2-arachidonoylglycerol | Ligand Activity Charts | IUPHAR/BPS Guide to PHARMACOLOGY

Home
Ligands
2-arachidonoylglycerol
Ligand Activity Charts

2-arachidonoylglycerol [Ligand Id: 729] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL122972 (2-Arachidonoylglycerol, 2-Arachidonoyl Glycerol, 2-Arachidonoyl-Glycerol, 2-Oarachidonoyl Glycerol)
Fatty acid amide hydrolase/Anandamide amidohydrolase in Human [ChEMBL: CHEMBL2243] [GtoPdb: 1400] [UniProtKB: O00519] There should be some charts here, you may need to enable JavaScript!
CB₁ receptor/Cannabinoid CB1 receptor in Human [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554] 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 Rat [ChEMBL: CHEMBL2470] [GtoPdb: 57] [UniProtKB: Q9QZN9] There should be some charts here, you may need to enable JavaScript!
GPR55 in Human [GtoPdb: 109] [UniProtKB: Q9Y2T6] 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
Fatty acid amide hydrolase/Anandamide amidohydrolase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2243] [GtoPdb: 1400] [UniProtKB: O00519]
ChEMBL	Inhibition of Fatty-acid amide hydrolase (FAAH) activity in human lymphoma U937 cell using [3H]AEA as substrate in the 0-25 uM conc	B	5.3	pKi	5000	nM	Ki	J. Med. Chem. (2002) 45: 3709-3720 [PMID:12166944]
CB₁ receptor/Cannabinoid CB1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
ChEMBL	Binding affinity to CB1R (unknown origin)	B	6	pKi	1000	nM	Ki	J Med Chem (2017) 60: 4-46 [PMID:27766867]
ChEMBL	Displacement of [3H]-CP55940 from human CB1 receptor expressed in HEK-293-EBNA cell membranes after 90 mins by scintillation counting	B	6.32	pKi	480	nM	Ki	J. Med. Chem. (2011) 54: 5265-5269 [PMID:21675776]
ChEMBL	Binding affinity to CB1 receptor (unknown origin)	B	6.33	pKi	472	nM	Ki	Bioorg Med Chem (2016) 24: 5291-5301 [PMID:27624523]
ChEMBL	Displacement of [3H]CP55940 from human CB1 receptor expressed in human HEK293 cells	B	6.33	pKi	470	nM	Ki	J. Med. Chem. (2011) 54: 8278-8288 [PMID:22044209]
ChEMBL	Agonist activity at CB1 receptor expressed in NG108-15 cells assessed as increase in intracellular free calcium concentrations	F	7.64	pEC50	23	nM	EC50	Bioorg. Med. Chem. (2007) 15: 854-867 [PMID:17110113]
CB₁ receptor/Cannabinoid CB1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272]
ChEMBL	Binding affinity to rat CB1 receptor	B	6.33	pKi	472	nM	Ki	J. Med. Chem. (2013) 56: 8224-8256 [PMID:23865723]
ChEMBL	Displacement of [3H]CP55940 from CB1 receptor in Wistar rat brain incubated for 60 mins by radioactive filter binding assay	B	6.33	pKi	472	nM	Ki	Eur. J. Med. Chem. (2016) 112: 66-80 [PMID:26890113]
ChEMBL	Displacement of [3H]CP-55940 from rat forebrain membrane which expresses Cannabinoid receptor 1 in the presence of PMSF	B	7	pKi	100	nM	Ki	J. Med. Chem. (2002) 45: 3709-3720 [PMID:12166944]
GtoPdb	-	-	7.2	pKi	-	-	-	Biochem Pharmacol (1995) 50: 83-90 [PMID:7605349]; Eur J Pharmacol (1998) 353: 23-31 [PMID:9721036]
ChEMBL	Potency at CB1 receptor in rat brain by [35S]GTP-gamma-S binding assay	F	6	pEC50	1000	nM	EC50	Bioorg. Med. Chem. Lett. (2006) 16: 2437-2440 [PMID:16466915]
CB₂ receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
ChEMBL	Displacement of [3H]CP55940 from human CB2 receptor expressed in human HEK293 cells	B	5.85	pKi	1400	nM	Ki	J. Med. Chem. (2011) 54: 8278-8288 [PMID:22044209]
ChEMBL	Binding affinity to human CB2 receptor	B	5.85	pKi	1400	nM	Ki	J. Med. Chem. (2013) 56: 8224-8256 [PMID:23865723]
ChEMBL	Binding affinity to CB2 receptor (unknown origin)	B	5.85	pKi	1400	nM	Ki	Bioorg Med Chem (2016) 24: 5291-5301 [PMID:27624523]
ChEMBL	Displacement of [3H]-CP55940 from human CB2 receptor expressed in HEK-293-EBNA cell membranes after 90 mins by scintillation counting	B	5.89	pKi	1300	nM	Ki	J. Med. Chem. (2011) 54: 5265-5269 [PMID:21675776]
GtoPdb	-	-	6.8	pKi	-	-	-	Biochem Pharmacol (1995) 50: 83-90 [PMID:7605349]; Eur J Pharmacol (1998) 353: 23-31 [PMID:9721036]
ChEMBL	Agonist activity at CB2 receptor expressed in HL60 cells assessed as increase in intracellular free calcium concentrations	F	7.77	pEC50	17	nM	EC50	Bioorg. Med. Chem. (2007) 15: 854-867 [PMID:17110113]
CB₂ receptor/Cannabinoid CB2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2470] [GtoPdb: 57] [UniProtKB: Q9QZN9]
ChEMBL	Displacement of [3H]CP-55940 from rat forebrain membrane which expresses Cannabinoid receptor 2 in the presence of PMSF	B	7	pKi	100	nM	Ki	J. Med. Chem. (2002) 45: 3709-3720 [PMID:12166944]
GPR55 in Human [GtoPdb: 109] [UniProtKB: Q9Y2T6]
GtoPdb	-	-	8.52	pEC50	3	nM	EC50	Br J Pharmacol (2007) 152: 1092-101 [PMID:17876302]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]