Chemical biology is the study of chemical means, especially in small organic molecules as a tool to study the biology of an emerging interdisciplinary frontier, is an important basic course for the chemical and biological science in the new century. This course aims to enable students to master the basic theory, knowledge and concepts of chemical biology knowledge to establish organic links between chemistry, bio-chemistry, chemical biology and cell biology. This course focuses on eliminating the gap between organic chemistry and biology. This course combines the classic chemical biology textbook and the state-of-the-art chemical biology research, with emphasis on cultivating a strong interest of students in learning and thinking, so that students would have a solid theoretical foundation as well as a clear view of multidisciplinary and comprehensive development.