Applied Biophysics for Drug Discovery

Applied Biophysics for Drug Discovery is a guide to new techniques and approaches to identifying and characterizing small molecules in early drug discovery. Biophysical methods are reasserting their utility in drug discovery and through a combination of the rise of fragment–based drug discovery and an increased focus on more nuanced characterisation of small molecule binding, these methods are playing an increasing role in discovery campaigns.

This text emphasizes practical considerations for selecting and deploying core biophysical method, including but not limited to ITC, SPR, and both ligand–detected and protein–detected NMR.

Topics covered include:

Design considerations in biophysical–based lead screening

Thermodynamic characterization of protein–compound interactions

Characterizing targets and screening reagents with HDX–MS

Microscale thermophoresis methods (MST)

Screening with Weak Affinity Chromatography

Methods to assess compound residence time

1D–NMR methods for hit identification

Protein–based NMR methods for SAR development

Industry case studies integrating multiple biophysical methods

This text is ideal for academic investigators and industry scientists planning hit characterization campaigns or designing and optimizing screening strategies.