Designing screens: how to make your hits a hit.
The basic goal of small-molecule screening is the identification of chemically 'interesting' starting points for elaboration towards a drug. A number of innovative approaches for pursuing this goal have evolved, and the right approach is dictated by the target class being pursued and the capabilities of the organization involved. A recent trend in high-throughput screening has been to place less emphasis on the number of data points that can be produced, and to focus instead on the quality of the data obtained. Several computational and technological advances have aided in the selection of compounds for screening and widened the variety of assay formats available for screening. The effect on the efficiency of the screening process is discussed.
Walters
W Patrick
WP
Vertex Pharmaceuticals, 130 Waverley Street, Cambridge, Massachusetts 02139, USA.
Namchuk
Mark
M
D015195:Drug Design; D004353:Drug Evaluation, Preclinical / Q000379:methods*; D006801:Humans; D004364:Pharmaceutical Preparations / Q000032:analysis*; D010601:Pharmacology, Clinical / Q000639:trends*; D047428:Protein Kinase Inhibitors; D011494:Protein Kinases / Q000235:genetics / Q000502:physiology
D004364:Pharmaceutical Preparations; D047428:Protein Kinase Inhibitors; D011494:Protein Kinases