Schefflera, the largest and an important genus belonging to the family Araliaceae has a wide range of ethnic medicinal importance among various cultures of the world. The genus has been studied for its ethnomedicinal uses, which mainly includes its use in the treatment of asthma and liver diseases. The major phytochemicals identified from Schefflera species are saponins and triterpenoid glycosides. Extensive work has been carried out on the isolation and identification of compounds present in the genus, but, their role in biological activities has not been much reported. This review highlights the distribution of the genus the ethno-medicinal uses, major phytochemicals identified, reported biological activities and compounds isolated and identified from Schefflera species and from some major species of Araliaceae.