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This lecture introduces the fundamentals of medicinal chemistry, focusing on the design, optimization, and development of chemical compounds for drug use. It covers the limited synthetic toolbox of medicinal chemists, the importance of high-throughput screening in lead discovery, and the key milestones to reduce late-stage attrition of drug candidates. The lecture also delves into the concepts of reversible vs. irreversible binders, compound selectivity in SAR evaluations, and the determination of reversible inhibition modality during SAR studies.
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