Discovery Plus Inhibition Screening

Overview


Sekisui XenoTech's Discovery Plus™ Inhibition Screen 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 service that provides customers with a data summary of results in about a week. This service is best utilized for compounds that are in the early discovery phase/early development phase. For compounds that will be submitted for regulatory agency approval, please visit our standard CYP inhibition service page for definitive screening.

View XenoTech's Discovery Plus™ Inhibition Poster
 

IC50 Determinations


XenoTech offers the ability to perform IC50 experiments based on values that are calculated from area ratios with the flexibility to evaluate direct inhibition and time-dependent inhibition using a seven substrate cocktail.  The global P450 inhibitor, 1-aminobenzotriazole (1-ABT), can be added as a positive control upon request.

Cocktail Substrate:
 
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
 

Test System & Incubation Conditions


Test system: pool of 200 individuals, mixed gender, human liver microsomes
Designed to minimize inhibitor and substrate depletion
Zero-minute (direct) and/or 30-minute (time-dependent) pre-incubation
​Robotic incubations
 

Results


A tabulated summary of IC50 values will be provided
Note: Results are provided in ~1 week for every 24 compounds submitted
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