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J Biomol Tech. 2010 September; 21(3 Suppl): S8.
PMCID: PMC2918009

The Impact of Biophysical Techniques on the Small Molecule Drug Discovery Process



Biophysical analysis impacts speed and quality when applied to the small molecule discovery cascade by identifying better leads from screening campaigns providing more insight into inhibitor binding. Benefits include: 1) defining inhibitor binding stoichiometry 2) characterizing binding kinetics (kon/koff) 3) validating biochemical assays (KD vs Ki) 4) fine mapping of the molecular underpinnings of binding. The value of biophysical data may be offset by the intensive nature of acquisition. Therefore the impact of biophysical studies can be maximized when applied at key stages in the discovery process. Generally, this at the extremes of high and low affinity where automated screening methods are at their technical limit. Practical examples including, characterization of a XIAP BIR3 mutant for fragment based drug discovery and the VEGF Receptor-2 juxtramembrane on inhibition by Axitinib will be discussed.

Articles from Journal of Biomolecular Techniques : JBT are provided here courtesy of The Association of Biomolecular Resource Facilities