Enzyme inhibition-based drug screening is a critical strategy in drug development. However, significant limitations arise from the instability, limited reusability, and narrow applicability of traditional enzyme assays when screening for inhibitors in complex matrices, such as extracts of traditional Chinese medicines (TCMs). A screening strategy was developed that combines capillary electrophoresis (CE) with an enzymatic assay utilizing covalently immobilized α-glucosidase (α-Glu). NH