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Binding affinity to rat CYP3A2
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of rat CYP3A2
Inhibition of CYP3A2 in rat liver microsomes using midazolam as substrate
Inhibition of CYP3A2-mediated metabolite formation in rat liver microsomes assessed as reduction in N-(1-((2R,4R,5R)-3,3-difluoro-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-2-oxo-1,2-dihydropyrimidin-4-yl)pentadecanamide metabolism
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Drug metabolism in male rat liver microsomes assessed as CYP3A2-mediated 2-(4-(2-((1H-Benzo[d]imidazol-2-yl)thio)ethyl)piperazin-1-yl)-N-(6-methyl-2-(methyl-sulfinyl)-4-(methylthio)pyridin-3-yl)acetamide formation
Drug metabolism in male rat liver microsomes assessed as CYP3A2-mediated 2-(4-(2-((1H-Benzo[d]imidazol-2-yl)thio)ethyl)piperazin-1-yl)-N-(6-methyl-4-(methylsulfinyl)-2-(methylthio)pyridin-3-yl)acetamide formation
Drug metabolism assessed as rat recombinant CYP3A2-mediated sulindac sulfone formation measured per pmol of protein at 200 uM after 90 mins by HPLC analysis
Drug metabolism assessed as rat recombinant CYP3A2-mediated sulindac sulfone formation measured per pmol of protein at 500 uM after 90 mins by HPLC analysis
Activity of rat recombinant CYP3A2 expressed in baculovirus-infected insect cells assessed as enzyme-mediated N-((4-(4-fluorophenyl)-2-oxochroman-7-yl)methyl)-2-((S)-2-hydroxy-2-(trifluoromethyl)butanoyl)hydrazinecarboxamide formation preincubated for 3 mins by Michaelis-Menten equation in presence of NADPH for 10 mins
Activity of rat recombinant CYP3A2 expressed in baculovirus-infected insect cells assessed as enzyme-mediated compound formation treated with setileuton at 10 uM preincubated for 3 mins measured after 30 mins in presence of 1 mM NADPH
Activity of rat recombinant CYP3A2 expressed in baculovirus-infected insect cells assessed as enzyme-mediated N-((4-(4-fluorophenyl)-2-oxochroman-7-yl)methyl)-2-((S)-2-hydroxy-2-(trifluoromethyl)butanoyl)hydrazinecarboxamide formation at 10 uM preincubated for 3 mins measured after 30 mins in presence of 1 mM NADPH
Mechanism based inhibition of rat cytochrome P450 CYP3A2 measured by testosterone hydroxylation at positions 2-beta and 6-beta
Mechanism based inhibition of rat cytochrome P450 CYP3A2
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