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In contrast to previous texts focusing on either computational, structural or synthetic methods, this one-of-a-kind guide integrates all three skill sets for a complete picture of contemporary structure-based design. As a result, this practical book demonstrates how to develop a high-affinity ligand with drug-like properties for any given drug target for which a high-resolution structure exists. The authors, both of whom have successfully designed drug-like molecules that were later developed into marketed drugs, use numerous examples of recently developed drugs to present best practice in structure-based drug design with the novice in mind. By way of a carefully balanced mix of theoretical background and case studies from medicinal chemistry applications, readers will quickly and efficiently master the basic skills of successful drug design.