UNIT 3.9 Cytochrome P450 Assays

  1. Enock Delaporte,
  2. A. David Rodrigues

Published Online: 1 FEB 2002

DOI: 10.1002/0471141755.ph0309s15

Current Protocols in Pharmacology

Current Protocols in Pharmacology

How to Cite

Delaporte, E. and Rodrigues, A. D. 2002. Cytochrome P450 Assays. Current Protocols in Pharmacology. 15:3.9:3.9.1–3.9.32.

Author Information

  1. Merck Research Labs, West Point, Pennsylvania

Publication History

  1. Published Online: 1 FEB 2002
  2. Published Print: DEC 2001


Cytochrome P450s (CYPs) play a major role in drug detoxification, and inhibition of CYP-mediated metabolism may lead to accumulation of toxic drug levels in the plasma. To prevent adverse drug-drug interactions, new drug candidates are routinely tested for their ability to inhibit these enzymes. This unit describes a variety of protocols for evaluating new chemical entities as inhibitors of CYP activity. An example protocol illustrates a high-throughput screening format using a fluorogenic probe, and a method for evaluating a test compound as a time-dependent inhibitor of CYP is also described.