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This lecture focuses on identifying correct drug targets, ensuring efficacy, and maintaining safety in medical chemistry. It covers topics such as the importance of genetic sufficiency tests, leveraging chirality for on-target responses, and the role of stereochemistry in drug action. Case studies, including the discovery of imatinib mesylate, illustrate key concepts. The discussion extends to the challenges of drug resistance, the impact of physicochemical properties on drug development, and the rules of 'drug-likeness' in compounds. Additionally, the lecture addresses safety concerns, structural alerts to avoid in drug design, and the importance of understanding differences between in vitro and in vivo efficacy.