Broad-Spectrum Cellular Kinase Selectivity Profiling In Live Cells With NanoBRET

Kinase profiling is a necessary process to confirm inhibitor selectivity and assess off-target activity.  Promega’s new compound kinase cellular selectivity profiling service takes advantage of the NanoBRET™ Target Engagement technology to quantitatively measure direct compound binding to kinases in live cells. Profiling using NanoBRET™ Target Engagement intracellular kinase assays allows for the unique enablement of drug and chemical probe development, and aids in drug repurposing via comprehensive profiling against a broad spectrum of kinases or kinase subfamilies.  Furthermore, live cell analysis is critical to accurately characterize inhibitor selectivity, as the spectrum of activity observed for kinase inhibitors may be altered in lives cells compared to cell-free biochemical systems.  Compounds can be tested at a single concentration against each full-length kinase in a 192- or 234- kinase panel, transiently expressed in HEK293 cells. Ratiometric BRET data provides reproducibility with low error rates and the output provided includes percent occupancy of test compounds against each kinase tested.