<p><i>Grewia tiliifolia</i> (Dhaman) of the Malvaceae family has been widely used in traditional medicine for several years. In traditional medical systems, it is widely used to treat wounds, rhinopathy, skin conditions, ulcers, diarrhea, jaundice, aphrodisiac and urinary tract infections. The present comprehensive review provides an overview of the botany, phytochemistry, pharmacology, phytotoxicity and nutritive value of the plant. The review aimed to overcome the inconsistency between the ethnobotanical and pharmacological applications of this plant by describing its folklore use and present novel insights for future researchers. For this review, published data were retrieved from academic databases, including PubMed (02), Web of Science (04), Scopus (04) and Google Scholar (40) using relevant keywords. The chemical structures of the phytoconstituents presented in this review were determined using ChemDraw Ultra Pro 23.1.1. Dhaman is a medium-sized tree, distributed across wet tropical regions ranging from the Indian subcontinent to China and Peninsular Malaysia. Phytochemical investigations revealed the presence of flavones, alkaloids, saponins, sesquiterpenes, coumarins, esters and terpenoids. These bioactive compounds in plants have various pharmacological effects such as antimicrobial, anticancer, neuroprotective, and antidiabetic effects. The clinical investigations included in this review were performed to validate the folk uses of <i>G</i>. <i>tiliifolia</i>. However, the antiviral potential and conservation genetics of this plant have been neglected and need to be explored for the development of therapeutic advances and the sustainable use of the species. The gaps need to be the focus of future investigations in the form of coordinated pharmacological, clinical, and conservation-genetic research.</p>