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 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]