arachidonyl trifluoromethyl ketone [Ligand Id: 5142] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL281211 (Arachidonyltrifluoromethylketone, Arachidonyl Trifluoromethyl Ketone)
  • Fatty acid amide hydrolase/Anandamide amidohydrolase in Human [ChEMBL: CHEMBL2243] [GtoPdb: 1400] [UniProtKB: O00519]
  • Fatty acid amide hydrolase/Anandamide amidohydrolase in Rat [ChEMBL: CHEMBL3229] [GtoPdb: 1400] [UniProtKB: P97612]
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  • CB1 receptor/Cannabinoid CB1 receptor in Rat [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272]
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  • cPLA2-4C/Cytosolic phospholipase A2 gamma in Human [ChEMBL: CHEMBL4834] [GtoPdb: 1426] [UniProtKB: Q9UP65]
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  • Monoacylglycerol lipase/Monoglyceride lipase in Human [ChEMBL: CHEMBL4191] [GtoPdb: 1399] [UniProtKB: Q99685]
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  • cPLA2-4B/Phospholipase A2 group 1VB in Human [ChEMBL: CHEMBL4136] [GtoPdb: 1425] [UniProtKB: P0C869]
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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 28:

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]