To find a potent small molecule inhibitor of a protein-protein interaction we develop a robust AlphaLISA competition assay. After optimization of this homogeneous assay we completed a 500.000 compound high throughput screen and successfully selected several lead classes of inhibitor molecules. The talk will focus on the lessons learned during this effort and will cover the advantages of this powerful technology, things to keep in mind when setting up an AlphaLISA assay, useful optimizations, pitfalls (like false positive hits), optimal controls, and possible orthogonal assay strategies to confirm hits.
Börries Brandenburg, Crucell (Johnson & Johnson)