The discovery of a new medicine typically takes over a decade and costs more than $1 billion. This course will provide an overview of the key steps involved in small molecule drug discovery and give an appreciation for the challenges that arise along the way. Topics include: 1) target based vs. phenotypic screening; 2) considerations for performing a high throughput screen (i.e., assay development; chemical library selection; natural products vs. drug-like compounds, etc); 3) approaches to triaging hits from a screen to identify leads; and 4) strategies to optimize the structure of leads to increase potency and selectivity for in vivo studies (i.e., medicinal chemistry, structure-based drug design). In addition to in-class instruction, there will be two hours of live demos and experiments at the Drug Discovery facility at (SPARC BioCentre).