In recent times, numerous edible resources, such as millets, have proven highly effective in combating a variety of ailments, including cancer, diabetes, inflammation, cardiovascular disease, and gastric ulcers. Millets have a rich nutritional profile and have the capability to survive harsh environmental conditions. Millets with a low glycemic index can regulate the release of glucose into the bloodstream at a very slow rate. This functional food is rich in a variety of nutraceuticals and antioxidant compounds, offering numerous health benefits, including improved digestive system function, reduced cholesterol levels, cardiovascular disease prevention, diabetes protection, and reduced risks of tumors and gastrointestinal diseases. Millets comprise several bioactive compounds, like phenolic compounds, flavonoids, and antioxidants, which display potential anti-inflammatory and antioxidant effects, which are relevant not only for diabetes management but also for gastroprotection. Preclinical studies demonstrated that millets and their bioactive compounds could prevent oxidative stress, reduce inflammation, and maintain the integrity of the gastric mucosa. Regardless of the potential health benefits of these grains, there is still a need to increase responsiveness amongst populations worldwide about their health, nutritional, and nutraceutical properties. This updated review discusses the major bioactive compounds, the extraction process, and the enormous medicinal value of millets.