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

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ChEMBL ligand: CHEMBL122972 (2-Oarachidonoyl Glycerol, 2-Arachidonoyl-Glycerol, 2-Arachidonoyl Glycerol, 2-Arachidonoylglycerol)
  • Fatty acid amide hydrolase/Anandamide amidohydrolase in Human [ChEMBL: CHEMBL2243] [GtoPdb: 1400] [UniProtKB: O00519]
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  • 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]
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  • 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]
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  • GPR55 in Human [GtoPdb: 109] [UniProtKB: Q9Y2T6]
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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 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 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 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]