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 Displacement of (1R,3S)-N-(4-methoxy-2-(trifluoromethyl)benzyl)-3-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)cyclohexane-1-carboxamide from NanoLuc-fused human sEH ( 1 to 555 residues) expressed in HEK293T cells incubated for 5 hrs by NanoBRET analysis B 7.62 pKi 24 nM Ki ACS Med Chem Lett (2022) 13: 1062-1067 [PMID:35859883]
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 C-terminal domain of human sEH-H assessed as reduction in fluorescent naphthalene aldehyde formation using PHOME as substrate preincubated with enzyme for 30 mins followed by substrate addition and measured every minute for 45 mins by fluorescence based analysis B 9.05 pIC50 0.9 nM IC50 ACS Med Chem Lett (2022) 13: 1062-1067 [PMID:35859883]
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 human sEH BacMam transduced HEK293 cells assessed as reduction in 14,15-DHET formation using 14,15-EET as substrate preincubated for 30 mins followed by susbtrate addition and measured after 90 mins by fluorescence polarization assay B 9.18 pIC50 0.66 nM IC50 ACS Med Chem Lett (2022) 13: 1062-1067 [PMID:35859883]
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 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]