GSK2256294 [Ligand Id: 9718] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3818875 (Gsk2256294, GSK-2256294, GSK-2256294A)
  • epoxide hydrolase 2/Epoxide hydratase in Human [ChEMBL: CHEMBL2409] [GtoPdb: 2970] [UniProtKB: P34913]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
epoxide hydrolase 2/Epoxide hydratase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2409] [GtoPdb: 2970] [UniProtKB: P34913]
ChEMBL Inhibition of recombinant human sHE assessed as product formation preincubated for 30 mins followed by addition of (3-phenyl-cyano-(6-methoxy-2-naphthalenyl)methyl ester-2-oxirane-acetic acid as substrate measured after 30 mins by fluorescence analysis B 6.96 pIC50 110 nM IC50 Medchemcomm (2016) 7: 1209-1216
GtoPdb In a biochemical enzyme assay. - 6.96 pIC50 110 nM IC50 Medchemcomm (2016) 7: 1209-1216
ChEMBL Inhibition of soluble epoxide hydrolase in human whole blood B 8.17 pIC50 6.83 nM IC50 J Med Chem (2020) 63: 6578-6599 [PMID:32039601]
ChEMBL Inhibition of soluble epoxide hydrolase (unknown origin) B 8.8 pIC50 1.58 nM IC50 J Med Chem (2020) 63: 6578-6599 [PMID:32039601]
ChEMBL Inhibition of human sEH (1 to 555 residues) expressed in Escherichia coli BL21-(DE3) using PHOME substrate incubated for 30 to 45 mins by fluorescence based assay B 9.15 pIC50 0.7 nM IC50 J Med Chem (2020) 63: 11498-11521 [PMID:33044073]
ChEMBL Inhibition of recombinant human soluble epoxide hydrolase expressed in HEK293 cells B 9.18 pIC50 0.66 nM IC50 J Med Chem (2020) 63: 6578-6599 [PMID:32039601]
ChEMBL Inhibition of human recombinant sEH using 14,15-epoxy-5Z,8Z,11Z-eicosatrienoic acid as substrate assessed as formation of 14,15-dihydroxy-5Z,8Z,11Zeicosatrienoic acid preincubated for 2 hrs followed by substrate addition measured after 1 hr by LC/MS method B 10.55 pIC50 0.03 nM IC50 J Med Chem (2016) 59: 6629-6644 [PMID:26914744]
ChEMBL Inhibition of recombinant human soluble epoxide hydrolase B 10.57 pIC50 0.03 nM IC50 J Med Chem (2020) 63: 6578-6599 [PMID:32039601]
ChEMBL Inhibition of recombinant human sEH using MNPC as substrate by fluorescence-based assay B 10.57 pIC50 0.03 nM IC50 J Med Chem (2018) 61: 3541-3550 [PMID:29614224]

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]