Re-energise your kinase discovery programme
If the answer to any of these questions is important to your drug discovery programme, then we might have the perfect solution for you!
Target Engagement (TE) Intracellular Kinase Assays
Using Promega’s NanoBRET™ technology, we have implemented intracellular kinase assays designed to study the interaction of compounds on kinase targets in intact living cells. NanoBRET™ Target Engagement Assay measures compound binding at specific target kinases. This quantitative analysis can be performed in cultured cells via energy transfer between a 19-kDa luciferase (NanoLuc, Nluc)-tagged target protein and a cell-permeable fluorescent energy transfer probe introduced to the assay medium. Addition of competing compounds results in a dose-dependent decrease in NanoBRET™ signal, which allows quantification of the intracellular affinity of the target kinase for the test compound.
Aurelia Bioscience offers compound profiling services using Target Engagement (TE) Intracellular Kinase Assays to help you make better choices in selecting your lead molecule
Some of the advantages of this technique are:
Example data for DDR1 Kinase:
Competitive inhibition (A) of compound binding to DDR1 kinase in living cells. By studying both the association (B) and dissociation (C) rate of compounds from each of the target kinase, it is possible to consider introducing kinetic binding parameter evaluation during compound SAR development.