2-arachidonoylglycerol [Ligand Id: 729] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL122972 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| CB1 receptor/Cannabinoid receptor 1 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 receptor 1 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] |
| ChEMBL | Agonist activity at rat CB1 receptor stably expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 5 mins by Lance Ultra cAMP assay | F | 7.6 | pEC50 | 25 | nM | EC50 | ACS Med Chem Lett (2024) 15: 965-971 [PMID:38894922] |
| CB2 receptor/Cannabinoid receptor 2 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 receptor 2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5373] [GtoPdb: 57] [UniProtKB: P47936] | ||||||||
| ChEMBL | Agonist activity at mouse CB2 receptor stably expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 5 mins by Lance Ultra cAMP assay | F | 7.74 | pEC50 | 18 | nM | EC50 | ACS Med Chem Lett (2024) 15: 965-971 [PMID:38894922] |
| CB2 receptor/Cannabinoid receptor 2 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] |
| Fatty acid amide hydrolase/Fatty-acid amide hydrolase 1 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] |
| FFA4 receptor/Free fatty acid receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5339] [GtoPdb: 127] [UniProtKB: Q5NUL3] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: FFAR4 | F | 5 | pIC50 | >10000 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| 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 36:
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]
