qHTS to Identify Activators and Inhibitors of Wip1

该项目的总体目标是开发有效的，选择性的和生物活性的Wip 1小分子调节剂，用作化学探针和治疗开发的起点。 在此期间，项目团队使用RapidFire质谱分析法对NCATS注释文库和多种化学文库进行了高通量筛选。通过多种另外的测定进一步评价初步筛选命中以表征其活性，包括荧光报告正交测定和通过表面等离子体共振（SPR）的结合研究。目前，粉末订单已被放置在顶级化学型/单例中，并且额外的努力集中在酶作用机制的详细机制研究上，这可以在化学先导物的药物化学优化期间利用。

The overall objective of this project is to develop potent, selective, and bioactive small molecule modulators of Wip1 for use as chemical probes and starting points for therapeutic development. During this period, the project team performed high-throughput screening against NCATS annotated libraries and diverse chemical library using a RapidFire mass spectrometry assay. The primary screening hits were further evaluated by a variety of additional assays to characterize their activities, including fluorescence reporter orthogonal assay, and binding studies by surface plasmon resonance (SPR). Currently powder order has been placed for the top ranking chemotypes/singletons and additional efforts have focused on detailed mechanistic studies of the enzymes mechanism of action, which could be exploited during medicinal chemistry optimization of chemical leads.