ABX-1431 [Ligand Id: 10062] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3945728
  • Fatty acid amide hydrolase/Anandamide amidohydrolase in Mouse [ChEMBL: CHEMBL3455] [GtoPdb: 1400] [UniProtKB: O08914]
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  • Monoacylglycerol lipase in Human [GtoPdb: 1399] [UniProtKB: Q99685]
  • Monoacylglycerol lipase in Mouse [GtoPdb: 1399] [UniProtKB: O35678]
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  • PLA2-G7 in Human [GtoPdb: 1432] [UniProtKB: Q13093]
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  • αβ-Hydrolase 6 in Human [GtoPdb: 2919] [UniProtKB: Q9BV23]
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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 Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3455] [GtoPdb: 1400] [UniProtKB: O08914]
ChEMBL In Vitro Competitive Activity-Based Protein Assay: Proteomes (mouse brain membrane fraction or cell lysates) (50 uL, 1.0 mg/mL total protein concentration) were preincubated with varying concentrations of inhibitors at 37 C. After 30 min, FP-Rh (1.0 uL, 50 uM in DMSO) was added and the mixture was incubated for another 30 min at 37 C. Reactions were quenched with SDS loading buffer (50 uL-4x) and run on SDS-PAGE. Following gel imaging, serine hydrolase activity was determined by measuring fluorescent intensity of gel bands corresponding to MAGL, ABHD6 and FAAH using ImageJ 1.43u software.Preparation of Mouse Brain Proteomes from Inhibitor Treated Mice. Inhibitors were administered to wild-type C57Bl/6J by oral gavage in a vehicle of polyethylene glycol. Each animal was sacrificed 4 h following administration and brain proteomes were prepared and analyzed according to previously established methods (See Niphakis, M. J., et al. (2011) ACS Chem. Neurosci. and Long, J. Z., et al. Nat. Chem. Biol. 5:37-44). B 5 pIC50 >10000 nM IC50 US-9133148-B2. Carbamate compounds and of making and using same (2015)
Monoacylglycerol lipase in Human [GtoPdb: 1399] [UniProtKB: Q99685]
GtoPdb - - 7.85 pIC50 14 nM IC50 J. Med. Chem. (2018) 61: 9062-9084 [PMID:30067909]
Monoacylglycerol lipase in Mouse [GtoPdb: 1399] [UniProtKB: O35678]
GtoPdb - - 7.57 pIC50 27 nM IC50 J. Med. Chem. (2018) 61: 9062-9084 [PMID:30067909]
PLA2-G7 in Human [GtoPdb: 1432] [UniProtKB: Q13093]
GtoPdb - - 5 pIC50 >10000 nM IC50 J. Med. Chem. (2018) 61: 9062-9084 [PMID:30067909]
αβ-Hydrolase 6 in Human [GtoPdb: 2919] [UniProtKB: Q9BV23]
GtoPdb - - 5.57 pIC50 2700 nM IC50 J. Med. Chem. (2018) 61: 9062-9084 [PMID:30067909]

ChEMBL data shown on this page come from version 27:

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]