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ChEMBL ligand: CHEMBL3818875 (Gsk2256294, GSK-2256294, GSK-2256294A) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]