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Inhibition Screening

Our inhibition screening service offers fluorimetry based assays to determine the CYP inhibition potential of novel compounds, using bactosomes as the enzyme source.

Our approach ensures cost-effective results that you can rely on.

 

What you can expect:

  • 8 major human CYPs covered: CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP3A4, and CYP3A5.
  • Dog and pig CYPs covered
  • CYP activity determined at 7 different compound concentrations plus zero and fitted to a model using XLfit® software, before determining an IC50 value.
  • 30-minute incubation time – shifts in IC50 value over time can indicate whether the compound has the potential to be a time-dependent inhibitor of each CYP isoform.
  • Positive control inhibitor and multi-well negative control are run in parallel on every plate, giving confidence in the end result.
  • Recommended solvents are DMSO and methanol up to 2.5% (v/v), assuming compound solubility.
  • Cost effective and fast turnaround of data after receipt of compound.

 

Download details of the assay

 

We have recently developed a fluorimetry based inhibition screen for human CYP51, details were presented at the 2019 International ISSX meeting in portland Oregon.  Download the poster

Contact our specialist team for more information

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