Various diseases such as cancer, hyperglycemia, and obesity negatively influence people's health and daily life. Mushroom species are miniature pharmaceutical factories producing hundreds of novel constituents with a long history of use in Oriental medicine. As a new therapy, they have attracted much attention owing to their potent therapeutic activity. Phellinus sensu lato (s.l.) is a well-known medicinal mushroom genus that has long been used in preventing ailments, including gastroenteric dysfunction, diarrhea, hemorrhage, and cancers, in Oriental countries, particularly in China, Japan, and Korea. Isolated compounds or complex extracts from Phellinus demonstrate specific bioactivity. Low-molecular-weight components, especially terpenoids, polyphenols, and other secondary metabolites, still exhibit biological activity. This review highlights the bioactive compounds from Phellinus s. l. mushrooms as being potent and having unlimited applications, especially the bioactive low-molecular-weight compounds, such as terpenoids, polyphenols, and their derivatives; also, pharmacological properties of the extracts and fractions from the fruiting bodies and the mycelia of Phellinus s. l., and the mechanism of the pharmacological activity have been discussed. This review summarized the two parts as mentioned above over a period of 7 years from 2011 to 2017.