ChEMBL ligand: CHEMBL3945728 (Abx-1431, ABX-1431, ABX1431, Elcubragistat)
Fatty acid amide hydrolase/Anandamide amidohydrolase in Mouse [ChEMBL: CHEMBL3455] [GtoPdb: 1400] [UniProtKB: O08914] There should be some charts here, you may need to enable JavaScript!
PLA2-G7/LDL-associated phospholipase A2 in Human [ChEMBL: CHEMBL3514] [GtoPdb: 1432] [UniProtKB: Q13093] There should be some charts here, you may need to enable JavaScript!
αβ-Hydrolase 6/Monoacylglycerol lipase ABHD6 in Human [ChEMBL: CHEMBL2189127] [GtoPdb: 2919] [UniProtKB: Q9BV23] There should be some charts here, you may need to enable JavaScript!
monoacylglycerol lipase/Monoglyceride lipase in Human [ChEMBL: CHEMBL4191] [GtoPdb: 1399] [UniProtKB: Q99685] monoacylglycerol lipase/Monoglyceride lipase in Mouse [ChEMBL: CHEMBL5774] [GtoPdb: 1399] [UniProtKB: O35678] There should be some charts here, you may need to enable JavaScript!

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 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]