arachidonyl trifluoromethyl ketone [Ligand Id: 5142] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL281211 (Arachidonyltrifluoromethylketone, Arachidonyl Trifluoromethyl Ketone) |
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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; 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/Anandamide amidohydrolase 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] |
| CB1 receptor/Cannabinoid CB1 receptor 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] |
| cPLA2-4C/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] |
| 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] |
| cPLA2-4B/Phospholipase A2 group 1VB 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] |
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]
