Abstract: Traditional Chinese medicine (TCM), as a treasure of traditional medicine, has complex and diverse active ingredients and mechanisms of action. For the purpose of thoroughly investigate the direct targets of active ingredients in traditional Chinese medicine, promote research into the efficacy mechanisms of TCM, and advance new drug development. This paper presents a review of new technologies that are widely used or have potential in the field of target discovery for active ingredients in TCM. It is intended to provide new perspectives and ideas for related fields. Currently, active ingredient target discovery technologies for TCM are mainly divided into labelling methods and non-labelling methods. Labelling methods identify and capture targets through the design of specific molecular probes, offering high sensitivity and specificity. The non-labelling method identifies targets by monitoring changes in biophysical properties such as target protein stability. It is simple, accurate, and does not require drug modification. Both approaches have their unique advantages, revealing the mechanisms of interaction between active components of traditional Chinese medicine and biomolecules from different perspectives. This provides scientific basis and innovative ideas for the study of the efficacy mechanisms of traditional Chinese medicine and the development of new drugs. This paper reviews the research achievements and methodological advances from February 2006 to January 2025, in the identification of active components in TCM, natural products research, and the application of proteomics technologies for target identification. The review focuses on research methodologies and application dimensions, aiming to supply traditional drug discovery approaches and provide insights for future studies in this field.