化合物依赖性测定干扰代表药物和化学探针发现的持续负担。美国国立卫生研究院/美国国家促进转化科学中心(NIH/NCATS)测定指导手册(AGM)建立了“测定工件和干扰”部分,以解决生物测定中工件和干扰的不同来源。除了在这个重要的主题领域频繁引入新的章节之外,较旧的章节由学术界的专家定期更新,工业,和政府包括新技术和实践。章节描述了减轻和识别化合物依赖性测定干扰的许多最佳实践。使用先前报道的两个针对表观遗传靶标Rtt109和NSD2的小分子抑制剂的生化高通量筛选活动,作者回顾了最佳实践,并将读者引导到AGM和其他地方的高产资源,以缓解和鉴定化合物依赖性反应性和聚集测定干扰。
Compound-dependent assay interferences represent a continued burden in drug and chemical probe discovery. The open-source National Institutes of Health/National Center for Advancing Translational Sciences (NIH/NCATS) Assay Guidance Manual (AGM) established an \"Assay Artifacts and Interferences\" section to address different sources of artifacts and interferences in biological assays. In addition to the frequent introduction of new chapters in this important topic area, older chapters are periodically updated by experts from academia, industry, and government to include new technologies and practices. Section chapters describe many best practices for mitigating and identifying compound-dependent assay interferences. Using two previously reported biochemical high-throughput screening campaigns for small-molecule inhibitors of the epigenetic targets Rtt109 and NSD2, the authors review best practices and direct readers to high-yield resources in the AGM and elsewhere for the mitigation and identification of compound-dependent
reactivity and aggregation assay interferences.