinant cannabinoid CB1 receptor expressed in HEK cells transfected with CNG assessed as decrease in cAMP level measured up to 1 hr by ACTOne membrane potential dye based assay	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1016/j.bmc.2021.116035
	730	1157	23	None	-9	9	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human recombinant cannabinoid CB1 receptor expressed in HEK cells transfected with CNG assessed as decrease in cAMP level measured up to 1 hr by ACTOne membrane potential dye based assayAgonist activity at human recombinant cannabinoid CB1 receptor expressed in HEK cells transfected with CNG assessed as decrease in cAMP level measured up to 1 hr by ACTOne membrane potential dye based assay	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1016/j.bmc.2021.116035
	734	1157	23	None	-9	9	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human recombinant cannabinoid CB1 receptor expressed in HEK cells transfected with CNG assessed as decrease in cAMP level measured up to 1 hr by ACTOne membrane potential dye based assayAgonist activity at human recombinant cannabinoid CB1 receptor expressed in HEK cells transfected with CNG assessed as decrease in cAMP level measured up to 1 hr by ACTOne membrane potential dye based assay	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1016/j.bmc.2021.116035
	CHEMBL559612	1157	23	None	-9	9	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human recombinant cannabinoid CB1 receptor expressed in HEK cells transfected with CNG assessed as decrease in cAMP level measured up to 1 hr by ACTOne membrane potential dye based assayAgonist activity at human recombinant cannabinoid CB1 receptor expressed in HEK cells transfected with CNG assessed as decrease in cAMP level measured up to 1 hr by ACTOne membrane potential dye based assay	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1016/j.bmc.2021.116035
	121283196	158630	0	None	-	1	Rat	8.0	pEC50	=	8	Functional	Agonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 minsAgonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 mins	ChEMBL	383	6	1	5	4.8	CC1=CC[C@@H]2[C@@H](C1)c1c(O)cc(CC(=O)OCCCCC#N)cc1OC2(C)C	10.1021/jm501165d
	CHEMBL4098489	158630	0	None	-	1	Rat	8.0	pEC50	=	8	Functional	Agonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 minsAgonist activity at CB1 receptor in rat brain membranes assessed as reduction in forskolin-stimulated cAMP level measured from 3 data points after 30 mins	ChEMBL	383	6	1	5	4.8	CC1=CC[C@@H]2[C@@H](C1)c1c(O)cc(CC(=O)OCCCCC#N)cc1OC2(C)C	10.1021/jm501165d
	54752945	64943	34	None	-1	3	Human	8.0	pEC50	=	8	Functional	Agonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid releaseAgonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid release	ChEMBL	356	6	1	2	6.2	CCCCCn1cc(C(=O)Nc2cccc3ccccc23)c2ccccc21	10.1016/j.ejmech.2011.08.021
	CHEMBL1828805	64943	34	None	-1	3	Human	8.0	pEC50	=	8	Functional	Agonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid releaseAgonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid release	ChEMBL	356	6	1	2	6.2	CCCCCn1cc(C(=O)Nc2cccc3ccccc23)c2ccccc21	10.1016/j.ejmech.2011.08.021
	11453673	60692	9	None	-	1	Human	8.0	pEC50	=	8	Functional	Agonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assayAgonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assay	ChEMBL	447	8	1	6	5.0	CC(C)N(CCO)Cc1csc(-c2cn(CC3CCOCC3)c3c(Cl)cccc23)n1	10.1016/j.bmcl.2011.02.023
	CHEMBL1762808	60692	9	None	-	1	Human	8.0	pEC50	=	8	Functional	Agonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assayAgonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assay	ChEMBL	447	8	1	6	5.0	CC(C)N(CCO)Cc1csc(-c2cn(CC3CCOCC3)c3c(Cl)cccc23)n1	10.1016/j.bmcl.2011.02.023
	54582096	62759	0	None	-	1	Human	8.0	pEC50	=	8	Functional	Agonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assayAgonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assay	ChEMBL	481	8	1	6	5.7	CC(C)N(CCO)Cc1nc(-c2cn(CC3CCOCC3)c3c(Cl)cccc23)sc1Cl	10.1016/j.bmcl.2011.02.023
	CHEMBL1762816	62759	0	None	-	1	Human	8.0	pEC50	=	8	Functional	Agonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assayAgonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assay	ChEMBL	481	8	1	6	5.7	CC(C)N(CCO)Cc1nc(-c2cn(CC3CCOCC3)c3c(Cl)cccc23)sc1Cl	10.1016/j.bmcl.2011.02.023
	CHEMBL1789209	62759	0	None	-	1	Human	8.0	pEC50	=	8	Functional	Agonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assayAgonist activity at human CB1 receptor expressed in CHO cells by luciferase reporter gene assay	ChEMBL	481	8	1	6	5.7	CC(C)N(CCO)Cc1nc(-c2cn(CC3CCOCC3)c3c(Cl)cccc23)sc1Cl	10.1016/j.bmcl.2011.02.023
	25195469	109488	0	None	-10	2	Human	8.0	pEC50	=	8	Functional	Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation by TR-FRET assayAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation by TR-FRET assay	ChEMBL	420	4	1	4	3.8	O=C(NC1CCCC1)c1ccc2c(c1)N(S(=O)(=O)c1ccc(F)cc1)CCS2	10.1021/jm4005626
	CHEMBL3234688	109488	0	None	-10	2	Human	8.0	pEC50	=	8	Functional	Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation by TR-FRET assayAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation by TR-FRET assay	ChEMBL	420	4	1	4	3.8	O=C(NC1CCCC1)c1ccc2c(c1)N(S(=O)(=O)c1ccc(F)cc1)CCS2	10.1021/jm4005626
	11201613	18779	0	None	-	1	Human	8.0	pEC50	=	8	Functional	Agonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assay	ChEMBL	407	2	0	4	4.5	O=C(c1cn2c3c(cccc13)OC[C@H]2C1CCCCC1)N1CCN2CCCC[C@H]2C1	10.1016/j.bmcl.2010.10.061
	CHEMBL1287847	18779	0	None	-	1	Human	8.0	pEC50	=	8	Functional	Agonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assay	ChEMBL	407	2	0	4	4.5	O=C(c1cn2c3c(cccc13)OC[C@H]2C1CCCCC1)N1CCN2CCCC[C@H]2C1	10.1016/j.bmcl.2010.10.061
	CHEMBL1287876	18779	0	None	-	1	Human	8.0	pEC50	=	8	Functional	Agonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assay	ChEMBL	407	2	0	4	4.5	O=C(c1cn2c3c(cccc13)OC[C@H]2C1CCCCC1)N1CCN2CCCC[C@H]2C1	10.1016/j.bmcl.2010.10.061
	11589652	14931	0	None	-	1	Human	8.0	pEC50	=	8	Functional	Agonist activity at human cannabinoid CB1 receptor expressed in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human cannabinoid CB1 receptor expressed in CHO cells after 5 hrs by luciferase reporter gene assay	ChEMBL	411	5	0	4	4.8	CCN1[C@@H](C)CN(C(=O)c2cn(CC3CCCCC3)c3c(OC)cccc23)C[C@H]1C	10.1016/j.bmcl.2010.06.067
	CHEMBL1209647	14931	0	None	-	1	Human	8.0	pEC50	=	8	Functional	Agonist activity at human cannabinoid CB1 receptor expressed in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human cannabinoid CB1 receptor expressed in CHO cells after 5 hrs by luciferase reporter gene assay	ChEMBL	411	5	0	4	4.8	CCN1[C@@H](C)CN(C(=O)c2cn(CC3CCCCC3)c3c(OC)cccc23)C[C@H]1C	10.1016/j.bmcl.2010.06.067
	CHEMBL3347358	14931	0	None	-	1	Human	8.0	pEC50	=	8	Functional	Agonist activity at human cannabinoid CB1 receptor expressed in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human cannabinoid CB1 receptor expressed in CHO cells after 5 hrs by luciferase reporter gene assay	ChEMBL	411	5	0	4	4.8	CCN1[C@@H](C)CN(C(=O)c2cn(CC3CCCCC3)c3c(OC)cccc23)C[C@H]1C	10.1016/j.bmcl.2010.06.067
	3929482	92978	11	None	-	1	Human	8.0	pEC50	=	8	Functional	Agonist activity at human recombinant CB1 receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayAgonist activity at human recombinant CB1 receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	ChEMBL	410	4	0	5	3.9	Cc1ccc(C(=O)Oc2cccc3cccnc23)cc1S(=O)(=O)N1CCCCC1	10.1016/j.bmcl.2006.09.049
	CHEMBL245876	92978	11	None	-	1	Human	8.0	pEC50	=	8	Functional	Agonist activity at human recombinant CB1 receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayAgonist activity at human recombinant CB1 receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	ChEMBL	410	4	0	5	3.9	Cc1ccc(C(=O)Oc2cccc3cccnc23)cc1S(=O)(=O)N1CCCCC1	10.1016/j.bmcl.2006.09.049
	5311501	4007	8	None	-11	7	Rat	8.0	pEC50	=	8	Functional	Agonist activity at rat CB1 receptor assessed as inhibition of forskolin-induced cAMP production by cell based assayAgonist activity at rat CB1 receptor assessed as inhibition of forskolin-induced cAMP production by cell based assay	ChEMBL	426	4	0	5	4.6	O=C(c1c(C)n2c3c1cccc3OC[C@H]2CN1CCOCC1)c1cccc2c1cccc2	10.1021/jm901214q
	733	4007	8	None	-11	7	Rat	8.0	pEC50	=	8	Functional	Agonist activity at rat CB1 receptor assessed as inhibition of forskolin-induced cAMP production by cell based assayAgonist activity at rat CB1 receptor assessed as inhibition of forskolin-induced cAMP production by cell based assay	ChEMBL	426	4	0	5	4.6	O=C(c1c(C)n2c3c1cccc3OC[C@H]2CN1CCOCC1)c1cccc2c1cccc2	10.1021/jm901214q
	CHEMBL188	4007	8	None	-11	7	Rat	8.0	pEC50	=	8	Functional	Agonist activity at rat CB1 receptor assessed as inhibition of forskolin-induced cAMP production by cell based assayAgonist activity at rat CB1 receptor assessed as inhibition of forskolin-induced cAMP production by cell based assay	ChEMBL	426	4	0	5	4.6	O=C(c1c(C)n2c3c1cccc3OC[C@H]2CN1CCOCC1)c1cccc2c1cccc2	10.1021/jm901214q
	DB13950	4007	8	None	-11	7	Rat	8.0	pEC50	=	8	Functional	Agonist activity at rat CB1 receptor assessed as inhibition of forskolin-induced cAMP production by cell based assayAgonist activity at rat CB1 receptor assessed as inhibition of forskolin-induced cAMP production by cell based assay	ChEMBL	426	4	0	5	4.6	O=C(c1c(C)n2c3c1cccc3OC[C@H]2CN1CCOCC1)c1cccc2c1cccc2	10.1021/jm901214q
	10717065	72300	1	None	-	1	Rat	8.0	pEC50	=	8	Functional	Displacement of [35S]GTP-gamma-S from rat cerebellar CB1 receptorDisplacement of [35S]GTP-gamma-S from rat cerebellar CB1 receptor	ChEMBL	420	5	1	2	6.8	CC1=CC[C@@H]2[C@@H](C1)c1c(O)cc(C(C)(C)CCCCBr)cc1OC2(C)C	10.1021/jm0505157
	CHEMBL199561	72300	1	None	-	1	Rat	8.0	pEC50	=	8	Functional	Displacement of [35S]GTP-gamma-S from rat cerebellar CB1 receptorDisplacement of [35S]GTP-gamma-S from rat cerebellar CB1 receptor	ChEMBL	420	5	1	2	6.8	CC1=CC[C@@H]2[C@@H](C1)c1c(O)cc(C(C)(C)CCCCBr)cc1OC2(C)C	10.1021/jm0505157
	44358262	116085	0	None	-	1	Rat	8.0	pEC50	=	8	Functional	Displacement of [35S]GTP-gamma-S from rat cerebellar CB1 receptorDisplacement of [35S]GTP-gamma-S from rat cerebellar CB1 receptor	ChEMBL	367	5	1	3	6.4	CC1=CC[C@@H]2[C@@H](C1)c1c(O)cc(C(C)(C)CCCCC#N)cc1OC2(C)C	10.1021/jm0505157
	CHEMBL336670	116085	0	None	-	1	Rat	8.0	pEC50	=	8	Functional	Displacement of [35S]GTP-gamma-S from rat cerebellar CB1 receptorDisplacement of [35S]GTP-gamma-S from rat cerebellar CB1 receptor	ChEMBL	367	5	1	3	6.4	CC1=CC[C@@H]2[C@@H](C1)c1c(O)cc(C(C)(C)CCCCC#N)cc1OC2(C)C	10.1021/jm0505157
	118916083	180367	0	None	165	2	Human	8.0	pEC50	=	8	Functional	Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 30 mins by HTRF assayInverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 30 mins by HTRF assay	ChEMBL	654	11	3	6	7.2	O=C(COc1nc(NCc2cccc(C(F)(F)F)c2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)ccc2n1)NCCO	10.1021/acsmedchemlett.0c00495
	CHEMBL4758427	180367	0	None	165	2	Human	8.0	pEC50	=	8	Functional	Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 30 mins by HTRF assayInverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 30 mins by HTRF assay	ChEMBL	654	11	3	6	7.2	O=C(COc1nc(NCc2cccc(C(F)(F)F)c2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)ccc2n1)NCCO	10.1021/acsmedchemlett.0c00495
	118329970	148660	0	None	83	2	Human	8.0	pEC50	=	8	Functional	Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assayInverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assay	ChEMBL	619	6	2	6	5.8	O=c1cc(NC2CCN(S(=O)(=O)C(F)(F)F)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc4c(c3)OCO4)ccc2[nH]1	10.1021/acs.jmedchem.8b01467
	CHEMBL3943971	148660	0	None	83	2	Human	8.0	pEC50	=	8	Functional	Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assayInverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assay	ChEMBL	619	6	2	6	5.8	O=c1cc(NC2CCN(S(=O)(=O)C(F)(F)F)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc4c(c3)OCO4)ccc2[nH]1	10.1021/acs.jmedchem.8b01467
	155541870	172472	0	None	2	2	Rat	8.0	pEC50	=	8	Functional	Positive allosteric modulatory activity at N-terminal GFP-tagged rat CB1R receptor expressed in HEK293 cells assessed as CP55940 EC50 for inhibition of forskolin-induced cAMP accumulation at 0.1 microM after 30 mins by TR-FRET assay (Rvb = 22 +/- 6 nM)Positive allosteric modulatory activity at N-terminal GFP-tagged rat CB1R receptor expressed in HEK293 cells assessed as CP55940 EC50 for inhibition of forskolin-induced cAMP accumulation at 0.1 microM after 30 mins by TR-FRET assay (Rvb = 22 +/- 6 nM)	ChEMBL	396	5	1	2	5.7	O=[N+]([O-])CC(c1ccccc1F)c1c(-c2cccc(F)c2)[nH]c2c(F)cccc12	10.1021/acs.jmedchem.9b01142
	CHEMBL4519310	172472	0	None	2	2	Rat	8.0	pEC50	=	8	Functional	Positive allosteric modulatory activity at N-terminal GFP-tagged rat CB1R receptor expressed in HEK293 cells assessed as CP55940 EC50 for inhibition of forskolin-induced cAMP accumulation at 0.1 microM after 30 mins by TR-FRET assay (Rvb = 22 +/- 6 nM)Positive allosteric modulatory activity at N-terminal GFP-tagged rat CB1R receptor expressed in HEK293 cells assessed as CP55940 EC50 for inhibition of forskolin-induced cAMP accumulation at 0.1 microM after 30 mins by TR-FRET assay (Rvb = 22 +/- 6 nM)	ChEMBL	396	5	1	2	5.7	O=[N+]([O-])CC(c1ccccc1F)c1c(-c2cccc(F)c2)[nH]c2c(F)cccc12	10.1021/acs.jmedchem.9b01142
	155532408	171187	0	None	3	2	Rat	8.0	pEC50	=	8	Functional	Positive allosteric modulatory activity at N-terminal GFP-tagged rat CB1R receptor expressed in HEK293 cells assessed as CP55940 EC50 for inhibition of forskolin-induced cAMP accumulation at 0.3 microM after 30 mins by TR-FRET assay (Rvb = 22 +/- 6 nM)Positive allosteric modulatory activity at N-terminal GFP-tagged rat CB1R receptor expressed in HEK293 cells assessed as CP55940 EC50 for inhibition of forskolin-induced cAMP accumulation at 0.3 microM after 30 mins by TR-FRET assay (Rvb = 22 +/- 6 nM)	ChEMBL	396	5	1	2	5.7	O=[N+]([O-])CC(c1ccccc1F)c1c(-c2cccc(F)c2)[nH]c2cc(F)ccc12	10.1021/acs.jmedchem.9b01142
	CHEMBL4467516	171187	0	None	3	2	Rat	8.0	pEC50	=	8	Functional	Positive allosteric modulatory activity at N-terminal GFP-tagged rat CB1R receptor expressed in HEK293 cells assessed as CP55940 EC50 for inhibition of forskolin-induced cAMP accumulation at 0.3 microM after 30 mins by TR-FRET assay (Rvb = 22 +/- 6 nM)Positive allosteric modulatory activity at N-terminal GFP-tagged rat CB1R receptor expressed in HEK293 cells assessed as CP55940 EC50 for inhibition of forskolin-induced cAMP accumulation at 0.3 microM after 30 mins by TR-FRET assay (Rvb = 22 +/- 6 nM)	ChEMBL	396	5	1	2	5.7	O=[N+]([O-])CC(c1ccccc1F)c1c(-c2cccc(F)c2)[nH]c2cc(F)ccc12	10.1021/acs.jmedchem.9b01142
	118324097	145087	0	None	5	2	Human	8.0	pEC50	=	8	Functional	cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.	ChEMBL	687	6	2	4	7.5	O=c1cc(NC2CCN(S(=O)(=O)C(F)(F)F)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)cc(Br)c2[nH]1	nan
	CHEMBL3915692	145087	0	None	5	2	Human	8.0	pEC50	=	8	Functional	cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.	ChEMBL	687	6	2	4	7.5	O=c1cc(NC2CCN(S(=O)(=O)C(F)(F)F)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)cc(Br)c2[nH]1	nan
	118329970	148660	0	None	83	2	Human	8.0	pEC50	=	8	Functional	cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.	ChEMBL	619	6	2	6	5.8	O=c1cc(NC2CCN(S(=O)(=O)C(F)(F)F)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc4c(c3)OCO4)ccc2[nH]1	nan
	CHEMBL3943971	148660	0	None	83	2	Human	8.0	pEC50	=	8	Functional	cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.	ChEMBL	619	6	2	6	5.8	O=c1cc(NC2CCN(S(=O)(=O)C(F)(F)F)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc4c(c3)OCO4)ccc2[nH]1	nan
	118329975	151345	0	None	416	2	Human	8.0	pEC50	=	8	Functional	cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.	ChEMBL	587	6	2	3	7.4	O=C(CC(F)(F)F)N1CCC(Nc2cc(=O)[nH]c3ccc(C(c4ccc(Cl)cc4)c4ccc(Cl)cc4)cc23)CC1	nan
	CHEMBL3965825	151345	0	None	416	2	Human	8.0	pEC50	=	8	Functional	cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.	ChEMBL	587	6	2	3	7.4	O=C(CC(F)(F)F)N1CCC(Nc2cc(=O)[nH]c3ccc(C(c4ccc(Cl)cc4)c4ccc(Cl)cc4)cc23)CC1	nan
	118329979	153374	0	None	-	1	Human	8.0	pEC50	=	8	Functional	cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.	ChEMBL	522	5	2	2	8.6	O=c1cc(Nc2ccc(F)c(Cl)c2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)ccc2[nH]1	nan
	CHEMBL3983340	153374	0	None	-	1	Human	8.0	pEC50	=	8	Functional	cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.	ChEMBL	522	5	2	2	8.6	O=c1cc(Nc2ccc(F)c(Cl)c2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)ccc2[nH]1	nan
	104850	3266	93	None	1	6	Human	8.0	pEC50	=	8	Functional	Activity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assayActivity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assay	ChEMBL	462	4	1	4	5.9	Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1	10.1021/jm0503906
	4150	3266	93	None	1	6	Human	8.0	pEC50	=	8	Functional	Activity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assayActivity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assay	ChEMBL	462	4	1	4	5.9	Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1	10.1021/jm0503906
	743	3266	93	None	1	6	Human	8.0	pEC50	=	8	Functional	Activity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assayActivity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assay	ChEMBL	462	4	1	4	5.9	Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1	10.1021/jm0503906
	CHEMBL111	3266	93	None	1	6	Human	8.0	pEC50	=	8	Functional	Activity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assayActivity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assay	ChEMBL	462	4	1	4	5.9	Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1	10.1021/jm0503906
	DB06155	3266	93	None	1	6	Human	8.0	pEC50	=	8	Functional	Activity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assayActivity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assay	ChEMBL	462	4	1	4	5.9	Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1	10.1021/jm0503906
	104850	3266	93	None	1	6	Human	8.0	pEC50	=	8	Functional	Potency at human CB1 receptor in a [35S]GTP-gamma-S functional assayPotency at human CB1 receptor in a [35S]GTP-gamma-S functional assay	ChEMBL	462	4	1	4	5.9	Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1	10.1021/jm050484f
	4150	3266	93	None	1	6	Human	8.0	pEC50	=	8	Functional	Potency at human CB1 receptor in a [35S]GTP-gamma-S functional assayPotency at human CB1 receptor in a [35S]GTP-gamma-S functional assay	ChEMBL	462	4	1	4	5.9	Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1	10.1021/jm050484f
	743	3266	93	None	1	6	Human	8.0	pEC50	=	8	Functional	Potency at human CB1 receptor in a [35S]GTP-gamma-S functional assayPotency at human CB1 receptor in a [35S]GTP-gamma-S functional assay	ChEMBL	462	4	1	4	5.9	Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1	10.1021/jm050484f
	CHEMBL111	3266	93	None	1	6	Human	8.0	pEC50	=	8	Functional	Potency at human CB1 receptor in a [35S]GTP-gamma-S functional assayPotency at human CB1 receptor in a [35S]GTP-gamma-S functional assay	ChEMBL	462	4	1	4	5.9	Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1	10.1021/jm050484f
	DB06155	3266	93	None	1	6	Human	8.0	pEC50	=	8	Functional	Potency at human CB1 receptor in a [35S]GTP-gamma-S functional assayPotency at human CB1 receptor in a [35S]GTP-gamma-S functional assay	ChEMBL	462	4	1	4	5.9	Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1	10.1021/jm050484f
	104895	1157	23	None	-9	9	Human	8.0	pEC50	=	8.0	Functional	Inverse agonist activity at human recombinant CB1 receptor expressed CHO cells membrane by [35S]GTPgamma binding assayInverse agonist activity at human recombinant CB1 receptor expressed CHO cells membrane by [35S]GTPgamma binding assay	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1021/jm801353p
	730	1157	23	None	-9	9	Human	8.0	pEC50	=	8.0	Functional	Inverse agonist activity at human recombinant CB1 receptor expressed CHO cells membrane by [35S]GTPgamma binding assayInverse agonist activity at human recombinant CB1 receptor expressed CHO cells membrane by [35S]GTPgamma binding assay	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1021/jm801353p
	734	1157	23	None	-9	9	Human	8.0	pEC50	=	8.0	Functional	Inverse agonist activity at human recombinant CB1 receptor expressed CHO cells membrane by [35S]GTPgamma binding assayInverse agonist activity at human recombinant CB1 receptor expressed CHO cells membrane by [35S]GTPgamma binding assay	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1021/jm801353p
	CHEMBL559612	1157	23	None	-9	9	Human	8.0	pEC50	=	8.0	Functional	Inverse agonist activity at human recombinant CB1 receptor expressed CHO cells membrane by [35S]GTPgamma binding assayInverse agonist activity at human recombinant CB1 receptor expressed CHO cells membrane by [35S]GTPgamma binding assay	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1021/jm801353p
	145970762	164228	0	None	-	1	Rat	8.0	pEC50	=	8.0	Functional	Agonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 minsAgonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins	ChEMBL	355	15	1	1	6.1	C#CCNC(=O)CCC/C=C\C/C=C\C/C=C\[C@@H](C)/C=C\CCCCC	10.1021/acs.jmedchem.8b00611
	CHEMBL4218304	164228	0	None	-	1	Rat	8.0	pEC50	=	8.0	Functional	Agonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 minsAgonist activity at rat CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins	ChEMBL	355	15	1	1	6.1	C#CCNC(=O)CCC/C=C\C/C=C\C/C=C\[C@@H](C)/C=C\CCCCC	10.1021/acs.jmedchem.8b00611
	118323946	142439	0	None	371	2	Human	8.0	pEC50	=	8.0	Functional	Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assayInverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assay	ChEMBL	555	6	2	5	6.9	O=c1cc(NC2CCN(c3ncccn3)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)ccc2[nH]1	10.1021/acs.jmedchem.8b01467
	CHEMBL3894411	142439	0	None	371	2	Human	8.0	pEC50	=	8.0	Functional	Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assayInverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assay	ChEMBL	555	6	2	5	6.9	O=c1cc(NC2CCN(c3ncccn3)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)ccc2[nH]1	10.1021/acs.jmedchem.8b01467
	118324060	145972	0	None	602	2	Human	8.0	pEC50	=	8.0	Functional	Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assayInverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assay	ChEMBL	610	6	2	5	6.1	O=c1cc(NC2CCN(S(=O)(=O)C(F)(F)F)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)nc3)ccc2[nH]1	10.1021/acs.jmedchem.8b01467
	CHEMBL3922599	145972	0	None	602	2	Human	8.0	pEC50	=	8.0	Functional	Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assayInverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assay	ChEMBL	610	6	2	5	6.1	O=c1cc(NC2CCN(S(=O)(=O)C(F)(F)F)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)nc3)ccc2[nH]1	10.1021/acs.jmedchem.8b01467
	56642428	64933	0	None	-	1	Human	7.0	pEC50	=	7	Functional	Agonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid releaseAgonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid release	ChEMBL	342	6	0	3	5.6	CCCCCn1cc(C(=O)c2cccc3ccccc23)c2ccncc21	10.1016/j.ejmech.2011.08.021
	CHEMBL1828632	64933	0	None	-	1	Human	7.0	pEC50	=	7	Functional	Agonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid releaseAgonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid release	ChEMBL	342	6	0	3	5.6	CCCCCn1cc(C(=O)c2cccc3ccccc23)c2ccncc21	10.1016/j.ejmech.2011.08.021
	155535617	171490	1	None	-3	2	Human	7.0	pEC50	=	7	Functional	Agonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assayAgonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assay	ChEMBL	330	8	2	4	2.5	CCCCCn1cc(C(=O)N[C@H](C(N)=O)C(C)C)c2cccnc21	10.1039/d1md00242b
	CHEMBL4472094	171490	1	None	-3	2	Human	7.0	pEC50	=	7	Functional	Agonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assayAgonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assay	ChEMBL	330	8	2	4	2.5	CCCCCn1cc(C(=O)N[C@H](C(N)=O)C(C)C)c2cccnc21	10.1039/d1md00242b
	52944884	18806	0	None	-	1	Human	7.0	pEC50	=	7	Functional	Agonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assay	ChEMBL	409	4	0	4	4.5	COc1cccc2c(C(=O)N3CCN4CCCC[C@@H]4C3)cn(CC3CCCCC3)c12	10.1016/j.bmcl.2010.10.061
	CHEMBL1288054	18806	0	None	-	1	Human	7.0	pEC50	=	7	Functional	Agonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assay	ChEMBL	409	4	0	4	4.5	COc1cccc2c(C(=O)N3CCN4CCCC[C@@H]4C3)cn(CC3CCCCC3)c12	10.1016/j.bmcl.2010.10.061
	52943703	18813	0	None	-	1	Human	7.0	pEC50	=	7	Functional	Agonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assay	ChEMBL	409	4	0	4	4.5	COc1cccc2c(C(=O)N3C[C@@H]4CCCN4C[C@@H]3C)cn(CC3CCCCC3)c12	10.1016/j.bmcl.2010.10.061
	CHEMBL1288114	18813	0	None	-	1	Human	7.0	pEC50	=	7	Functional	Agonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assay	ChEMBL	409	4	0	4	4.5	COc1cccc2c(C(=O)N3C[C@@H]4CCCN4C[C@@H]3C)cn(CC3CCCCC3)c12	10.1016/j.bmcl.2010.10.061
	52944916	18821	0	None	-	1	Human	7.0	pEC50	=	7	Functional	Agonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assay	ChEMBL	423	4	0	4	4.9	COc1cccc2c(C(=O)N3C[C@@H]4CCCN4CC3(C)C)cn(CC3CCCCC3)c12	10.1016/j.bmcl.2010.10.061
	CHEMBL1288176	18821	0	None	-	1	Human	7.0	pEC50	=	7	Functional	Agonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assay	ChEMBL	423	4	0	4	4.9	COc1cccc2c(C(=O)N3C[C@@H]4CCCN4CC3(C)C)cn(CC3CCCCC3)c12	10.1016/j.bmcl.2010.10.061
	49862566	14915	0	None	-	1	Human	7.0	pEC50	=	7	Functional	Agonist activity at human cannabinoid CB1 receptor expressed in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human cannabinoid CB1 receptor expressed in CHO cells after 5 hrs by luciferase reporter gene assay	ChEMBL	367	2	0	4	3.5	CN1CCN(C(=O)c2cn3c4c(cccc24)OC[C@H]3C2CCCCC2)CC1	10.1016/j.bmcl.2010.06.067
	CHEMBL1209576	14915	0	None	-	1	Human	7.0	pEC50	=	7	Functional	Agonist activity at human cannabinoid CB1 receptor expressed in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human cannabinoid CB1 receptor expressed in CHO cells after 5 hrs by luciferase reporter gene assay	ChEMBL	367	2	0	4	3.5	CN1CCN(C(=O)c2cn3c4c(cccc24)OC[C@H]3C2CCCCC2)CC1	10.1016/j.bmcl.2010.06.067
	53326154	57929	0	None	-	1	Human	7.0	pEC50	=	7	Functional	Agonist activity at human cannabinoid CB1 receptor expressed in CHO cells by luciferase reporter gene assayAgonist activity at human cannabinoid CB1 receptor expressed in CHO cells by luciferase reporter gene assay	ChEMBL	400	5	0	6	4.4	Clc1cccc2c(-c3noc(CN4CCCC4)n3)cn(CC3CCOCC3)c12	10.1016/j.bmcl.2011.01.082
	CHEMBL1682271	57929	0	None	-	1	Human	7.0	pEC50	=	7	Functional	Agonist activity at human cannabinoid CB1 receptor expressed in CHO cells by luciferase reporter gene assayAgonist activity at human cannabinoid CB1 receptor expressed in CHO cells by luciferase reporter gene assay	ChEMBL	400	5	0	6	4.4	Clc1cccc2c(-c3noc(CN4CCCC4)n3)cn(CC3CCOCC3)c12	10.1016/j.bmcl.2011.01.082
	24863396	15821	0	None	-	1	Human	7.0	pEC50	=	7	Functional	Agonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release assayAgonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release assay	ChEMBL	399	6	1	2	5.6	CCCCC1=NN(C(=O)NC(C)(C)c2ccc(F)cc2)CC1c1cccc(F)c1	10.1016/j.bmcl.2010.07.056
	CHEMBL1223590	15821	0	None	-	1	Human	7.0	pEC50	=	7	Functional	Agonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release assayAgonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release assay	ChEMBL	399	6	1	2	5.6	CCCCC1=NN(C(=O)NC(C)(C)c2ccc(F)cc2)CC1c1cccc(F)c1	10.1016/j.bmcl.2010.07.056
	104895	1157	23	None	-22	9	Rat	7.0	pEC50	=	7	Functional	Displacement of [35S]GTP-gamma-S from rat cerebellar CB1 receptorDisplacement of [35S]GTP-gamma-S from rat cerebellar CB1 receptor	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1021/jm0505157
	730	1157	23	None	-22	9	Rat	7.0	pEC50	=	7	Functional	Displacement of [35S]GTP-gamma-S from rat cerebellar CB1 receptorDisplacement of [35S]GTP-gamma-S from rat cerebellar CB1 receptor	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1021/jm0505157
	734	1157	23	None	-22	9	Rat	7.0	pEC50	=	7	Functional	Displacement of [35S]GTP-gamma-S from rat cerebellar CB1 receptorDisplacement of [35S]GTP-gamma-S from rat cerebellar CB1 receptor	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1021/jm0505157
	CHEMBL559612	1157	23	None	-22	9	Rat	7.0	pEC50	=	7	Functional	Displacement of [35S]GTP-gamma-S from rat cerebellar CB1 receptorDisplacement of [35S]GTP-gamma-S from rat cerebellar CB1 receptor	ChEMBL	376	10	3	3	5.7	CCCCCCC(c1ccc(c(c1)O)[C@@H]1C[C@H](O)CC[C@H]1CCCO)(C)C	10.1021/jm0505157
	CHEMBL5092514	213589	0	None	-	1	Human	7.0	pEC50	=	7	Functional	Positive allosteric modulation of human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP production incubated for 30 mins in presence of forskolin by HitHunter chemiluminescence based assayPositive allosteric modulation of human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP production incubated for 30 mins in presence of forskolin by HitHunter chemiluminescence based assay	ChEMBL		None	None	None		O=[N+]([O-])CC(c1ccccc1)c1c(-c2ccoc2)[nH]c2ccccc12	10.1016/j.bmc.2021.116421
	118323987	149701	0	None	2	2	Human	7.0	pEC50	=	7	Functional	cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.	ChEMBL	623	7	1	5	7.5	COc1cc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)cc2c(NC3CCN(S(=O)(=O)C(F)(F)F)CC3)ccnc12	nan
	CHEMBL3952365	149701	0	None	2	2	Human	7.0	pEC50	=	7	Functional	cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.	ChEMBL	623	7	1	5	7.5	COc1cc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)cc2c(NC3CCN(S(=O)(=O)C(F)(F)F)CC3)ccnc12	nan
	162668450	182132	0	None	-10	2	Human	7.0	pEC50	=	7	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	295	6	2	4	2.5	CCCCn1nc(C(=O)NC(C)(C)CO)cc1C(C)(C)C	10.1021/acs.jmedchem.0c01023
	CHEMBL4789723	182132	0	None	-10	2	Human	7.0	pEC50	=	7	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	295	6	2	4	2.5	CCCCn1nc(C(=O)NC(C)(C)CO)cc1C(C)(C)C	10.1021/acs.jmedchem.0c01023
	70683294	73231	0	None	-	1	Human	6.0	pEC50	=	6	Functional	Agonist activity at CB1 receptorAgonist activity at CB1 receptor	ChEMBL	549	8	2	9	2.5	O=C(NCCO)C1CCN(Cc2nc(-c3cn(CC4CCS(=O)(=O)CC4)c4c(Cl)cccc34)no2)CC1	10.1016/j.bmcl.2012.02.048
	CHEMBL2017689	73231	0	None	-	1	Human	6.0	pEC50	=	6	Functional	Agonist activity at CB1 receptorAgonist activity at CB1 receptor	ChEMBL	549	8	2	9	2.5	O=C(NCCO)C1CCN(Cc2nc(-c3cn(CC4CCS(=O)(=O)CC4)c4c(Cl)cccc34)no2)CC1	10.1016/j.bmcl.2012.02.048
	71454145	83327	0	None	-70	2	Human	6.0	pEC50	=	6	Functional	Agonist activity at human CB1 receptor after 4 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor after 4 hrs by luciferase reporter gene assay	ChEMBL	456	3	1	4	4.9	O=C(Nc1sc2c(c1C(=O)N1CCCCC1)CCOC2)c1c(F)cccc1C(F)(F)F	10.1016/j.bmcl.2012.10.087
	CHEMBL2205617	83327	0	None	-70	2	Human	6.0	pEC50	=	6	Functional	Agonist activity at human CB1 receptor after 4 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor after 4 hrs by luciferase reporter gene assay	ChEMBL	456	3	1	4	4.9	O=C(Nc1sc2c(c1C(=O)N1CCCCC1)CCOC2)c1c(F)cccc1C(F)(F)F	10.1016/j.bmcl.2012.10.087
	52941290	54999	0	None	-	1	Human	6.0	pEC50	=	6	Functional	Agonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assay	ChEMBL	409	4	0	4	4.5	COc1cccc2c(C(=O)N3C[C@@H]4CCCN4C[C@H]3C)cn(CC3CCCCC3)c12	10.1016/j.bmcl.2010.10.061
	CHEMBL1288145	54999	0	None	-	1	Human	6.0	pEC50	=	6	Functional	Agonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assay	ChEMBL	409	4	0	4	4.5	COc1cccc2c(C(=O)N3C[C@@H]4CCCN4C[C@H]3C)cn(CC3CCCCC3)c12	10.1016/j.bmcl.2010.10.061
	CHEMBL1618454	54999	0	None	-	1	Human	6.0	pEC50	=	6	Functional	Agonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assay	ChEMBL	409	4	0	4	4.5	COc1cccc2c(C(=O)N3C[C@@H]4CCCN4C[C@H]3C)cn(CC3CCCCC3)c12	10.1016/j.bmcl.2010.10.061
	11510814	188511	0	None	20	2	Human	6.0	pEC50	=	6	Functional	Antagonist activity at human cannabinoid CB1 receptor expressed in CHOK1 cells assessed as cAMP activityAntagonist activity at human cannabinoid CB1 receptor expressed in CHOK1 cells assessed as cAMP activity	ChEMBL	454	4	1	5	5.6	Cc1c(C(=O)NN2CCCC2)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)s1	10.1016/j.bmcl.2009.03.046
	CHEMBL510262	188511	0	None	20	2	Human	6.0	pEC50	=	6	Functional	Antagonist activity at human cannabinoid CB1 receptor expressed in CHOK1 cells assessed as cAMP activityAntagonist activity at human cannabinoid CB1 receptor expressed in CHOK1 cells assessed as cAMP activity	ChEMBL	454	4	1	5	5.6	Cc1c(C(=O)NN2CCCC2)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)s1	10.1016/j.bmcl.2009.03.046
	118728139	117101	0	None	-707	2	Human	6.0	pEC50	=	6	Functional	Inhibition of human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsInhibition of human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins	ChEMBL	450	2	1	4	4.1	O=C(Nc1cc(C(F)(F)F)on1)N1CCCN(C(=O)c2ccc(C(F)(F)F)cc2)CC1	10.1016/j.bmcl.2014.12.033
	CHEMBL3400938	117101	0	None	-707	2	Human	6.0	pEC50	=	6	Functional	Inhibition of human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 minsInhibition of human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins	ChEMBL	450	2	1	4	4.1	O=C(Nc1cc(C(F)(F)F)on1)N1CCCN(C(=O)c2ccc(C(F)(F)F)cc2)CC1	10.1016/j.bmcl.2014.12.033
	5282280	54	38	None	-331	4	Rat	6.0	pEC50	=	6	Functional	Potency at CB1 receptor in rat brain by [35S]GTP-gamma-S binding assayPotency at CB1 receptor in rat brain by [35S]GTP-gamma-S binding assay	ChEMBL	378	17	2	4	5.0	CCCCC/C=C\C/C=C\C/C=C\C/C=C\CCCC(=O)OC(CO)CO	10.1016/j.bmcl.2006.01.101
	729	54	38	None	-331	4	Rat	6.0	pEC50	=	6	Functional	Potency at CB1 receptor in rat brain by [35S]GTP-gamma-S binding assayPotency at CB1 receptor in rat brain by [35S]GTP-gamma-S binding assay	ChEMBL	378	17	2	4	5.0	CCCCC/C=C\C/C=C\C/C=C\C/C=C\CCCC(=O)OC(CO)CO	10.1016/j.bmcl.2006.01.101
	CHEMBL122972	54	38	None	-331	4	Rat	6.0	pEC50	=	6	Functional	Potency at CB1 receptor in rat brain by [35S]GTP-gamma-S binding assayPotency at CB1 receptor in rat brain by [35S]GTP-gamma-S binding assay	ChEMBL	378	17	2	4	5.0	CCCCC/C=C\C/C=C\C/C=C\C/C=C\CCCC(=O)OC(CO)CO	10.1016/j.bmcl.2006.01.101
	141463776	161090	0	None	-63	2	Human	5.0	pEC50	=	5	Functional	Agonist activity at CB1 receptor (unknown origin) expressed in CHO cells assessed as induction of calcium mobilization by fluo-4 AM dye-based fluorescence assayAgonist activity at CB1 receptor (unknown origin) expressed in CHO cells assessed as induction of calcium mobilization by fluo-4 AM dye-based fluorescence assay	ChEMBL	370	7	2	4	4.5	CCCCNc1cc(C(C)C)c(C(=O)NC23CC4CC(CC(C4)C2)C3)nn1	10.1016/j.ejmech.2017.05.060
	CHEMBL4130290	161090	0	None	-63	2	Human	5.0	pEC50	=	5	Functional	Agonist activity at CB1 receptor (unknown origin) expressed in CHO cells assessed as induction of calcium mobilization by fluo-4 AM dye-based fluorescence assayAgonist activity at CB1 receptor (unknown origin) expressed in CHO cells assessed as induction of calcium mobilization by fluo-4 AM dye-based fluorescence assay	ChEMBL	370	7	2	4	4.5	CCCCNc1cc(C(C)C)c(C(=O)NC23CC4CC(CC(C4)C2)C3)nn1	10.1016/j.ejmech.2017.05.060
	118722160	115618	0	None	-478	2	Human	5.0	pEC50	=	5	Functional	Agonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production	ChEMBL	464	5	2	7	1.7	CC(C)(C)Cc1nc2cc(S(=O)(=O)C3CN(C(N)=O)C3)ccc2n1CC1(O)CCOCC1	10.1016/j.bmcl.2014.11.062
	CHEMBL3357387	115618	0	None	-478	2	Human	5.0	pEC50	=	5	Functional	Agonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production	ChEMBL	464	5	2	7	1.7	CC(C)(C)Cc1nc2cc(S(=O)(=O)C3CN(C(N)=O)C3)ccc2n1CC1(O)CCOCC1	10.1016/j.bmcl.2014.11.062
	45486215	195930	0	None	-125	2	Human	5.0	pEC50	=	5	Functional	Agonist activity at human CB1 receptor expressed in yeast cellsAgonist activity at human CB1 receptor expressed in yeast cells	ChEMBL	433	3	0	4	4.9	O=C(c1cc(-c2cccc(Cl)c2Cl)cnc1N1CCCCCC1)N1CCOCC1	10.1016/j.bmcl.2009.10.041
	CHEMBL570683	195930	0	None	-125	2	Human	5.0	pEC50	=	5	Functional	Agonist activity at human CB1 receptor expressed in yeast cellsAgonist activity at human CB1 receptor expressed in yeast cells	ChEMBL	433	3	0	4	4.9	O=C(c1cc(-c2cccc(Cl)c2Cl)cnc1N1CCCCCC1)N1CCOCC1	10.1016/j.bmcl.2009.10.041
	45486166	196624	0	None	-251	2	Human	5.0	pEC50	=	5	Functional	Agonist activity at human CB1 receptor expressed in yeast cellsAgonist activity at human CB1 receptor expressed in yeast cells	ChEMBL	320	2	0	2	5.4	Clc1cccc(-c2ccc(N3CCCCCC3)nc2)c1Cl	10.1016/j.bmcl.2009.10.041
	CHEMBL576079	196624	0	None	-251	2	Human	5.0	pEC50	=	5	Functional	Agonist activity at human CB1 receptor expressed in yeast cellsAgonist activity at human CB1 receptor expressed in yeast cells	ChEMBL	320	2	0	2	5.4	Clc1cccc(-c2ccc(N3CCCCCC3)nc2)c1Cl	10.1016/j.bmcl.2009.10.041
	45375898	196625	0	None	-100	2	Human	5.0	pEC50	=	5	Functional	Agonist activity at human CB1 receptor expressed in yeast cellsAgonist activity at human CB1 receptor expressed in yeast cells	ChEMBL	345	2	0	3	5.3	N#Cc1cc(N2CCCCCC2)ncc1-c1cccc(Cl)c1Cl	10.1016/j.bmcl.2009.10.041
	CHEMBL576087	196625	0	None	-100	2	Human	5.0	pEC50	=	5	Functional	Agonist activity at human CB1 receptor expressed in yeast cellsAgonist activity at human CB1 receptor expressed in yeast cells	ChEMBL	345	2	0	3	5.3	N#Cc1cc(N2CCCCCC2)ncc1-c1cccc(Cl)c1Cl	10.1016/j.bmcl.2009.10.041
	44475348	195338	0	None	-15	2	Human	5.0	pEC50	=	5	Functional	Agonist activity at human recombinant cannabinoid CB1 receptor expressed in MMY23 Saccharomyces cerevisiae assessed as degradation of FDGlu to fluorescein after 24 hrs by spectrofluorimetryAgonist activity at human recombinant cannabinoid CB1 receptor expressed in MMY23 Saccharomyces cerevisiae assessed as degradation of FDGlu to fluorescein after 24 hrs by spectrofluorimetry	ChEMBL	384	3	1	5	3.8	Cc1cn(C)c2c(Nc3cccc(Cl)c3)ncc(C(=O)N3CCOCC3)c12	10.1021/jm9009857
	CHEMBL567087	195338	0	None	-15	2	Human	5.0	pEC50	=	5	Functional	Agonist activity at human recombinant cannabinoid CB1 receptor expressed in MMY23 Saccharomyces cerevisiae assessed as degradation of FDGlu to fluorescein after 24 hrs by spectrofluorimetryAgonist activity at human recombinant cannabinoid CB1 receptor expressed in MMY23 Saccharomyces cerevisiae assessed as degradation of FDGlu to fluorescein after 24 hrs by spectrofluorimetry	ChEMBL	384	3	1	5	3.8	Cc1cn(C)c2c(Nc3cccc(Cl)c3)ncc(C(=O)N3CCOCC3)c12	10.1021/jm9009857
	11689242	195470	0	None	-912	2	Human	5.0	pEC50	=	5	Functional	Agonist activity at human recombinant cannabinoid CB1 receptor expressed in MMY23 Saccharomyces cerevisiae assessed as degradation of FDGlu to fluorescein after 24 hrs by spectrofluorimetryAgonist activity at human recombinant cannabinoid CB1 receptor expressed in MMY23 Saccharomyces cerevisiae assessed as degradation of FDGlu to fluorescein after 24 hrs by spectrofluorimetry	ChEMBL	370	3	2	4	3.7	Cc1c[nH]c2c(Nc3cccc(Cl)c3)ncc(C(=O)N3CCOCC3)c12	10.1021/jm9009857
	CHEMBL567911	195470	0	None	-912	2	Human	5.0	pEC50	=	5	Functional	Agonist activity at human recombinant cannabinoid CB1 receptor expressed in MMY23 Saccharomyces cerevisiae assessed as degradation of FDGlu to fluorescein after 24 hrs by spectrofluorimetryAgonist activity at human recombinant cannabinoid CB1 receptor expressed in MMY23 Saccharomyces cerevisiae assessed as degradation of FDGlu to fluorescein after 24 hrs by spectrofluorimetry	ChEMBL	370	3	2	4	3.7	Cc1c[nH]c2c(Nc3cccc(Cl)c3)ncc(C(=O)N3CCOCC3)c12	10.1021/jm9009857
	44410687	137829	0	None	-	1	Rat	5.0	pEC50	=	5	Functional	Potency at CB1 receptor in rat brain by [35S]GTP-gamma-S binding assayPotency at CB1 receptor in rat brain by [35S]GTP-gamma-S binding assay	ChEMBL	392	17	2	4	5.3	CCCCC/C=C\C/C=C\C/C=C\C/C=C\CC[C@@H](C)C(=O)OC(CO)CO	10.1016/j.bmcl.2006.01.101
	CHEMBL377180	137829	0	None	-	1	Rat	5.0	pEC50	=	5	Functional	Potency at CB1 receptor in rat brain by [35S]GTP-gamma-S binding assayPotency at CB1 receptor in rat brain by [35S]GTP-gamma-S binding assay	ChEMBL	392	17	2	4	5.3	CCCCC/C=C\C/C=C\C/C=C\C/C=C\CC[C@@H](C)C(=O)OC(CO)CO	10.1016/j.bmcl.2006.01.101
	71105652	150779	0	None	-776	2	Human	5.0	pEC50	=	5	Functional	cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.	ChEMBL	419	8	1	7	2.9	Cc1nc(C(NC(=O)c2ccc(N3CC(F)(F)C3)c(OCC3CC3)n2)C2CC2)no1	nan
	CHEMBL3960990	150779	0	None	-776	2	Human	5.0	pEC50	=	5	Functional	cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.	ChEMBL	419	8	1	7	2.9	Cc1nc(C(NC(=O)c2ccc(N3CC(F)(F)C3)c(OCC3CC3)n2)C2CC2)no1	nan
	162643760	181100	0	None	1	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	315	4	2	4	2.7	CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccccc2)n1	10.1021/acs.jmedchem.0c01023
	CHEMBL4776615	181100	0	None	1	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	315	4	2	4	2.7	CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccccc2)n1	10.1021/acs.jmedchem.0c01023
	162644317	181184	0	None	1	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	361	7	1	3	5.0	CCCCCn1nc(C(=O)NCc2ccc(Cl)cc2)cc1C(C)(C)C	10.1021/acs.jmedchem.0c01023
	CHEMBL4777738	181184	0	None	1	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	361	7	1	3	5.0	CCCCCn1nc(C(=O)NCc2ccc(Cl)cc2)cc1C(C)(C)C	10.1021/acs.jmedchem.0c01023
	162663645	181450	0	None	-144	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	333	4	2	4	2.8	CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccc(F)cc2)n1	10.1021/acs.jmedchem.0c01023
	CHEMBL4781040	181450	0	None	-144	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	333	4	2	4	2.8	CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccc(F)cc2)n1	10.1021/acs.jmedchem.0c01023
	162664518	181490	0	None	1	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	317	4	2	6	1.5	CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ncccn2)n1	10.1021/acs.jmedchem.0c01023
	CHEMBL4781576	181490	0	None	1	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	317	4	2	6	1.5	CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ncccn2)n1	10.1021/acs.jmedchem.0c01023
	162664931	181507	0	None	-57	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	351	4	2	4	2.9	CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccc(F)cc2F)n1	10.1021/acs.jmedchem.0c01023
	CHEMBL4781800	181507	0	None	-57	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	351	4	2	4	2.9	CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccc(F)cc2F)n1	10.1021/acs.jmedchem.0c01023
	162665007	181529	0	None	1	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	347	6	1	3	5.3	CCCCCn1nc(C(C)(C)C)cc1C(=O)Nc1ccc(Cl)cc1	10.1021/acs.jmedchem.0c01023
	CHEMBL4782074	181529	0	None	1	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	347	6	1	3	5.3	CCCCCn1nc(C(C)(C)C)cc1C(=O)Nc1ccc(Cl)cc1	10.1021/acs.jmedchem.0c01023
	162666213	181693	0	None	-512	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	329	4	2	4	3.0	Cc1ccc(-n2nc(C(=O)NC(C)(C)CO)cc2C(C)(C)C)cc1	10.1021/acs.jmedchem.0c01023
	CHEMBL4783974	181693	0	None	-512	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	329	4	2	4	3.0	Cc1ccc(-n2nc(C(=O)NC(C)(C)CO)cc2C(C)(C)C)cc1	10.1021/acs.jmedchem.0c01023
	162666580	181742	0	None	1	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	345	5	2	5	2.7	COc1ccc(-n2nc(C(=O)NC(C)(C)CO)cc2C(C)(C)C)cc1	10.1021/acs.jmedchem.0c01023
	CHEMBL4784418	181742	0	None	1	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	345	5	2	5	2.7	COc1ccc(-n2nc(C(=O)NC(C)(C)CO)cc2C(C)(C)C)cc1	10.1021/acs.jmedchem.0c01023
	162666392	181792	0	None	1	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	361	7	1	3	5.0	CCCCCn1nc(C(C)(C)C)cc1C(=O)NCc1ccc(Cl)cc1	10.1021/acs.jmedchem.0c01023
	CHEMBL4785185	181792	0	None	1	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	361	7	1	3	5.0	CCCCCn1nc(C(C)(C)C)cc1C(=O)NCc1ccc(Cl)cc1	10.1021/acs.jmedchem.0c01023
	162665956	181797	0	None	1	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	371	6	1	3	5.1	CCCCCn1nc(C(C)(C)C)cc1C(=O)NC12CC3CC(CC(C3)C1)C2	10.1021/acs.jmedchem.0c01023
	CHEMBL4785295	181797	0	None	1	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	371	6	1	3	5.1	CCCCCn1nc(C(C)(C)C)cc1C(=O)NC12CC3CC(CC(C3)C1)C2	10.1021/acs.jmedchem.0c01023
	162667222	181869	0	None	-489	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	349	4	2	4	3.3	CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccc(Cl)cc2)n1	10.1021/acs.jmedchem.0c01023
	CHEMBL4786352	181869	0	None	-489	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	349	4	2	4	3.3	CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccc(Cl)cc2)n1	10.1021/acs.jmedchem.0c01023
	162669636	181974	0	None	-549	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	299	6	2	4	2.0	CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(CCCF)n1	10.1021/acs.jmedchem.0c01023
	CHEMBL4787759	181974	0	None	-549	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	299	6	2	4	2.0	CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(CCCF)n1	10.1021/acs.jmedchem.0c01023
	162623028	182032	0	None	1	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	383	4	2	4	3.7	CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccc(C(F)(F)F)cc2)n1	10.1021/acs.jmedchem.0c01023
	CHEMBL4788470	182032	0	None	1	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	383	4	2	4	3.7	CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccc(C(F)(F)F)cc2)n1	10.1021/acs.jmedchem.0c01023
	162668533	182053	0	None	-33	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	365	8	2	4	3.5	CCCCCn1nc(C(=O)NC(C)(C)CO)cc1-c1ccc(F)cc1F	10.1021/acs.jmedchem.0c01023
	CHEMBL4788749	182053	0	None	-33	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	365	8	2	4	3.5	CCCCCn1nc(C(=O)NC(C)(C)CO)cc1-c1ccc(F)cc1F	10.1021/acs.jmedchem.0c01023
	162668965	182188	0	None	1	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	335	8	2	4	3.6	CCCCCn1nc(C(=O)NC(C)(C)CO)cc1C1CCCCC1	10.1021/acs.jmedchem.0c01023
	CHEMBL4790368	182188	0	None	1	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	335	8	2	4	3.6	CCCCCn1nc(C(=O)NC(C)(C)CO)cc1C1CCCCC1	10.1021/acs.jmedchem.0c01023
	162671037	182210	0	None	1	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	316	4	2	5	2.1	CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2cccnc2)n1	10.1021/acs.jmedchem.0c01023
	CHEMBL4790704	182210	0	None	1	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	316	4	2	5	2.1	CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2cccnc2)n1	10.1021/acs.jmedchem.0c01023
	162671764	182230	0	None	1	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	387	6	2	4	4.2	CCCCCn1nc(C(C)(C)C)cc1C(=O)NC12CC3CC(CC(O)(C3)C1)C2	10.1021/acs.jmedchem.0c01023
	CHEMBL4791040	182230	0	None	1	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	387	6	2	4	4.2	CCCCCn1nc(C(C)(C)C)cc1C(=O)NC12CC3CC(CC(O)(C3)C1)C2	10.1021/acs.jmedchem.0c01023
	162671765	182238	0	None	1	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	293	8	2	4	2.5	CCCCCn1nc(C(=O)NC(C)(C)CO)cc1C1CC1	10.1021/acs.jmedchem.0c01023
	CHEMBL4791212	182238	0	None	1	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	293	8	2	4	2.5	CCCCCn1nc(C(=O)NC(C)(C)CO)cc1C1CC1	10.1021/acs.jmedchem.0c01023
	162671780	182248	0	None	-13	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	350	4	2	5	2.7	CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccc(Cl)cn2)n1	10.1021/acs.jmedchem.0c01023
	CHEMBL4791388	182248	0	None	-13	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	350	4	2	5	2.7	CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccc(Cl)cn2)n1	10.1021/acs.jmedchem.0c01023
	141747275	182301	0	None	-331	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	293	5	1	3	3.9	CCCCCn1nc(C(C)(C)C)cc1C(=O)NC(C)(C)C	10.1021/acs.jmedchem.0c01023
	CHEMBL4792134	182301	0	None	-331	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	293	5	1	3	3.9	CCCCCn1nc(C(C)(C)C)cc1C(=O)NC(C)(C)C	10.1021/acs.jmedchem.0c01023
	162671856	182380	0	None	-316	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	309	7	2	4	2.9	CCCCCn1nc(C(C)(C)C)cc1C(=O)NC(C)(C)CO	10.1021/acs.jmedchem.0c01023
	CHEMBL4793164	182380	0	None	-316	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	309	7	2	4	2.9	CCCCCn1nc(C(C)(C)C)cc1C(=O)NC(C)(C)CO	10.1021/acs.jmedchem.0c01023
	162672350	182446	0	None	-741	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	334	4	2	5	2.2	CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccc(F)cn2)n1	10.1021/acs.jmedchem.0c01023
	CHEMBL4793976	182446	0	None	-741	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	334	4	2	5	2.2	CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccc(F)cn2)n1	10.1021/acs.jmedchem.0c01023
	162673695	182580	0	None	-42	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	347	6	1	3	5.3	CCCCCn1nc(C(=O)Nc2ccc(Cl)cc2)cc1C(C)(C)C	10.1021/acs.jmedchem.0c01023
	CHEMBL4795529	182580	0	None	-42	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	347	6	1	3	5.3	CCCCCn1nc(C(=O)Nc2ccc(Cl)cc2)cc1C(C)(C)C	10.1021/acs.jmedchem.0c01023
	162623029	182594	0	None	1	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	399	5	2	5	3.6	CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccc(OC(F)(F)F)cc2)n1	10.1021/acs.jmedchem.0c01023
	CHEMBL4795667	182594	0	None	1	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	399	5	2	5	3.6	CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccc(OC(F)(F)F)cc2)n1	10.1021/acs.jmedchem.0c01023
	162675834	182673	0	None	-25	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	316	4	2	5	2.1	CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccccn2)n1	10.1021/acs.jmedchem.0c01023
	CHEMBL4796542	182673	0	None	-25	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	316	4	2	5	2.1	CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ccccn2)n1	10.1021/acs.jmedchem.0c01023
	162676075	182708	0	None	1	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	418	4	2	5	3.7	CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ncc(C(F)(F)F)cc2Cl)n1	10.1021/acs.jmedchem.0c01023
	CHEMBL4797039	182708	0	None	1	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	418	4	2	5	3.7	CC(C)(CO)NC(=O)c1cc(C(C)(C)C)n(-c2ncc(C(F)(F)F)cc2Cl)n1	10.1021/acs.jmedchem.0c01023
	162676388	182787	0	None	-478	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	281	5	2	4	2.1	CCCn1nc(C(=O)NC(C)(C)CO)cc1C(C)(C)C	10.1021/acs.jmedchem.0c01023
	CHEMBL4797941	182787	0	None	-478	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	281	5	2	4	2.1	CCCn1nc(C(=O)NC(C)(C)CO)cc1C(C)(C)C	10.1021/acs.jmedchem.0c01023
	162675814	182855	0	None	1	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	297	6	2	5	1.3	COCCn1nc(C(=O)NC(C)(C)CO)cc1C(C)(C)C	10.1021/acs.jmedchem.0c01023
	CHEMBL4798902	182855	0	None	1	2	Human	4.0	pEC50	=	4	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	297	6	2	5	1.3	COCCn1nc(C(=O)NC(C)(C)CO)cc1C(C)(C)C	10.1021/acs.jmedchem.0c01023
	57606070	74213	0	None	-	1	Human	7.0	pEC50	=	7	Functional	Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma bindingAgonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma binding	ChEMBL	455	7	2	5	2.7	CNC(=O)CC[C@@H](CO)N(C)C(=O)c1ccc2c(c1)c1c(n2C)CC[C@@H](C2CCOCC2)C1	10.1016/j.bmcl.2012.04.128
	CHEMBL2029737	74213	0	None	-	1	Human	7.0	pEC50	=	7	Functional	Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma bindingAgonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma binding	ChEMBL	455	7	2	5	2.7	CNC(=O)CC[C@@H](CO)N(C)C(=O)c1ccc2c(c1)c1c(n2C)CC[C@@H](C2CCOCC2)C1	10.1016/j.bmcl.2012.04.128
	155535617	171490	1	None	-3	2	Human	7.0	pEC50	=	7	Functional	Agonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assayAgonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assay	ChEMBL	330	8	2	4	2.5	CCCCCn1cc(C(=O)N[C@H](C(N)=O)C(C)C)c2cccnc21	10.1039/d1md00242b
	CHEMBL4472094	171490	1	None	-3	2	Human	7.0	pEC50	=	7	Functional	Agonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assayAgonist activity at human CB1 receptor expressed in mouse AtT20 cells incubated for 60 mins by FLIPR membrane potential assay	ChEMBL	330	8	2	4	2.5	CCCCCn1cc(C(=O)N[C@H](C(N)=O)C(C)C)c2cccnc21	10.1039/d1md00242b
	60155823	76628	0	None	-	1	Human	6.0	pEC50	=	6	Functional	Activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 5 mins in presence of CP55,940 by cAMP BRET assayActivity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 5 mins in presence of CP55,940 by cAMP BRET assay	ChEMBL	340	5	2	1	4.7	CCc1c(C(=O)NCCc2ccc(C)cc2)[nH]c2ccc(Cl)cc12	10.1021/acs.jmedchem.5b00579
	CHEMBL2071064	76628	0	None	-	1	Human	6.0	pEC50	=	6	Functional	Activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 5 mins in presence of CP55,940 by cAMP BRET assayActivity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 5 mins in presence of CP55,940 by cAMP BRET assay	ChEMBL	340	5	2	1	4.7	CCc1c(C(=O)NCCc2ccc(C)cc2)[nH]c2ccc(Cl)cc12	10.1021/acs.jmedchem.5b00579
	164624856	184946	0	None	-5	2	Human	6.0	pEC50	=	6	Functional	Agonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding assayAgonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding assay	ChEMBL	337	7	0	4	4.5	CCCCCc1cc(OC)c2cc(Cc3ccccn3)c(=O)oc2c1	10.1016/j.ejmech.2021.113354
	CHEMBL4862930	184946	0	None	-5	2	Human	6.0	pEC50	=	6	Functional	Agonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding assayAgonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding assay	ChEMBL	337	7	0	4	4.5	CCCCCc1cc(OC)c2cc(Cc3ccccn3)c(=O)oc2c1	10.1016/j.ejmech.2021.113354
	67953300	115180	0	None	-1288	2	Human	5.0	pEC50	=	5	Functional	Agonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 30 minsAgonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins	ChEMBL	291	4	1	4	2.8	CC(C)(C)c1cc(NC(=O)[C@@H]2CCCN2CC2CC2)no1	10.1016/j.bmcl.2014.12.019
	CHEMBL3353867	115180	0	None	-1288	2	Human	5.0	pEC50	=	5	Functional	Agonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 30 minsAgonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins	ChEMBL	291	4	1	4	2.8	CC(C)(C)c1cc(NC(=O)[C@@H]2CCCN2CC2CC2)no1	10.1016/j.bmcl.2014.12.019
	118324104	149881	0	None	-	1	Human	6.0	pEC50	=	6	Functional	cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.	ChEMBL	572	10	3	4	8.0	O=C(O)CCCOc1ccc(Nc2cc(=O)[nH]c3ccc(C(c4ccc(Cl)cc4)c4ccc(Cl)cc4)cc23)cc1	nan
	CHEMBL3953885	149881	0	None	-	1	Human	6.0	pEC50	=	6	Functional	cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.	ChEMBL	572	10	3	4	8.0	O=C(O)CCCOc1ccc(Nc2cc(=O)[nH]c3ccc(C(c4ccc(Cl)cc4)c4ccc(Cl)cc4)cc23)cc1	nan
	118323970	146898	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.	ChEMBL	722	12	2	6	7.7	CC(=O)NCCCCOc1cc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)cc2c(NC3CCN(S(=O)(=O)C(F)(F)F)CC3)ccnc12	nan
	CHEMBL3930097	146898	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.	ChEMBL	722	12	2	6	7.7	CC(=O)NCCCCOc1cc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)cc2c(NC3CCN(S(=O)(=O)C(F)(F)F)CC3)ccnc12	nan
	71087679	159419	0	None	-25	2	Human	7.0	pEC50	=	7.0	Functional	cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.	ChEMBL	389	7	2	5	2.4	CNC(=O)[C@@H](NC(=O)c1ccc(C2CC2)c(OCC2CCCO2)n1)C(C)(C)C	nan
	CHEMBL4107610	159419	0	None	-25	2	Human	7.0	pEC50	=	7.0	Functional	cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.	ChEMBL	389	7	2	5	2.4	CNC(=O)[C@@H](NC(=O)c1ccc(C2CC2)c(OCC2CCCO2)n1)C(C)(C)C	nan
	57403187	70282	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgamma binding assayAgonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgamma binding assay	ChEMBL	427	5	0	3	5.3	C=CCn1c2c(c3cc(C(=O)N4CCC(C)CC4)ccc31)CN(Cc1ccccc1)CC2	10.1016/j.bmcl.2011.12.124
	CHEMBL1950331	70282	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgamma binding assayAgonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgamma binding assay	ChEMBL	427	5	0	3	5.3	C=CCn1c2c(c3cc(C(=O)N4CCC(C)CC4)ccc31)CN(Cc1ccccc1)CC2	10.1016/j.bmcl.2011.12.124
	11856745	70291	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgamma binding assayAgonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgamma binding assay	ChEMBL	423	4	0	4	4.5	CCCn1c2c(c3cc(C(=O)N4CCC(C)CC4)ccc31)CN(C1CCOCC1)CC2	10.1016/j.bmcl.2011.12.124
	CHEMBL1950341	70291	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgamma binding assayAgonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgamma binding assay	ChEMBL	423	4	0	4	4.5	CCCn1c2c(c3cc(C(=O)N4CCC(C)CC4)ccc31)CN(C1CCOCC1)CC2	10.1016/j.bmcl.2011.12.124
	118324125	143674	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.	ChEMBL	605	8	2	5	7.6	CC(C)(C)OC(=O)CCN1CCC(Nc2cc(=O)[nH]c3ccc(C(c4ccc(Cl)cc4)c4ccc(Cl)cc4)cc23)CC1	nan
	CHEMBL3904458	143674	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.	ChEMBL	605	8	2	5	7.6	CC(C)(C)OC(=O)CCN1CCC(Nc2cc(=O)[nH]c3ccc(C(c4ccc(Cl)cc4)c4ccc(Cl)cc4)cc23)CC1	nan
	162677250	182939	0	None	-2	2	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	319	6	1	3	4.4	CCCCCn1nc(C(=O)NC2CCCCC2)cc1C(C)(C)C	10.1021/acs.jmedchem.0c01023
	CHEMBL4799912	182939	0	None	-2	2	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assayAgonist activity at human CB1 receptor expressing CHO cells co-expressing Galpha16 by calcium mobilization assay	ChEMBL	319	6	1	3	4.4	CCCCCn1nc(C(=O)NC2CCCCC2)cc1C(C)(C)C	10.1021/acs.jmedchem.0c01023
	10141893	373	48	None	-72	3	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production	ChEMBL	503	5	0	5	4.9	CN1CCCCC1Cn1cc(c2c1cccc2)C(=O)c1cc(ccc1I)N(=O)=O	10.1016/j.bmcl.2014.11.003
	3316	373	48	None	-72	3	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production	ChEMBL	503	5	0	5	4.9	CN1CCCCC1Cn1cc(c2c1cccc2)C(=O)c1cc(ccc1I)N(=O)=O	10.1016/j.bmcl.2014.11.003
	CHEMBL408430	373	48	None	-72	3	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production	ChEMBL	503	5	0	5	4.9	CN1CCCCC1Cn1cc(c2c1cccc2)C(=O)c1cc(ccc1I)N(=O)=O	10.1016/j.bmcl.2014.11.003
	72948611	172335	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human CB1R expressed in CHO cells by Ca2+ flux assayAgonist activity at human CB1R expressed in CHO cells by Ca2+ flux assay	ChEMBL	359	6	0	2	6.4	CCCCCn1cc(C(=O)c2cccc3ccccc23)c2cccc(F)c21	10.1021/acs.jmedchem.6b00516
	CHEMBL4516360	172335	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human CB1R expressed in CHO cells by Ca2+ flux assayAgonist activity at human CB1R expressed in CHO cells by Ca2+ flux assay	ChEMBL	359	6	0	2	6.4	CCCCCn1cc(C(=O)c2cccc3ccccc23)c2cccc(F)c21	10.1021/acs.jmedchem.6b00516
	168297756	191888	0	None	1	2	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at CB1 receptor (unknown origin) expressed in human HEK293T cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment using furimazine as substrate by Nano-Glo live cell reagent assayAgonist activity at CB1 receptor (unknown origin) expressed in human HEK293T cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment using furimazine as substrate by Nano-Glo live cell reagent assay	ChEMBL	364	8	2	4	2.7	CCCCn1cc(C(=O)N[C@@H](Cc2ccccc2)C(N)=O)c2cccnc21	10.1039/d1md00242b
	CHEMBL5209051	191888	0	None	1	2	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at CB1 receptor (unknown origin) expressed in human HEK293T cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment using furimazine as substrate by Nano-Glo live cell reagent assayAgonist activity at CB1 receptor (unknown origin) expressed in human HEK293T cells co-expressing beta-arrestin2 assessed as beta-arrestin2 recruitment using furimazine as substrate by Nano-Glo live cell reagent assay	ChEMBL	364	8	2	4	2.7	CCCCn1cc(C(=O)N[C@@H](Cc2ccccc2)C(N)=O)c2cccnc21	10.1039/d1md00242b
	118720565	115439	0	None	-87	4	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human recombinant CB1 receptor expressed in CHOK1 cells assessed as cAMP accumulation by HTRF methodAgonist activity at human recombinant CB1 receptor expressed in CHOK1 cells assessed as cAMP accumulation by HTRF method	ChEMBL	359	4	2	4	2.5	O=C(NC1(CO)CCC1)c1nn(-c2ccc(F)cc2F)c2c1C[C@H]1C[C@@H]21	10.1016/j.bmcl.2014.11.040
	CHEMBL3354954	115439	0	None	-87	4	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human recombinant CB1 receptor expressed in CHOK1 cells assessed as cAMP accumulation by HTRF methodAgonist activity at human recombinant CB1 receptor expressed in CHOK1 cells assessed as cAMP accumulation by HTRF method	ChEMBL	359	4	2	4	2.5	O=C(NC1(CO)CCC1)c1nn(-c2ccc(F)cc2F)c2c1C[C@H]1C[C@@H]21	10.1016/j.bmcl.2014.11.040
	11524275	84605	1	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Activity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assayActivity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assay	ChEMBL	404	4	2	1	6.6	O=C(Nc1ccc(Cl)cc1)NC(c1ccc(Cl)cc1)c1ccc(Cl)cc1	10.1021/jm0503906
	CHEMBL224113	84605	1	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Activity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assayActivity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assay	ChEMBL	404	4	2	1	6.6	O=C(Nc1ccc(Cl)cc1)NC(c1ccc(Cl)cc1)c1ccc(Cl)cc1	10.1021/jm0503906
	53324282	56752	0	None	-104	2	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human cloned CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human cloned CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation	ChEMBL	351	4	1	2	5.4	Clc1cccc(-c2c[nH]c(-c3cccc(CN4CCCCC4)c3)n2)c1	10.1016/j.bmcl.2010.11.044
	CHEMBL1644739	56752	0	None	-104	2	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human cloned CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at human cloned CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation	ChEMBL	351	4	1	2	5.4	Clc1cccc(-c2c[nH]c(-c3cccc(CN4CCCCC4)c3)n2)c1	10.1016/j.bmcl.2010.11.044
	44828492	2906	72	None	-	1	Human	5.0	pEC50	=	5.0	Functional	Activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 5 mins in presence of CP55,940 by cAMP BRET assayActivity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 5 mins in presence of CP55,940 by cAMP BRET assay	ChEMBL	409	6	2	2	5.3	CCc1c([nH]c2c1cc(Cl)cc2)C(=O)NCCc1ccc(cc1)N1CCCCC1	10.1021/acs.jmedchem.5b00579
	7851	2906	72	None	-	1	Human	5.0	pEC50	=	5.0	Functional	Activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 5 mins in presence of CP55,940 by cAMP BRET assayActivity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 5 mins in presence of CP55,940 by cAMP BRET assay	ChEMBL	409	6	2	2	5.3	CCc1c([nH]c2c1cc(Cl)cc2)C(=O)NCCc1ccc(cc1)N1CCCCC1	10.1021/acs.jmedchem.5b00579
	CHEMBL1553629	2906	72	None	-	1	Human	5.0	pEC50	=	5.0	Functional	Activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 5 mins in presence of CP55,940 by cAMP BRET assayActivity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 5 mins in presence of CP55,940 by cAMP BRET assay	ChEMBL	409	6	2	2	5.3	CCc1c([nH]c2c1cc(Cl)cc2)C(=O)NCCc1ccc(cc1)N1CCCCC1	10.1021/acs.jmedchem.5b00579
	71093593	142307	0	None	-12	2	Human	6.0	pEC50	=	6.0	Functional	cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.	ChEMBL	356	7	1	6	3.1	Cc1nc(C(C)(C)NC(=O)c2ccc(C3CC3)c(OCC3CC3)n2)no1	nan
	CHEMBL3893213	142307	0	None	-12	2	Human	6.0	pEC50	=	6.0	Functional	cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.	ChEMBL	356	7	1	6	3.1	Cc1nc(C(C)(C)NC(=O)c2ccc(C3CC3)c(OCC3CC3)n2)no1	nan
	118323971	145115	0	None	22	2	Human	7.0	pEC50	=	7.0	Functional	Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assayInverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assay	ChEMBL	709	12	2	6	8.1	O=C(O)CCCCOc1cc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)cc2c(NC3CCN(S(=O)(=O)C(F)(F)F)CC3)ccnc12	10.1021/acs.jmedchem.8b01467
	CHEMBL3915918	145115	0	None	22	2	Human	7.0	pEC50	=	7.0	Functional	Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assayInverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assay	ChEMBL	709	12	2	6	8.1	O=C(O)CCCCOc1cc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)cc2c(NC3CCN(S(=O)(=O)C(F)(F)F)CC3)ccnc12	10.1021/acs.jmedchem.8b01467
	118323971	145115	0	None	22	2	Human	7.0	pEC50	=	7.0	Functional	cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.	ChEMBL	709	12	2	6	8.1	O=C(O)CCCCOc1cc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)cc2c(NC3CCN(S(=O)(=O)C(F)(F)F)CC3)ccnc12	nan
	CHEMBL3915918	145115	0	None	22	2	Human	7.0	pEC50	=	7.0	Functional	cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.	ChEMBL	709	12	2	6	8.1	O=C(O)CCCCOc1cc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)cc2c(NC3CCN(S(=O)(=O)C(F)(F)F)CC3)ccnc12	nan
	22475020	95544	15	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Activity at human CB1R expressed in HEK293 cells assessed as intracellular cAMP levelActivity at human CB1R expressed in HEK293 cells assessed as intracellular cAMP level	ChEMBL	491	3	0	4	5.4	O=C(c1cc2c(cc1F)OC(c1ccc(F)cc1)(c1ccc(Cl)cc1Cl)O2)N1CCOCC1	10.1021/jm701487t
	CHEMBL259656	95544	15	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Activity at human CB1R expressed in HEK293 cells assessed as intracellular cAMP levelActivity at human CB1R expressed in HEK293 cells assessed as intracellular cAMP level	ChEMBL	491	3	0	4	5.4	O=C(c1cc2c(cc1F)OC(c1ccc(F)cc1)(c1ccc(Cl)cc1Cl)O2)N1CCOCC1	10.1021/jm701487t
	22475055	158984	0	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Activity at human CB1R expressed in HEK293 cells assessed as intracellular cAMP levelActivity at human CB1R expressed in HEK293 cells assessed as intracellular cAMP level	ChEMBL	513	4	0	5	4.1	O=S(=O)(c1cc2c(cc1F)OC(c1ccc(F)cc1F)(c1ccc(F)cc1F)O2)N1CCOCC1	10.1021/jm701487t
	CHEMBL410247	158984	0	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Activity at human CB1R expressed in HEK293 cells assessed as intracellular cAMP levelActivity at human CB1R expressed in HEK293 cells assessed as intracellular cAMP level	ChEMBL	513	4	0	5	4.1	O=S(=O)(c1cc2c(cc1F)OC(c1ccc(F)cc1F)(c1ccc(F)cc1F)O2)N1CCOCC1	10.1021/jm701487t
	11853844	70300	0	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgamma binding assayAgonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgamma binding assay	ChEMBL	457	4	0	5	4.0	CCS(=O)(=O)n1c2c(c3cc(C(=O)N4CCC(C)CC4)ccc31)CN(C1CCCC1)CC2	10.1016/j.bmcl.2011.12.124
	CHEMBL1950350	70300	0	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgamma binding assayAgonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgamma binding assay	ChEMBL	457	4	0	5	4.0	CCS(=O)(=O)n1c2c(c3cc(C(=O)N4CCC(C)CC4)ccc31)CN(C1CCCC1)CC2	10.1016/j.bmcl.2011.12.124
	16078	1330	19	None	-3	7	Rat	8.0	pEC50	=	8.0	Functional	Effective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptorEffective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptor	ChEMBL	314	4	1	2	5.7	CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C	10.1021/jm970126f
	2424	1330	19	None	-3	7	Rat	8.0	pEC50	=	8.0	Functional	Effective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptorEffective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptor	ChEMBL	314	4	1	2	5.7	CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C	10.1021/jm970126f
	4109	1330	19	None	-3	7	Rat	8.0	pEC50	=	8.0	Functional	Effective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptorEffective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptor	ChEMBL	314	4	1	2	5.7	CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C	10.1021/jm970126f
	CHEMBL465	1330	19	None	-3	7	Rat	8.0	pEC50	=	8.0	Functional	Effective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptorEffective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptor	ChEMBL	314	4	1	2	5.7	CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C	10.1021/jm970126f
	DB00470	1330	19	None	-3	7	Rat	8.0	pEC50	=	8.0	Functional	Effective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptorEffective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptor	ChEMBL	314	4	1	2	5.7	CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C	10.1021/jm970126f
	134146936	149581	0	None	177	2	Human	8.0	pEC50	=	8.0	Functional	Inverse agonist activity at human CB1 receptor transfected in HEK293 cells assessed as increase of forskolin-induced cAMP production incubated for 30 mins followed by d2 labeled cAMP addition measured after 60 mins by HTRF assayInverse agonist activity at human CB1 receptor transfected in HEK293 cells assessed as increase of forskolin-induced cAMP production incubated for 30 mins followed by d2 labeled cAMP addition measured after 60 mins by HTRF assay	ChEMBL	619	8	2	7	5.4	COc1ccc(/C=C2\CN(C(=O)CC(=O)O)Cc3c(C(=O)N[C@H](C)c4ccccn4)nn(-c4ccc(Cl)cc4Cl)c32)cc1	10.1016/j.bmcl.2016.09.026
	CHEMBL3951226	149581	0	None	177	2	Human	8.0	pEC50	=	8.0	Functional	Inverse agonist activity at human CB1 receptor transfected in HEK293 cells assessed as increase of forskolin-induced cAMP production incubated for 30 mins followed by d2 labeled cAMP addition measured after 60 mins by HTRF assayInverse agonist activity at human CB1 receptor transfected in HEK293 cells assessed as increase of forskolin-induced cAMP production incubated for 30 mins followed by d2 labeled cAMP addition measured after 60 mins by HTRF assay	ChEMBL	619	8	2	7	5.4	COc1ccc(/C=C2\CN(C(=O)CC(=O)O)Cc3c(C(=O)N[C@H](C)c4ccccn4)nn(-c4ccc(Cl)cc4Cl)c32)cc1	10.1016/j.bmcl.2016.09.026
	134155808	150944	0	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Inverse agonist activity at human cannabinoid receptor 1 expressed in HEK293 cells assessed as increase in forskolin-induced cAMP production preincubated with cells followed by forskolin stimulation measured after 30 mins in presence of D2-labeled cAMP and Eu3+-TBP-NHS cryptate by HTRF assayInverse agonist activity at human cannabinoid receptor 1 expressed in HEK293 cells assessed as increase in forskolin-induced cAMP production preincubated with cells followed by forskolin stimulation measured after 30 mins in presence of D2-labeled cAMP and Eu3+-TBP-NHS cryptate by HTRF assay	ChEMBL	588	5	1	5	8.0	O=C(NC1(c2ccccn2)CC1)c1nn(-c2ccc(C(F)(F)F)cc2Cl)c2c1CCC/C2=C\c1ccc(Cl)s1	10.1016/j.bmcl.2016.09.025
	CHEMBL3962373	150944	0	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Inverse agonist activity at human cannabinoid receptor 1 expressed in HEK293 cells assessed as increase in forskolin-induced cAMP production preincubated with cells followed by forskolin stimulation measured after 30 mins in presence of D2-labeled cAMP and Eu3+-TBP-NHS cryptate by HTRF assayInverse agonist activity at human cannabinoid receptor 1 expressed in HEK293 cells assessed as increase in forskolin-induced cAMP production preincubated with cells followed by forskolin stimulation measured after 30 mins in presence of D2-labeled cAMP and Eu3+-TBP-NHS cryptate by HTRF assay	ChEMBL	588	5	1	5	8.0	O=C(NC1(c2ccccn2)CC1)c1nn(-c2ccc(C(F)(F)F)cc2Cl)c2c1CCC/C2=C\c1ccc(Cl)s1	10.1016/j.bmcl.2016.09.025
	24945315	186250	0	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level	ChEMBL	494	4	0	3	4.6	CC(C(=O)N1CCN(S(=O)(=O)c2cc(Cl)cc(Cl)c2)CC1)c1ccc(C(F)(F)F)cc1	10.1021/jm900063x
	CHEMBL489437	186250	0	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Inverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP levelInverse agonist activity at human recombinant CB1R expressed in CHO cells assessed as increase in forskolin-stimulated cAMP level	ChEMBL	494	4	0	3	4.6	CC(C(=O)N1CCN(S(=O)(=O)c2cc(Cl)cc(Cl)c2)CC1)c1ccc(C(F)(F)F)cc1	10.1021/jm900063x
	118323946	142439	0	None	371	2	Human	8.0	pEC50	=	8.0	Functional	cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.	ChEMBL	555	6	2	5	6.9	O=c1cc(NC2CCN(c3ncccn3)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)ccc2[nH]1	nan
	CHEMBL3894411	142439	0	None	371	2	Human	8.0	pEC50	=	8.0	Functional	cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.	ChEMBL	555	6	2	5	6.9	O=c1cc(NC2CCN(c3ncccn3)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)ccc2[nH]1	nan
	118329983	143209	0	None	-	1	Human	8.0	pEC50	=	8.0	Functional	cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.	ChEMBL	522	5	2	2	8.6	O=c1cc(Nc2ccc(Cl)c(F)c2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)ccc2[nH]1	nan
	CHEMBL3900808	143209	0	None	-	1	Human	8.0	pEC50	=	8.0	Functional	cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.	ChEMBL	522	5	2	2	8.6	O=c1cc(Nc2ccc(Cl)c(F)c2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)ccc2[nH]1	nan
	118324060	145972	0	None	602	2	Human	8.0	pEC50	=	8.0	Functional	cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.	ChEMBL	610	6	2	5	6.1	O=c1cc(NC2CCN(S(=O)(=O)C(F)(F)F)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)nc3)ccc2[nH]1	nan
	CHEMBL3922599	145972	0	None	602	2	Human	8.0	pEC50	=	8.0	Functional	cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.	ChEMBL	610	6	2	5	6.1	O=c1cc(NC2CCN(S(=O)(=O)C(F)(F)F)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)nc3)ccc2[nH]1	nan
	11951302	104352	0	None	3981	2	Human	7.9	pEC50	=	7.9	Functional	Antagonist activity at human CB1 receptor overexpressed in HEK cells assessed as [35S]GTPgamma binding after 1 hr by liquid scintillation counting analysisAntagonist activity at human CB1 receptor overexpressed in HEK cells assessed as [35S]GTPgamma binding after 1 hr by liquid scintillation counting analysis	ChEMBL	404	7	2	5	3.5	COCCOc1ncc(C(=O)N[C@@H]2CCCC[C@H]2O)cc1-c1ccc(Cl)cc1	10.1021/jm4010708
	CHEMBL3109772	104352	0	None	3981	2	Human	7.9	pEC50	=	7.9	Functional	Antagonist activity at human CB1 receptor overexpressed in HEK cells assessed as [35S]GTPgamma binding after 1 hr by liquid scintillation counting analysisAntagonist activity at human CB1 receptor overexpressed in HEK cells assessed as [35S]GTPgamma binding after 1 hr by liquid scintillation counting analysis	ChEMBL	404	7	2	5	3.5	COCCOc1ncc(C(=O)N[C@@H]2CCCC[C@H]2O)cc1-c1ccc(Cl)cc1	10.1021/jm4010708
	67953431	115198	0	None	-575	2	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 30 minsAgonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins	ChEMBL	396	3	1	5	3.5	CC(C)(C)c1cc(NC(=O)[C@@H]2CCC(=O)N2c2ccc(C(F)(F)F)cn2)on1	10.1016/j.bmcl.2014.12.019
	CHEMBL3353885	115198	0	None	-575	2	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 30 minsAgonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins	ChEMBL	396	3	1	5	3.5	CC(C)(C)c1cc(NC(=O)[C@@H]2CCC(=O)N2c2ccc(C(F)(F)F)cn2)on1	10.1016/j.bmcl.2014.12.019
	155553407	173546	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Positive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced inhibition of forskolin-stimulated cAMP production after 30 mins in presence of CP55940 at EC20 concentration by hit-hunter cAMP assayPositive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced inhibition of forskolin-stimulated cAMP production after 30 mins in presence of CP55940 at EC20 concentration by hit-hunter cAMP assay	ChEMBL	360	5	1	2	5.4	O=[N+]([O-])CC(c1ccccc1)c1c(-c2ccccc2)[nH]c2cc(F)ccc12	10.1021/acs.jmedchem.9b01142
	CHEMBL4546004	173546	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Positive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced inhibition of forskolin-stimulated cAMP production after 30 mins in presence of CP55940 at EC20 concentration by hit-hunter cAMP assayPositive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced inhibition of forskolin-stimulated cAMP production after 30 mins in presence of CP55940 at EC20 concentration by hit-hunter cAMP assay	ChEMBL	360	5	1	2	5.4	O=[N+]([O-])CC(c1ccccc1)c1c(-c2ccccc2)[nH]c2cc(F)ccc12	10.1021/acs.jmedchem.9b01142
	76284483	149550	0	None	-77	2	Human	7.0	pEC50	=	7.0	Functional	cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1×HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30° C. for 30 min. Compounds were added to a final assay volume of 100 μl and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 μl lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN3) and 50 μl detection solutions (20 μM mAb Alexa700-cAMP 1:1, and 48 μM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated as follows: FRET=T730-Alexa730-P(T645-B645) with P=Ru730-B730/Ru645-B645, where T730 is the test well measured at 730 nM, T645 is the test well measured at 645 nm, B730 and B645 are the buffer controls at 730 nm and 645 nm, respectively. cAMP content is determined from the function of a standard curve spanning from 10 μM to 0.13 nM cAMP.cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1×HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30° C. for 30 min. Compounds were added to a final assay volume of 100 μl and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 μl lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN3) and 50 μl detection solutions (20 μM mAb Alexa700-cAMP 1:1, and 48 μM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated as follows: FRET=T730-Alexa730-P(T645-B645) with P=Ru730-B730/Ru645-B645, where T730 is the test well measured at 730 nM, T645 is the test well measured at 645 nm, B730 and B645 are the buffer controls at 730 nm and 645 nm, respectively. cAMP content is determined from the function of a standard curve spanning from 10 μM to 0.13 nM cAMP.	ChEMBL	475	7	1	7	3.6	Cc1nc(C(C)(NC(=O)c2cc(O[C@@H](C)C(F)(F)F)c(N3CC(F)(F)C3)cn2)C2CC2)no1	nan
	CHEMBL3950922	149550	0	None	-77	2	Human	7.0	pEC50	=	7.0	Functional	cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1×HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30° C. for 30 min. Compounds were added to a final assay volume of 100 μl and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 μl lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN3) and 50 μl detection solutions (20 μM mAb Alexa700-cAMP 1:1, and 48 μM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated as follows: FRET=T730-Alexa730-P(T645-B645) with P=Ru730-B730/Ru645-B645, where T730 is the test well measured at 730 nM, T645 is the test well measured at 645 nm, B730 and B645 are the buffer controls at 730 nm and 645 nm, respectively. cAMP content is determined from the function of a standard curve spanning from 10 μM to 0.13 nM cAMP.cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1×HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30° C. for 30 min. Compounds were added to a final assay volume of 100 μl and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 μl lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN3) and 50 μl detection solutions (20 μM mAb Alexa700-cAMP 1:1, and 48 μM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated as follows: FRET=T730-Alexa730-P(T645-B645) with P=Ru730-B730/Ru645-B645, where T730 is the test well measured at 730 nM, T645 is the test well measured at 645 nm, B730 and B645 are the buffer controls at 730 nm and 645 nm, respectively. cAMP content is determined from the function of a standard curve spanning from 10 μM to 0.13 nM cAMP.	ChEMBL	475	7	1	7	3.6	Cc1nc(C(C)(NC(=O)c2cc(O[C@@H](C)C(F)(F)F)c(N3CC(F)(F)C3)cn2)C2CC2)no1	nan
	67953920	115199	0	None	-912	2	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 30 minsAgonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins	ChEMBL	353	3	1	6	2.4	CC(C)(C)c1cc(NC(=O)[C@@H]2CCC(=O)N2c2ccc(C#N)cn2)on1	10.1016/j.bmcl.2014.12.019
	CHEMBL3353886	115199	0	None	-912	2	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 30 minsAgonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins	ChEMBL	353	3	1	6	2.4	CC(C)(C)c1cc(NC(=O)[C@@H]2CCC(=O)N2c2ccc(C#N)cn2)on1	10.1016/j.bmcl.2014.12.019
	123627357	162382	0	None	-912	4	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at recombinant human CB1 receptor expressed in HEK293 cells assessed as increase in beta arrestin recruitment measured after 2 to 3 hrs by PathHunter assayAgonist activity at recombinant human CB1 receptor expressed in HEK293 cells assessed as increase in beta arrestin recruitment measured after 2 to 3 hrs by PathHunter assay	ChEMBL	359	4	1	5	1.7	CC(C)(C)[C@@H](CF)NC(=O)c1nn(-c2c[n+]([O-])ccn2)c2c1C[C@@H]1C[C@H]21	10.1021/acsmedchemlett.7b00396
	CHEMBL4174510	162382	0	None	-912	4	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at recombinant human CB1 receptor expressed in HEK293 cells assessed as increase in beta arrestin recruitment measured after 2 to 3 hrs by PathHunter assayAgonist activity at recombinant human CB1 receptor expressed in HEK293 cells assessed as increase in beta arrestin recruitment measured after 2 to 3 hrs by PathHunter assay	ChEMBL	359	4	1	5	1.7	CC(C)(C)[C@@H](CF)NC(=O)c1nn(-c2c[n+]([O-])ccn2)c2c1C[C@@H]1C[C@H]21	10.1021/acsmedchemlett.7b00396
	11591162	176332	0	None	18	2	Human	6.0	pEC50	=	6.0	Functional	Antagonist activity at human cannabinoid CB1 receptor expressed in CHOK1 cells assessed as cAMP activityAntagonist activity at human cannabinoid CB1 receptor expressed in CHOK1 cells assessed as cAMP activity	ChEMBL	482	4	1	5	6.4	Cc1c(C(=O)NN2CCCCCC2)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)s1	10.1016/j.bmcl.2009.03.046
	CHEMBL461862	176332	0	None	18	2	Human	6.0	pEC50	=	6.0	Functional	Antagonist activity at human cannabinoid CB1 receptor expressed in CHOK1 cells assessed as cAMP activityAntagonist activity at human cannabinoid CB1 receptor expressed in CHOK1 cells assessed as cAMP activity	ChEMBL	482	4	1	5	6.4	Cc1c(C(=O)NN2CCCCCC2)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)s1	10.1016/j.bmcl.2009.03.046
	4346308	193476	1	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Inverse agonist activity at human CB1 receptor by [35S]GTPgammaS incorporation assayInverse agonist activity at human CB1 receptor by [35S]GTPgammaS incorporation assay	ChEMBL	453	5	0	3	5.4	Cc1ccc(C2c3cccn3-c3ccccc3N2C(=O)CN(C(=O)C2CCCC2)C2CC2)cc1	10.1016/j.bmcl.2009.05.114
	CHEMBL550309	193476	1	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Inverse agonist activity at human CB1 receptor by [35S]GTPgammaS incorporation assayInverse agonist activity at human CB1 receptor by [35S]GTPgammaS incorporation assay	ChEMBL	453	5	0	3	5.4	Cc1ccc(C2c3cccn3-c3ccccc3N2C(=O)CN(C(=O)C2CCCC2)C2CC2)cc1	10.1016/j.bmcl.2009.05.114
	5031403	193503	1	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Inverse agonist activity at human CB1 receptor by [35S]GTPgammaS incorporation assayInverse agonist activity at human CB1 receptor by [35S]GTPgammaS incorporation assay	ChEMBL	461	5	0	3	5.7	CC(C)N(CC(=O)N1c2ccccc2-n2cccc2C1c1ccc(F)cc1)C(=O)CC(C)(C)C	10.1016/j.bmcl.2009.05.114
	CHEMBL550514	193503	1	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Inverse agonist activity at human CB1 receptor by [35S]GTPgammaS incorporation assayInverse agonist activity at human CB1 receptor by [35S]GTPgammaS incorporation assay	ChEMBL	461	5	0	3	5.7	CC(C)N(CC(=O)N1c2ccccc2-n2cccc2C1c1ccc(F)cc1)C(=O)CC(C)(C)C	10.1016/j.bmcl.2009.05.114
	118323979	147377	0	None	6	2	Human	6.0	pEC50	=	6.0	Functional	Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assayInverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assay	ChEMBL	607	7	2	4	6.4	O=c1cc(NC2CCN(S(=O)(=O)C(F)(F)F)CC2)c2cc(C(Cc3ccc(F)cc3)c3ccc(Cl)cc3)ccc2[nH]1	10.1021/acs.jmedchem.8b01467
	CHEMBL3933648	147377	0	None	6	2	Human	6.0	pEC50	=	6.0	Functional	Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assayInverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assay	ChEMBL	607	7	2	4	6.4	O=c1cc(NC2CCN(S(=O)(=O)C(F)(F)F)CC2)c2cc(C(Cc3ccc(F)cc3)c3ccc(Cl)cc3)ccc2[nH]1	10.1021/acs.jmedchem.8b01467
	155544651	172760	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Positive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced inhibition of forskolin-stimulated cAMP production after 30 mins in presence of CP55940 at EC20 concentration by hit-hunter cAMP assayPositive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced inhibition of forskolin-stimulated cAMP production after 30 mins in presence of CP55940 at EC20 concentration by hit-hunter cAMP assay	ChEMBL	343	5	1	3	4.6	O=[N+]([O-])CC(c1ccccc1)c1c(-c2cccnc2)[nH]c2ccccc12	10.1021/acs.jmedchem.9b01142
	CHEMBL4526885	172760	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Positive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced inhibition of forskolin-stimulated cAMP production after 30 mins in presence of CP55940 at EC20 concentration by hit-hunter cAMP assayPositive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced inhibition of forskolin-stimulated cAMP production after 30 mins in presence of CP55940 at EC20 concentration by hit-hunter cAMP assay	ChEMBL	343	5	1	3	4.6	O=[N+]([O-])CC(c1ccccc1)c1c(-c2cccnc2)[nH]c2ccccc12	10.1021/acs.jmedchem.9b01142
	155561427	175061	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Positive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced inhibition of forskolin-stimulated cAMP production after 30 mins in presence of CP55940 at EC20 concentration by hit-hunter cAMP assayPositive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced inhibition of forskolin-stimulated cAMP production after 30 mins in presence of CP55940 at EC20 concentration by hit-hunter cAMP assay	ChEMBL	343	5	1	3	4.6	O=[N+]([O-])CC(c1ccccc1)c1c(-c2ccccc2)[nH]c2ncccc12	10.1021/acs.jmedchem.9b01142
	CHEMBL4581106	175061	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Positive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced inhibition of forskolin-stimulated cAMP production after 30 mins in presence of CP55940 at EC20 concentration by hit-hunter cAMP assayPositive allosteric modulatory activity at human CB1R expressed in CHO-K1 cells assessed as increase in CP55940-induced inhibition of forskolin-stimulated cAMP production after 30 mins in presence of CP55940 at EC20 concentration by hit-hunter cAMP assay	ChEMBL	343	5	1	3	4.6	O=[N+]([O-])CC(c1ccccc1)c1c(-c2ccccc2)[nH]c2ncccc12	10.1021/acs.jmedchem.9b01142
	118323979	147377	0	None	6	2	Human	6.0	pEC50	=	6.0	Functional	cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.	ChEMBL	607	7	2	4	6.4	O=c1cc(NC2CCN(S(=O)(=O)C(F)(F)F)CC2)c2cc(C(Cc3ccc(F)cc3)c3ccc(Cl)cc3)ccc2[nH]1	nan
	CHEMBL3933648	147377	0	None	6	2	Human	6.0	pEC50	=	6.0	Functional	cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.	ChEMBL	607	7	2	4	6.4	O=c1cc(NC2CCN(S(=O)(=O)C(F)(F)F)CC2)c2cc(C(Cc3ccc(F)cc3)c3ccc(Cl)cc3)ccc2[nH]1	nan
	71105569	149718	0	None	-10	2	Human	6.0	pEC50	=	6.0	Functional	cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.	ChEMBL	391	4	1	4	5.2	CC(C)(NC(=O)c1ccc(Cl)c(-c2cccc(Cl)c2)n1)c1nccs1	nan
	CHEMBL3952505	149718	0	None	-10	2	Human	6.0	pEC50	=	6.0	Functional	cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.	ChEMBL	391	4	1	4	5.2	CC(C)(NC(=O)c1ccc(Cl)c(-c2cccc(Cl)c2)n1)c1nccs1	nan
	118329984	149274	0	None	33	2	Human	7.0	pEC50	=	7.0	Functional	cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.	ChEMBL	544	5	2	2	8.5	O=c1cc(NC2CCC(C(F)(F)F)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)ccc2[nH]1	nan
	CHEMBL3948754	149274	0	None	33	2	Human	7.0	pEC50	=	7.0	Functional	cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.	ChEMBL	544	5	2	2	8.5	O=c1cc(NC2CCC(C(F)(F)F)CC2)c2cc(C(c3ccc(Cl)cc3)c3ccc(Cl)cc3)ccc2[nH]1	nan
	11690547	140149	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Potency at human CB1 receptor in a [35S]GTP-gamma-S functional assayPotency at human CB1 receptor in a [35S]GTP-gamma-S functional assay	ChEMBL	430	3	0	2	6.4	O=C1C(c2ccc(Cl)cc2)N(c2ccc(Cl)cc2)C(=O)N1c1ccc(Cl)cc1	10.1021/jm050484f
	CHEMBL381560	140149	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Potency at human CB1 receptor in a [35S]GTP-gamma-S functional assayPotency at human CB1 receptor in a [35S]GTP-gamma-S functional assay	ChEMBL	430	3	0	2	6.4	O=C1C(c2ccc(Cl)cc2)N(c2ccc(Cl)cc2)C(=O)N1c1ccc(Cl)cc1	10.1021/jm050484f
	5311501	4007	8	None	-8	7	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma bindingAgonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma binding	ChEMBL	426	4	0	5	4.6	O=C(c1c(C)n2c3c1cccc3OC[C@H]2CN1CCOCC1)c1cccc2c1cccc2	10.1016/j.bmcl.2012.04.128
	733	4007	8	None	-8	7	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma bindingAgonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma binding	ChEMBL	426	4	0	5	4.6	O=C(c1c(C)n2c3c1cccc3OC[C@H]2CN1CCOCC1)c1cccc2c1cccc2	10.1016/j.bmcl.2012.04.128
	CHEMBL188	4007	8	None	-8	7	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma bindingAgonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma binding	ChEMBL	426	4	0	5	4.6	O=C(c1c(C)n2c3c1cccc3OC[C@H]2CN1CCOCC1)c1cccc2c1cccc2	10.1016/j.bmcl.2012.04.128
	DB13950	4007	8	None	-8	7	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma bindingAgonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma binding	ChEMBL	426	4	0	5	4.6	O=C(c1c(C)n2c3c1cccc3OC[C@H]2CN1CCOCC1)c1cccc2c1cccc2	10.1016/j.bmcl.2012.04.128
	164617205	183949	0	None	-251	2	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding assayAgonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding assay	ChEMBL	342	6	1	3	5.8	CCCCC1(c2cc(O)c3cc(CCC)c(=O)oc3c2)CCCCC1	10.1016/j.ejmech.2021.113354
	CHEMBL4847976	183949	0	None	-251	2	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding assayAgonist activity at human recombinant CB1 receptor expressed in CHO-K1 cell membrane assessed as increase in GTPgammaS binding pretreated for 30 mins followed by [35S]GTPgammaS addition for 90 mins by [35S]GTP-gammaS binding assay	ChEMBL	342	6	1	3	5.8	CCCCC1(c2cc(O)c3cc(CCC)c(=O)oc3c2)CCCCC1	10.1016/j.ejmech.2021.113354
	117923246	137120	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Negative allosteric modulator activity at human CB1R expressed in CHO-K1 cells assessed as effect on CP55,940-induced inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by CP55,940 addition measured for 30 mins by HitHunter assayNegative allosteric modulator activity at human CB1R expressed in CHO-K1 cells assessed as effect on CP55,940-induced inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by CP55,940 addition measured for 30 mins by HitHunter assay	ChEMBL	450	8	2	3	5.6	[N-]=[N+]=NCCc1c(C(=O)NCCc2ccc(N3CCCCC3)cc2)[nH]c2ccc(Cl)cc12	10.1021/acs.jmedchem.5b01303
	CHEMBL3758424	137120	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Negative allosteric modulator activity at human CB1R expressed in CHO-K1 cells assessed as effect on CP55,940-induced inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by CP55,940 addition measured for 30 mins by HitHunter assayNegative allosteric modulator activity at human CB1R expressed in CHO-K1 cells assessed as effect on CP55,940-induced inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by CP55,940 addition measured for 30 mins by HitHunter assay	ChEMBL	450	8	2	3	5.6	[N-]=[N+]=NCCc1c(C(=O)NCCc2ccc(N3CCCCC3)cc2)[nH]c2ccc(Cl)cc12	10.1021/acs.jmedchem.5b01303
	118324039	142308	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.	ChEMBL	738	12	3	7	7.5	CCOC(=O)CCCNc1cc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)cc2c(NC3CCN(S(=O)(=O)C(F)(F)F)CC3)cc(=O)[nH]c12	nan
	CHEMBL3893217	142308	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.	ChEMBL	738	12	3	7	7.5	CCOC(=O)CCCNc1cc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)cc2c(NC3CCN(S(=O)(=O)C(F)(F)F)CC3)cc(=O)[nH]c12	nan
	71450465	83221	0	None	-23	2	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human CB1 receptor after 4 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor after 4 hrs by luciferase reporter gene assay	ChEMBL	398	3	1	3	4.9	CC(C)(C)CC(=O)Nc1sc2c(c1C(=O)N1CCC(F)(F)CC1)CCCC2	10.1016/j.bmcl.2012.10.087
	CHEMBL2204905	83221	0	None	-23	2	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human CB1 receptor after 4 hrs by luciferase reporter gene assayAgonist activity at human CB1 receptor after 4 hrs by luciferase reporter gene assay	ChEMBL	398	3	1	3	4.9	CC(C)(C)CC(=O)Nc1sc2c(c1C(=O)N1CCC(F)(F)CC1)CCCC2	10.1016/j.bmcl.2012.10.087
	145982249	166149	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assayInverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assay	ChEMBL	509	6	1	4	6.5	O=c1cc(Cc2ccc(OC(F)(F)F)cc2)c2cc(C(c3ccc(Cl)cc3)n3ccnc3)ccc2[nH]1	10.1021/acs.jmedchem.8b01467
	CHEMBL4282821	166149	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assayInverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assay	ChEMBL	509	6	1	4	6.5	O=c1cc(Cc2ccc(OC(F)(F)F)cc2)c2cc(C(c3ccc(Cl)cc3)n3ccnc3)ccc2[nH]1	10.1021/acs.jmedchem.8b01467
	118324113	144556	0	None	6	2	Human	7.0	pEC50	=	7.0	Functional	cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.	ChEMBL	667	8	3	6	7.0	O=C(O)c1ccc(S(=O)(=O)N2CCC(Nc3cc(=O)[nH]c4ccc(C(c5ccc(Cl)cc5)c5ccc(Cl)cc5)cc34)CC2)s1	nan
	CHEMBL3911735	144556	0	None	6	2	Human	7.0	pEC50	=	7.0	Functional	cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.cAMP Assay: The following mixtures and buffer solutions were prepared: (a) Buffer 1: HBSS (Mediatech Cat#21-023-CV) with 5 mM HEPES (1 mM stock, Gibco BRL Cat#15630-056) and 0.1% BSA (7.5% stock, Invitrogen Cat#15260-037); (b) Buffer 2: 0.5 mM IBMX (200 mM stock in DMSO, Sigma 15879) in Buffer 1; (c) 1 uM cAMP Standard (50 uM stock, Perkin Elmer Cat# AD0262) diluted in Buffer 2 and serially diluted in Buffer 2, 12 doses at 1/2 dilutions resulting in a dose range of 1 uM to 0.5 nM; (d) d2 labelled cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 6 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); (e) anti-cAMP (CisBio HTRF Detection Kit Cat #62AM4PEB reconstituted with 5 ml dH2O) diluted 1/20 with lysis buffer (CisBio HTRF Detection Kit Cat #62AM4PEB); and (f) Forskolin (Sigma Cat# F6886, 10 mM in DMSO) diluted first in DMSO to 1 mM and then to 1.5 uM in Buffer 2.	ChEMBL	667	8	3	6	7.0	O=C(O)c1ccc(S(=O)(=O)N2CCC(Nc3cc(=O)[nH]c4ccc(C(c5ccc(Cl)cc5)c5ccc(Cl)cc5)cc34)CC2)s1	nan
	71105611	148168	0	None	-1412	2	Human	6.0	pEC50	=	6.0	Functional	cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.	ChEMBL	396	9	2	5	2.0	CC(C)C[C@H](NC(=O)c1ccc(N2CC(F)(F)C2)c(OCC2CC2)n1)C(N)=O	nan
	CHEMBL3940084	148168	0	None	-1412	2	Human	6.0	pEC50	=	6.0	Functional	cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1.times.HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30.degree. C. for 30 min Compounds were added to a final assay volume of 100 ul and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 ul lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN.sub.3) and 50 ul detection solutions (20 uM mAb Alexa700-cAMP 1:1, and 48 uM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10 s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively. The FRET signal is calculated.	ChEMBL	396	9	2	5	2.0	CC(C)C[C@H](NC(=O)c1ccc(N2CC(F)(F)C2)c(OCC2CC2)n1)C(N)=O	nan
	60155819	76625	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation in presence of CP55,940 by cAMP BRET assayActivity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation in presence of CP55,940 by cAMP BRET assay	ChEMBL	371	6	2	3	4.3	CCc1c(C(=O)NCCc2ccc([N+](=O)[O-])cc2)[nH]c2ccc(Cl)cc12	10.1021/acs.jmedchem.5b00579
	CHEMBL2071060	76625	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation in presence of CP55,940 by cAMP BRET assayActivity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation in presence of CP55,940 by cAMP BRET assay	ChEMBL	371	6	2	3	4.3	CCc1c(C(=O)NCCc2ccc([N+](=O)[O-])cc2)[nH]c2ccc(Cl)cc12	10.1021/acs.jmedchem.5b00579
	71525480	143841	0	None	-12	2	Human	5.9	pEC50	=	5.9	Functional	cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1×HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30° C. for 30 min. Compounds were added to a final assay volume of 100 μl and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 μl lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN3) and 50 μl detection solutions (20 μM mAb Alexa700-cAMP 1:1, and 48 μM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively.cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1×HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was exchanged with Krebs Ringer Bicarbonate buffer with 1 mM IBMX and incubated at 30° C. for 30 min. Compounds were added to a final assay volume of 100 μl and incubated for 30 min at 30° C. Using the cAMP-Nano-TRF detection kit the assay (Roche Diagnostics) was stopped by the addition of 50 μl lysis reagent (Tris, NaCl, 1.5% Triton X100, 2.5% NP40, 10% NaN3) and 50 μl detection solutions (20 μM mAb Alexa700-cAMP 1:1, and 48 μM Ruthenium-2-AHA-cAMP) and shaken for 2 h at room temperature. The time-resolved energy transfer is measured by a TRF reader (Evotec Technologies GmbH), equipped with a ND:YAG laser as excitation source. The plate is measured twice with the excitation at 355 nm and at the emission with a delay of 100 ns and a gate of 100 ns, total exposure time 10s at 730 (bandwidth 30 nm) or 645 nm (bandwidth 75 nm), respectively.	ChEMBL	397	5	1	6	4.0	Cc1nc(C(C)(C)NC(=O)c2cnc(C3CC3)c(-c3cccc(Cl)c3)n2)no1	nan
	CHEMBL3905931	143841	0	None	-12	2	Human	5.9	pEC50	=	5.9	Functional	cAMP Assay: CHO cells expressing human CB1 or CB2 receptors are seeded 17-24 hours prior to the experiment 50.000 cells per well in a black 96 well plate with flat clear bottom (Corning Costar #3904) in DMEM (Invitrogen No. 31331), 1×HT supplement, with 10% fetal calf serum and incubated at 5% CO2 and 37° C. in a humidified incubator. The growth medium was ex

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Ligand source activities (1 row/activity)