Cereal processing generates around 12.9% of all food waste globally. Wheat bran, wheat germ, rice bran, rice germ, corn germ, corn bran, barley bran, and brewery spent grain are just a few examples of wastes that may be exploited to recover bioactive compounds. As a result, a long-term strategy for developing novel food products and ingredients is encouraged. High-value compounds like proteins, essential amino acids, essential fatty acids, ferulic acid, and other phenols, tocopherols, or β-glucans are found in cereal by-products. This review aims to provide a critical and comprehensive overview of current knowledge regarding the bioactive compounds recovered from cereal by-products, emphasizing their functional values and potential human health benefits.