AbstractThe importance of bioactive plant species in the scientific world is increasing day by day. The relationship between health and traditional‐modern life, promotes the creation of new value‐added natural products. This is the first research to conduct a bioactivity and chemical composition analysis of Campanula baskilensis species, which belongs to the medicinally important genus Campanula L (Campanulaceae). The aim of the current study is to quantitatively investigate the phytochemical contents of aerial and root parts of different C. baskilensis extracts (ethanol, methanol, and water) by LC‐MS/MS and to evaluate their total phenolic and flavonoid contents, antioxidant and enzyme inhibitory activities. Remarkably, LC‐MS/MS results revealed that, high amounts of quinic acid (53.6 mg/g aerial‐MeOH extract), fumaric acid (6.3 mg/g aerial‐H2O extract, 2.5 mg/g root‐H2O extract), protocatechuic acid (11.4 mg/g aerial‐H2O extract), vanillic acid (1.4 mg/g aerial‐EtOH extract), quercetin‐3‐O‐rutinoside (rutin) (2.3 mg/g aerial‐EtOH extract), hesperetin 7‐rutinoside (hesperidin) (2.0 mg/g aerial‐EtOH extract), kaempferol‐3‐O‐rutinoside (nicotiflorin) (5.5 mg/g aerial‐EtOH extract) were detected in the extracts of the species. Considering the bioactivity tests performed on C. baskilensis extracts, aerial‐H2O extract showed significant activity in all antioxidant assays. However, ethanol extracts of root and aerial parts exhibited the highest activities in all enzyme inhibitory tests.