Conventional CYP Inhibition Screen

The DDI conventional inhibition screen is moderate throughput and can range from a few compounds per week to a few hundred per week depending on the amount of inhibitor concentrations, inhibition curve replicates and analytical methods used. This screen typically uses 96- or 384-well formats. The reaction components (HLM, 100 mM potassium phosphate buffer, specific probe substrate, NCE, NADPH cofactor or NAD PH-regenerating system) are pre-warmed to 37 °C and are mixed together to initiate the reaction, then incubated at 37 °C for the appropriate length of 

CYP Conventional probe Substrate Km Fluorescent probe Inhibitor Inhibitor Comments concentration Substrate Recommended screening concentration  

CYP1A2 Phenacetin O-deethylation 1.7-152 CEC 5 Furafylline 10 pM Inactivator, peincubation for 15 min 

CYP2B6 Bupropion hydroxylation 61-168 EEC 2.5 Methyl-phenyl-ethyl 10 pM  

CYP2C8 Taxol 6-hydroxylation 5.4-19 DBF 1 Montelukast 0.1 pM Potency decreases upon increased 

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