A recent article in Cell Chemical Biology demonstrates that Promega Corporation’s new NanoBRET™ Target Engagement (TE) Intracellular Kinase Assay is the first assay to quantify inhibitor drug engagement with kinase proteins inside live human cells. Broad spectrum, quantitative live-cell profiling using full-length kinases reveals improved intracellular selectivity for clinically relevant kinase inhibitors compared to biochemical profiling. These live-cell kinase NanoBRET TE assays further enable a mechanistic assessment of the effect of cellular ATP on inhibitor potency. (Graphic: Business Wire)
MADISON, Wis.--(BUSINESS WIRE)--Promega Corporation’s new NanoBRET™ Target Engagement (TE) Intracellular Kinase Assay is the first assay to quantify inhibitor drug binding to kinase proteins inside live human cells, as demonstrated in the recent Cell Chemical Biology article, “Quantitative, Wide-spectrum Kinase Profiling in Live Cells for Assessing the Effect of Cellular ATP on Target Engagement.” In collaboration with Structural Genomics Consortium (SGC), this article shows the greater predictive potential of NanoBRET Target Engagement compared to common traditional approaches that use purified kinase domains in non-cell-based assays.
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