The origination and status of the combinatorial chemistry are introduced and described and various approaches for building its libraries are mentioned and classified . Besides, the identification and characterization of the active compounds are recommended and the solid phase combinatorial synthesis and liquid phase combinatorial synthesis are presented. Meanwhile, some analytical methods including infrared spectroscopy, nuclear magnetic resonance spectroscopy, mass spectrometry and so on are applied into combinatorial chemistry. Some powerful chemometric methods and techniques are then discussed for their applying into combinatorial chemistry. From the view of green chemistry, combinatorial chemical techniques could be regarded as "green" methods to fully utilize the resource and materials. When rational drug design is integrated into it, combinatorial chemistry can more efficiently and perfectly be used for innovation of the new drugs. Finally, the combinatorial chemistry is prospected for the application and development in future.