Achillea schischkinii Sosn. is an endemic plant species and it belongs to Asteraceae family. It is distributed widely in the Central and East Anatolia. This study was carried out for evaluation of the antioxidant activity, enzyme inhibition effect, elemental and phenolic content of A. schischkinii. Briefly, acetylcholinesterase (AChE), butyrylcholinesterase (BChE), α-glycosidase (α-Gly), and glutathione S-transferase (GST) enzymes were strongly inhibited by A. schischkinii. IC₅₀ values for AChE, BChE, α-Gly, and GST enzymes were found as 19.3 mg/mL, 15.4 mg/mL, 69.3 mg/mL, and 34.7 mg/mL respectively. The antioxidant activity of the sample was evaluated by four different in vitro bioanalytical methods. Besides, the concentrations of twelve elements in A. schischkinii were analyzed by ICP-MS technique. Zn (50.6 ppm), Mn (23.0 ppm), and Cu (12.7 ppm) were found as major elements. Furthermore, catechin (20.8 µg/mg extract), trans-ferulic acid (18.3 µg/mg extract), and gallic acid (11.2 µg/mg extract) were characterized as major phenolic compounds by using HPLC. PRACTICAL APPLICATIONS: Acetylcholinesterase, butyrylcholinesterase, α-glycosidase, and glutathione s-transferase enzymes have crucial functions on metabolism. Enzyme inhibition or activation mostly attributed to some health disorders such as Alzheimer's disease, Diabetes mellitus, cancer and hyperglycemia. Phenolic contents are responsible for effective biological activity. This study evaluated the phenolic content and antioxidant activity of Achillea schischkinii as well as the inhibition effect against four metabolic enzymes. The results would be beneficial for using the plant in the food industry and pharmacological process.