Keseru György M, Makara Gergely M
CADD&HTS Unit, Gedeon Richter Ltd, 19-21 Gyömroi út, Budapest, H-1103, Hungary.
Drug Discov Today. 2006 Aug;11(15-16):741-8. doi: 10.1016/j.drudis.2006.06.016.
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.
命中发现技术涵盖从传统的高通量筛选到大型文库的亲和选择、基于片段的技术以及计算机辅助从头设计，其中许多技术都已得到广泛综述。利用命中确认和从命中到先导物的方法来开发高质量先导物会带来各自的挑战，这取决于用于识别初始命中的命中发现方法。在本文中，我们总结了为应对从命中到先导物阶段的挑战而采用的常见行业做法，并回顾了不同命中发现技术的优缺点如何影响从命中到先导物阶段团队所面临的各种问题。
