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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]