Authors

A Phillipou¹; 
¹ GSK, UK

Discussion

Drugs therapeutic value are driven by their effective binding to their target within a highly complex cellular system. Traditional screening cascades have focussed on reductionist biochemical and biophysical techniques to probe target engagement triaging into more complex phenotypic assays to assay drug function. Is there a need to probe drug target interaction within the cell earlier in drug discovery? Potentially placing this between our ‘simple’ biochemical assays and our more complex phenotypic assays. Promega’s NanoBRET toolbox was utilised in a variety of ways to interrogate drug target interactions within the cell, bridging the gap between reductionist biochemical assays and more complex phenotypic assays. Assays were developed for a selection of BET family members and run at scale, to drive both selectivity and ligand efficiency.