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A novel strategy was developed for dual-target screening of bioactive components from traditional Chinese medicines (TCMs). This strategy was based on the use of low-cost microporous hollow fibers filled with target enzymes as baits to “fish out” the ligands in TCM extracts, followed by identification of the ligands dissociated from the target-ligand complexes by liquid chromatography–mass spectrometry. Ganjiang Huangqin Huanglian Renshen Decoction (GHHRD), a classical TCM prescription for diabetes treatment, was chosen as a model sample to evaluate the feasibility of the proposed strategy. Three bioactive components were successfully screened out from GHHRD. Coptisine was identified as the ligand of α-glucosidase and baicalin as the ligand of angiotensin-converting enzyme (ACE). Berberine was found to be a dual inhibitor of α-glucosidase and ACE. The results were further verified by enzyme inhibitory assay and molecular docking simulation. The study suggested that our developed strategy would be a powerful tool for screening bioactive components from multi-component and multi-target TCMs.A novel ligand fishing strategy based on dual-target screening for TCM was developed.Hollow fiber-based ligand fishing in combination with LC–MS was devised.Ligands of α-glucosidase and ACE were identified from complex matrix simultaneously.Screening results were verified by enzyme inhibitory assay and molecular docking.