Hit and lead identification: Integrated technology-based approaches

For many targets in drug discovery, the identification of a small molecule ‘hit’ as a starting point for the hit-to-lead process is a critical early step. Over the years different technology-based strategies have evolved in an attempt to enhance the rate and efficiency of this important phase of the drug discovery process known as hit identification. In adapting the appropriate strategy or strategies to each hit and, subsequently, lead identification problem, it is important to consider the different types of available approaches, as well as take into account what may have been successful for a similar target in the past. In short, not all hit identification problems are the same and thus, should not be approached as if they were.

Section editors:Tudor Oprea – University of New Mexico School of Medicine, Albuquerque, USAAlex Tropsha – University of North Carolina, Chapel Hill, USA