Drugs derived from natural sources have been a vital part of drug discovery for centuries. Many of the most successful drugs on the market today are derived from natural sources. Traditional knowledge or the traditional system of medicines is often used to select the most appropriate sources for drug discovery and it is a valuable tool in the search for new lead molecules. In Ayurveda, Sida cordifolia L (SC) is regarded as a highly effective medicinal plant and most of its parts have been traditionally used to treat a wide range of illnesses. SC is also known as “Bala” in Hindi and is considered a “Rasayana”, which means that it has rejuvenating properties. All the relevant information on SC was retrieved through electronic databases, textbooks, and a library search. This review covers the available literature from 1980 to the end of December 2021. Phytochemical studies revealed that SC is rich in alkaloids, flavonoids, steroids, fatty acids, and other classes of secondary metabolites. Several studies have shown that SC extracts and their phytochemicals or isolated metabolites have anti-inflammatory, antioxidant, antibacterial, antiviral, anticancer, antihyperglycemic, and wound healing properties in in-vitro and in-vivo studies. The results of traditional uses, the presence of phytochemicals, and pharmacological investigations summarised in this review will help to further extend its therapeutic potential and give compelling evidence for its future therapeutic application in modern medicine.