N-ethylmaleimide [Ligand Id: 5335] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL8211
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  • monoacylglycerol lipase/Monoglyceride lipase in Human [ChEMBL: CHEMBL4191] [GtoPdb: 1399] [UniProtKB: Q99685]
  • 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
DAT/Dopamine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977]
ChEMBL Inhibition of [3H]dopamine uptake at DAT in rat brain striatal synaptosomes by liquid scintillation counting analysis B 4.33 pIC50 46773.51 nM IC50 J Med Chem (2017) 60: 839-885 [PMID:27996267]
monoacylglycerol lipase/Monoglyceride lipase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4191] [GtoPdb: 1399] [UniProtKB: Q99685]
ChEMBL Displacement of [3H]2-OG from human MGL by liquid scintillation counting B 4.78 pIC50 16600 nM IC50 J Med Chem (2009) 52: 7410-7420 [PMID:19583260]
monoacylglycerol lipase/Monoglyceride lipase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3321] [GtoPdb: 1399] [UniProtKB: Q8R431]
ChEMBL Inhibition of rat cerebellar membranes MAGL-like activity preincubated for 30 mins followed by 2-AG substrate addition after 90 mins by HPLC analysis B 4.28 pIC50 53000 nM IC50 J Med Chem (2017) 60: 4-46 [PMID:27766867]

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]