Measuring Intracellular Target Engagement and Drug Residence Time with NanoBRET
5 March 2015
Measuring target engagement in a cellular context is an important part of the drug discovery process, as it can address compound cell permeability, equilibrium binding affinity, as well as kinetic binding rates. However, assessing target engagement in a cellular context has been challenging. This poster presents a method to directly measure target engagement within intact mammalian cells using bioluminescence energy transfer (BRET).