Quercetin in Drug Discovery is a detailed reference exploring the multifaceted pharmacological potential of quercetin, a naturally occurring flavonoid with significant therapeutic promise. Addressing the critical need for consolidated knowledge, this guide highlights quercetin’s diverse biological activities and the translational challenges limiting its clinical applications, making it essential for researchers and pharmaceutical scientists. The comprehensive table of contents covers quercetin’s pharmacological properties, molecular docking studies, and ADME profiles, alongside therapeutic applications in cardiovascular diseases, cancer, and other conditions. It further examines bioavailability enhancement strategies, drug formulation, innovative delivery systems, and clinical trial evidence. Contributions from leading experts provide detailed insights into signaling pathways, molecular targets, and synthetic derivatives. Quercetin in Drug Discovery equips pharmacologists, medicinal chemists, and pharmaceutical scientists with critical information to advance research and drug development. By addressing bioavailability issues and regulatory considerations, this reference supports the translation of quercetin from bench to bedside, fostering innovation in natural product-based therapeutics.