Traditional Chinese medicine chemical biology (TCMCB) is an interdisciplinary discipline emerging in the modernization of traditional Chinese medicine (TCM). Guided by TCM theories, TCMCB employs bioactive components from Chinese medicines as molecular probes, focusing on the precise identification of action targets, regulation of signaling pathways, and intervention mechanisms of life processes induced by TCM bioactive ingredients. It provides critical technical support for the modern interpretation of the scientific connotation of TCM and its international promotion. This paper systematically reviews the disciplinary orientation, core technologies and methodologies of TCMCB, summarizes its applications and bottlenecks in the mechanistic elucidation of TCM bioactive components and innovative drug discovery and development, and highlights original research achievements over the past decade. TCMCB has gradually established an integrated research paradigm: “bioactive component screening-precise target identification-mechanism elucidation-clinical translational application” promoting the transformation of TCM theories from empirical description to mechanism-driven interpretation, and offering novel strategies for disease treatment in modern medicine and innovative drug development. Future efforts should focus on overcoming key challenges including the supply of TCM bioactive components, precise validation of targets, and international evaluation systems. Meanwhile, the construction of technology platforms with independent intellectual property rights and a global target database for traditional medicines will facilitate the advancement of TCM toward modern precision medicine.

traditional Chinese medicine chemical biology  /  active components of traditional Chinese medicine  /  target identification  /  molecular probes  /  mechanism elucidation