ChEMBL ligand: CHEMBL111 (Acomplia, Rimonabant, SR-14171, SR-141716, SR141716, SR-141716A, Zimulti)
CB1 receptor/Cannabinoid CB1 receptor in Human [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554] CB1 receptor/Cannabinoid CB1 receptor in Mouse [ChEMBL: CHEMBL3037] [GtoPdb: 56] [UniProtKB: P47746] CB1 receptor/Cannabinoid CB1 receptor in Rat [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272] There should be some charts here, you may need to enable JavaScript!
CB2 receptor/Cannabinoid CB2 receptor in Human [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972] CB2 receptor/Cannabinoid CB2 receptor in Mouse [ChEMBL: CHEMBL5373] [GtoPdb: 57] [UniProtKB: P47936] There should be some charts here, you may need to enable JavaScript!
GPR55/G-protein coupled receptor 55 in Human [ChEMBL: CHEMBL1075322] [GtoPdb: 109] [UniProtKB: Q9Y2T6] There should be some charts here, you may need to enable JavaScript!
Kv11.1/HERG in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] There should be some charts here, you may need to enable JavaScript!
GPR18/N-arachidonyl glycine receptor in Human [ChEMBL: CHEMBL2384898] [GtoPdb: 89] [UniProtKB: Q14330] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
CB1 receptor/Cannabinoid CB1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
ChEMBL	Antagonist activity at human brain CB1 receptor by calcium mobilization assay	F	8.59	pKd	2.57	nM	Kd	J Med Chem (2010) 53: 7048-7060 [PMID:20845959]
ChEMBL	Antagonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of CP-55940-stimulated [35S]GTPgammaS binding	F	8.59	pKd	2.57	nM	Kd	J Med Chem (2008) 51: 3526-3539 [PMID:18512901]
ChEMBL	In vitro cannabinoid receptor 1 antagonism of [3H]arachidonic acid release by CHO cells	F	8.6	pKd	2.51	nM	Kd	J Med Chem (2005) 48: 1823-1838 [PMID:15771428]
ChEMBL	Antagonistic activity against cannabinoid receptor 1 measured by CP-55940 induced arachnoid acid release in CHO cells	F	8.6	pKd	2.51	nM	Kd	Bioorg Med Chem Lett (2005) 15: 4794-4798 [PMID:16140010]
ChEMBL	Antagonistic activity towards cannabinoid receptor 1 expressed as [3H]Arachidonic acid release in CHO cells	F	8.6	pKd	2.51	nM	Kd	J Med Chem (2004) 47: 627-643 [PMID:14736243]
ChEMBL	Antagonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of CP-55940-induced [3H]arachidonic acid release	F	8.6	pKd	2.51	nM	Kd	Bioorg Med Chem Lett (2010) 20: 2770-2775 [PMID:20363132]
ChEMBL	Displacement of [3H]SR-141716 from human CB1 receptor expressed in HEK293 cells	B	8.74	pKd	1.8	nM	Kd	J Med Chem (2006) 49: 5969-5987 [PMID:17004712]
ChEMBL	Binding affinity towards cloned human Cannabinoid receptor 1	B	1.09	pKi	1.09	nM	Log Ki	J Med Chem (2000) 43: 2300-2309 [PMID:10882356]
ChEMBL	Displacement of [3H]-CP55940 from human recombinant cannabinoid CB1 receptor expressed in CHO cells by radioligand binding assay	B	6.84	pKi	143	nM	Ki	J Med Chem (2019) 62: 9078-9102 [PMID:31609608]
ChEMBL	Displacement of [3H]-CP55950 from human CB1 receptor expressed in CHO cell membranes after 3 hrs by scintillation counting method	B	6.84	pKi	143	nM	Ki	J Med Chem (2018) 61: 1646-1663 [PMID:29400965]
ChEMBL	Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells	B	7.33	pKi	47	nM	Ki	J Med Chem (2007) 50: 5951-5966 [PMID:17979261]
ChEMBL	Displacement of [3H]CP-55940 form human recombinant CB1 receptor expressed in HEK293 cells by liquid scintillation counting	B	7.4	pKi	40	nM	Ki	Eur J Med Chem (2009) 44: 593-608 [PMID:18511157]
ChEMBL	Ability to displace [3H]CP-55940 from the membranes prepared from HEK cell line with W6 48(357)A mutant Cannabinoid receptor 1	B	7.48	pKi	33	nM	Ki	J Med Chem (2003) 46: 5139-5152 [PMID:14613317]
ChEMBL	Displacement of [3H]CP-55940 from human CB1 receptor expressed in CHO cells	B	7.6	pKi	25	nM	Ki	Eur J Med Chem (2008) 43: 2627-2638 [PMID:18342403]
ChEMBL	In vitro displacement of CP-55940 binding to human CB1 receptor expressed in CHO cells	B	7.6	pKi	25	nM	Ki	J Med Chem (2005) 48: 1823-1838 [PMID:15771428]
ChEMBL	Displacement of specific CP-55940 binding in CHO cells stably transfected with human cannabinoid receptor 1	B	7.6	pKi	25	nM	Ki	Bioorg Med Chem Lett (2005) 15: 4794-4798 [PMID:16140010]
ChEMBL	Displacement of CP-55940 binding from recombinant human cannabinoid receptor 1 expressed in CHO cells	B	7.6	pKi	25	nM	Ki	J Med Chem (2004) 47: 627-643 [PMID:14736243]
ChEMBL	Displacement of [3H]CP-55940 from human CB1 receptor expressed in CHO cells	B	7.6	pKi	25	nM	Ki	Bioorg Med Chem Lett (2010) 20: 2770-2775 [PMID:20363132]
ChEMBL	Antagonist activity at human CB1R expressed in CHO-K1 cell membranes assessed as stimulation of [35S]-GTPgammaS binding by liquid scintillation counting method	F	7.7	pKi	20	nM	Ki	J Med Chem (2022) 65: 2374-2387 [PMID:35084860]
ChEMBL	Displacement of [3H]WIN-55212-2 from human CB1 receptor expressed in HEK293 cells	B	7.74	pKi	18	nM	Ki	J Med Chem (2006) 49: 5969-5987 [PMID:17004712]
ChEMBL	Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells	B	7.8	pKi	16	nM	Ki	Bioorg Med Chem Lett (2007) 17: 6505-6510 [PMID:17942307]
ChEMBL	Ability to displace [3H]CP-55940 from the membranes prepared from HEK cell line with F3.36 (201)A mutant Cannabinoid receptor 1	B	7.85	pKi	14	nM	Ki	J Med Chem (2003) 46: 5139-5152 [PMID:14613317]
ChEMBL	Displacement of [3H]CP55,940 from human CB1 receptor expressed in CHO cells after 2 hrs by liquid scintillation counter	B	7.9	pKi	12.6	nM	Ki	J Med Chem (2012) 55: 7967-7977 [PMID:22916707]
ChEMBL	Displacement of [3H]CP55,940 from recombinant human CB1 receptor expressed in CHO cells after 2 hrs by liquid scintillation counting	B	7.9	pKi	12.6	nM	Ki	ACS Med Chem Lett (2013) 4: 41-45 [PMID:24900561]
ChEMBL	Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells	B	7.92	pKi	12	nM	Ki	Bioorg Med Chem (2009) 17: 5549-5564 [PMID:19595596]
ChEMBL	Displacement of [3H]CP55940 from human recombinant CB1 receptor transfected in HEK cell membrane	B	7.92	pKi	12	nM	Ki	Eur J Med Chem (2012) 58: 30-43 [PMID:23085772]
ChEMBL	Displacement of [3H]CP-55,940 from human recombinant CB1 receptor transfected in HEK cells	B	7.92	pKi	12	nM	Ki	J Med Chem (2012) 55: 5391-5402 [PMID:22548457]
ChEMBL	Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells	B	7.92	pKi	12	nM	Ki	J Med Chem (2011) 54: 5444-5453 [PMID:21702498]
ChEMBL	Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells	B	7.92	pKi	12	nM	Ki	J Med Chem (2008) 51: 5075-5084 [PMID:18680276]
ChEMBL	Displacement of [3H]CP-55,940 from recombinant human CB1 receptor transfected in HEK cells	B	7.92	pKi	12	nM	Ki	Eur J Med Chem (2010) 45: 5878-5886 [PMID:20943290]
ChEMBL	Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK cells	B	7.92	pKi	12	nM	Ki	J Med Chem (2010) 53: 5915-5928 [PMID:20718492]
ChEMBL	Evaluated for binding affinity towards human Cannabinoid receptor 1	B	7.92	pKi	12	nM	Ki	Bioorg Med Chem Lett (2004) 14: 1151-1154 [PMID:14980654]
ChEMBL	Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells	B	7.92	pKi	12	nM	Ki	J Med Chem (2008) 51: 1560-1576 [PMID:18293908]
ChEMBL	Displacement of [3H]CP-55940 from human CB1 receptor expressed in CHO cell membranes after 1 hr by scintillation counting analysis	B	7.96	pKi	11	nM	Ki	ACS Med Chem Lett (2013) 4: 387-392 [PMID:24729834]
ChEMBL	Displacement of [3H]CP-55,940 from CB1 receptor (unknown origin) after 1 hr by scintillation counting analysis	B	7.97	pKi	10.6	nM	Ki	J Med Chem (2013) 56: 2045-2058 [PMID:23406429]
ChEMBL	Displacement of [3H]CP55940 from human CB1 receptor expressed in CHO cells incubated for 1 hr	B	7.97	pKi	10.6	nM	Ki	J Med Chem (2012) 55: 9973-9987 [PMID:23072339]
ChEMBL	Ability to displace [3H]CP-55940 from the membranes prepared from HEK cell line with F3.25 (190)A mutant Cannabinoid receptor 1	B	8.02	pKi	9.6	nM	Ki	J Med Chem (2003) 46: 5139-5152 [PMID:14613317]
ChEMBL	Compound was evaluated for affinity towards human Cannabinoid receptor 1 using [3H]- SR-141716A as radioligand	B	8.05	pKi	8.9	nM	Ki	J Med Chem (2002) 45: 1748-1756 [PMID:11960486]
ChEMBL	Ability to displace [3H]-SR- 141716A binding to human CB1 receptor expressed in CHO cell membranes	B	8.05	pKi	8.9	nM	Ki	Bioorg Med Chem Lett (1999) 9: 2233-2236 [PMID:10465552]
ChEMBL	Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells	B	8.1	pKi	8	nM	Ki	Bioorg Med Chem (2008) 16: 7510-7515 [PMID:18579386]
ChEMBL	Displacement of [3H]-CP55940 from human CB1 receptor after 90 mins by liquid scintillation spectrophotometer analysis	B	8.14	pKi	7.3	nM	Ki	Bioorg Med Chem (2013) 21: 1708-1716 [PMID:23434135]
ChEMBL	Displacement of [3H]-CP55940 from CB1 receptor after 90 mins by liquid scintillation counting	B	8.14	pKi	7.3	nM	Ki	ACS Med Chem Lett (2011) 2: 793-797 [PMID:24936232]
ChEMBL	Displacement of [3H]-CP55940 from human CB1 receptor expressed in HEK293 EBNA cell membranes after 90 mins by liquid scintillation counting method	B	8.14	pKi	7.3	nM	Ki	J Med Chem (2016) 59: 6753-6771 [PMID:27309150]
ChEMBL	Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells	B	8.15	pKi	7.1	nM	Ki	J Med Chem (2006) 49: 5969-5987 [PMID:17004712]
ChEMBL	Displacement of [3H]- CP55940 from human CB1R expressed in CHO-K1 cells membrane by Cheng-Prusoff equation analysis	B	8.15	pKi	7	nM	Ki	J Med Chem (2022) 65: 2374-2387 [PMID:35084860]
ChEMBL	Displacement of [3H]CP55940 from human CB1 receptor expressed in CHO-K1 cells	B	8.21	pKi	6.2	nM	Ki	J Med Chem (2012) 55: 2820-2834 [PMID:22372835]
ChEMBL	Displacement of [3H]CP55940 from human CB1 receptor expressed in CHO cell membranes	B	8.21	pKi	6.2	nM	Ki	Bioorg Med Chem (2016) 24: 1063-1070 [PMID:26827137]
ChEMBL	Displacement of [3H]CP55940 from human CB1 receptor expressed in HEK293 cells	B	8.21	pKi	6.18	nM	Ki	J Med Chem (2010) 53: 7048-7060 [PMID:20845959]
ChEMBL	Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells	B	8.21	pKi	6.18	nM	Ki	J Med Chem (2008) 51: 3526-3539 [PMID:18512901]
ChEMBL	Displacement of [3H]CP-55940 from human CB1R expressed in HEK293 cells	B	8.22	pKi	6	nM	Ki	J Med Chem (2008) 51: 2115-2127 [PMID:18335976]
ChEMBL	Displacement of [3H]CP55940 from human CB1 receptor expressed in CHOK1 cells after 1 hr by liquid scintillation counting analysis	B	8.23	pKi	5.9	nM	Ki	J Med Chem (2013) 56: 9874-9896 [PMID:24175572]
ChEMBL	Binding affinity to human CB1 receptor	B	8.25	pKi	5.6	nM	Ki	Bioorg Med Chem Lett (2009) 19: 1022-1025 [PMID:19095444]
ChEMBL	Inhibition of [3H]SR-141,716A binding to human CB1 receptor expressed in CHO cells	B	8.27	pKi	5.4	nM	Ki	J Med Chem (2005) 48: 2509-2517 [PMID:15801840]
ChEMBL	Displacement of [3H]SR141716A from human CB1 receptor expressed in CHO cells	B	8.27	pKi	5.4	nM	Ki	J Med Chem (2005) 48: 7486-7490 [PMID:16279809]
ChEMBL	Displacement of [3H]SR-141716A from human CB1 receptor	B	8.27	pKi	5.37	nM	Ki	J Med Chem (2006) 49: 70-79 [PMID:16392793]
ChEMBL	Ability to displace [3H]CP-55940 from the membranes prepared from HEK cell line with wild type Cannabinoid receptor 1	B	8.32	pKi	4.8	nM	Ki	J Med Chem (2003) 46: 5139-5152 [PMID:14613317]
ChEMBL	Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells	B	8.62	pKi	2.4	nM	Ki	J Med Chem (2008) 51: 2439-2446 [PMID:18363352]
ChEMBL	Binding affinity to human CB1 receptor	B	8.62	pKi	2.4	nM	Ki	Bioorg Med Chem Lett (2010) 20: 1278-1283 [PMID:20018510]
ChEMBL	Displacement of [3H]SR-141716 from human CB1 receptor transfected in HEK293 cells	B	8.68	pKi	2.1	nM	Ki	Bioorg Med Chem Lett (2006) 16: 731-736 [PMID:16263283]
GtoPdb	-	-	8.7	pKi	1.99	nM	Ki	Mol Pharmacol (1995) 48: 443-50 [PMID:7565624]; J Pharmacol Exp Ther (1996) 278: 989-99 [PMID:8819477]; J Pharmacol Exp Ther (1998) 284: 291-7 [PMID:9435190]; FEBS Lett (1994) 350: 240-4 [PMID:8070571]; J Pharmacol Exp Ther (2003) 306: 363-70 [PMID:12663689]
ChEMBL	Displacement of [3H]SR141716 from human recombinant CB1 receptor expressed in HEK293 cells	B	8.7	pKi	2	nM	Ki	J Med Chem (2009) 52: 1975-1982 [PMID:19338356]
ChEMBL	Binding affinity to CB1 receptor	B	8.7	pKi	1.98	nM	Ki	J Med Chem (2008) 51: 2439-2446 [PMID:18363352]
ChEMBL	Antagonist activity at CB1 receptor (unknown origin)	B	8.7	pKi	1.98	nM	Ki	Eur J Med Chem (2014) 74: 73-84 [PMID:24445310]
ChEMBL	Displacement of [3H]rimonabant from human CB1 receptor expressed in HEK293 cells by liquid scintillation counting	B	8.72	pKi	1.9	nM	Ki	Bioorg Med Chem Lett (2009) 19: 4183-4190 [PMID:19520572]
ChEMBL	Displacement of radioligand from human CB1 receptor expressed in HEK293 cells	B	8.74	pKi	1.8	nM	Ki	Bioorg Med Chem Lett (2008) 18: 1199-1206 [PMID:18083560]
ChEMBL	Binding affinity to CB1 receptor	B	8.74	pKi	1.8	nM	Ki	J Med Chem (2009) 52: 2652-2655 [PMID:19351113]
ChEMBL	Displacement of [3H]SR141716A form human CB1 receptor expressed in HEK293 cells after 60 mins by beta counting	B	8.74	pKi	1.8	nM	Ki	ACS Med Chem Lett (2012) 3: 397-401 [PMID:24900484]
ChEMBL	Antagonist activity at human CB1 receptor transfected in CHO-K1cells by GTPgamma[35S] binding assay	F	8.8	pKi	1.6	nM	Ki	Bioorg Med Chem Lett (2009) 19: 5351-5354 [PMID:19683918]
ChEMBL	Antagonist activity at human CB1 receptor expressed in CHOK1 cells assessed as inhibition of CP-55940-induced response after 10 mins by GTPgamma[35S] binding assay	F	8.8	pKi	1.6	nM	Ki	J Med Chem (2009) 52: 2652-2655 [PMID:19351113]
ChEMBL	Antagonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP-55940-induced [35S]GTPgammaS binding incubated for 10 mins prior to CP-55940-challenge measured after 1 hr by beta counting	F	8.8	pKi	1.6	nM	Ki	ACS Med Chem Lett (2012) 3: 397-401 [PMID:24900484]
ChEMBL	Displacement of [3H]CP55940 from CB1 receptor	B	8.85	pKi	1.4	nM	Ki	J Med Chem (2011) 54: 2961-2970 [PMID:21428406]
ChEMBL	Displacement of [3H]CP-55940 from CB1 receptor by scintillation counting	B	8.86	pKi	1.38	nM	Ki	Bioorg Med Chem Lett (2009) 19: 6209-6212 [PMID:19767206]
ChEMBL	Displacement of [3H]SR141716 from human CB1 receptor expressed in HEK293 cells	B	8.93	pKi	1.18	nM	Ki	J Med Chem (2010) 53: 7048-7060 [PMID:20845959]
ChEMBL	Displacement of [3H]SR141716 from human CB1 receptor expressed in CHO-K1 cells	B	8.93	pKi	1.18	nM	Ki	J Med Chem (2008) 51: 3526-3539 [PMID:18512901]
ChEMBL	Displacement of [3H]CP-559440 from human CB1 receptor expressed in HEK293 cells	B	8.96	pKi	1.1	nM	Ki	Bioorg Med Chem Lett (2007) 17: 2706-2711 [PMID:17383180]
ChEMBL	Functional activity at human CB1 receptor transfected in CHOK1 cells by [35SGTP]gammaS assay	F	9	pKi	1	nM	Ki	Bioorg Med Chem Lett (2006) 16: 731-736 [PMID:16263283]
ChEMBL	Displacement of [3H]SR141716A from human CB1 receptor expressed in CHO cells	B	9.03	pKi	0.93	nM	Ki	Bioorg Med Chem Lett (2011) 21: 2034-2039 [PMID:21334892]
ChEMBL	Displacement of [3H]SR141716A from human CB1 receptor expressed in HEK293 cells	B	9.05	pKi	0.9	nM	Ki	J Med Chem (2009) 52: 234-237 [PMID:19102698]
ChEMBL	Displacement of [3H]CP-55940 from human recombinant cannabinoid CB1 receptor expressed in CHO cells after 3 hrs by liquid scintillation counting	B	9.13	pKi	0.74	nM	Ki	Eur J Med Chem (2010) 45: 1133-1139 [PMID:20047779]
ChEMBL	Displacement of [3H]BMS-725519 from human CB1 receptor expressed in CHO cells after 90 mins by scintillation counting	B	9.14	pKi	0.73	nM	Ki	Bioorg Med Chem Lett (2011) 21: 6856-6860 [PMID:21962575]
ChEMBL	Displacement of [3H]-SR141716A from human CB1 receptor expressed in CHO cell membranes after 1 hr by liquid scintillation spectrometry	B	9.15	pKi	0.7	nM	Ki	Bioorg Med Chem (2018) 26: 4518-4531 [PMID:30077609]
ChEMBL	Antagonist activity at human CB1 receptor expressed in SF9 cells assessed as inhibition of CP-55940-stimulated GTPgammaS binding	F	9.37	pKi	0.43	nM	Ki	Bioorg Med Chem Lett (2008) 18: 3376-3381 [PMID:18448340]
ChEMBL	Binding affinity to human CB1 receptor by [35S]GTPgammaS binding assay	F	9.4	pKi	0.4	nM	Ki	J Med Chem (2008) 51: 5608-5616 [PMID:18754613]
ChEMBL	Antagonist activity against human CB1 receptor expressed in CHO-K1 cells by [35S]GTPgamma binding assay	F	9.72	pKi	0.19	nM	Ki	J Med Chem (2009) 52: 234-237 [PMID:19102698]
ChEMBL	Displacement of [3H]-CP55950 from human CB1 receptor expressed in CHO cell membranes after 3 hrs by scintillation counting method	B	6.8	pIC50	158.49	nM	IC50	J Med Chem (2018) 61: 1646-1663 [PMID:29400965]
ChEMBL	Antagonist activity at human CB1 receptor expressed in CHOK1 cells by luciferase assay	F	6.92	pIC50	120	nM	IC50	Bioorg Med Chem (2008) 16: 4035-4051 [PMID:18243711]
ChEMBL	Inverse agonist activity at human recombinant CB1 receptor expressed in CHO cells by luciferase reporter gene assay	F	6.97	pIC50	108	nM	IC50	Bioorg Med Chem (2010) 18: 1149-1162 [PMID:20045337]
ChEMBL	Inverse agonist activity at CB1 receptor assessed as repression of basal receptor activity by mammalian cell-based receptor selection and amplification technology method	F	7.2	pIC50	63.1	nM	IC50	J Med Chem (2009) 52: 1975-1982 [PMID:19338356]
ChEMBL	Inverse agonist activity against CB1 receptor expressed in human CHO cells assessed as effect on forskolin-stimulated cAMP level	F	7.29	pIC50	51	nM	IC50	Bioorg Med Chem Lett (2012) 22: 6173-6180 [PMID:22959249]
ChEMBL	Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells	B	7.82	pIC50	15	nM	IC50	J Med Chem (2008) 51: 5397-5412 [PMID:18712856]
ChEMBL	Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells	B	7.82	pIC50	15	nM	IC50	Bioorg Med Chem Lett (2009) 19: 1022-1025 [PMID:19095444]
ChEMBL	Antagonist activity against CB1R (unknown origin) CHO cells stably expressing Galpha16 assessed as inhibition of CP55940-induced increase in intracellular calcium level pre-treated 10 mins before CP55940 stimulation by microplate reader based assay	F	7.87	pIC50	13.5	nM	IC50	J Med Chem (2015) 58: 5751-5769 [PMID:26151231]
ChEMBL	Displacement of [3H]CP-55940 from human recombinant CB1R expressed in HEK293 cells	B	7.88	pIC50	13.2	nM	IC50	J Med Chem (2009) 52: 4496-4510 [PMID:19530697]
ChEMBL	Antagonist activity at human CB1 receptor stably expressed in CHO cells co-expressing co-expressing Ga15/16 assessed as calcium current after 45 mins by fluo-4 AM assay	F	7.89	pIC50	13	nM	IC50	Eur J Med Chem (2014) 74: 73-84 [PMID:24445310]
ChEMBL	Antagonist activity against human CB1 receptor	F	7.95	pIC50	11.22	nM	IC50	Bioorg Med Chem Lett (2011) 21: 2034-2039 [PMID:21334892]
ChEMBL	Antagonist activity at human CB1 receptor expressed in CHO cell membranes assessed as reduction in GTPgammaS binding after 30 mins by microbeta counting method	F	8.01	pIC50	9.7	nM	IC50	Bioorg Med Chem (2018) 26: 295-307 [PMID:29229226]
ChEMBL	Displacement of [3H]-CP-55940 from human CB1 receptor expressed in CHO-K1 cell membranes	B	8.16	pIC50	6.9	nM	IC50	J Med Chem (2018) 61: 10276-10298 [PMID:30339387]
ChEMBL	Inhibitory concentration tested against human Cannabinoid receptor 1 (hCB1)	B	8.21	pIC50	6.2	nM	IC50	Bioorg Med Chem Lett (2005) 15: 645-651 [PMID:15664830]
ChEMBL	Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in CHO cells	B	8.21	pIC50	6.1	nM	IC50	Bioorg Med Chem Lett (2007) 17: 2184-2187 [PMID:17293109]
ChEMBL	Inhibition of [3H]CP-55940 binding to human recombinant CB1 receptor in CHO cells	B	8.21	pIC50	6.1	nM	IC50	J Med Chem (2006) 49: 7584-7587 [PMID:17181138]
ChEMBL	Inhibitory concentration against human recombinant cannabinoid receptor type 1 expressed in Chinese Hamster Ovary (CHO) cells	B	8.22	pIC50	6	nM	IC50	Bioorg Med Chem Lett (2005) 15: 1441-1446 [PMID:15713403]
ChEMBL	Displacement of [3H]CP-55940 from human CB1 receptor expressed in COS7 cells	B	8.29	pIC50	5.1	nM	IC50	Bioorg Med Chem Lett (2010) 20: 453-457 [PMID:20015647]
ChEMBL	Displacement of [3H]-rimonabant from human CB1 receptor expressed in CHO cell membranes after 60 mins by TopCount method	B	8.34	pIC50	4.6	nM	IC50	J Med Chem (2018) 61: 10276-10298 [PMID:30339387]
ChEMBL	Antagonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP-55940-induced GTPgammaS binding	F	8.35	pIC50	4.5	nM	IC50	Bioorg Med Chem Lett (2010) 20: 453-457 [PMID:20015647]
ChEMBL	Antagonist activity at human recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP-55940-stimulated GTPgammaS binding	F	8.35	pIC50	4.5	nM	IC50	Bioorg Med Chem Lett (2010) 20: 26-30 [PMID:19954978]
ChEMBL	Antagonist activity at CB1 receptor transfected in CHO cells expressing apoaequorin as a reporter for G-protein-coupled receptor-mediated calcium signaling by bioluminescence assay	F	8.4	pIC50	4	nM	IC50	Bioorg Med Chem Lett (2011) 21: 1962-1964 [PMID:21376588]
ChEMBL	Antagonist activity at human cannabinoid CB1 receptor expressed in CHO cells coexpressing Galpha15/16 assessed as inhibition of CP-55940-induced Ca2+ release after 10 mins by micro plate reader	F	8.49	pIC50	3.2	nM	IC50	Eur J Med Chem (2010) 45: 1133-1139 [PMID:20047779]
ChEMBL	Antagonist activity at CB1 receptor by [35S]GTP-gamma-S binding assay	F	8.52	pIC50	3	nM	IC50	Bioorg Med Chem (2007) 15: 4077-4084 [PMID:17433696]
ChEMBL	Inverse agonist activity at human CB1 receptor expressed in CHO-K1 cells by GTPgammaS binding assay	F	8.54	pIC50	2.9	nM	IC50	Bioorg Med Chem Lett (2010) 20: 453-457 [PMID:20015647]
ChEMBL	Binding affinity to human CB1 receptor by [35S]GTPgammaS binding assay	F	8.66	pIC50	2.2	nM	IC50	J Med Chem (2008) 51: 5608-5616 [PMID:18754613]
ChEMBL	Agonist activity at human CB1 receptor assessed as stimulation of [35S]GTPgammaS binding	F	8.68	pIC50	2.1	nM	IC50	Bioorg Med Chem Lett (2010) 20: 479-482 [PMID:20005704]
ChEMBL	Inverse agonist at human CB1 receptor expressed in SF9 cells assessed as decrease in GTPgammaS level	F	8.87	pIC50	1.35	nM	IC50	Bioorg Med Chem Lett (2008) 18: 3376-3381 [PMID:18448340]
ChEMBL	Inverse agonist activity at human CB1 receptor expressed in HEK293 cells co-expressing Galphaq16 assessed as inhibition of calcium mobilization after 90 secs by calcein-4 AAM dye-based FLIPR assay	F	6.23	pEC50	586	nM	EC50	Bioorg Med Chem (2018) 26: 4518-4531 [PMID:30077609]
ChEMBL	Antagonist activity at human cannabinoid CB1 receptor expressed in CHOK1 cells assessed as cAMP activity	F	6.62	pEC50	240	nM	EC50	Bioorg Med Chem Lett (2009) 19: 2546-2550 [PMID:19328683]
ChEMBL	Inverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assay	B	7.3	pEC50	50.12	nM	EC50	Bioorg Med Chem Lett (2014) 24: 4209-4214 [PMID:25096297]
ChEMBL	Inverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assay	B	7.3	pEC50	50	nM	EC50	Bioorg Med Chem Lett (2014) 24: 4209-4214 [PMID:25096297]
ChEMBL	Agonist activity at human CB1 receptor expressed in CHO cell membranes after 90 mins by [35S]GTPgammaS binding assay	F	7.44	pEC50	36	nM	EC50	Eur J Med Chem (2018) 154: 155-171 [PMID:29793210]
ChEMBL	Antagonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of Eu-GTP binding	B	7.74	pEC50	18.2	nM	EC50	Bioorg Med Chem Lett (2009) 19: 1022-1025 [PMID:19095444]
ChEMBL	Antagonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of Eu-GTP binding	B	7.74	pEC50	18.2	nM	EC50	J Med Chem (2008) 51: 5397-5412 [PMID:18712856]
ChEMBL	Inverse agonist activity at human recombinant CB1R expressed in HEK293 cells assessed as inhibition of CP-55940-stimulated Eu-GTP binding	B	7.8	pEC50	15.7	nM	EC50	J Med Chem (2009) 52: 4496-4510 [PMID:19530697]
ChEMBL	Activity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assay	F	8	pEC50	10.1	nM	EC50	J Med Chem (2005) 48: 7486-7490 [PMID:16279809]
ChEMBL	Inverse agonist activity at human CB1 receptor expressed in CHO cells assessed as increase in intracellular calcium mobilization after 90 secs by Calcein-4 AM-staining based FLIPR assay	F	8.3	pEC50	5	nM	EC50	Bioorg Med Chem (2016) 24: 1063-1070 [PMID:26827137]
ChEMBL	Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as forskolin-stimulated cAMP accumulation after 30 mins by HTRF assay	F	8.39	pEC50	4.1	nM	EC50	ACS Med Chem Lett (2020) 11: 2504-2509 [PMID:33335674]
ChEMBL	Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assay	F	8.39	pEC50	4.1	nM	EC50	J Med Chem (2018) 61: 10276-10298 [PMID:30339387]
ChEMBL	Inverse agonist activity at human CB1 receptor by [35S]GTPgammaS incorporation assay	F	8.4	pEC50	4	nM	EC50	Bioorg Med Chem Lett (2009) 19: 4183-4190 [PMID:19520572]
ChEMBL	Inverse agonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgammaS incorporation assay	F	8.4	pEC50	4	nM	EC50	Bioorg Med Chem Lett (2008) 18: 1199-1206 [PMID:18083560]
ChEMBL	Antagonist activity at human CB1 receptor overexpressed in HEK cells assessed as [35S]GTPgamma binding after 1 hr by liquid scintillation counting analysis	F	8.82	pEC50	1.5	nM	EC50	J Med Chem (2013) 56: 9874-9896 [PMID:24175572]
ChEMBL	Inverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 mins	F	9.96	pEC50	0.11	nM	EC50	Eur J Med Chem (2010) 45: 1133-1139 [PMID:20047779]
CB1 receptor/Cannabinoid CB1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3037] [GtoPdb: 56] [UniProtKB: P47746]
ChEMBL	Antagonist activity at CB1 receptor in ICR mouse vas deferens assessed as reversal of WIN-55212-2-induced effect on electrically-stimulated contraction	F	6.72	pKd	190.55	nM	Kd	Bioorg Med Chem (2007) 15: 7480-7493 [PMID:17870539]
ChEMBL	Displacement of [3H]CP55940 from mouse brain CB1R expressed in CHOK1 cell membranes	B	8.3	pKi	5	nM	Ki	J Med Chem (2017) 60: 1126-1141 [PMID:28085283]
ChEMBL	Displacement of [3H]-CP55,940 from CB1 receptor in mouse whole brain membranes after 60 mins by liquid scintillation spectrometry	B	8.55	pKi	2.82	nM	Ki	Eur J Med Chem (2016) 121: 194-208 [PMID:27240274]
ChEMBL	Displacement of [3H]CP-55940 from CB1 receptor in CD1 mouse brain	B	8.74	pKi	1.8	nM	Ki	J Med Chem (2005) 48: 7351-7362 [PMID:16279795]
ChEMBL	Displacement of [3H]-CP55,940 from CB1 receptor in CD1 mouse brain membranes after 60 mins by liquid scintillation counting method	B	8.74	pKi	1.8	nM	Ki	Eur J Med Chem (2016) 121: 194-208 [PMID:27240274]
ChEMBL	Displacement of [3H]CP55940 from CB1 receptor in CD1 mouse brain membrane without cerebellum by liquid scintillation counting analysis	B	8.82	pKi	1.5	nM	Ki	Eur J Med Chem (2013) 62: 256-269 [PMID:23357307]
ChEMBL	Inverse agonist at mouse brain CB1R expressed in CHOK1 cell membranes assessed as inhibition of CP55940-stimulated [35S]GTP-gammaS binding measured after 60 mins by scintillation spectrometry	B	7.6	pIC50	25	nM	IC50	J Med Chem (2017) 60: 1126-1141 [PMID:28085283]
ChEMBL	Agonist activity at CB1 receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated contraction	F	5.05	pEC50	8990	nM	EC50	Bioorg Med Chem (2007) 15: 7480-7493 [PMID:17870539]
CB1 receptor/Cannabinoid CB1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272]
ChEMBL	Binding affinity against Cannabinoid receptor 1 in rat forebrain	B	7.94	pKi	11.5	nM	Ki	J Med Chem (1999) 42: 769-776 [PMID:10052983]
ChEMBL	Displacement of [3H]SR141716A from CB1 receptor in rat cerebellum membrane	B	8.19	pKi	6.5	nM	Ki	Bioorg Med Chem Lett (2009) 19: 3471-3475 [PMID:19457667]
ChEMBL	Binding affinity in a competition assay by displacement of [3H]CP-55940 from Cannabinoid receptor 1 in rat whole brain membrane preparation	B	8.21	pKi	6.18	nM	Ki	J Med Chem (2002) 45: 2708-2719 [PMID:12061874]
ChEMBL	Displacement of [3H]SR141716A from CB1 receptor in rat cerebellum by scintillation spectrometry	B	8.22	pKi	6	nM	Ki	J Med Chem (2009) 52: 4329-4337 [PMID:19527048]
ChEMBL	Displacement of [3H]WIN-55212-2 from CB1 receptor in rat cerebellar membrane by liquid scintillation counting	B	8.7	pKi	1.98	nM	Ki	Bioorg Med Chem Lett (2009) 19: 639-643 [PMID:19128970]
ChEMBL	Binding affinity was determined by using a competition assay with [125 I]- AM251 against rat cannabinoid receptor 1	B	8.74	pKi	1.8	nM	Ki	J Med Chem (2003) 46: 642-645 [PMID:12570386]
ChEMBL	Inhibition of [3H]CP-55940 binding to cannabinoid receptor 1 in rat brain membranes.	B	8.89	pKi	1.3	nM	Ki	J Med Chem (2002) 45: 1447-1459 [PMID:11906286]
ChEMBL	Binding affinity in a competition assay by displacement of [3H]- SR-141716 from Cannabinoid receptor 1 in rat whole brain membrane preparation	B	8.93	pKi	1.18	nM	Ki	J Med Chem (2002) 45: 2708-2719 [PMID:12061874]
ChEMBL	Displacement of [3H]SR141716A from rat brain CB1 receptor	B	9.05	pKi	0.9	nM	Ki	Bioorg Med Chem Lett (2009) 19: 5351-5354 [PMID:19683918]
ChEMBL	Displacement of [3H]SR141716A from CB1 receptor in rat brain	B	9.19	pKi	0.65	nM	Ki	J Med Chem (2009) 52: 234-237 [PMID:19102698]
ChEMBL	Antagonist activity at rat CB1 receptor in SF9 cells assessed as inhibition of CP-55940-stimulated GTPgammaS binding	F	9.51	pKi	0.31	nM	Ki	Bioorg Med Chem Lett (2008) 18: 3376-3381 [PMID:18448340]
ChEMBL	Displacement of [3H]SR141716A from CB1 receptor in Sprague-Dawley rat cerebellum membrane	B	5.41	pIC50	3920	nM	IC50	Eur J Med Chem (2008) 43: 513-539 [PMID:17582659]
ChEMBL	Displacement of [3H]SR141716A from rat brain CB1 receptor at pH 7.4 after 1 hr by liquid scintillation counting	B	7.74	pIC50	18	nM	IC50	Bioorg Med Chem Lett (2011) 21: 4913-4918 [PMID:21741835]
ChEMBL	Displacement of [3H]WIN-55212-2 from CB1 receptor in rat cerebellar membrane by liquid scintillation counting	B	8.28	pIC50	5.2	nM	IC50	Bioorg Med Chem Lett (2009) 19: 639-643 [PMID:19128970]
ChEMBL	Displacement of [3H]CP-55940 from CB1R in Sprague-Dawley rat cerebellar membrane	B	8.3	pIC50	5	nM	IC50	Bioorg Med Chem (2009) 17: 3080-3092 [PMID:19328001]
ChEMBL	Displacement of [3H]CP-55940 from CB1 receptor in Sprague-Dawley rat cerebellar membrane	B	8.3	pIC50	5	nM	IC50	Bioorg Med Chem Lett (2009) 19: 142-145 [PMID:19022666]
ChEMBL	Displacement of [3H]CP-55940 from cannabinoid CB1 receptor in Sprague-Dawley rat cerebellar membrane by liquid scintillation spectrometry	B	8.3	pIC50	5	nM	IC50	Bioorg Med Chem Lett (2009) 19: 1899-1902 [PMID:19269817]
ChEMBL	Displacement of [3H]CP-55940 from cannabinoid CB1 receptor in Sprague-Dawley rat cerebellar membrane by liquid scintillation spectrometry	B	8.3	pIC50	5	nM	IC50	Bioorg Med Chem Lett (2009) 19: 4692-4697 [PMID:19596576]
ChEMBL	Displacement of [3H]CP-55940 from CB1 receptor in Sprague-Dawley rat cerebellar membrane	B	8.3	pIC50	5	nM	IC50	Bioorg Med Chem Lett (2009) 19: 6632-6636 [PMID:19850473]
ChEMBL	Displacement of [3H]CP-55940 from CB1 receptor in Sprague-Dawley rat cerebellum after 1 hr by liquid scintillation counting	B	8.34	pIC50	4.53	nM	IC50	Bioorg Med Chem (2010) 18: 6377-6388 [PMID:20673729]
ChEMBL	Displacement of [3H]CP-55940 from CB1 receptor in Sprague-Dawley rat cerebellar membrane	B	8.34	pIC50	4.53	nM	IC50	Bioorg Med Chem (2010) 18: 1149-1162 [PMID:20045337]
ChEMBL	Displacement of [3H]CP-55940 from CB1 receptor in Sprague-Dawley rat cerebellum by liquid scintillation spectrometry	B	8.34	pIC50	4.53	nM	IC50	J Med Chem (2008) 51: 7216-7233 [PMID:18954042]
ChEMBL	Inhibition of cannabinoid CB1 receptor in Sprague-Dawley rat brain	B	8.35	pIC50	4.5	nM	IC50	Bioorg Med Chem Lett (2008) 18: 2385-2389 [PMID:18337096]
ChEMBL	Binding affinity to CB1 receptor in rat brain synaptosomal membranes	B	8.6	pIC50	2.5	nM	IC50	Bioorg Med Chem Lett (2010) 20: 4573-4577 [PMID:20584609]
ChEMBL	Displacement of [3H]CP-55940 from CB1 receptor in Sprague-Dawley rat cerebella membrane	B	8.72	pIC50	1.9	nM	IC50	Bioorg Med Chem (2008) 16: 4035-4051 [PMID:18243711]
ChEMBL	Antagonist activity at rat brain CB1 receptor assessed as inhibition of [35S]GTPgammaS binding	F	4.25	pEC50	56305	nM	EC50	J Med Chem (2010) 53: 7048-7060 [PMID:20845959]
ChEMBL	Displacement of [3H]SR141716 from Long-Evans rat striatal membrane CB1 receptor	B	9.77	pEC50	0.17	nM	EC50	Proc Natl Acad Sci U S A (2007) 104: 20588-20593 [PMID:18077343]
CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
ChEMBL	Binding affinity towards cloned human cannabinoid receptor 2	B	2.85	pKi	2.85	nM	Log Ki	J Med Chem (2000) 43: 2300-2309 [PMID:10882356]
ChEMBL	Displacement of [3H]-CP55940 from human CB2 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method	B	4.4	pKi	>40000	nM	Ki	J Med Chem (2016) 59: 6753-6771 [PMID:27309150]
ChEMBL	Displacement of [3H]-CP55940 from human CB2 receptor expressed in CHO cell membranes after 1 hr by liquid scintillation spectrometry	B	5.11	pKi	7700	nM	Ki	Bioorg Med Chem (2018) 26: 4518-4531 [PMID:30077609]
ChEMBL	Displacement of [3H]WIN-552122 from human recombinant CB2 receptor expressed in CHOK1 cells	B	5.7	pKi	1990	nM	Ki	J Med Chem (2007) 50: 5951-5966 [PMID:17979261]
ChEMBL	Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK293 cells	B	5.79	pKi	1640	nM	Ki	Bioorg Med Chem Lett (2007) 17: 6505-6510 [PMID:17942307]
ChEMBL	In vitro displacement of CP-55940 binding to human CB2 receptor expressed in CHO cells	B	5.8	pKi	1580	nM	Ki	J Med Chem (2005) 48: 1823-1838 [PMID:15771428]
ChEMBL	Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHO cells	B	5.8	pKi	1580	nM	Ki	Bioorg Med Chem Lett (2010) 20: 2770-2775 [PMID:20363132]
ChEMBL	Affinity to displace CP-55940 binding from Cannabinoid receptor 2 of human expressed in CHO cells	B	5.8	pKi	1580	nM	Ki	J Med Chem (2004) 47: 627-643 [PMID:14736243]
ChEMBL	Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHO cells	B	5.8	pKi	1580	nM	Ki	Eur J Med Chem (2008) 43: 2627-2638 [PMID:18342403]
ChEMBL	Displacement of specific CP-55940 binding in CHO cells stably transfected with human cannabinoid receptor 2	B	5.8	pKi	1580	nM	Ki	Bioorg Med Chem Lett (2005) 15: 4794-4798 [PMID:16140010]
ChEMBL	Binding affinity to CB2 receptor	B	5.8	pKi	1569	nM	Ki	J Med Chem (2009) 52: 2652-2655 [PMID:19351113]
ChEMBL	Displacement of [3H]-CP55,940 from human CB2 receptor transfected in CHO cell membranes after 60 mins by liquid scintillation spectrometry	B	5.85	pKi	1400	nM	Ki	Eur J Med Chem (2016) 121: 194-208 [PMID:27240274]
ChEMBL	Binding affinity to CB2 receptor	B	6	pKi	>1000	nM	Ki	J Med Chem (2008) 51: 2439-2446 [PMID:18363352]
ChEMBL	Displacement of [3H]rimonabant from human CB2 receptor expressed in HEK293 cells by liquid scintillation counting	B	6	pKi	>1000	nM	Ki	Bioorg Med Chem Lett (2009) 19: 4183-4190 [PMID:19520572]
ChEMBL	Displacement of [3H]- CP55940 from human CB2R expressed in CHO-K1 cells membrane by Cheng-Prusoff equation analysis	B	6	pKi	>1000	nM	Ki	J Med Chem (2022) 65: 2374-2387 [PMID:35084860]
ChEMBL	Displacement of [3H]CP-55940 from CB2 receptor by scintillation counting	B	6.03	pKi	927	nM	Ki	Bioorg Med Chem Lett (2009) 19: 6209-6212 [PMID:19767206]
ChEMBL	Displacement of [3H]CP55940 from CB2 receptor	B	6.03	pKi	927	nM	Ki	J Med Chem (2011) 54: 2961-2970 [PMID:21428406]
ChEMBL	Displacement of [3H]CP55,940 from human CB2 receptor expressed in CHO cells after 2 hrs by liquid scintillation counter	B	6.05	pKi	900	nM	Ki	J Med Chem (2012) 55: 7967-7977 [PMID:22916707]
ChEMBL	Displacement of [3H]CP55,940 from recombinant human CB2 receptor expressed in CHO cells after 2 hrs by liquid scintillation counting	B	6.05	pKi	900	nM	Ki	ACS Med Chem Lett (2013) 4: 41-45 [PMID:24900561]
ChEMBL	Displacement of [3H]CP55940 from human recombinant CB2 receptor expressed in Sf9 cells	B	6.07	pKi	851.14	nM	Ki	Bioorg Med Chem Lett (2011) 21: 2034-2039 [PMID:21334892]
ChEMBL	Antagonist activity at human CB2 receptor in SF9 cells assessed as inhibition of CP-55940-stimulated GTPgammaS binding	F	6.09	pKi	815	nM	Ki	Bioorg Med Chem Lett (2008) 18: 3376-3381 [PMID:18448340]
ChEMBL	Displacement of [3H]CP-55,940 from recombinant human CB2 receptor transfected in HEK cells	B	6.1	pKi	790	nM	Ki	Eur J Med Chem (2010) 45: 5878-5886 [PMID:20943290]
ChEMBL	Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells	B	6.1	pKi	790	nM	Ki	J Med Chem (2008) 51: 1560-1576 [PMID:18293908]
ChEMBL	Displacement of [3H]CP-55940 from human CB2 receptor expressed in HEK293 cells	B	6.1	pKi	790	nM	Ki	J Med Chem (2008) 51: 5075-5084 [PMID:18680276]
ChEMBL	Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells	B	6.1	pKi	790	nM	Ki	Bioorg Med Chem (2008) 16: 7510-7515 [PMID:18579386]
ChEMBL	Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells	B	6.1	pKi	790	nM	Ki	Bioorg Med Chem (2009) 17: 5549-5564 [PMID:19595596]
ChEMBL	Displacement of [3H]CP-55940 from human CB2 receptor expressed in HEK cells	B	6.1	pKi	790	nM	Ki	J Med Chem (2010) 53: 5915-5928 [PMID:20718492]
ChEMBL	Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells	B	6.1	pKi	790	nM	Ki	J Med Chem (2011) 54: 5444-5453 [PMID:21702498]
ChEMBL	Displacement of [3H]CP-55,940 from human recombinant CB2 receptor transfected in HEK cells	B	6.1	pKi	790	nM	Ki	J Med Chem (2012) 55: 5391-5402 [PMID:22548457]
ChEMBL	Displacement of [3H]CP55940 from human recombinant CB2 receptor transfected in HEK cell membranes	B	6.1	pKi	790	nM	Ki	Eur J Med Chem (2012) 58: 30-43 [PMID:23085772]
ChEMBL	Binding affinity to human CB2 receptor by [35S]GTPgammaS binding assay	F	6.16	pKi	697	nM	Ki	J Med Chem (2008) 51: 5608-5616 [PMID:18754613]
ChEMBL	Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHO cells	B	6.25	pKi	560	nM	Ki	J Med Chem (2008) 51: 2439-2446 [PMID:18363352]
ChEMBL	Binding affinity to human CB2 receptor	B	6.25	pKi	560	nM	Ki	Bioorg Med Chem Lett (2010) 20: 1278-1283 [PMID:20018510]
ChEMBL	Displacement of radioligand from human CB2 receptor expressed in HEK293 cells	B	6.26	pKi	554	nM	Ki	Bioorg Med Chem Lett (2008) 18: 1199-1206 [PMID:18083560]
ChEMBL	Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHO-K1 cells after 60 mins by beta counting	B	6.28	pKi	522	nM	Ki	ACS Med Chem Lett (2012) 3: 397-401 [PMID:24900484]
ChEMBL	Displacement of [3H]SR141716 from human recombinant CB2 receptor expressed in HEK293 cells	B	6.4	pKi	398.11	nM	Ki	J Med Chem (2009) 52: 1975-1982 [PMID:19338356]
ChEMBL	Displacement of [3H]CP 55940 from human CB2 receptor in cell free system	B	6.4	pKi	398.11	nM	Ki	Eur J Med Chem (2011) 46: 547-555 [PMID:21183257]
ChEMBL	Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHO-K1 cells	B	6.5	pKi	313	nM	Ki	J Med Chem (2008) 51: 3526-3539 [PMID:18512901]
ChEMBL	Displacement of [3H]CP55940 from human CB2 receptor expressed in CHOK1 cells	B	6.5	pKi	313	nM	Ki	J Med Chem (2010) 53: 7048-7060 [PMID:20845959]
ChEMBL	Binding affinity at cannabinoid receptor 2 in a competition assay with [3H]CP-55940 as radioligand	B	6.5	pKi	313	nM	Ki	J Med Chem (2002) 45: 2708-2719 [PMID:12061874]
ChEMBL	Displacement of [3H]CP55940 from CB2 receptor expressed in CHO-K1 cells	B	6.5	pKi	313	nM	Ki	J Med Chem (2012) 55: 2820-2834 [PMID:22372835]
ChEMBL	Displacement of [3H]CP55940 from human CB2 receptor expressed in CHO cell membranes	B	6.5	pKi	313	nM	Ki	Bioorg Med Chem (2016) 24: 1063-1070 [PMID:26827137]
ChEMBL	Displacement of [3H]CP-55940 from human recombinant cannabinoid CB2 receptor expressed in CHO cells after 3 hrs by liquid scintillation counting	B	6.9	pKi	126	nM	Ki	Eur J Med Chem (2010) 45: 1133-1139 [PMID:20047779]
ChEMBL	Displacement of [3H]-CP-55940 from human CB2 receptor expressed in HEK293T cell membranes by scintillation counting	B	8.96	pKi	1.1	nM	Ki	Bioorg Med Chem (2014) 22: 3245-3251 [PMID:24856183]
ChEMBL	Antagonist activity at CB2 receptor (unknown origin) stably expressed in CHO cells co-expressing co-expressing Ga15/16 assessed as calcium current after 45 mins by fluo-4 AM assay	F	5.01	pIC50	9800	nM	IC50	Eur J Med Chem (2014) 74: 73-84 [PMID:24445310]
ChEMBL	Antagonist activity against CB2R (unknown origin) CHO cells stably expressing Galpha16 assessed as inhibition of CP55940-induced increase in intracellular calcium level pre-treated 10 mins before CP55940 stimulation by microplate reader based assay	F	5.04	pIC50	9100	nM	IC50	J Med Chem (2015) 58: 5751-5769 [PMID:26151231]
ChEMBL	Binding affinity to human CB2 receptor by [35S]GTPgammaS binding assay	F	5.34	pIC50	4570	nM	IC50	J Med Chem (2008) 51: 5608-5616 [PMID:18754613]
ChEMBL	Displacement of [3H]CP55940 from human cannabinoid CB2 receptor expressed in CHO cells at pH 7.4 after 1 hr by liquid scintillation counting	B	5.7	pIC50	1980	nM	IC50	Bioorg Med Chem Lett (2011) 21: 4913-4918 [PMID:21741835]
ChEMBL	Displacement of [3H]CP-55940 from human CB2 receptor expressed in HEK293 cells	B	5.71	pIC50	1939.8	nM	IC50	J Med Chem (2008) 51: 5397-5412 [PMID:18712856]
ChEMBL	Displacement of [3H]WIN-55212-2 from human recombinant cannabinoid CB2 receptor expressed in CHOK1 cells by liquid scintillation spectrometry	B	5.75	pIC50	1760	nM	IC50	Bioorg Med Chem Lett (2009) 19: 1899-1902 [PMID:19269817]
ChEMBL	Displacement of [3H]WIN-55212-2 from human cannabinoid CB2 receptor expressed in CHO cells	B	5.75	pIC50	1760	nM	IC50	Bioorg Med Chem Lett (2008) 18: 2385-2389 [PMID:18337096]
ChEMBL	Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHOK1 cells	B	5.75	pIC50	1760	nM	IC50	Bioorg Med Chem (2008) 16: 4035-4051 [PMID:18243711]
ChEMBL	Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHO cells	B	5.75	pIC50	1760	nM	IC50	Bioorg Med Chem Lett (2009) 19: 142-145 [PMID:19022666]
ChEMBL	Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHOK1 cells by liquid scintillation spectrometry	B	5.75	pIC50	1760	nM	IC50	J Med Chem (2008) 51: 7216-7233 [PMID:18954042]
ChEMBL	Displacement of [3H]WIN-552122 from human CB2 receptor expressed in CHOK1 cells	B	5.75	pIC50	1760	nM	IC50	Bioorg Med Chem Lett (2009) 19: 6632-6636 [PMID:19850473]
ChEMBL	Displacement of [3H]WIN-55212-2 from human recombinant CB2 receptor expressed in CHO-K1 cell membrane	B	5.75	pIC50	1760	nM	IC50	Bioorg Med Chem (2010) 18: 1149-1162 [PMID:20045337]
ChEMBL	Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHO-K1 cells after 1 hr by liquid scintillation counting	B	5.75	pIC50	1760	nM	IC50	Bioorg Med Chem (2010) 18: 6377-6388 [PMID:20673729]
ChEMBL	Displacement of [3H]CP-55940 from human recombinant CB2R expressed in HEK293 cells	B	5.79	pIC50	1631.1	nM	IC50	J Med Chem (2009) 52: 4496-4510 [PMID:19530697]
ChEMBL	Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHO-K1 cells by liquid scintillation counting	B	6	pIC50	>1000	nM	IC50	Bioorg Med Chem Lett (2009) 19: 639-643 [PMID:19128970]
ChEMBL	Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in CHO cells	B	6.22	pIC50	603.3	nM	IC50	Bioorg Med Chem Lett (2007) 17: 2184-2187 [PMID:17293109]
ChEMBL	Inhibition of [3H]CP-55940 binding to human recombinant CB2 receptor in CHO cells	B	6.22	pIC50	600	nM	IC50	J Med Chem (2006) 49: 7584-7587 [PMID:17181138]
ChEMBL	Binding affinity to human CB2 receptor expressed in CHO cells by luciferase reporter gene assay	B	7.03	pIC50	92.5	nM	IC50	Bioorg Med Chem Lett (2009) 19: 6632-6636 [PMID:19850473]
ChEMBL	Displacement of [3H]CP-55940 from human CB2 receptor expressed in HEK293 cells	B	8.72	pIC50	1.9	nM	IC50	Bioorg Med Chem Lett (2009) 19: 1022-1025 [PMID:19095444]
ChEMBL	Antagonist activity at human cannabinoid CB2 receptor expressed in CHOK1 cells assessed as cAMP activity	F	4.51	pEC50	31210	nM	EC50	Bioorg Med Chem Lett (2009) 19: 2546-2550 [PMID:19328683]
ChEMBL	Inverse agonist activity at human CB2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assay	F	5	pEC50	>10000	nM	EC50	J Med Chem (2018) 61: 10276-10298 [PMID:30339387]
CB2 receptor/Cannabinoid CB2 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5373] [GtoPdb: 57] [UniProtKB: P47936]
ChEMBL	Binding affinity against Cannabinoid receptor 2 in mouse spleen	B	5.79	pKi	1640	nM	Ki	J Med Chem (1999) 42: 769-776 [PMID:10052983]
ChEMBL	Displacement of [3H]CP-55940 from CB2 receptor in CD1 mouse spleen	B	6.29	pKi	514	nM	Ki	J Med Chem (2005) 48: 7351-7362 [PMID:16279795]
ChEMBL	Displacement of [3H]-CP55,940 from CB2 receptor in CD1 mouse spleen homogenates after 60 mins by liquid scintillation counting method	B	6.29	pKi	514	nM	Ki	Eur J Med Chem (2016) 121: 194-208 [PMID:27240274]
ChEMBL	Displacement of [3H]CP55940 from CB2 receptor in CD1 mouse spleen membrane by liquid scintillation counting analysis	B	6.43	pKi	375	nM	Ki	Eur J Med Chem (2013) 62: 256-269 [PMID:23357307]
ChEMBL	Inverse agonist activity at C-terminally prolink-tagged mouse CB2 receptor expressed in CHOK1 cells harboring beta-galactosidase enzyme fused beta-arrestin assessed as increase in beta-arrestin recruitment after 90 mins by chemiluminescent assay	B	7.82	pEC50	15	nM	EC50	J Med Chem (2018) 61: 9841-9878 [PMID:29939744]
GPR55/G-protein coupled receptor 55 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075322] [GtoPdb: 109] [UniProtKB: Q9Y2T6]
ChEMBL	Agonist activity at GPR55 (unknown origin) expressed in CHO cells assessed as inhibition of LPI-induced beta-arrestin translocation after 90 mins by luminescence assay	B	5.7	pEC50	2010	nM	EC50	ACS Med Chem Lett (2013) 4: 41-45 [PMID:24900561]
ChEMBL	Agonist activity at human GPR55 expressed in CHO cells assessed as induction of LPI-induced beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method	B	5.7	pEC50	2010	nM	EC50	Medchemcomm (2014) 5: 632-649
GtoPdb	-	-	6.55	pEC50	280	nM	EC50	Br J Pharmacol (2010) 160: 604-14 [PMID:20136841]; J Pharmacol Exp Ther (2011) 337: 236-46 [PMID:21233197]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL	Inhibition of human ERG at holding potential of -80 mV to +40 mV	B	5.32	pIC50	4800	nM	IC50	Bioorg Med Chem (2010) 18: 6377-6388 [PMID:20673729]
ChEMBL	Inhibition of human ERG expressed in HEK293 cells assessed as inhibition of potassium channel current after 5 mins by patch clamp assay	B	5.55	pIC50	2790	nM	IC50	Bioorg Med Chem Lett (2011) 21: 4913-4918 [PMID:21741835]
GPR18/N-arachidonyl glycine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2384898] [GtoPdb: 89] [UniProtKB: Q14330]
ChEMBL	Antagonist activity at human GPR18 transfected in CHO cells assessed as delta9-THC-induced beta-arrestin recruitment incubated 60 mins prior to delta9-THC addition by beta-arrestin translocation assay	B	5	pIC50	10100	nM	IC50	J Med Chem (2013) 56: 4798-4810 [PMID:23679955]
ChEMBL	Agonist activity at human GPR18 expressed in CHO cells assessed as induction of beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method	B	5	pEC50	10100	nM	EC50	Medchemcomm (2014) 5: 632-649

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]