ADMET and DMPK (Dec 2019)

Biophysical methods in early drug discovery

  • Geoffrey Holdgate,
  • Kevin Embrey,
  • Alexander Milbradt,
  • Gareth Davies

DOI
https://doi.org/10.5599/admet.733
Journal volume & issue
Vol. 7, no. 4
pp. 222 – 241

Abstract

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Biophysical methods such as mass spectrometry, surface plasmon resonance, nuclear magnetic resonance, and both differential scanning isothermal titration calorimetry are now well established as key components of the early drug discovery process. These approaches are used successfully for a range of activities, including assay development, primary screening, hit confirmation and detailed mechanistic characterisation of compound binding. Matching the speed, sensitivity and information content of the various techniques to the generation of critical data and information required at each phase of the drug discovery process has been key. This review describes the framework by which these methods have been applied in the drug discovery process and provides case studies to exemplify the impact.

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