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The objective of this study was to investigate health-promoting bioactive compounds and related enzymes of grape in response to regulated deficit irrigation under greenhouse and rain-shelter. The experiment had five treatments in 2016: FI (75%–90% of FC [field water holding capacity] from budburst to full maturation), DI (50%–60% of FC from budburst to full maturation), DI1(same as FI except 50%–60% of FC from budburst to anthesis), DI2(same as FI except 50%–60% of FC from anthesis to pea size) and DI3 (same as FI except 50%–60% of FC from pea size to full maturation). Another three treatments were setted in 2017: DI4(same as FI except 50%–60% of FC from pea size to véraison), DI5 (same as FI except 50%–60% of FC from véraison to mid ripening) and DI6 (same as FI except 50%–60% of FC from mid ripening to full maturation). Results showed that deficit irrigation post véraison was an efficient approach for inducing the bioactive compounds biosynthesis. Greenhouse cultivate could increase WUE, yield and improve the content of soluble sugar, Vc, soluble protein. While rain-shelter cultivate could accumulated higher bioactive compounds in grape tissue. Abbreviations: L-Phe, L-Phenylalanine; RES, Resveratrol; PAL, phenylalanine ammonialyase; C4H, cinnamate-4-hydroxylase; 4CL, 4-coumarate: coenzyme A ligase; PPO, polyphenol oxidase; L*, lightness; C*, chrome; SS, soluble sugar; TA, titratable acidity; Vc, vitamin C; SP, soluble protein; TSS, total soluble solids and MI, maturity index; ET, plant evapotranspiration; WUEET, water use efficiency based on plant evapotranspiration. [ABSTRACT FROM AUTHOR]