As combinatorial chemistry matures, diversity-oriented synthetic chemists are achieving more structural complexity, tackling compounds with multiple stereocenters and complex natural product-like core structures. Recent advances in multi-component reactions and asymmetric catalysis push the frontiers of effectively populated chemical space. Structurally complex and diverse compound libraries effectively probe biological space for finding initial leads, while targeted, focused libraries enable more rapid lead optimization. Attend this event to hear the latest developments in diversity-oriented synthesis and its impact on drug development.