Click chemistry has revolutionized the field of drug discovery and delivery by providing a modular and efficient approach to synthesizing complex molecules. This review article provides an overview of click chemistry, its classification, and applications in drug discovery and delivery, with a focus on nanoparticles and polymer synthesis. We discuss the principles and types of click reactions, including CuAAC, SPAAC, and others, and their advantages in synthesizing biologically active compounds. We also explore the applications of click chemistry in drug discovery, including target identification, lead optimization, and library synthesis. Furthermore, we highlight the role of click chemistry in drug delivery, including the design of prodrugs, targeted delivery systems, and diagnostic agents, with a special emphasis on nanoparticles and polymer synthesis. We discuss how click chemistry has enabled the development of novel nanoparticles and polymers with tailored properties for drug delivery and targeting. Finally, we discuss the future perspectives and challenges of click chemistry in drug discovery and delivery. This review aims to provide a comprehensive understanding of click chemistry and its potential to revolutionize drug discovery and delivery”.