In this chapter, the principles and processes of bio-specific extraction/receptor fishing, such as equilibrium dialysis, centrifugation, and material-based ligand screening assay, are briefly introduced, respectively. All these screening methods have been proven to be effective, and each method has its advantages and disadvantages in terms of complexity, time spending, solvent consumption, equip-ment, and labor-intensiveness. Then, the major emphases are focused on summa-rizing and discussing the reported various types of biomaterials, such as enzymes, receptors, cell membranes, and living cells, for the screening of active components in Chinese medicines. The trends of applications of bio-specific extraction/receptor fishing in the screening of active components were also discussed.