Abstract

Recent advances in high-content imaging, CRISPR/Cas-based genome editing and induced pluripotent stem cell technologies are converging to stimulate the new discipline of Phenomics Drug Discovery. I will describe how Phenomics Drug Discovery incorporates state-of-the-art imaging, genomics, proteomics and informatics tools to explore drug mechanism-of-action (MOA) across genetically defined in vitro cell models. We demonstrate how multiparametric high content screening assays combined with novel image-informatics and machine learning methods advance in vitro pharmacogenomic studies across a broader variety of phenotypes, disease models and therapeutic classes. Finally, I present recent examples of how our Phenomics Drug Discovery platform enabled the rapid discovery of a novel orally-available, ATP-competitive, kinase inhibitor and novel drug combinations which display potent anti-tumour activity across 2D, 3D and in vivo models.