With the growing need to streamline the drug discovery process, screening against fragment libraries rather than drug-like molecules has become increasingly adopted as an integral part of many drug discovery programmes. However, success depends on the quality of the fragment library, and many factors dictate quality. This review will look at how recent research has influenced the paradigms underlining fragment library design, and its evolution from infancy to its current status today.
For HTS laboratories worldwide, the mission is to supply therapeutic groups – in the shortest time possible – with high quality hits and leads that will become drug candidates. Mounting pressure to screen more targets against more compounds while providing more information per screen has HTS directors seeking improvements to existing technologies as well as innovative new approaches and tools.