Transcription of Hit discovery and hit-to-lead approaches
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Hit discovery and hit-to-lead approaches
Drug discovery Today Volume 11, Numbers 15/16 August 2006 REVIEWS. Reviews POST SCREEN. Hit discovery and hit-to-lead approaches Gyo rgy M. Keseru 1 and Gergely M. Makara2. 1. CADD&HTS Unit, Gedeon Richter Ltd, 19-21 Gyo mro i u t, Budapest, H-1103, Hungary 2. Merck Research Laboratories, Merck & Co, RY80Y-325, 126 E. Lincoln Ave, Rahway, New Jersey, 07065, USA. 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.
Drug Discovery Today Volume 11,Numbers 15/16 August 2006 REVIEWS Hit discovery and hit-to-lead approaches Gyo¨rgy M. Keseru˝1 and Gergely M. Makara2 1CADD&HTS Unit, Gedeon Richter Ltd, 19-21 Gyo¨mro˝iu´t, Budapest, H-1103, Hungary
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