DATE: May 18, 2017
TIME: 8:00AM PDT, 11:00AM ET
It is well established that ligand binding can protect proteins from thermal denaturation in a cellular milieu; however, the broad application of this cellular target engagement concept to drug discovery has been hindered by a lack of simple platforms with sensitive quantitative readouts. Cell-based thermal stabilization assays are valuable methods for particular applications, but they can require target-specific antibodies for immuno-assay readouts, can be low-throughput for Western blot formats, and can be biased against multi-domain proteins.
Here we will describe InCELL Pulse™, which uses DiscoverX's Enzyme Fragment Complementation (EFC) technology to overcome these limitations of current thermal stabilization assays. This unique platform allows you to rapidly measure quantitative cellular target engagement potency values for inhibitors of diverse protein classes, including kinases, methyltransferases, and hydrolases. The tools and workflow for designing your own InCELL Pulse assays for your favorite target will be described and validation data will be highlighted.