JZL195 [Ligand Id: 8606] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL606201
  • 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]
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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]
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  • acyloxyacyl hydrolase in Human [GtoPdb: 2873] [UniProtKB: P28039]
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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 using AMC-AA as substrate preincubated with enzyme for 10 mins followed by substrate addition for 2 hrs by fluorometric analysis B 7.72 pIC50 19 nM IC50 Eur J Med Chem (2022) 237: 114358-114358 [PMID:35462163]
ChEMBL Inhibition of recombinant human FAAH using AMC-AA as substrate preincubated for 10 mins followed by substrate addition measured after 2 hrs by fluorometric assay B 7.72 pIC50 19 nM IC50 J Med Chem (2023) 66: 235-250 [PMID:36542836]
ChEMBL Inhibition of recombinant human FAAH incubated for 5 mins followed by substrate addition by cayman fluorescence based multimode microplate reader assay B 8.7 pIC50 2 nM IC50 Bioorg Med Chem (2022) 60: 116698-116698 [PMID:35296453]
ChEMBL Inhibition of recombinant FAAH (unknown origin) expressed in COS7 cells assessed as blockade of substrate hydrolysis using 2-AG as substrate preincubated with compound for 30 mins followed by substrate addition B 8.7 pIC50 2 nM IC50 Bioorg Med Chem Lett (2022) 68: 128763-128763 [PMID:35500728]
GtoPdb in vitro assay - 8.7 pIC50 2 nM IC50 Proc Natl Acad Sci USA (2009) 106: 20270-5 [PMID:19918051]
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 B 7.89 pIC50 13 nM IC50 J Med Chem (2010) 53: 1830-1842 [PMID:20099888]
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 7.3 pIC50 50 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 human recombinant MAGL pre-incubated for 5 mins before MAGL substrate addition and further incubated for 10 mins B 6.69 pIC50 204.5 nM IC50 J Med Chem (2020) 63: 5783-5796 [PMID:32429662]
ChEMBL Inhibition of human recombinant MAGL incubated for 5 mins followed by substrate addition by cayman fluorescence based multimode microplate reader assay B 8.4 pIC50 4 nM IC50 Bioorg Med Chem (2022) 60: 116698-116698 [PMID:35296453]
ChEMBL Inhibition of recombinant MAGL (unknown origin) expressed in COS7 cells assessed as blockade of substrate hydrolysis using AEA as substrate preincubated with compound for 30 mins followed by susbstrate addition B 8.4 pIC50 4 nM IC50 Bioorg Med Chem Lett (2022) 68: 128763-128763 [PMID:35500728]
GtoPdb in vitro assay - 8.4 pIC50 4 nM IC50 Proc Natl Acad Sci USA (2009) 106: 20270-5 [PMID:19918051]
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 7.72 pIC50 19 nM IC50 J Med Chem (2010) 53: 1830-1842 [PMID:20099888]
Neuropathy target esterase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3259506] [UniProtKB: Q3TRM4]
ChEMBL Inhibition of NTE in mouse brain membrane B 4.3 pIC50 >50000 nM IC50 J Med Chem (2010) 53: 1830-1842 [PMID:20099888]
acyloxyacyl hydrolase in Human [GtoPdb: 2873] [UniProtKB: P28039]
GtoPdb - - 7.36 pIC50 44 nM IC50 Nat Chem Biol (2014) 10: 656-63 [PMID:24997602]

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]