JZL184 [Ligand Id: 5207] activity data from GtoPdb and ChEMBL

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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]
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  • αβ-Hydrolase 6/Monoacylglycerol lipase ABHD6 in Mouse [ChEMBL: CHEMBL5010] [GtoPdb: 2919] [UniProtKB: Q8R2Y0]
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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]
  • monoacylglycerol lipase/Monoglyceride lipase in Rat [ChEMBL: CHEMBL3321] [GtoPdb: 1399] [UniProtKB: Q8R431]
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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 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 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]