Cell membrane chromatography (CMC) is a biomimetic chromatographic method based on the ability of membrane receptors to selectively interact with their ligands in vivo. Using membrane receptors as a stationary phase, the CMC method helps in determining the binding characteristics between ligands and membrane receptors and in efficiently identifying specific target components in a complex sample that produce the cellular biological effects of ligands (drugs, antibodies, enzymes, cytokines, etc.). CMC is an analytical tool for revealing characteristics of ligand-receptor interactions, screening and discovering target substances, and accurately controlling the quality of drugs. Since establishment of CMC in the early 1990s, with the rapid development of cell biology, significant progress has been made in the development of high-expression receptors, engineered cell cultures, and standardized preparations, which allowed in vitro immobilization of cell membrane receptors and miniaturization of binding assays. A variety of CMC models have been established using different membrane receptors as a stationary phase, and many new methods have been developed by combining CMC with high-performance liquid chromatography (HPLC)/mass spectrometry or HPLC-IT-TOF technologies. CMC methods have been widely used to study drug-receptor interactions and to screen complex samples for effective or harmful components.