Hit discovery and hit-to-lead approaches.
Hit discovery technologies range from traditional high-throughput screening to affinity selection of large libraries, fragment-based techniques and computer-aided de novo design, many of which have been extensively reviewed. Development of quality leads using hit confirmation and hit-to-lead approaches present their own challenges, depending on the hit discovery method used to identify the initial hits. In this paper, we summarize common industry practices adopted to tackle hit-to-lead challenges and review how the advantages and drawbacks of different hit discovery techniques could affect the various issues hit-to-lead groups face.
Keseru
György M
GM
CADD&HTS Unit, Gedeon Richter Ltd, 19-21 Gyömroi út, Budapest, H-1103, Hungary.
Makara
Gergely M
GM
D000818:Animals; D017076:Computer-Aided Design; D015195:Drug Design; D004353:Drug Evaluation, Preclinical / Q000379:methods; D004345:Drug Industry / Q000379:methods; D006801:Humans; D013678:Technology, Pharmaceutical / Q000379:methods*