Analytical approaches to determine cytochrome P450 inhibitory potential of new chemical entities in drug discovery.

@article{Smith2007AnalyticalAT,
  title={Analytical approaches to determine cytochrome P450 inhibitory potential of new chemical entities in drug discovery.},
  author={Danielle M. Smith and N. Sadagopan and Michael A. Zientek and A. Raghuram Reddy and Lucinda H Cohen},
  journal={Journal of chromatography. B, Analytical technologies in the biomedical and life sciences},
  year={2007},
  volume={850 1-2},
  pages={455-63}
}
The use of a cassette incubation of probe substrates with human liver microsomes (HLM) - also known as the 'cocktail' approach - is becoming a widely accepted approach to determine the interaction of new chemical entities (NCEs) with cytochrome P450 enzymes (CYP450) in early drug discovery. This article describes two LC-MS/MS-based analytical methods used at the high-throughput (HT) stage and late discovery (LD) stage for analysis of 'cocktail' incubates to analyze the probe metabolites 1… CONTINUE READING

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