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Expert Knowledge


Concerned about CYP Inhibition in your current chemical series? Whether to pool or not to pool …

Concerned about CYP Inhibition in your current chemical series? Would you like a solution which allows you to test using a smaller budget and less of your precious material? Investigate whether to pool or not to pool…

CYP450 inhibition refers to the ability of a drug or compound to interfere with the activity of these enzymes, thereby reducing their ability to metabolize other drugs. This can result in elevated levels of the affected drugs in the bloodstream, potentially leading to adverse effects or toxicity.

In drug discovery, assessing the potential for a new compound to inhibit CYP450 enzymes is important for several reasons:

  • Drug-Drug Interactions: Most drugs undergo metabolic transformation via CYP450 enzymes, so if a new drug inhibits these enzymes, it can interfere with the metabolism of other drugs taken concurrently by a patient. This can lead to unexpected interactions and adverse effects.
  • Pharmacokinetics: CYP450 inhibition can alter the absorption, distribution, metabolism, and excretion of drugs, affecting their bioavailability, half-life, and clearance from the body. Understanding how a new compound interacts with CYP450 enzymes helps predict its potential effects in vivo.
  • Safety: Inhibition of specific CYP450 enzymes can lead to the accumulation of toxic metabolites or parent compounds, increasing the risk of adverse reactions or toxicity. Assessing CYP450 inhibition during drug discovery helps identify compounds with a lower risk of causing such issues.

For all these reasons, assessing CYP450 inhibition early is critical to any drug discovery project. Whilst over 50 genes encoding for CYP450 enzymes have been identified in human, 5 isoforms, CYP1A2, 2C9, 2C19,2D6 and 3A4 are responsible for nearly 80% of all CYP450-mediated metabolism. CYP450 inhibition assays for these isoforms are therefore integral to drug discovery campaigns and typically embedded early within a screening cascade.

We have incubated within our laboratories a pooled CYP450 assay whereby all 5 main isoforms listed above are concomitantly tested. The fully validated assay available as part of our in vitro ADMET services offers many advantages over single isoform testing, including saving precious material and significantly reducing testing costs. This means more compounds can be characterised for CYP450 inhibition and insightful Structure Activity Relationships derived, providing powerful tools to reduce risk of clinical attrition.

Download our assay card here to learn more.

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