The CYP inhibition assay is one of the in vitro ADME studies that assesses the ability of compounds to inhibit cytochrome P450 (CYP) enzymes. Cytochrome P450 is a superfamily of heme-containing enzymes that mediate the inactivation and metabolism of many drugs and endogenous substances. It is important to assess the ability of compounds to inhibit specific CYP enzymes because drugs may inhibit each other's metabolism when used together. This may affect drug concentrations in the body and may lead to adverse drug reactions or toxicity.
CYP inhibition profiling examined the effect of the test compounds on the metabolism of five major human metabolisms of other known substrates of CYP: 1A2, 2B6, 2C9, 2D6, and 3A4. IC50 values (concentration of the test compounds that produces 50% inhibition) were calculated by comparing reductions in metabolite formation as compared to a blank control.
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