Wright, Kirk (2017) Biophysics: for HTS hit validation, chemical lead optimization and beyond. Expert opinion on drug discovery, 12 (9). pp. 1-11. ISSN 1746-045X

Abstract

Introduction: There are many challenges to the drug discovery process, including the complexity of the target, its interactions, and how these factors play a role in causing the disease. Traditionally, biophysics has been used for hit validation and chemical lead optimization. With its increased throughput and sensitivity, biophysics is now being applied earlier in this process to empower target characterization and hit finding.

Areas covered: In this article, we will provide an overview of how biophysics can be utilized to assess the quality of the reagents used in screening assays, to validate potential tool compounds, to test the integrity of screening assays, and to create follow-up strategies for compound characterization. We will also briefly discuss the utilization of different biophysical methods in hit validation to help avoid the resource consuming pitfalls caused by the lack of hit overlap between biophysical methods.

Item Type:	Article
Keywords:	Biophysics; screening; hit validation; chemical lead optimization; covalent modification; allosteric; thermal shift assays; surface plasmon resonance; cellular thermal shift assays
Date Deposited:	29 Aug 2017 00:45
Last Modified:	29 Aug 2017 00:45
URI:	https://oak.novartis.com/id/eprint/32697