Target engagement in a cellular environment can be confirmed using a cellular thermal shift assay (CETSA), which reports quantifiable changes in the thermal stability of proteins bound by small molecules. CETSA can be used to drive lead optimization or as a screening strategy to identify small molecule binders. To enable these approaches in a scalable manner, several groups have developed high-throughput CETSA (HT-CETSA) methods using reporter proteins or immunoassays. Despite recent successes in implementing HT-CETSA for diverse targets, caveats and challenges exist. This presentation provides an overview of the current landscape of HT-CETSA methodologies and shares lessons learned. Additionally, a forward-looking perspective on HT-CETSA in research and drug discovery will be discussed.<br/>

High-throughput cellular thermal shift assays (CETSA) for screening and lead optimization

ACS Fall 2020 Virtual Meeting

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