Enriching chemical space to drug undruggable targets Seminar

The pharmaceutical industry is an enormously successful business sector. However, the current challenges facing the industry are unprecedented. Foremost among these challenges are the industry’s diminishing revenue forecasts due to the decreasing number of new chemical entity (NCE) approvals. A high attrition rate of clinical candidates (ca. 93–96%) is prevalent throughout the industry. Pharma’s recent dramatic restructuring is largely due to this high attrition rate. My talk aims to highlight some of the underlying factors of this. Namely, (1) the relative lack of structural diversity and (2) the relative lack of targets exploited in drug discovery. The talk will include recent research within my laboratory aimed at addressing these issues using diversity-oriented synthesis and constrained variants of the approach. [H. Beckmann, C. J. O' Connor, D. R. Spring, Chem. Soc. Rev. 2012, 41, 4444-4456.]