铅(地质)
仿形(计算机编程)
计算机科学
风险分析(工程)
鉴定(生物学)
过程(计算)
药物发现
生化工程
工程类
生物信息学
医学
生物
植物
操作系统
古生物学
作者
Frank Narjes,Garry Pairaudeau,Dušan Petrović
出处
期刊:The Royal Society of Chemistry eBooks
[The Royal Society of Chemistry]
日期:2023-02-03
卷期号:: 682-719
标识
DOI:10.1039/9781788018982-00682
摘要
The lead generation phase is the stage in early drug discovery that refers to the process of identifying hit molecules that interact with the desired target, followed by a limited optimisation of those hits. During this period the project aims to identify high-quality chemical tools suitable for advanced cellular and in vivo studies which will help to strengthen the validation of the target and increase confidence in the proposed therapeutic hypothesis. This chapter gives an overview of the major hit finding approaches together with their strengths and limitations. The process of hit profiling and hit selection, as well as hit expansion, are illustrated, and complications that can be encountered during this initial phase are highlighted. The advantage of using an integrated lead generation strategy is emphasised. A well-defined lead generation strategy, where two or more complementary hit finding approaches are executed in parallel, combined with a screening cascade containing relevant biological assays, will often result in the identification of structurally diverse lead series, leading ultimately to successful clinical candidates.
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