Screening of compound libraries for modulators of cellular function can require high throughput technologies amenable to automation. Protein phosphorylation within different cellular pathways is a common event for measurement of drug effectiveness. The AlphaLISA SureFire Ultra panel of protein phosphorylation kits provide such rapid, homogeneous assays, allowing drug effectiveness to be analysed for large or small sample numbers. More recently there has been an increased focus on ‘Total’ SureFire Ultra assay development and its combination with PROTACS for targeted protein degradation analysis. For such work, ideally, we require assays against the ’Total’ proteins for directly assessing target engagement as well as assays that measure the downstream phosphorylation effects resulting from targetengagement.
Data will be presented on numerous recently developed assays and PROTACS examples, highlighting the utility of Alpha SureFire technology as a platform of choice for both high and low throughput screening applications in drug discovery.