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 drug discovery and give an appreciation for the challenges that arise along the way. Topics include: (1) small molecules vs biologics; (2) target-based vs. phenotypic screening; (3) considerations for performing a high throughput screen (i.e., assay development; chemical library selection; natural products vs. drug-like compounds, etc); (4) approaches to triaging hits from a screen to identify leads; (5) strategies to optimize the structure of leads to increase potency and selectivity for in vivo studies (i.e., medicinal chemistry, structure-based drug design), and (6) what roles AI may play along the drug discovery continuum in the future.