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

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ChEMBL ligand: CHEMBL3945728 (Abx-1431, ABX-1431)
  • Fatty acid amide hydrolase/Anandamide amidohydrolase in Mouse [ChEMBL: CHEMBL3455] [GtoPdb: 1400] [UniProtKB: O08914]
  • This target only has 0 pki data point
  • 0
1 CHEMBL3945728_lig_chart_1 Anandamide amidohydrolase Mouse
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  • PLA2-G7/LDL-associated phospholipase A2 in Human [ChEMBL: CHEMBL3514] [GtoPdb: 1432] [UniProtKB: Q13093]
  • This target only has 0 pki data point
  • 0
2 CHEMBL3945728_lig_chart_2 LDL-associated phospholipase A2 Human
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  • αβ-Hydrolase 6/Monoacylglycerol lipase ABHD6 in Human [ChEMBL: CHEMBL2189127] [GtoPdb: 2919] [UniProtKB: Q9BV23]
  • This target only has 0 pki data point
  • 0
3 CHEMBL3945728_lig_chart_3 Monoacylglycerol lipase ABHD6 Human
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  • Monoacylglycerol lipase/Monoglyceride lipase in Human [ChEMBL: CHEMBL4191] [GtoPdb: 1399] [UniProtKB: Q99685]
  • Monoacylglycerol lipase/Monoglyceride lipase in Mouse [ChEMBL: CHEMBL5774] [GtoPdb: 1399] [UniProtKB: O35678]
  • This target only has 0 pki data point
  • 0
4 CHEMBL3945728_lig_chart_4 Monoglyceride lipase HumanMouse
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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)
PLA2-G7/LDL-associated phospholipase A2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3514] [GtoPdb: 1432] [UniProtKB: Q13093]
GtoPdb - - 5 pIC50 >10000 nM IC50 J Med Chem (2018) 61: 9062-9084 [PMID:30067909]
ChEMBL Inhibition of PLA2G7 derived from human PC3 cell lysates preincubated for 30 mins followed by JW912 addition after 30 mins by gel-based ABPP assay B 5 pIC50 >10000 nM IC50 J Med Chem (2018) 61: 9062-9084 [PMID:30067909]
αβ-Hydrolase 6/Monoacylglycerol lipase ABHD6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2189127] [GtoPdb: 2919] [UniProtKB: Q9BV23]
ChEMBL Inhibition of ABHD6 derived from human PC3 cell lysates preincubated for 30 mins followed by JW912 addition after 30 mins by gel-based ABPP assay B 5.57 pIC50 2700 nM IC50 J Med Chem (2018) 61: 9062-9084 [PMID:30067909]
GtoPdb - - 5.57 pIC50 2700 nM IC50 J Med Chem (2018) 61: 9062-9084 [PMID:30067909]
ChEMBL Inhibition of ABHD6 in human intact PC3 cells preincubated for 30 mins followed by JW912 addition after 30 mins by gel-based ABPP assay B 6.6 pIC50 253 nM IC50 J Med Chem (2018) 61: 9062-9084 [PMID:30067909]
Monoacylglycerol lipase/Monoglyceride lipase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4191] [GtoPdb: 1399] [UniProtKB: Q99685]
GtoPdb - - 7.85 pIC50 14 nM IC50 J Med Chem (2018) 61: 9062-9084 [PMID:30067909]
ChEMBL Inhibition of MGLL derived from human PC3 cell lysates preincubated for 30 mins followed by JW912 addition after 30 mins by gel-based ABPP assay B 7.85 pIC50 14 nM IC50 J Med Chem (2018) 61: 9062-9084 [PMID:30067909]
ChEMBL Inhibition of MGLL in human intact PC3 cells preincubated for 30 mins followed by JW912 addition after 30 mins by gel-based ABPP assay B 8.66 pIC50 2.2 nM IC50 J Med Chem (2018) 61: 9062-9084 [PMID:30067909]
Monoacylglycerol lipase/Monoglyceride lipase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5774] [GtoPdb: 1399] [UniProtKB: O35678]
ChEMBL Inhibition of MGLL derived from mouse brain homogenates preincubated for 30 mins followed by JW912 addition after 30 mins by gel-based ABPP assay B 7.57 pIC50 27 nM IC50 J Med Chem (2018) 61: 9062-9084 [PMID:30067909]
GtoPdb - - 7.57 pIC50 27 nM IC50 J Med Chem (2018) 61: 9062-9084 [PMID:30067909]

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]