Due to the complex compositions of Chinese medicine (CM), how to rapidly and efficiently discovery the biologically active components from them is a huge challenge. Traditionally, tedious extraction-isolation-purification-(bio)assay procedures are usually involved in the lead compounds discovery from them, resulting in a large amount of raw material, organic solvents, time and labor consumption, and the major chemical degradation risks of the unstable compounds. The fortu-nate thing is that with the rapid technological development of chromatographic sepa-ration, compound identification, and (bio)assay, two emerging strategies including functional-base screening and affinity-based screening have been developed for rapid profiling and distinguish individual active components from CM in the past two decades. The research status of screening strategies for active ingredients of CM was reviewed, and the online chromatographic screening and analysis methods for active ingredients were emphatically introduced.