The phytochemical composition of essential oils and extracts of Tanacetum haussknechtii were investigated with GC-FID-MS and LC-MS/MS techniques and evaluated against oxidation, acetylcholinesterase, tyrosinase, and -amylase enzymes. The major volatile constituents of T. haussknectii were found to be - and -pinene, and borneol. Caffeoylquinic acid derivatives and flavonoids were detected in the aqueous, alcohol, and ethyl acetate extracts. In DPPH assay, the methanol extracts exhibited the highest activity. TEAC assay resulted with superiority of all methanol and the capitula ethyl acetate extract. In -carotene bleaching assay, linoleic acid was the best protected by the ethyl acetate extract of flower. The flower oil inhibited higher acetylcholinesterase activity than the remaining extracts. The flower ethyl acetate extract was found as the most effective inhibitor of -amylase. The herb and the leaf+stem water extracts possess highest inhibitory effect on tyrosinase.