Sorghum is the fifth most commonly used cereal worldwide and is a rich source of many bioactive compounds. We summarized phenolic compounds and carotenoids, vitamin E, amines, and phytosterols in sorghum grains. Recently, with the development of detection technology, new bioactive compounds such as formononetin, glycitein, and ononin have been detected. In addition, multiple in vitro and in vivo studies have shown that sorghum grains have extensive bio-logical activities, such as antioxidative, anticancer, antidiabetic, antiinflammatory, and antiobesity properties. Finally, with the establishment of sorghum phenolic compounds database, the bound phenolics and their biological activities and the mechanisms of biological activities of sorghum bioactive compounds using clinical trials may be researched.