This study investigated the bioactive potential of phenolics in the flower, stem and leaf parts of Aubrieta pinardii and A. canescens subsp. canescens, in conjunction with their antioxidant capacities and enzyme inhibitory activities. The extraction yields (%) of the plant parts varied significantly within and between the species, the flowers exhibiting the highest value. Phenolic acids identified in soluble free, ester-conjugated, and glycoside-conjugated forms exhibited species- and plant parts-specific significant variations between the species. The leaves of A. pinardii exhibited higher total phenolic, flavonoid and anthocyanin contents than A. canescens. DPPH, ABTS, and ORAC assays revealed notable antioxidant potential, particularly in total extracts of the ester- and glycoside-conjugated forms of phenolic acid forms. Metal chelating capacity highlighted the leaves’ superior activity. Enzyme inhibitory activity investigation of the total phenolics/sub-fractions and phenolic acid extracts demonstrated significant inhibitory activity against acetylcholinesterase, butyrylcholinesterase, α-amylase, α-glucosidase and tyrosinase, the highest values being determined in the extract of the soluble glycoside-conjugated form of phenolic acid. These findings underline the therapeutic potential of the phenolic compounds of Aubrieta. species in terms of oxidative stress and metabolic disorders emphasizing their potential role in the development of enzyme-targeted therapies.