With the emergence of epidemics, pandemics, and infectious diseases, several research activities have been carried out on natural products to tackle them. As there are structural diversities in natural products, researchers are focused on exploring them for treatment and/or management of various infections and/or diseases. Acacia catechu (L.f.) Willd. belonging to the order Fabales and family Fabaceae shows a wide range of pharmacological functions in the management of diseases in humankind. This review was carried out to gather and provide information about the chemical constituents and pharmacological activities of A. catechu through the literature survey of scientific articles. On preliminary assessments, A. catechu is demonstrated as a significant wellspring of bioactive compounds with a wide range of biological and pharmaceutical applications such as antidiabetic, antioxidant, antimicrobial, anticancer, antidiarrheal, anti-inflammatory, antiviral, hepatoprotective, immunomodulatory, and so on. Although the metabolites from the plant are reported with diverse pharmacological applications, there is little information in regards to toxicity and clinical trials on bioactive compounds of this plant. Further research on diverse bioactive compounds from the plant is required to develop them as a successful potent drug.