Application of BRET Technology to Quantitatively Determine Kinase Inhibitor Potency in Live Cells
- Learn how NanoBRET™ target engagement technology enables quantitative determination of kinase inhibitor occupancy in live cells, without disruption of cellular membrane integrity
While ready-to-use biochemical kinase assays exist that cover large portions of the kinome, there is a need for a similar broad set of cellular kinase assays that can interrogate compound potency in live cells.
In this webinar, we describe the NanoBRET™ Target Engagement (TE) technique—the first biophysical technique to broadly enable the quantitative determination of kinase inhibitor occupancy in live cells, without disruption of cellular membrane integrity. NanoBRET TE has enabled the development of live cell quantitative compound binding assays for >200 individual full-length protein kinases.
We will also discuss our collaboration with Reaction Biology Corporation (RBC) to enable services using NanoBRET TE kinase assays. In-cell potency determinations for various types of kinase inhibitors will be shown, including type I, II and allosteric compounds. Additionally, we will show a comparative analysis between NanoBRET TE cellular assays and biochemical kinase assays that reveals a surprising intracellular selectivity profile for an approved drug. These results demonstrate the value of assessing live-cell kinase target engagement, as the cellular environment may influence potency and selectivity profiles.
Sr Research Scientist & Group Leader
Sr. Director of Business Development
Reaction Biology Corporation
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