The Fabaceae is recognized as the third largest and one of the most influential families among the flowering plants. Furthermore, its name is linked to “Legumes”, which represent a vast group of angiosperms in the continents utilized as crops, forages, and green manures. It is recognized for diverse constituents, covering both primary metabolites include lectins, chitinases, various proteases, and α-amylase inhibitors, as well as secondary metabolites include flavonoids, alkaloids, terpenoids, tannins, and phenolics. Fabaceae flavonoid plays an important role in the legumes’ adaptability to biological surroundings as defensive agents (phytoalexins) and as chemical signals in a symbiotic relationship with a bacterial species known as rhizobia. Considering their important role in plant defense and benefits to human healthiness, a number of studies on the Fabaceae plant have been performed, namely isolation and screening of the purified compounds and their biological activity. This study outlines specified issues on the chemical structure, biosynthesis, biological activities, and medicinal uses of Fabaceae compounds. © 2022 Walter de Gruyter GmbH, Berlin/Boston.