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Introduction to drug target selection, lead compound discovery, and application of structure-activity relationships and computational chemistry towards refinement and optimization of lead compounds and their derivatives. Use of molecular graphics software and publicly available macromolecular structure databases will provide the foundation for evaluating macromolecular models of drug targets and allow a hands-on exploration of the structure/function relationships of proteins that have been successful targets of rational drug design. Prerequisite(s): (CHM 420 or CHM 452) or equivalent.