Rhaponticum uniflorum (L.) DC. is a plant species of the Asteraceae family, widely used in traditional medicine in the Easteren Asia. Currently R. uniflorum is a subject of scientific interest of the chemists, biologists, pharmacologists, and others. This review includes scientific data from 1991 to 2017. The investigation of the chemodiversity of R. uniflorum showed the presence of more than 100 compounds, including sesquiterpenes, diterpenes, ecdysteroids, triterpenes, sterols, thiophenes, flavonoids, amino acids, fatty acids, etc. Ecdysteroids and triterpenes (more than 40 compounds) are the most studied groups of substances of R. uniflorum. The data about the methods of chromatographic analysis of terpenoids and phenolic compounds, as well as the quantitative content of some compounds in various organs of R. uniflorum are summarized in this paper. It is shown that the extracts and some compounds of R. uniflorum possess a wide spectrum of biological activity, including anxiolytic, stress-protective, actoprotective, antihypoxic, anabolic, hepatoprotective, inhibiting PPARγ receptors, anti-inflammatory, antitumor, immunostimulating, antiatherosclerotic, hypolipidemic effects. However, in spite of the known information about the pharmacological activity of R. uniflorum, the data of clinical trials are absent, thereby further investigations of this plant species is necessary.