Immobilized artificial membrane chromatography (IAMC) is a system of covalently bonding monolayer of phospholipid analogs onto the solid surface of silica particles, thus establishing the emulating process of drug-cellular membrane interactions in terms of chromatographic method, and is applied to profile the drug membrane permeability and biological activity. IAMC phases prepared from phosphocholine analogues closely mimic the surface of the biological cell membrane, and the capacity factor of drugs can be used to predict the interaction between drug molecules and cell membranes. IAMC, compared with n-octanol/water, liposome/water and ODS chromatography, can simulate other forces besides hydrophobic interaction. IAMC is getting more and more profound research because of its convenience and high efficiency. The primary screening by means of IAMC in the early stage of drug development would effectively lower failure in the preclinical and clinical development, since efficacy and safety are related in the larger part to membrane permeability. The interaction mechanism of drug-IAM and its profiling in membrane transport are reviewed.