Discovery Plus™ Screening: Cytochrome P450 (CYP) Enzyme Inhibition
Our Discovery Plus™ CYP Inhibition Screening service gives you quick, low-cost inhibition data for one or more compounds to inform you of your drug candidates’ potential to inhibit major cytochrome P450 (CYP) drug-metabolizing enzymes within 15 business days, allowing preliminary ADME evaluation and efficient prediction of drug-drug interactions (DDI) in early stages of drug development.
Discovery Plus™ CYP Inhibition is more than just a screening service. Our 96-well plate format offers data for the seven enzymes recommended by regulatory agencies for both direct and time-dependent inhibition. Discovery Plus™ Inhibition is a non-GLP, medium-throughput service that quickly provides customers with a data summary of results. This service is best utilized for compounds that are in the discovery or early development phase.
For compounds that will be submitted for regulatory agency approval, please see our definitive CYP Inhibition service.
Our Approach to Medium-Throughput Enzyme Inhibition Screening for IC50 Calculation
Our Discovery Plus™ design offers the most value in the industry, providing you important data quickly at an attractive price point.This abbreviated study design uses pooled human liver microsomes in an assay designed to minimize inhibitor and substrate depletion. Incubations are conducted using automated liquid handling systems and IC50 values can be determined for time-dependent (i.e., 30-min preincubation) and/or direct inhibition (i.e., zero-min preincubation). Substrates are incubated in a cocktail format, and a tabular summary of IC50 values will be provided upon completion. The global CYP inhibitor, 1-aminobenzotriazole (1-ABT), can be added as a positive control upon request.
CYP Substrate Cocktail
| Enzyme | Substrate |
|---|---|
| CYP1A2 | Phenacetin O-dealkylation |
| CYP2B6 | Bupropion hydroxylation |
| CYP2C8 | Paclitaxel 6α-hydroxylation |
| CYP2C9 | Diclofenac 4´ -hydroxylation |
| CYP2C19 | S-Mephenytoin 4´ -hydroxylation |
| CYP2D6 | Dextromethorphan O-demethylation |
| CYP3A4/5 | Midazolam 1´ -hydroxylation |
See the Science
Check out our poster discussing “High Content Automated Metabolic Stability and CYP Inhibition Cocktail Screening Assays for Early Drug Development.”
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