ChEMBL ligand: CHEMBL381791
CB1 receptor/Cannabinoid CB1 receptor in Human [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554] 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] 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	Displacement of [3H]CP55,940 from N-terminal HA-tagged human CB1 receptor expressed in HEK293 cell membranes after 1 hr by microbeta scintillation counting method	B	5.25	pKi	5628	nM	Ki	Eur J Med Chem (2018) 145: 770-789 [PMID:29407590]
ChEMBL	Displacement of [3H]CP55,940 from human CB1 receptor	B	5.77	pKi	1698.24	nM	Ki	Eur J Med Chem (2018) 145: 770-789 [PMID:29407590]
ChEMBL	Displacement of [3H]CP55,940 from human CB1 receptor	B	5.77	pKi	1698.2	nM	Ki	Eur J Med Chem (2018) 145: 770-789 [PMID:29407590]
ChEMBL	Displacement of [3H]-CP55940 from human recombinant cannabinoid CB1 receptor expressed in CHO cells by radioligand binding assay	B	6.16	pKi	687	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	6.16	pKi	687	nM	Ki	J Med Chem (2018) 61: 1646-1663 [PMID:29400965]
ChEMBL	Displacement of [3H]-CP 55,940 from human CB1 receptor expressed in CHO cells by liquid scintillation counting method	B	6.4	pKi	400	nM	Ki	Medchemcomm (2015) 6: 1978-1986
ChEMBL	Displacement of [3H]-CP55940 from human CB1 receptor transfected in CHO cell membranes by liquid scintillation counting analysis	B	6.4	pKi	400	nM	Ki	Eur J Med Chem (2015) 101: 651-667 [PMID:26209834]
ChEMBL	Displacement of [3H]-CP55950 from human CB1 receptor expressed in CHO cell membranes after 90 mins	B	6.6	pKi	254	nM	Ki	J Med Chem (2018) 61: 1646-1663 [PMID:29400965]
ChEMBL	Displacement of [3H]CP55940 from recombinant human CB1 receptor expressed in human HEK293 cell membrane after 90 mins	B	6.92	pKi	121.2	nM	Ki	Eur J Med Chem (2012) 52: 284-294 [PMID:22483967]
ChEMBL	Displacement of [3H]-CP-55,940 from recombinant human CB1R expressed in HEK293 cell membranes	B	6.94	pKi	116	nM	Ki	J Med Chem (2020) 63: 7369-7391 [PMID:32515588]
ChEMBL	Displacement of [3H]CP55940 from recombinant human CB1R expressed in HEK293 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis	B	8.7	pKi	2	nM	Ki	Eur J Med Chem (2019) 180: 154-170 [PMID:31302448]
ChEMBL	Displacement of [3H]-CP55950 from human CB1 receptor expressed in CHO cell membranes after 3 hrs by scintillation counting method	B	6.1	pIC50	794.33	nM	IC50	J Med Chem (2018) 61: 1646-1663 [PMID:29400965]
CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
ChEMBL	Displacement of 3[H]-CP55940 from human recombinant CB2 receptor expressed in HEK293 cell membranes measured after 90 mins by Cheng-Prusoff equation analysis	B	5.74	pKi	1820	nM	Ki	Eur J Med Chem (2019) 178: 243-258 [PMID:31185414]
ChEMBL	Displacement of [3H]CP55940 from recombinant human CB2R expressed in HEK293 cell membranes incubated for 90 mins by Cheng-Prusoff equation analysis	B	6.93	pKi	117	nM	Ki	Eur J Med Chem (2019) 180: 154-170 [PMID:31302448]
ChEMBL	Displacement of [3H]CP55,940 from N-terminal HA-tagged human CB2 receptor expressed in HEK293 cell membranes after 1 hr by microbeta scintillation counting method	B	7.29	pKi	51	nM	Ki	Eur J Med Chem (2018) 145: 770-789 [PMID:29407590]
ChEMBL	Displacement of [3H]-CP55940 from human recombinant cannabinoid CB2 receptor expressed in human HEK cells by radioligand binding assay	B	7.71	pKi	19.7	nM	Ki	J Med Chem (2019) 62: 9078-9102 [PMID:31609608]
ChEMBL	Displacement of [3H]-CP55950 from human CB2 receptor expressed in HEK cell membranes after 3 hrs by scintillation counting method	B	7.71	pKi	19.7	nM	Ki	J Med Chem (2018) 61: 1646-1663 [PMID:29400965]
ChEMBL	Displacement of [3H]CP55,940 from human CB2 receptor	B	7.88	pKi	13.2	nM	Ki	Eur J Med Chem (2018) 145: 770-789 [PMID:29407590]
ChEMBL	Displacement of [3H]CP55,940 from human CB2 receptor	B	7.88	pKi	13.18	nM	Ki	Eur J Med Chem (2018) 145: 770-789 [PMID:29407590]
ChEMBL	Displacement of [3H]-CP55950 from human CB2 receptor expressed in HEK cell membranes after 90 mins	B	8.25	pKi	5.6	nM	Ki	J Med Chem (2018) 61: 1646-1663 [PMID:29400965]
ChEMBL	Displacement of [3H]CP55940 from recombinant human CB2 receptor expressed in human HEK293 cell membrane after 90 mins	B	8.36	pKi	4.35	nM	Ki	Eur J Med Chem (2012) 52: 284-294 [PMID:22483967]
ChEMBL	Displacement of [3H]CP-55,940 from human CB2 receptor after 1 hr by competitive binding assay	B	8.65	pKi	2.23	nM	Ki	J Med Chem (2013) 56: 6593-6612 [PMID:23855811]
ChEMBL	Displacement of [3H]-CP-55940 from human CB2 receptor expressed in HEK293 cell membranes after 90 mins by radioligand binding assay	B	8.74	pKi	1.82	nM	Ki	Eur J Med Chem (2016) 122: 619-634 [PMID:27448919]
ChEMBL	Displacement of [3H]-CP-55,940 from recombinant human CB2R expressed in HEK293 cell membranes	B	8.74	pKi	1.8	nM	Ki	J Med Chem (2020) 63: 7369-7391 [PMID:32515588]
ChEMBL	Displacement of [3H]CP55940 from recombinant human CB2R expressed in HEK293 cell membranes measured after 90 mins	B	8.74	pKi	1.8	nM	Ki	Eur J Med Chem (2019) 161: 239-251 [PMID:30359820]
GtoPdb	-	-	9.2	pKi	0.63	nM	Ki	Br J Pharmacol (1999) 126: 665-672 [PMID:10188977]; J Pharmacol Exp Ther (1998) 284: 644-50 [PMID:9454810]
ChEMBL	Binding affinity to human CB2 receptor expressed in CHO cells	B	9.22	pKi	0.6	nM	Ki	J Med Chem (2013) 56: 6593-6612 [PMID:23855811]
ChEMBL	Displacement of [3H]-CP55940 from human CB2 receptor transfected in CHO cell membranes by liquid scintillation counting analysis	B	9.22	pKi	0.6	nM	Ki	Eur J Med Chem (2015) 101: 651-667 [PMID:26209834]
ChEMBL	Displacement of [3H]-CP 55,940 from human CB2 receptor expressed in CHO cells by liquid scintillation counting method	B	9.22	pKi	0.6	nM	Ki	Medchemcomm (2015) 6: 1978-1986
ChEMBL	Displacement of [3H]-CP55940 from human CB2 receptor transfected in HEK293EBNA cell membranes after 90 mins by liquid scintillation counting analysis	B	9.51	pKi	0.31	nM	Ki	Eur J Med Chem (2015) 101: 651-667 [PMID:26209834]
ChEMBL	Displacement of 3[H]-CP55940 from human recombinant CB2 receptor expressed in HEK293 cell membranes measured after 90 mins	B	5.15	pIC50	7160	nM	IC50	Eur J Med Chem (2019) 178: 243-258 [PMID:31185414]
ChEMBL	Inverse agonist activity at N-terminal HA-tagged human CB2 receptor expressed in HEK293 cells transfected with YFP-Epac-RLuc assessed as increase in forskolin-stimulated cAMP level by BRET assay	F	6.12	pIC50	760	nM	IC50	Eur J Med Chem (2018) 145: 770-789 [PMID:29407590]
ChEMBL	Inverse agonist activity at human CB2 receptor expressed in HEK293 EBNA cell membranes after 30 mins by [35S]-GTPgammaS binding assay	F	7.02	pIC50	96.2	nM	IC50	Eur J Med Chem (2017) 127: 398-412 [PMID:28088085]
ChEMBL	Displacement of [3H]-CP55950 from human CB2 receptor expressed in HEK cell membranes after 3 hrs by scintillation counting method	B	7.7	pIC50	19.95	nM	IC50	J Med Chem (2018) 61: 1646-1663 [PMID:29400965]
ChEMBL	Inverse agonist activity at recombinant human CB2R expressed in CHOK1 cells assessed as increase in NKH477-stimulated intracellular cAMP levels after 30 mins by chemiluminescent based cAMP Hunter assay	F	4.57	pEC50	26690	nM	EC50	J Med Chem (2020) 63: 7369-7391 [PMID:32515588]
ChEMBL	Agonist activity at N-terminal Flag epitope tagged CB2 (unknown origin) expressed in HTLA cells assessed as increase of beta-arrestin recruitment by Tango assay	B	5.87	pEC50	1360	nM	EC50	Eur J Med Chem (2019) 180: 154-170 [PMID:31302448]
ChEMBL	Inverse agonist activity at cannabinoid CB2 receptor in human U2OS cells assessed as induction of beta-arrestin recruitment using CCF4/AM as substrate preincubated for 5 hrs followed by substrate addition and measured after 2 hrs by Tango assay	B	5.93	pEC50	1174.9	nM	EC50	Bioorg Med Chem (2021) 33: 116035-116035 [PMID:33550084]
ChEMBL	Antagonist activity at N-terminal Flag epitope tagged CB2 (unknown origin) expressed in HTLA cells assessed as decrease in CP55940-induced beta-arrestin recruitment pretreated with non-selective cannabinoid receptor agonist CP55940 for 30 mins and measured after 20 mins by Tango assay	B	7.39	pEC50	41	nM	EC50	Eur J Med Chem (2019) 180: 154-170 [PMID:31302448]
ChEMBL	Antagonist activity at CB2 receptor in HEK293 cells assessed as increase in CP-55,940 EC50 measuring inhibition of forskolin-stimulated cAMP accumulation at 1 uM incubated 20 mins prior to CP-55,940 addition measured after 7 mins by spectrophotometry (Rvb = 4.21+/-1.16 nM)	F	7.63	pEC50	23.31	nM	EC50	J Med Chem (2013) 56: 6593-6612 [PMID:23855811]

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]