The Chemical Biology and Therapeutics program has been a longstanding component of the research efforts at the MGH CVRC. Historically the CVRC has employed a variety of model organisms and high throughput methodologies coupled with medicinal chemistry, mass-spectroscopy, structural biology, and molecular modeling to probe the determinants of biological and disease phenotypes. These robust approaches have generated high-profile discoveries in the CVRC with respect to cardiac and vascular developmental patterning, iron metabolism, neuropsychiatric disorders, and musculoskeletal disease. These efforts have generated several candidate molecules that have subsequently been developed further for therapeutic applications, several of which are currently in clinical trials. The CVRC continues to develop new probe molecules to facilitate the interrogation of developmental and homeostatic pathways.