ChEMBL ligand: CHEMBL188 (WIN-55212-2)
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] CB2 receptor/Cannabinoid CB2 receptor in Rat [ChEMBL: CHEMBL2470] [GtoPdb: 57] [UniProtKB: Q9QZN9] There should be some charts here, you may need to enable JavaScript!
glycine receptor α2 subunit in Human [GtoPdb: 424] [UniProtKB: P23416] There should be some charts here, you may need to enable JavaScript!
glycine receptor α3 subunit in Human [GtoPdb: 425] [UniProtKB: O75311] 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	Binding affinity towards cloned human Cannabinoid receptor 1	B	0.28	pKi	0.28	nM	Log Ki	J Med Chem (2000) 43: 2300-2309 [PMID:10882356]
ChEMBL	Inhibition of [3H]SR-141,716A binding to human CB1 receptor expressed in CHO cells	B	5.42	pKi	3802	nM	Ki	J Med Chem (2005) 48: 2509-2517 [PMID:15801840]
ChEMBL	Displacement of [3H]SR141716A from human CB1 receptor	B	5.42	pKi	3802	nM	Ki	J Med Chem (2006) 49: 872-882 [PMID:16451053]
ChEMBL	Displacement of [3H]SR141716A from human CB1 receptor expressed in CHO cells	B	5.42	pKi	3800	nM	Ki	J Med Chem (2005) 48: 7486-7490 [PMID:16279809]
ChEMBL	Ability to displace [3H]CP-55940 from the membranes prepared from HEK cell line with W5 43(280)A mutant Cannabinoid receptor 1 at 5 uM	B	6.7	pKi	199	nM	Ki	J Med Chem (2003) 46: 5139-5152 [PMID:14613317]
ChEMBL	Ability to displace [3H]-SR- 141716A binding to human CB1 receptor expressed in CHO cell membranes	B	6.82	pKi	152.2	nM	Ki	Bioorg Med Chem Lett (1999) 9: 2233-2236 [PMID:10465552]
ChEMBL	Displacement of [3H]SR141716A from human recombinant CB1 receptor expressed in CHEM1 cells after 90 mins	B	6.82	pKi	150	nM	Ki	Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082]
ChEMBL	Displacement of [3H]CP-55940 from human CB1 receptor	B	6.85	pKi	140	nM	Ki	Bioorg Med Chem Lett (2008) 18: 3695-3700 [PMID:18522867]
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	6.97	pKi	107	nM	Ki	J Med Chem (2003) 46: 5139-5152 [PMID:14613317]
ChEMBL	Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in CHO cells	B	7.02	pKi	94.5	nM	Ki	Bioorg Med Chem Lett (2010) 20: 4992-4998 [PMID:20688519]
ChEMBL	Displacement of [3H]-CP55940 from human CB1 receptor expressed in CHO cells by liquid scintillation counting	B	7.1	pKi	79.43	nM	Ki	Eur J Med Chem (2011) 46: 5086-5098 [PMID:21885167]
ChEMBL	Displacement of [3H]-CP55940 from human recombinant CB1 receptor expressed in CHO cells membrane by scintillation counting	B	7.28	pKi	52.4	nM	Ki	J Med Chem (2012) 55: 8948-8952 [PMID:23017078]
ChEMBL	Displacement of [3H]CP55940 from human CB1 receptor expressed in CHO cell membranes after 1 hr by scintillation counting	B	7.28	pKi	52.4	nM	Ki	Eur J Med Chem (2012) 58: 396-404 [PMID:23151320]
ChEMBL	Displacement of [3H]-CP55940 from human CB1 receptor after 1 hr by scintillation counting analysis	B	7.28	pKi	52.4	nM	Ki	ACS Med Chem Lett (2015) 6: 198-203 [PMID:25699149]
ChEMBL	Displacement of [3H]CP55940 from human CB1 receptor expressed in HEK293 cells	B	7.34	pKi	46	nM	Ki	Bioorg Med Chem Lett (2012) 22: 3884-3889 [PMID:22607668]
ChEMBL	Displacement of [3H]-CP55940 from human CB1 receptor expressed in HEK293 EBNA cell membranes after 90 mins by liquid scintillation counting method	B	7.34	pKi	45.6	nM	Ki	J Med Chem (2016) 59: 6753-6771 [PMID:27309150]
ChEMBL	Displacement of [3H]CP55940 from human cannabinoid CB1 receptor expressed in HEK293 EBNA cells after 90 mins by liquid scintillation counting	B	7.34	pKi	45.6	nM	Ki	Eur J Med Chem (2013) 70: 111-119 [PMID:24141201]
ChEMBL	Displacement of [3H]CP55940 from human CB1 receptor expressed in HEK293 EBNA cells after 90 mins by liquid scintillation spectrophotometer	B	7.34	pKi	45.6	nM	Ki	J Med Chem (2016) 59: 1840-1853 [PMID:26789378]
ChEMBL	Displacement of [3H]-CP55940 from CB1 receptor after 90 mins by liquid scintillation counting	B	7.34	pKi	45.6	nM	Ki	ACS Med Chem Lett (2011) 2: 793-797 [PMID:24936232]
ChEMBL	Displacement of [3H]-CP55940 from human CB1 receptor after 90 mins by liquid scintillation spectrophotometer analysis	B	7.34	pKi	45.59	nM	Ki	Bioorg Med Chem (2013) 21: 1708-1716 [PMID:23434135]
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	7.35	pKi	45	nM	Ki	J Med Chem (2003) 46: 5139-5152 [PMID:14613317]
ChEMBL	Binding affinity to human CB1 receptor	B	7.39	pKi	40.9	nM	Ki	Bioorg Med Chem Lett (2007) 17: 6183-6187 [PMID:17884494]
ChEMBL	Binding affinity against human Cannabinoid receptor 1 expressed in CHO cells by using CP-55940 as Radioactive tracer	B	7.4	pKi	40	nM	Ki	Bioorg Med Chem Lett (2002) 12: 2399-2402 [PMID:12161142]
ChEMBL	Displacement of [3H]-CP55940 from human CB1 receptor transfected in HEK-293EBNA cells after 90 mins by luminescence counting analysis	B	7.44	pKi	36.2	nM	Ki	Eur J Med Chem (2014) 73: 56-72 [PMID:24378710]
ChEMBL	Displacement of [3H]-CP55940 from human CB1 receptor transfected in HEK293EBNA cell membranes after 90 mins by liquid scintillation counting analysis	B	7.44	pKi	36.2	nM	Ki	Eur J Med Chem (2015) 101: 651-667 [PMID:26209834]
ChEMBL	Displacement of [3H]CP55940 from human CB1R transfected in HEK293EBNA cell membranes incubated for 90 mins by Microbeta TriLux based luminescence analysis	B	7.44	pKi	36.2	nM	Ki	Bioorg Med Chem (2020) 28: 115672-115672 [PMID:32912440]
ChEMBL	Displacement of [3H]CP55940 from human CB1 receptor expressed in HEK293 EBNA cell membranes after 90 mins by liquid scintillation and luminescence counting method	B	7.54	pKi	28.8	nM	Ki	Eur J Med Chem (2017) 127: 398-412 [PMID:28088085]
ChEMBL	Displacement of [3H]CP,55-940 from recombinant human CB1 receptor expressed in HEK293 EBNA cell membranes after 90 mins by microbeta scintillation counting method	B	7.54	pKi	28.8	nM	Ki	Bioorg Med Chem (2018) 26: 295-307 [PMID:29229226]
ChEMBL	Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells	B	7.64	pKi	23	nM	Ki	J Nat Prod (2001) 64: 1322-1325 [PMID:11678659]
ChEMBL	Displacement of [3H]CP-55940 from human CB1 receptor expressed in COS cells	B	7.68	pKi	21	nM	Ki	J Med Chem (2005) 48: 7343-7350 [PMID:16279794]
ChEMBL	Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells	B	7.68	pKi	21	nM	Ki	Bioorg Med Chem Lett (2007) 17: 6505-6510 [PMID:17942307]
ChEMBL	Binding affinity to human recombinant CB1 receptor expressed in african green monkey COS cells by radioligand binding assay	B	7.68	pKi	21	nM	Ki	J Med Chem (2009) 52: 2506-2514 [PMID:19331413]
ChEMBL	Displacement of [3H]-CP55940 from human recombinant CB1 receptor expressed in HEK cell membrane	B	7.68	pKi	21	nM	Ki	Bioorg Med Chem (2020) 28: 115513-115513 [PMID:32340793]
ChEMBL	Displacement of [3H]CP-55,940 from human recombinant CB1 receptor expressed in HEK293 cell membranes	B	7.68	pKi	21	nM	Ki	Bioorg Med Chem (2014) 22: 4770-4783 [PMID:25065940]
ChEMBL	Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK cells	B	7.68	pKi	21	nM	Ki	Bioorg Med Chem (2007) 15: 5406-5416 [PMID:17561406]
ChEMBL	Displacement of [3H]CP-55940 from human recombinant CB1 receptor	B	7.68	pKi	21	nM	Ki	Bioorg Med Chem Lett (2006) 16: 138-141 [PMID:16213718]
ChEMBL	Displacement of [3H]CP55940 from human CB1 receptor expressed in human HEK293 cells	B	7.7	pKi	20	nM	Ki	J Med Chem (2011) 54: 8278-8288 [PMID:22044209]
ChEMBL	Displacement of [3H]-CP-55940 from human CB1 receptor expressed in CHO cell membranes after 1 hr by beta-counting analysis	B	7.72	pKi	19	nM	Ki	Eur J Med Chem (2019) 165: 347-362 [PMID:30583970]
ChEMBL	Binding affinity to human CB1 receptor	B	7.79	pKi	16.1	nM	Ki	Bioorg Med Chem Lett (2014) 24: 1322-1326 [PMID:24508127]
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	7.82	pKi	15	nM	Ki	J Med Chem (2003) 46: 5139-5152 [PMID:14613317]
ChEMBL	Displacement of [3H]CP-55940 from human CB1 receptor	B	7.85	pKi	14	nM	Ki	Bioorg Med Chem Lett (2007) 17: 4030-4034 [PMID:17521907]
ChEMBL	Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in CHO cells	B	7.88	pKi	13.3	nM	Ki	J Med Chem (2010) 53: 295-315 [PMID:19921781]
ChEMBL	Displacement of [3H]CP 55940 from human CB1 receptor in cell free system	B	7.88	pKi	13.3	nM	Ki	Eur J Med Chem (2011) 46: 547-555 [PMID:21183257]
ChEMBL	Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells	B	7.88	pKi	13.3	nM	Ki	J Med Chem (2008) 51: 1904-1912 [PMID:18311894]
ChEMBL	Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells	B	7.88	pKi	13.18	nM	Ki	J Med Chem (2008) 51: 1904-1912 [PMID:18311894]
ChEMBL	Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in CHO cells	B	7.88	pKi	13.18	nM	Ki	J Med Chem (2010) 53: 295-315 [PMID:19921781]
ChEMBL	Displacement of [3H]-CP55940 from human cannabinoid CB1 receptor expressed in Sf9 insect cells after 70 mins by scintillation counting	B	7.9	pKi	12.59	nM	Ki	Medchemcomm (2010) 1: 54-60
ChEMBL	Displacement of [3H]-CP55940 from human CB1 expressed in insect Sf9 membranes	B	7.9	pKi	12.59	nM	Ki	Bioorg Med Chem Lett (2010) 20: 7327-7330 [PMID:21074434]
ChEMBL	Displacement of [3H]CP55940 from human cannabinoid CB1 receptor expressed in insect Sf9 cells	B	7.9	pKi	12.59	nM	Ki	Bioorg Med Chem Lett (2011) 21: 1748-1753 [PMID:21316962]
ChEMBL	Displacement of [3H]CP-55,940 from human CB1 receptor expressed in CHO cell membranes after 90 mins by scintillation counting analysis	B	7.9	pKi	12.5	nM	Ki	Eur J Med Chem (2016) 113: 11-27 [PMID:26922225]
ChEMBL	Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in CHO cell membranes incubated for 90 mins by scintillation counting	B	7.91	pKi	12.4	nM	Ki	J Med Chem (2012) 55: 6608-6623 [PMID:22738271]
ChEMBL	Ability to displace [3H]CP-55940 from the membranes prepared from HEK cell line with wild type Cannabinoid receptor 1	B	7.92	pKi	12	nM	Ki	J Med Chem (2003) 46: 5139-5152 [PMID:14613317]
ChEMBL	Displacement of [3H]CP-55,940 from human recombinant CB1 receptor expressed in CHO cell membranes after 90 mins by scintillation counting analysis	B	7.95	pKi	11.3	nM	Ki	J Med Chem (2013) 56: 1098-1112 [PMID:23350768]
ChEMBL	Displacement of [3H]-CP-55,940 from human recombinant CB1 receptor expressed in HEK293 cells membrane incubated for 90 mins	B	8.04	pKi	9.2	nM	Ki	J Nat Prod (2011) 74: 2019-2022 [PMID:21902175]
ChEMBL	Displacement of [3H]CP55940 from human recombinant CB1 receptor expressed in HEK293 cells after 90 mins	B	8.04	pKi	9.2	nM	Ki	J Nat Prod (2011) 74: 2313-2317 [PMID:21999614]
ChEMBL	Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells after 90 mins	B	8.04	pKi	9.2	nM	Ki	Bioorg Med Chem Lett (2010) 20: 1210-1213 [PMID:20022504]
ChEMBL	Displacement of [3H]-CP55940 from human recombinant CB1 receptor expressed in HEK293 cells after 90 mins by scintillation counting analysis	B	8.06	pKi	8.8	nM	Ki	J Nat Prod (2015) 78: 1671-1682 [PMID:26149623]
ChEMBL	Displacement of [3H]CP55940 from beta-galactosidase reporter fused human CB1 receptor expressed in CHOK1 cell membranes after 1 hr by scintillation spectrometric analysis	B	8.06	pKi	8.72	nM	Ki	Medchemcomm (2017) 8: 1697-1705 [PMID:30108881]
ChEMBL	Binding affinity to human cannabinoid CB1 receptor	B	8.22	pKi	6.06	nM	Ki	Bioorg Med Chem (2009) 17: 2842-2851 [PMID:19278853]
ChEMBL	Displacement of [3H]-CP55940 from human CB1 receptor expressed in CHO cell membranes after 90 mins	B	8.6	pKi	2.5	nM	Ki	Eur J Med Chem (2018) 154: 155-171 [PMID:29793210]
ChEMBL	Displacement of [3H]CP55940 from human cannabinoid CB1 receptor expressed in CHO-K1 cells by liquid scintillation counting	B	8.6	pKi	2.5	nM	Ki	Eur J Med Chem (2014) 85: 77-86 [PMID:25072877]
ChEMBL	Displacement of [3H]CP55940 from recombinant human CB1R expressed in CHO cell membranes incubated for 90 mins	B	8.6	pKi	2.5	nM	Ki	Eur J Med Chem (2020) 208: 112858-112858 [PMID:33002735]
ChEMBL	Compound was evaluated for its binding affinity against Cannabinoid receptor 1 in Guinea pig ileum (GPI) using [3H]CP-55940 ligand	B	8.61	pKi	2.48	nM	Ki	J Med Chem (1998) 41: 5177-5187 [PMID:9857088]
GtoPdb	-	-	8.7	pKi	-	-	-	Mol Pharmacol (1995) 48: 443-50 [PMID:7565624]; J Pharmacol Exp Ther (1996) 278: 989-99 [PMID:8819477]; Biochim Biophys Acta (1996) 1307: 132-6 [PMID:8679694]
ChEMBL	Binding affinity of compound was determined against to human cannabinoid receptor 1 in chinese hamster ovary cells	B	8.72	pKi	1.9	nM	Ki	J Med Chem (2003) 46: 2110-2116 [PMID:12747783]
ChEMBL	Binding affinity to CB1 receptor	B	8.72	pKi	1.9	nM	Ki	J Med Chem (2008) 51: 5019-5034 [PMID:18680277]
ChEMBL	Binding affinity to CB1 receptor (unknown origin)	B	8.72	pKi	1.9	nM	Ki	J Med Chem (2013) 56: 7161-7176 [PMID:23672690]
ChEMBL	Binding affinity to human CB1 receptor by filtration assay	B	8.72	pKi	1.9	nM	Ki	Bioorg Med Chem (2012) 20: 2067-2081 [PMID:22341572]
ChEMBL	Binding affinity to CB1 receptor (unknown origin)	B	8.72	pKi	1.9	nM	Ki	J Med Chem (2013) 56: 8224-8256 [PMID:23865723]
ChEMBL	Binding affinity to CB1 receptor (unknown origin)	B	8.72	pKi	1.9	nM	Ki	Bioorg Med Chem Lett (2013) 23: 2019-2021 [PMID:23466226]
ChEMBL	Displacement of [3H]SR141716A from human recombinant CB1 receptor expressed in CHEM1 cells after 90 mins	B	6.7	pIC50	200	nM	IC50	Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082]
ChEMBL	Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells	B	6.85	pIC50	140	nM	IC50	J Med Chem (2007) 50: 3851-3856 [PMID:17630726]
ChEMBL	Binding affinity to human recombinant CB1 receptor	B	7.2	pIC50	63.1	nM	IC50	Bioorg Med Chem Lett (2007) 17: 272-277 [PMID:17027269]
ChEMBL	Displacement of [3H]-CP55,940 from human CB1 receptor expressed in HEK293S cell membranes by scintillation counting analysis	B	7.23	pIC50	59	nM	IC50	J Med Chem (2013) 56: 220-240 [PMID:23227781]
ChEMBL	Agonist activity at human CB1 in CHO cells assessed as inhibition of cAMP production	F	7.77	pIC50	17	nM	IC50	Bioorg Med Chem Lett (2007) 17: 4030-4034 [PMID:17521907]
ChEMBL	Inhibition of human cannabinoid CB1 receptor	B	7.8	pIC50	16	nM	IC50	Bioorg Med Chem (2010) 18: 7675-7699 [PMID:20875743]
ChEMBL	Agonist activity at CB1 receptor	F	8.7	pIC50	2	nM	IC50	Eur J Med Chem (2008) 43: 513-539 [PMID:17582659]
ChEMBL	Agonist activity at human CB1 receptor transfected in human U2OS cells assessed as beta-arrestin2-GFP aggregation after 40 mins	B	5.75	pEC50	1760	nM	EC50	J Med Chem (2013) 56: 3904-3921 [PMID:23621789]
ChEMBL	Agonist activity at human recombinant CB1 receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	F	6.5	pEC50	316.23	nM	EC50	Bioorg Med Chem Lett (2007) 17: 272-277 [PMID:17027269]
ChEMBL	Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma binding	F	6.95	pEC50	112	nM	EC50	Bioorg Med Chem Lett (2012) 22: 3884-3889 [PMID:22607668]
ChEMBL	Agonist activity at human CB1 receptor expressed in HEK293S cell membranes after 1 hr by GTPgamma[35S] binding assay	B	6.96	pEC50	110	nM	EC50	J Med Chem (2013) 56: 220-240 [PMID:23227781]
ChEMBL	Agonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assay	F	7.3	pEC50	50.12	nM	EC50	Bioorg Med Chem Lett (2010) 20: 7327-7330 [PMID:21074434]
ChEMBL	Agonist activity at human cannabinoid CB1 receptor expressed in CHO cells by luciferase reporter gene assay	F	7.3	pEC50	50.12	nM	EC50	Bioorg Med Chem Lett (2011) 21: 1748-1753 [PMID:21316962]
ChEMBL	Agonist activity at human cannabinoid CB1 receptor expressed in CHO cells co-expressing AP-1 response element after 5 hrs by luciferase reporter gene assay	B	7.3	pEC50	50.12	nM	EC50	Medchemcomm (2010) 1: 54-60
ChEMBL	Agonist activity at human CB1 receptor expressed in HEK293 cell membranes assessed as induction of [35S]-GTPgammaS binding after 60 mins by liquid scintillation spectrometric method	F	7.36	pEC50	44	nM	EC50	J Med Chem (2016) 59: 6753-6771 [PMID:27309150]
ChEMBL	Displacement of [3H]WIN-55212-2 from human CB1 receptor in HEK293 cells	B	7.42	pEC50	37.6	nM	EC50	J Nat Prod (2006) 69: 432-435 [PMID:16562853]
ChEMBL	Agonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production	F	7.43	pEC50	37	nM	EC50	J Med Chem (2010) 53: 295-315 [PMID:19921781]
ChEMBL	Agonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid release	F	7.5	pEC50	31.62	nM	EC50	Eur J Med Chem (2011) 46: 5086-5098 [PMID:21885167]
ChEMBL	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 assay	F	7.5	pEC50	31.62	nM	EC50	Bioorg Med Chem Lett (2010) 20: 4992-4998 [PMID:20688519]
ChEMBL	Agonist activity at CB1 receptor (unknown origin) assessed as increase in cAMP accumulation after 1 hr by FLIPR assay	F	7.8	pEC50	16	nM	EC50	J Med Chem (2018) 61: 9841-9878 [PMID:29939744]
ChEMBL	Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as reversal of forskolin-evoked cAMP accumulation	F	7.91	pEC50	12.3	nM	EC50	J Med Chem (2007) 50: 3851-3856 [PMID:17630726]
ChEMBL	Agonist activity at CB1 receptor (unknown origin) assessed as increase in beta-arrestin2 recruitment after 20 mins by BRET-based luciferase reporter gene assay	B	8.14	pEC50	7.2	nM	EC50	J Med Chem (2018) 61: 9841-9878 [PMID:29939744]
CB1 receptor/Cannabinoid CB1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3037] [GtoPdb: 56] [UniProtKB: P47746]
ChEMBL	Binding affinity towards mouse hippocampal membranes cannabinoid receptor 1 using [3H]SR-141,716A	B	7.7	pKi	20	nM	Ki	J Med Chem (2005) 48: 6386-6392 [PMID:16190764]
ChEMBL	Displacement of [3H]CP-55940 from mouse CB1 receptor	B	8.15	pKi	7	nM	Ki	Bioorg Med Chem Lett (2007) 17: 4030-4034 [PMID:17521907]
ChEMBL	Binding affinity towards mouse hippocampal membranes cannabinoid receptor 1 using [131I]-(R)-8	B	8.8	pKi	1.6	nM	Ki	J Med Chem (2005) 48: 6386-6392 [PMID:16190764]
ChEMBL	Agonist activity at CB1 receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated contraction	F	5.84	pEC50	1450	nM	EC50	Bioorg Med Chem (2007) 15: 7480-7493 [PMID:17870539]
ChEMBL	Activity at CB1 receptor assessed as stimulation of [35S]GTP-gamma-S binding in DBA/J2 mouse brain	F	6.69	pEC50	204	nM	EC50	J Med Chem (2006) 49: 5947-5957 [PMID:17004710]
CB1 receptor/Cannabinoid CB1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272]
ChEMBL	Displacement of [3H]-CP55940 from CB1 receptor in rat brain homogenate after 1.5 hrs by microbeta liquid scintillation counting analysis	B	7.44	pKi	36	nM	Ki	Eur J Med Chem (2013) 69: 881-907 [PMID:24125850]
ChEMBL	Displacement of [3H]CP-55940 from CB1 receptor in Sprague-Dawley rat brain by scintillation counting	B	7.81	pKi	15.6	nM	Ki	J Med Chem (2012) 55: 6608-6623 [PMID:22738271]
ChEMBL	Displacement of [3H]CP-55,940 from Sprague-Dawley rat brain CB1 receptor by scintillation counting analysis	B	7.84	pKi	14.4	nM	Ki	J Med Chem (2013) 56: 1098-1112 [PMID:23350768]
ChEMBL	Displacement of [3H]-WIN55212-2 from CB1R in rat brain membranes incubated for 60 mins by radioligand competitive binding assay	B	7.96	pKi	11	nM	Ki	ACS Med Chem Lett (2023) 14: 479-486 [PMID:37077391]
ChEMBL	Binding affinity for cannabinoid receptor 1	B	8	pKi	9.9	nM	Ki	J Med Chem (2005) 48: 5059-5087 [PMID:16078824]
ChEMBL	Displacement of [3H]CP-55940 from cannabinoid CB1 receptor in rat brain cortical membrane	B	8.22	pKi	6.06	nM	Ki	Bioorg Med Chem (2009) 17: 2842-2851 [PMID:19278853]
ChEMBL	Binding affinity to CB1 cannabinoid receptor using [3H]WIN-55212-2 in rat cerebellum membranes	B	8.35	pKi	4.5	nM	Ki	J Med Chem (2001) 44: 4505-4508 [PMID:11741470]
ChEMBL	Binding affinity to displace [3H]CP-55940 from CB1 receptor of rat brain	B	8.72	pKi	1.9	nM	Ki	Bioorg Med Chem Lett (2005) 15: 4110-4113 [PMID:16005223]
ChEMBL	Displacement of [3H]SR141716A from CB1 receptor in Sprague-Dawley rat cerebellum membrane	B	6.37	pIC50	430	nM	IC50	Eur J Med Chem (2008) 43: 513-539 [PMID:17582659]
ChEMBL	Agonist activity at rat brain membrane CB1 receptor assessed as stimulation of [35S]GTPgammaS binding incubated for 60 mins	B	6.84	pEC50	143	nM	EC50	ACS Med Chem Lett (2023) 14: 479-486 [PMID:37077391]
ChEMBL	Agonist activity at rat CB1 receptor assessed as inhibition of forskolin-induced cAMP production by cell based assay	F	8	pEC50	10	nM	EC50	J Med Chem (2010) 53: 295-315 [PMID:19921781]
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	0.55	pKi	0.55	nM	Log Ki	J Med Chem (2000) 43: 2300-2309 [PMID:10882356]
ChEMBL	Displacement of [3H]CP-55,940 from human recombinant cannabinoid CB2 receptor expressed in CHO cells	B	7.15	pKi	70	nM	Ki	Bioorg Med Chem (2013) 21: 7481-7498 [PMID:24139843]
ChEMBL	Displacement of [3H]CP-55940 from human CB2 receptor	B	7.7	pKi	20	nM	Ki	Bioorg Med Chem Lett (2008) 18: 3695-3700 [PMID:18522867]
ChEMBL	Displacement of [3H]-SR141716A from human CB1 receptor expressed in CHO membranes after 1 hr by liquid scintillation counting	B	7.79	pKi	16.1	nM	Ki	Bioorg Med Chem (2013) 21: 5383-5394 [PMID:23849204]
ChEMBL	Displacement of [3H]-CP55940 from human CB2 receptor expressed in HEK293 cells after 1.5 hrs by microbeta liquid scintillation counting analysis	B	7.89	pKi	13	nM	Ki	Eur J Med Chem (2013) 69: 881-907 [PMID:24125850]
ChEMBL	Displacement of [3H]CP-55940 from human CB2 receptor	B	8.04	pKi	9.1	nM	Ki	J Med Chem (2006) 49: 70-79 [PMID:16392793]
ChEMBL	Binding affinity to human CB2 receptor	B	8.04	pKi	9.1	nM	Ki	Bioorg Med Chem Lett (2014) 24: 1322-1326 [PMID:24508127]
ChEMBL	Displacement of [3H]-CP55,940 from human CB2 receptor expressed in CHO membranes after 1 hr by liquid scintillation counting	B	8.04	pKi	9.1	nM	Ki	Bioorg Med Chem (2013) 21: 5383-5394 [PMID:23849204]
ChEMBL	Displacement of [3H]-CP55940 from human CB2 receptor expressed in CHO cells after 1 hr	B	8.04	pKi	9.1	nM	Ki	J Med Chem (2010) 53: 7918-7931 [PMID:20979417]
ChEMBL	Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in CHO cells	B	8.04	pKi	9.1	nM	Ki	Bioorg Med Chem Lett (2010) 20: 4992-4998 [PMID:20688519]
ChEMBL	Displacement of [3H]CP55940 from beta-galactosidase reporter fused human CB2 receptor expressed in CHOK1 cell membranes after 1 hr by scintillation spectrometric analysis	B	8.07	pKi	8.57	nM	Ki	Medchemcomm (2017) 8: 1697-1705 [PMID:30108881]
ChEMBL	Displacement of [3H]-CP55940 from human CB2 receptor expressed in CHO cells by liquid scintillation counting	B	8.2	pKi	6.31	nM	Ki	Eur J Med Chem (2011) 46: 5086-5098 [PMID:21885167]
ChEMBL	Displacement of [3H]CP-55,940 from human recombinant CB2 receptor expressed in CHO cell membranes after 60 mins by scintillation counting analysis	B	8.31	pKi	4.95	nM	Ki	J Med Chem (2013) 56: 1098-1112 [PMID:23350768]
ChEMBL	Displacement of [3H]CP-55,940 from human CB2 receptor expressed in CHO cell membranes after 60 mins by scintillation counting analysis	B	8.34	pKi	4.6	nM	Ki	Eur J Med Chem (2016) 113: 11-27 [PMID:26922225]
ChEMBL	Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in CHO cell membranes incubated for 60 mins by scintillation counting	B	8.34	pKi	4.53	nM	Ki	J Med Chem (2012) 55: 6608-6623 [PMID:22738271]
ChEMBL	Binding affinity against human Cannabinoid receptor 2 expressed in CHO cells by using WIN-55212-2 Mesylate [573H] as Radioactive tracer	B	8.4	pKi	4	nM	Ki	Bioorg Med Chem Lett (2002) 12: 2399-2402 [PMID:12161142]
ChEMBL	Binding affinity to human CB2 cannabinoid receptor using [3H]CP-55940 in HEK293 EBNA transfected cells	B	8.41	pKi	3.9	nM	Ki	J Med Chem (2001) 44: 4505-4508 [PMID:11741470]
ChEMBL	Displacement of [3H]-CP55940 from human CB2 receptor after 90 mins by liquid scintillation spectrophotometer analysis	B	8.43	pKi	3.73	nM	Ki	Bioorg Med Chem (2013) 21: 1708-1716 [PMID:23434135]
ChEMBL	Displacement of [3H]CP55940 from human CB2 receptor expressed in HEK293 EBNA cells after 90 mins by liquid scintillation spectrophotometer	B	8.43	pKi	3.7	nM	Ki	J Med Chem (2016) 59: 1840-1853 [PMID:26789378]
ChEMBL	Displacement of [3H]CP55940 from human CB2 receptor expressed in HEK293 EBNA cell membranes after 90 mins by liquid scintillation and luminescence counting method	B	8.43	pKi	3.7	nM	Ki	Eur J Med Chem (2017) 127: 398-412 [PMID:28088085]
ChEMBL	Displacement of [3H]-CP55940 from human CB2 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method	B	8.43	pKi	3.7	nM	Ki	J Med Chem (2016) 59: 6753-6771 [PMID:27309150]
ChEMBL	Displacement of [3H]CP55940 from human CB2R transfected in HEK293EBNA cell membrane incubated for 90 mins by Microbeta TriLux based luminescence analysis	B	8.43	pKi	3.7	nM	Ki	Bioorg Med Chem (2020) 28: 115672-115672 [PMID:32912440]
ChEMBL	Displacement of [3H]-CP55940 from human CB2 receptor transfected in HEK293EBNA cell membranes after 90 mins by liquid scintillation counting analysis	B	8.43	pKi	3.7	nM	Ki	Eur J Med Chem (2015) 101: 651-667 [PMID:26209834]
ChEMBL	Displacement of [3H]CP55940 from human cannabinoid CB2 receptor expressed in HEK293 EBNA cells after 90 mins by liquid scintillation counting	B	8.43	pKi	3.7	nM	Ki	Eur J Med Chem (2013) 70: 111-119 [PMID:24141201]
ChEMBL	Displacement of [3H]CP,55-940 from recombinant human CB2 receptor expressed in HEK293 EBNA cell membranes after 90 mins by microbeta scintillation counting method	B	8.43	pKi	3.7	nM	Ki	Bioorg Med Chem (2018) 26: 295-307 [PMID:29229226]
ChEMBL	Displacement of [3H]-CP55940 from human CB2 receptor transfected in HEK-293EBNA cells after 90 mins by luminescence counting analysis	B	8.43	pKi	3.7	nM	Ki	Eur J Med Chem (2014) 73: 56-72 [PMID:24378710]
ChEMBL	Displacement of [3H]-CP55940 from recombinant human CB2 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by radioligand binding assay	B	8.45	pKi	3.55	nM	Ki	Eur J Med Chem (2021) 226: 113878-113878 [PMID:34634742]
ChEMBL	Displacement of [3H]-CP55940 from human CB2 receptor after 1 hr by scintillation counting analysis	B	8.51	pKi	3.1	nM	Ki	ACS Med Chem Lett (2015) 6: 198-203 [PMID:25699149]
ChEMBL	Displacement of [3H]CP55940 from human CB2 receptor expressed in CHO cell membranes after 1 hr by scintillation counting	B	8.51	pKi	3.1	nM	Ki	Eur J Med Chem (2012) 58: 396-404 [PMID:23151320]
ChEMBL	Displacement of [3H]-CP55940 from human recombinant CB2 receptor expressed in CHO cells membrane by scintillation counting	B	8.51	pKi	3.1	nM	Ki	J Med Chem (2012) 55: 8948-8952 [PMID:23017078]
ChEMBL	Displacement of [3H]-CP-55940 from human CB2 expressed in CHO cells after 90 mins by TopCount scintillation counting method	B	8.52	pKi	3.01	nM	Ki	Eur J Med Chem (2018) 146: 68-78 [PMID:29360044]
ChEMBL	Binding affinity to human CB2 receptor	B	8.54	pKi	2.9	nM	Ki	Bioorg Med Chem Lett (2007) 17: 6183-6187 [PMID:17884494]
ChEMBL	Displacement of [3H]-CP55940 from human CB2 expressed in insect Sf9 membranes	B	8.6	pKi	2.51	nM	Ki	Bioorg Med Chem Lett (2010) 20: 7327-7330 [PMID:21074434]
ChEMBL	Displacement of [3H]CP55940 from human cannabinoid CB2 receptor expressed in insect Sf9 cells	B	8.6	pKi	2.51	nM	Ki	Bioorg Med Chem Lett (2011) 21: 1748-1753 [PMID:21316962]
ChEMBL	Displacement of [3H]-CP55940 from human cannabinoid CB2 receptor expressed in Sf9 insect cells after 70 mins by scintillation counting	B	8.6	pKi	2.51	nM	Ki	Medchemcomm (2010) 1: 54-60
ChEMBL	Displacement of [3H]CP-55940 from human CB2 receptor	B	8.66	pKi	2.2