Abstract: Aquilaria sinensis (Thymelaeaceae) is widely cultivated in southern China for its significant medicinal usage. The resinous wood, the most used part of the plant as traditional Chinese medicine (TCM), locally called "Chen Xiang (沉香)" or Chinese agarwood, has been traditionally used for the treatment of circulatory disorders, abdominal pain, vomiting, and dyspnea. Till date, over 249 compounds have been isolated and identified from this plant. A range of bioactivities, including α-glucosidase inhibitory effects, anti-inflammatory, cytotoxicity, neuroprotective, anti-neuroinflammatory, antimicrobial and acetylcholinesterase inhibitory effects, along with some of the pharmacological mechanisms have been reported for the pure compounds or extracts of Aquilaria sinensis. For the purpose of quality control and clinical safety of drug usage, modern analytical instruments and chemical analysis methods have been applied for analyses of Aquilaria sinensis. In order to comprehensively understand the medicinal application and to fully utilize the plant, a literature search on the herb based on databases including SciFinder, Web of Science, Pubmed, Google Scholar and others was performed and the information regarding to the phytochemistry investigations, pharmacological studies and quality control was summarized in this paper.