ChEMBL ligand: CHEMBL1553629
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	Allosteric antagonist activity at human CB1 receptor expressed in HEK293 cell membrane assessed as inhibition of CP55940-stimulated [35S]GTPgammaS binding incubated for 60 mins by [35S]GTP-gammaS binding assay	F	6	pIC50	1000	nM	IC50	Bioorg Med Chem (2021) 41: 116215-116215 [PMID:34015703]
ChEMBL	Allosteric antagonist activity at human CB1 receptor by Ca2+ assay	F	6.07	pIC50	853	nM	IC50	J Med Chem (2019) 62: 9806-9823 [PMID:31596583]
ChEMBL	Antagonist activity at human CB1 receptor expressed in CHO-RD-HGA16 cells assessed as inhibition of CP55940-induced calcium mobilization incubated for 15 mins prior to CP55940 addition by FLIPR assay	F	6.07	pIC50	853	nM	IC50	Bioorg Med Chem (2015) 23: 2195-2203 [PMID:25797163]
ChEMBL	Allosteric antagonist activity at human CB1 receptor expressed in CHO-RD-HGA16 cells overexpressing Galpha16 assessed as inhibition of CP55940-stimulated calcium mobilization preincubated for 15 mins followed by agonist addition and measured every 1 sec for 90 secs by Calcium-3 dye based FLIPR assay	F	6.1	pIC50	794.33	nM	IC50	Bioorg Med Chem (2021) 41: 116215-116215 [PMID:34015703]
ChEMBL	Allosteric antagonist activity at N-terminal 3HA-tagged human CB1 receptor expressed in HEK293 cells assessed as reduction in CP55940-stimulated inhibition of forskolin-induced cAMP accumulation measured for 20 mins by BRET assay	F	6.8	pIC50	158.49	nM	IC50	Bioorg Med Chem (2021) 41: 116215-116215 [PMID:34015703]
ChEMBL	Negative allosteric modulation of human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP55940 induced beta arrestin recruitment preincubated for 30 mins followed by addition of CP55940 for 90 mins by chemiluminescence assay	F	8.7	pIC50	2	nM	IC50	Bioorg Med Chem Lett (2016) 26: 4403-4407 [PMID:27542310]
ChEMBL	Positive allosteric modulatory activity at C-terminal GFP-tagged human CB1R expressed in HEK293 cell membrane after 90 mins in presence of [3H]CP55940/[3H]SR141716A by liquid scintillation counting assay	B	9.54	pIC50	0.29	nM	IC50	ACS Med Chem Lett (2020) 11: 1810-1819 [PMID:33062158]
ChEMBL	Activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 5 mins in presence of CP55,940 by cAMP BRET assay	F	4.98	pEC50	10590	nM	EC50	J Med Chem (2015) 58: 5979-5988 [PMID:26203658]
ChEMBL	Activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation in presence of CP55,940 by cAMP BRET assay	F	5.65	pEC50	2240	nM	EC50	J Med Chem (2015) 58: 5979-5988 [PMID:26203658]
ChEMBL	Activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 10 mins in presence of CP55,940 by cAMP BRET assay	F	5.68	pEC50	2090	nM	EC50	J Med Chem (2015) 58: 5979-5988 [PMID:26203658]
ChEMBL	Activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 15 mins in presence of CP55,940 by cAMP BRET assay	F	6.19	pEC50	640	nM	EC50	J Med Chem (2015) 58: 5979-5988 [PMID:26203658]
ChEMBL	Negative allosteric modulator activity at human CB1R expressed in CHO-K1 cells assessed as effect on CP55,940-induced inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by CP55,940 addition measured for 30 mins by HitHunter assay	F	6.49	pEC50	324	nM	EC50	J Med Chem (2016) 59: 44-60 [PMID:26529344]
GtoPdb	Measured as increased binding of radiolabelled orthosteric agonist CP55940	-	6.85	pEC50	140	nM	EC50	J Med Chem (2012) 55: 5627-31 [PMID:22571451]
ChEMBL	Allosteric modulation of human recombinant CB1 receptor expressed in HEK293 cells assessed as stimulation of [3H]CP55940 binding	B	6.85	pEC50	140	nM	EC50	J Med Chem (2012) 55: 5627-5631 [PMID:22571451]
ChEMBL	Positive allosteric modulator activity at human CB1R expressed in CHO cells assessed as enhanced binding of [3H]CP55,940 after 60 mins by liquid scintillation spectrometric analysis	B	7.08	pEC50	83	nM	EC50	J Med Chem (2016) 59: 44-60 [PMID:26529344]
ChEMBL	Negative allosteric modulator activity at human CB1R expressed in CHO-K1 cells assessed as inhibition of CP55,940-induced beta-arrestin recruitment preincubated for 30 mins followed by CP55,940 addition measured for 90 mins by PathHunter assay	B	8.04	pEC50	9.05	nM	EC50	J Med Chem (2016) 59: 44-60 [PMID:26529344]
CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
ChEMBL	Allosteric modulation of human recombinant CB2 receptor expressed in HEK293 cells assessed as inhibition of [3H]CP55940 binding	B	5	pIC50	>10000	nM	IC50	J Med Chem (2012) 55: 5627-5631 [PMID:22571451]
ChEMBL	Antagonist activity at human CB2 receptor expressed in CHO-RD-HGA16 cells overexpressing Galpha16 assessed as inhibition of CP55940-stimulated calcium mobilization preincubated for 15 mins followed by agonist addition and measured every 1 sec for 90 secs by Calcium-3 dye based FLIPR assay	F	5	pIC50	>10000	nM	IC50	Bioorg Med Chem (2021) 41: 116215-116215 [PMID:34015703]

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]