High-throughput screening (HTS) of small-molecule libraries accelerates the discovery of chemical leads to serve as starting points for probe or therapeutic development. With this approach, thousands of unique small molecules, representing a diverse chemical space, can be rapidly evaluated by biologically and physiologically relevant assays. The origins of numerous United States Food and Drug Administration–approved cancer drugs are linked to HTS, which emphasizes the value in this methodology. The National Institutes of Health Molecular Libraries Program made HTS accessible to the public sector, enabling the development of chemical probes and drug-repurposing initiatives. In this work, the impact of HTS in the field of oncology is considered among both private and public sectors. Examples are given for the discovery and development of approved cancer drugs. The importance of target validation is discussed, and common assay approaches for screening are reviewed. A rigorous examination of the PubChem database demonstrates that public screening centers are contributing to early-stage drug discovery in oncology by focusing on new targets and developing chemical probes. Several case studies highlight the value of different screening strategies and the potential for drug repurposing.

中文翻译：

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小分子筛查：通向食品和药物管理局批准药物的案例研究的癌症治疗剂的途径

小分子文库的高通量筛选（HTS）加快了化学引线的发现，可将其用作探针或治疗开发的起点。通过这种方法，可以通过生物学和生理学相关的分析方法快速评估代表不同化学空间的数千个独特小分子。许多获得美国食品和药物管理局批准的抗癌药物的起源都与高温超导有关，这强调了这种方法的价值。美国国立卫生研究院分子图书馆计划使HTS可供公共部门使用，从而能够开发化学探针和药物替代计划。在这项工作中，在私人和公共部门中都考虑了HTS在肿瘤学领域的影响。给出了发现和开发批准的抗癌药物的实例。讨论了靶标验证的重要性，并综述了用于筛选的常用测定方法。对PubChem数据库的严格检查表明，公共筛查中心通过关注新靶标和开发化学探针，为肿瘤学中的早期药物发现做出了贡献。一些案例研究强调了不同筛查策略的价值以及药物再利用的潜力。