ABSTRACT
The rapid pace of gene discovery in the 1990s has accelerated the innovation and application of related discovery sciences: medicinal chemistry and highthroughput screening (HTS). To understand a gene product’s function and definitively ascertain its therapeutic potential, more targets are screened against everexpanding collections of small molecules than before. It is now commonplace to describe compound collections in the millions and the throughput of a screen in hundreds of thousands per week. The numbers are staggering, but the process of target discovery, lead discovery, lead optimization, and development of a drug candidate demands testing numerous and diverse molecules against newly identified gene products to ascertain their biological, and potentially pathological, roles.
