DiscussionFragment-Based Lead Discovery (FBLD) has emerged as a powerful strategy for the generation of therapeutic lead compounds. We are applying Diversity-Oriented Synthesis (DOS) as a means of expanding the fragment chemical space. Additionally, the DOS paradigm allows for rapid fragment modification to produce high-affinity binders. Our diverse fragment collection will be screened against a swath of biologically interesting disease targets. The lecture will detail the various aspects of applying DOS to FBLD.