ADMET and DMPK, Vol. 7 No. 4, 2019.
Review article
https://doi.org/10.5599/admet.733
Biophysical methods in early drug discovery
Geoffrey Holdgate
; Hit Discovery, Discovery Sciences, R&D, AstraZeneca, Alderley Park, UK
Kevin Embrey
; Structure, Biophysics and FBLG, Discovery Sciences, R&D, AstraZeneca, Cambridge, UK
Alexander Milbradt
; Structure, Biophysics and FBLG, Discovery Sciences, R&D, AstraZeneca, Cambridge, UK
Gareth Davies
; Hit Discovery, Discovery Sciences, R&D, AstraZeneca, Alderley Park, UK
Abstract
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.
Keywords
Affinity selection mass spectrometry; surface plasmon resonance; nuclear magnetic resonance; differential scanning fluorimetry; isothermal titration calorimetry; microscale thermophoresis
Hrčak ID:
229486
URI
Publication date:
11.12.2019.
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