Abstract: Cell membrane chromatography (CMC) was first proposed by Professor He in 1996. As one of bio-affinity chromatography technique, CMC was a simple and convenient technology in the study of interactions of active components in traditional Chinese medicines (TCMs) with membrane receptors in vitro, and screen active components from complicated TCMs. Recently, the CMC technology was developed rapidly, and widely applied in the discovery of lead compounds from nature product. This review article is focused on the application of cell membrane chromatography in the identification of active components in traditional Chinese medicine, together with the recent development of CMC methodology. Combining with our previous works in the analysis of the composition of complex substances, biochromatography and TLC bioautography for quality evaluation of TCM, we proposed a new holistic quality evaluation strategy of TCM related with bioactivity, which could be summarized as the integration of screen (screening of quality control marker by CMC), macroscopic characterization (characterizing the chemical material basis by multi-dimension and multi data fingerprinting) and microscopic description (multi-component quantification). The proposed strategy would provide a new idea for the holistic quality evaluation of TCM in the composition and concentration of bioactive components as quality evaluation indicators.