The use of medicinal plants to treat human ailments has received more attention recently. Eruca sativa (E. sativa; jarjeer) is a very popular edible plant of the Brassicaceae family with remarkable nutritional and therapeutic properties. In this frame, bioactive metabolites derived from E. sativa biomass have captured more attention in pharmacotherapy and biomedicine. This review focuses on recent advances in high-resolution mass spectrometry (HRMS), which have made the characterization of Eruca metabolites, such as glucosinolates and their derivatives, more feasible. Moreover, bio-pharmacological impact, viz. antiulcer, anticancer, antioxidant and antimicrobial, anti-obesity and hypoglycemic activities, cardiovascular benefits, and neuroprotective effects are discussed. This review concentrates all important research findings on these topics, and stresses upon the activities of chemistry and pharmacological areas. By stressing upon additional investigations, this paper emphasizes and appeals researchers and industrials to attempt a comprehensive knowledge of the pharmacological implications of Eruca species and improve their application in modern medicine.