Ziziphora is a plant used in Turkish and Iran traditional medicine for its antibacterial activity, sedative and stomach soothing properties. Although the chemical profile of the essential oil of different Ziziphora species is well documented, data regarding plant extracts are incomplete. In this study extracts from Ziziphora taurica subsp. cleonioides were obtained using ethyl acetate, methanol and water and the chemical profile of the aerial part of the plant was elucidated. Among the compounds identified, rosmarinic acid was the most abundant (3375.67 ± 38.02 μg/mL), at the extract of methanol, followed by chlorogenic acid (3225.10 ± 16.44). Enzyme inhibition activity against α-amylase and tyrosinase was also estimated. The ethyl acetate extract showed the highest α-amylase activity (1.95 ± 0.04 mg/mL), while the best anti-tyrosinase activity was calculated for the methanolic extract (1.25 ± 0.01 mg/mL). In addition, total phenolic, flavonoid content and antioxidant activity were evaluated. According to our results, bioactivity of the plant is of great interest, nonetheless, at the same time, it is strongly depended on the solvent used during the extraction process. Our data suggest that the plant under study may be an important source to consider against metabolic, skin pigmentation and oxidative stress related disorders.