2-arachidonoylglycerol [Ligand Id: 729] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL122972 (2-Arachidonoylglycerol, 2-Arachidonoyl Glycerol, 2-Arachidonoyl-Glycerol, 2-Oarachidonoyl Glycerol) |
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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 | 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 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]
