ChEMBL ligand: CHEMBL576786
Fatty acid amide hydrolase/Anandamide amidohydrolase in Human [ChEMBL: CHEMBL2243] [GtoPdb: 1400] [UniProtKB: O00519] Fatty acid amide hydrolase/Anandamide amidohydrolase in Mouse [ChEMBL: CHEMBL3455] [GtoPdb: 1400] [UniProtKB: O08914] Fatty acid amide hydrolase/Anandamide amidohydrolase in Rat [ChEMBL: CHEMBL3229] [GtoPdb: 1400] [UniProtKB: P97612] There should be some charts here, you may need to enable JavaScript!
αβ-Hydrolase 6/Monoacylglycerol lipase ABHD6 in Mouse [ChEMBL: CHEMBL5010] [GtoPdb: 2919] [UniProtKB: Q8R2Y0] 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] monoacylglycerol lipase/Monoglyceride lipase in Rat [ChEMBL: CHEMBL3321] [GtoPdb: 1399] [UniProtKB: Q8R431] 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 Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2243] [GtoPdb: 1400] [UniProtKB: O00519]
ChEMBL	Inhibition of human recombinant FAAH assessed as [3H]-AEA hydrolysis preincubated for 30 mins before [3H]-2-OG addition measured after 10 mins by liquid scintillation counting	B	4.44	pIC50	36308	nM	IC50	Bioorg Med Chem (2012) 20: 6260-6275 [PMID:23036333]
ChEMBL	Inhibition of recombinant human FAAH using fluorogenic arachidonoyl-AMC as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by fluorescence based assay	B	4.96	pIC50	>11000	nM	IC50	J Med Chem (2018) 61: 3008-3026 [PMID:29498843]
ChEMBL	Inhibition of FAAH	B	5.33	pIC50	4690	nM	IC50	Bioorg Med Chem (2012) 20: 6260-6275 [PMID:23036333]
ChEMBL	Inhibition of human FAAH	B	5.4	pIC50	4000	nM	IC50	J Med Chem (2009) 52: 7410-7420 [PMID:19583260]
ChEMBL	Inhibition of FAAH	B	5.4	pIC50	4000	nM	IC50	Nat Chem Biol (2009) 5: 8-9 [PMID:19088712]
ChEMBL	Inhibition of recombinant FAAH expressed in Cos7 cells after 30 mins by using anandamide as a substrate by LC-MS method	B	8.4	pIC50	4	nM	IC50	Nat Chem Biol (2009) 5: 37-44 [PMID:19029917]
Fatty acid amide hydrolase/Anandamide amidohydrolase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3455] [GtoPdb: 1400] [UniProtKB: O08914]
ChEMBL	Inhibition of FAAH in mouse brain membrane using [13C]oleamide as substrate by LC-MS analysis	B	5	pIC50	>10000	nM	IC50	J Med Chem (2016) 59: 2612-2632 [PMID:26888301]
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	5.33	pIC50	4700	nM	IC50	US-9133148-B2. Carbamate compounds and of making and using same (2015)
ChEMBL	Inhibition of FAAH in mouse brain membrane	B	5.33	pIC50	4690	nM	IC50	J Med Chem (2010) 53: 1830-1842 [PMID:20099888]
ChEMBL	Inhibition of FAAH in C57B1/6J mouse brain membrane after 20 mins by using oleamide as a substrate by LC-MS method	B	5.4	pIC50	4000	nM	IC50	Nat Chem Biol (2009) 5: 37-44 [PMID:19029917]
ChEMBL	Inhibition of FAAH in mouse brain membrane using oleamide as substrate preincubated for 30 mins	B	5.4	pIC50	4000	nM	IC50	Eur J Med Chem (2013) 63: 64-75 [PMID:23455058]
Fatty acid amide hydrolase/Anandamide amidohydrolase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3229] [GtoPdb: 1400] [UniProtKB: P97612]
ChEMBL	Inhibition of rat histidine tagged FAAH expressed in Escherichia coli by coumarin ester substrate fluorescence assay	B	6.01	pIC50	974	nM	IC50	Bioorg Med Chem Lett (2012) 22: 4585-4592 [PMID:22738638]
αβ-Hydrolase 6/Monoacylglycerol lipase ABHD6 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5010] [GtoPdb: 2919] [UniProtKB: Q8R2Y0]
ChEMBL	Inhibition of ABHD6 in mouse brain membrane	B	5.49	pIC50	3270	nM	IC50	J Med Chem (2010) 53: 1830-1842 [PMID:20099888]
monoacylglycerol lipase/Monoglyceride lipase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4191] [GtoPdb: 1399] [UniProtKB: Q99685]
ChEMBL	Inhibition of recombinant C-terminal His6-tagged human MAGL expressed in Escherichia coli using 2-arachidonoyl-[3H]-glycerol as substrate preincubated for 10 mins followed by substrate addition measured after 20 mins by scintillation counting method	B	5.35	pIC50	4440	nM	IC50	J Med Chem (2016) 59: 2612-2632 [PMID:26888301]
ChEMBL	Inhibition of human recombinant MAGL-mediated 1,3-dihydroxypropan-1-yl 4-pyren-1-ylbutanoate conversion to 4-pyren-1-ylbutanoic acid preincubated for 15 mins measured after 45 mins by HPLC analysis	B	5.77	pIC50	1700	nM	IC50	Eur J Med Chem (2013) 63: 64-75 [PMID:23455058]
ChEMBL	Inhibition of human His-tagged MAGL assessed as formation of arachidonic acid using 2-acylglycerol incubated for 10 mins by mass spectrometry	B	5.96	pIC50	1100	nM	IC50	J Med Chem (2021) 64: 11014-11044 [PMID:34328319]
ChEMBL	Inhibition of human recombinant MAGL	B	6.28	pIC50	520	nM	IC50	Eur J Med Chem (2013) 63: 64-75 [PMID:23455058]
ChEMBL	Inhibition of recombinant C-terminal His6-tagged human MAGL expressed in Escherichia coli using 2-arachidonoyl-[3H]-glycerol as substrate incubated for 20 mins by scintillation counting method	B	6.54	pIC50	285.2	nM	IC50	J Med Chem (2016) 59: 2612-2632 [PMID:26888301]
ChEMBL	Inhibition of human N-terminal histidine tagged full length MAGL expressed in Escherichia coli by by coumarin ester substrate fluorescence assay	B	7.24	pIC50	57	nM	IC50	Bioorg Med Chem Lett (2012) 22: 4585-4592 [PMID:22738638]
ChEMBL	Inhibition of human recombinant MAGL using 4-NPA as substrate after 30 mins	B	7.31	pIC50	49.3	nM	IC50	J Med Chem (2019) 62: 1932-1958 [PMID:30715876]
ChEMBL	Inhibition of human recombinant MAGL using 4-NPA substrate incubated for 30 mins	B	7.32	pIC50	48	nM	IC50	J Med Chem (2016) 59: 10299-10314 [PMID:27809504]
ChEMBL	Inhibition of human MAGL assessed as [3H]-2-OG hydrolysis preincubated for 30 mins before [3H]-2-OG addition measured after 10 mins by liquid scintillation counting	B	7.43	pIC50	37	nM	IC50	Bioorg Med Chem (2012) 20: 6260-6275 [PMID:23036333]
ChEMBL	Inhibition of MAGL	B	8	pIC50	10	nM	IC50	Bioorg Med Chem (2012) 20: 6260-6275 [PMID:23036333]
ChEMBL	Inhibition of recombinant MAGL (unknown origin) expressed in monkey COS7 cells	B	8.1	pIC50	8	nM	IC50	Eur J Med Chem (2013) 63: 64-75 [PMID:23455058]
GtoPdb	-	-	8.1	pIC50	7.94	nM	-	Nat Chem Biol (2009) 5: 37-44 [PMID:19029917]
ChEMBL	Inhibition of human MGL	B	8.22	pIC50	6	nM	IC50	J Med Chem (2009) 52: 7410-7420 [PMID:19583260]
ChEMBL	Inhibition of MAGL (unknown origin)	B	8.22	pIC50	6	nM	IC50	Eur J Med Chem (2016) 121: 318-330 [PMID:27267002]
ChEMBL	Inhibition of recombinant MAGL expressed in Cos7 cells after 30 mins by using 2-AG as a substrate by LC-MS method	B	8.22	pIC50	6	nM	IC50	Nat Chem Biol (2009) 5: 37-44 [PMID:19029917]
ChEMBL	Inhibition of recombinant human MAGL using fluorogenic-7HCA as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by fluorescence based assay	B	8.25	pIC50	5.6	nM	IC50	J Med Chem (2018) 61: 3008-3026 [PMID:29498843]
GtoPdb	-	-	8.4	pIC50	3.9	nM	IC50	Chem Biol (2012) 19: 579-88 [PMID:22542104]
ChEMBL	Inhibition of human MAGL expressed in monkey COS7 cells	B	8.7	pIC50	2	nM	IC50	Eur J Med Chem (2013) 63: 64-75 [PMID:23455058]
ChEMBL	Inhibition of human MAGL expressed in COS7 cells using endogenous 2-AG substrate	B	8.7	pIC50	2	nM	IC50	Bioorg Med Chem Lett (2012) 22: 4585-4592 [PMID:22738638]
monoacylglycerol lipase/Monoglyceride lipase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5774] [GtoPdb: 1399] [UniProtKB: O35678]
ChEMBL	Inhibition of MAGL in mouse brain membrane	B	8	pIC50	10	nM	IC50	J Med Chem (2010) 53: 1830-1842 [PMID:20099888]
ChEMBL	Inhibition of MAGL in C57B1/6J mouse brain membrane after 30 mins by using 2-AG as a substrate by LC-MS method	B	8.1	pIC50	8	nM	IC50	Nat Chem Biol (2009) 5: 37-44 [PMID:19029917]
ChEMBL	Inhibition of mouse recombinant MAGL expressed in african green monkey COS7 cells assessed as inhibition of 2-AG hydrolysis after 30 mins by LC-MS analysis	B	8.1	pIC50	8	nM	IC50	Bioorg Med Chem Lett (2011) 21: 6782-6787 [PMID:21982493]
ChEMBL	Inhibition of mouse MAGL	B	8.1	pIC50	8	nM	IC50	J Med Chem (2020) 63: 5783-5796 [PMID:32429662]
ChEMBL	Inhibition of MAGL-mediated 2-arachidonoylglycerol hydrolysis in mouse brain membranes preincubated for 30 mins	B	8.22	pIC50	6	nM	IC50	Eur J Med Chem (2013) 63: 64-75 [PMID:23455058]
ChEMBL	Inhibition of MAGL in mouse brain membrane using 2-AG as substrate by LC-MS analysis	B	8.22	pIC50	6	nM	IC50	Bioorg Med Chem Lett (2021) 41: 127986-127986 [PMID:33766770]
monoacylglycerol lipase/Monoglyceride lipase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3321] [GtoPdb: 1399] [UniProtKB: Q8R431]
ChEMBL	Inhibition of rat MAGL expressed in monkey COS7 cells	B	7.6	pIC50	25	nM	IC50	Eur J Med Chem (2013) 63: 64-75 [PMID:23455058]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]