Scutellaria (Lamiaceae), which contains over 350 species, usually known as skullcaps, is found throughout Europe, the United States, and East Asia. In traditional Chinese medicine, several species are used to wipe out heat-evil and remove surface ills (TCM). The current study examines the ethnopharmacology, biological activity, and chemical substances associated with Scutellaria species. More than 295 chemicals, including flavonoids and diterpenes, have been identified. Scutellaria and its active principles have been shown in studies to have a wide range of pharmacological activities, including antioxidant, antimicrobial, antifeedant, phytotoxic, acaricidal toxicity, antibacterial, anti-inflammatory, and antianalgesic activities. Currently, effective monomeric compounds or active components from Scutellaria have been evaluated for pharmacological action in vivo and in vitro. More data facilitates applications and exploitation of novel medication development.