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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
Assay data:4 Active, 4 Activity ≤ 1 µM, 4 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
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
Assay data:5 Active, 1 Activity ≤ 1 nM, 5 Activity ≤ 1 µM, 5 Tested
Inhibition of recombinant human C-terminal sEH (222 to 555 residues) expressed in Escherichia coli BL21-DE3 using PHOME as substrate assessed as reduction in 6-methoxy-2-naphthaldehyde formation incubated for 30 mins followed by substarte addition and measured after 30 mins by fluorescence based assay
Assay data:3 Active, 3 Activity ≤ 1 µM, 3 Tested
Assays for Epoxide Hydrolase Activity from US Patent US11123311: "Methods of treating mental disorders"
Assay data:62 Active, 26 Activity ≤ 1 nM, 57 Activity ≤ 1 µM, 62 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Inhibition Assay from US Patent US10383835: "Treatment of inflammatory disorders in non-human mammals"
Assay data:25 Active, 6 Activity ≤ 1 nM, 20 Activity ≤ 1 µM, 25 Tested
FRET-displacement assay from US Patent US10377744: "Potent soluble epdxide hydrolase inhibitors"
Assay data:55 Active, 29 Activity ≤ 1 nM, 55 Activity ≤ 1 µM, 55 Tested
Fluorescent Based Assay from US Patent US9296693: "Acyl piperidine inhibitors of soluble epoxide hydrolase"
Assay data:50 Active, 17 Activity ≤ 1 nM, 47 Activity ≤ 1 µM, 52 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
Binding affinity to purified recombinant human sEH by FRET-displacement assay
Assay data:8 Active, 6 Activity ≤ 1 nM, 8 Activity ≤ 1 µM, 8 Tested
Inhibition of recombinant human full length sEH (1 to 555 residues) expressed in Escherichia coli BL21 DE3 cells assessed as reduction in 6-methoxynaphthaldehyde formation using PHOME as substrate incubated for 45 mins followed by substrate addition and measured for 45 mins by fluorescence based assay
Assay data:6 Active, 3 Activity ≤ 1 µM, 9 Tested
Inhibition of soluble epoxide hydrolase in human HepG2 cells assessed as reduction in conversion of EET to DHET at 10 nM using (+/-)14(15)-EET-d11 as substrate preincubated for 15 mins followed by substrate addition and measured after 10 mins by LC-MS/MS analysis
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of rat soluble epoxide hydrolase using [3H]-t-DPPO as a substrate by radiometric assay
Assay data:6 Active, 6 Activity ≤ 1 µM, 6 Tested
Cmax in Swiss Webster mouse at 0.3 mg/kg, po administered as cassette dosing
Assay data:20 Active, 19 Activity ≤ 1 µM, 20 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed Citation
Inhibition of human recombinant soluble epoxide hydrolase by FRET-based ACPU displacement assay
Assay data:32 Active, 17 Activity ≤ 1 nM, 32 Activity ≤ 1 µM, 32 Tested
Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB
Assay data:3598 Active, 421 Activity ≤ 1 nM, 2233 Activity ≤ 1 µM, 3598 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Inhibition of human recombinant soluble epoxide hydrolase assessed as cyano(6-methoxy-naphthalen-2-yl)methyl trans-[(3-phenyloxyran-2-yl)methyl] carbonate conversion to 6-methoxy-2-naphthaldehyde preincubated for 5 mins prior to substrate addition by fluorescence assay
Assay data:19 Active, 14 Activity ≤ 1 nM, 19 Activity ≤ 1 µM, 20 Tested
Inhibition of mouse recombinant soluble epoxide hydrolase by fluorescence assay
Assay data:47 Active, 12 Activity ≤ 1 nM, 45 Activity ≤ 1 µM, 52 Tested
Inhibition of human recombinant soluble epoxide hydrolase by fluorescence assay
Assay data:50 Active, 12 Activity ≤ 1 nM, 46 Activity ≤ 1 µM, 52 Tested
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