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Drug Discov Today. 2006 Aug;11(15-16):741-8.

Hit discovery and hit-to-lead approaches.

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  • 1CADD&HTS Unit, Gedeon Richter Ltd, 19-21 Gyömroi út, Budapest, H-1103, Hungary.


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.

[PubMed - indexed for MEDLINE]
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