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Inhibitory Effect on the Activity of Isoenzymes (CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYP3A4) of Human Liver Microsomal Cytochrome P450 from US Patent US20240294526: "FUSED TRI-CYCLIC COMPOUND AS A PDE3/PDE4 DUAL INHIBITOR"
Assay data:2 Tested
SummaryRelated BioAssays by DepositorRelated BioAssays by Target
Selectivity interaction (Time-dependent inactivation of CYP3A4 kinetics determination assay (using human liver microsomes)) EUB0001868a CYP3A4
Assay data:1 Tested
SummaryRelated BioAssays by Target
Selectivity interaction (Inhibition of CYP enzymes in human liver microsomes (LC/MS/MS based assay)) EUB0001868a CYP3A4
Selectivity interaction (CYP450 inhibition assay (in human liver microsomes)) EUB0000041b CYP3A4
Selectivity interaction (BET inhibitor selectivity panel (Human Vivid Red assay)) EUB0000102c CYP3A4
Selectivity interaction (BET inhibitor selectivity panel (Human Vivid Green assay)) EUB0000102c CYP3A4
The compounds are incubated at 0, 0.15, 0.5, 1.5, 5, 15 and 50 uM concentration at 37 C, CYP3A4 is pooled in a ratio such that biotransformation of each probe substrate is specific for the CYP450. Substrates (at their Km) are also pooled within the same solution to create an enzyme-substrate stock and test compound is added. The final solvent concentration is 1% DMSO. After equilibration to 37 C, addition of NADPH initiates substrate biotransformation. The incubation is stopped at 10 min by methanol containing internal standard. The quenched samples are centrifuged to precipitate the protein and the supernatants are analyzed by LC-MS/MS to measure metabolite formation. IC50 of test compounds against CYP3A4 is calculated. The assay has been performed by Concept Life Sciences Ltd.
Assay data:6 Active, 9 Tested
SummaryCompounds, ActiveRelated BioAssays by Target
Inhibition of CYP3A4 (unknown origin) at 10 uM relative to control
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of human liver microsomes CYP3A4 using Midazolam as substrate incubated for 5 mins with compound followed by substrate and NADPH addition measured after 5 mins by LC-MS/MS analysis
Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate assessed as midazolam 1'-hydroxylation preincubated for 5 mins followed by NADPH addition by UPLC-MS/MS analysis
Inhibition of CYP3A4 (unknown origin) expressed in baculovirus infected insect cells at 10 uM by P450-Glo assay relative to control
Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate at 10 uM incubated for 5 mins in presence of NADPH by LC-MS/MS analysis relative to control
Inhibition of human recombinant CYP3A4 using midazolam as substrate in presence of NADPH by LC-MS/MS analysis
Assay data:4 Active, 8 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Induction of CYP3A4 activity in human HepaRG cells at 5 to 10 uM incubated for 96 hrs by liquid chromatography with tandem mass spectrometry-based substrate cocktail assay
Induction of CYP3A4 activity in human HepaRG cells assessed as increase in fold change at 10 uM incubated for 96 hrs by liquid chromatography with tandem mass spectrometry-based substrate cocktail assay
Induction of CYP3A4 activity in human HepaRG cells assessed as increase in fold change at 0.5 uM incubated for 96 hrs by liquid chromatography with tandem mass spectrometry-based substrate cocktail assay
Inhibition of CYP3A4 (unknown origin)
Assay data:2 Active, 3 Tested
Induction of human liver CYP3A4 by qRT-PCR analysis
Inhibition of human liver microsomes CYP3A4 using midazolam as substrate by LC-MS/MS analysis
Assay data:1 Active, 5 Tested
Inhibition of CYP3A in human liver microsomes
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
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