Researchers have extensively studied Withania somnifera (L.) Dunal, a woody shrub renowned for its multifaceted medicinal attributes such as antibacterial, anti-inflammatory, adaptogenic, aphrodisiac, and tonifying properties, because of its medicinal and traditional values. However, comprehensive information about its medicinal uses and pharmacological implications is scattered across various sources. Thus, this study aims to provide a comprehensive review of its ethnomedicinal uses, phytochemistry, and pharmacological attributes, consolidating information from diverse data sources. Systematic investigations have revealed the presence of diverse phytochemicals in W. somnifera, including major alkaloids, withanolides, flavonoids, tannins, oils, phytosterols, and amino acids. Extracts, fractions, and bioactive compounds derived from W. somnifera exhibited potent antibacterial, anti-inflammatory, anti-aging, anti-analgesic, anti-cancer, antivenom, anti-fungal, and anti-viral activities. W. somnifera serves as a valuable source of phytochemicals with diverse biological activities, offering significant therapeutic benefits globally. However, further studies are needed to assess potential side effects. Additionally, while several isolated compounds have demonstrated notable bioactivities, future research should focus on elucidating their mechanistic features to facilitate their integration into drug discovery endeavors.