arachidonyl trifluoromethyl ketone [Ligand Id: 5142] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL281211 |
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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 Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272] | ||||||||
| ChEMBL | Displacement of [35S]GTP-gamma-S from rat cerebellar CB1 receptor | F | 4.6 | pEC50 | 25118.86 | nM | EC50 | J Med Chem (2006) 49: 554-566 [PMID:16420041] |
| cPLA2-4A/Cytosolic phospholipase A2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3816] [GtoPdb: 1424] [UniProtKB: P47712] | ||||||||
| ChEMBL | Inhibition of human platelet cPLA2-alpha assessed as arachidonic acid release by vesicle assay | B | 5.64 | pIC50 | 2300 | nM | IC50 | Bioorg Med Chem (2007) 15: 2883-2891 [PMID:17320401] |
| ChEMBL | Inhibition of human platelet cPLA2-alpha activity | B | 5.64 | pIC50 | 2300 | nM | IC50 | Bioorg Med Chem (2008) 16: 3489-3500 [PMID:18321717] |
| ChEMBL | Inhibition of cPLA2 from human platelets by RP-HPLC | B | 5.64 | pIC50 | 2300 | nM | IC50 | Bioorg Med Chem (2010) 18: 945-952 [PMID:20005725] |
| Cytosolic phospholipase A2 in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2304401] [UniProtKB: A4IFJ5] | ||||||||
| ChEMBL | Inhibitory activity against cPLA2 (cytosolic Phospholipase A2) by measuring the calcium ionophore A-23,187-induced arachidonic acid release from bovine platelets | F | 4.96 | pIC50 | 11000 | nM | IC50 | J Med Chem (1997) 40: 2694-2705 [PMID:9276015] |
| ChEMBL | Inhibition of cPLA2 measuring Calcium ionophore A-23,187-induced arachidonic acid release from bovine platelets with HPLC/UV detection. | F | 4.96 | pIC50 | 11000 | nM | IC50 | J Med Chem (1997) 40: 3381-3392 [PMID:9341913] |
| cPLA2-4B/Cytosolic phospholipase A2 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4136] [GtoPdb: 1425] [UniProtKB: P0C869] | ||||||||
| ChEMBL | Inhibitory activity against cytosolic Phospholipase A2 (PLA2) by soluble assay | B | 6.1 | pIC50 | 800 | nM | IC50 | J Med Chem (2002) 45: 1348-1362 [PMID:11882004] |
| cPLA2-4C/Cytosolic phospholipase A2 gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4834] [GtoPdb: 1426] [UniProtKB: Q9UP65] | ||||||||
| ChEMBL | Concentration required to inhibit human Cytosolic phospholipase A2 | B | 6.38 | pIC50 | 420 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 587-590 [PMID:11229777] |
| 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; range =. 23-3 uM | B | 5.52 | pIC50 | 3000 | nM | IC50 | J Med Chem (2005) 48: 5059-5087 [PMID:16078824] |
| ChEMBL | Inhibition of human FAAH | B | 7.91 | pIC50 | 12.3 | nM | IC50 | J Med Chem (2009) 52: 7410-7420 [PMID:19583260] |
| ChEMBL | Inhibition of human recombinant FAAH-maltose binding protein | B | 7.91 | pIC50 | 12.3 | nM | IC50 | J Med Chem (2009) 52: 7310-7314 [PMID:19883085] |
| Fatty acid amide hydrolase/Fatty-acid amide hydrolase 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3229] [GtoPdb: 1400] [UniProtKB: P97612] | ||||||||
| ChEMBL | Inhibition of FAAH from rat brain microsomes by RP-HPLC | B | 5.43 | pIC50 | 3700 | nM | IC50 | Bioorg Med Chem (2010) 18: 945-952 [PMID:20005725] |
| monoacylglycerol lipase/Monoglyceride lipase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4191] [GtoPdb: 1399] [UniProtKB: Q99685] | ||||||||
| ChEMBL | Inhibition of human MGL activity using [3H]2-oleoylglycerol substrate by liquid scintillation counting | B | 5.19 | pIC50 | 6456.54 | nM | IC50 | J Med Chem (2009) 52: 7310-7314 [PMID:19883085] |
| ChEMBL | Inhibition of human MGL | B | 5.2 | pIC50 | 6310 | nM | IC50 | J Med Chem (2009) 52: 7410-7420 [PMID:19583260] |
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]
