This course aims to enable students to gain knowledge and training in chemical biology and to understand how to use chemical approaches to study biological systems. Building from fundamental knowledge in both chemistry and biology aspects, the course will cover different topics in chemical biology including the fundamentals of chemical biology, metal‐based drugs, drug delivery, combinatorial synthesis, high‐throughput screening, DNA‐based self‐assembly, biomolecular sensing and bioimaging, and other advanced topics in chemical biology. The skills and understanding accumulated during this course will prepare students for more advanced and specialized research projects at the interface of chemistry and biology.