This study investigated the effects of drought stress on Chinese cabbage (Chcab) by measuring plant growth responses, total antioxidant enzyme activities, the contents of bioactive compounds including glucosinolates (GLS, aliphatic and indolic), and binding with human serum albumin (HSA). Forty-day-old Chinese cabbage (Brassica rapa L. ssp. pekinensis) seedlings were transplanted into pots and maintained for three weeks at 10% (drought-treated, D-T) and 30% (control, C) soil water. The total leaf number, leaf area, and fresh and dry weights were significantly lower in D-T Chcab than in controls. Total GLSs and catalase activities were found to be significantly higher in D-T Chcab than in controls. Indolic GLSs were significantly higher than aliphatic GLSs in D-T Chcab. These results show that D-T Chcab reduced growth parameters and binding properties with HSA and influenced total contents of GLSs, polyphenols, flavonoids, total antioxidant enzyme activities, catalase and peroxidase.