The fruit of Schisandra chinensis (Chinese magnolia vine), the medicinal plant well-known in Traditional Chinese Medicine, gains great popularity in the modern phytopharmacology. This phenomena is related to the wide and powerful healing properties, including supporting immune, nervous and digestive systems activity. S. chinensis is also known for its adaptogenic properties which can support the treatment of neurodegenerative disorders, particularly Alzheimer's disease. The components of S. chinensis have been analyzed mostly using chromatography, including HPLC, GC and TLC. The last technique can be easily hyphenated with biological assays performed directly on a TLC plate that is using effect directed detection. TLC-direct bioautography (TLC-DB) for acetylcholinesterase (AChE) inhibition and TLC-DB against Bacillus subtilis were performed, followed by micro-preparative separation of fractions which were subsequently subjected to LC-MS tentative identification. Additionally, screening analysis was done using both biological detection and derivatization reagents (e.g. PMA, thymol, NP-PEG). Both TLC screening and effect-directed analysis (TLC-DB followed by MS analysis) of S. chinensis fruit revealed components with biological activity, especially antibacterials (e.g. citric acid) and inhibitors of AChE (mainly dibenzocyclooctadiene lignans). AChE inhibition activities were confirmed by TLC-DB for nine standards that is: 6-O-benzoylgomisin, deoxyschisandrin, gomisin A, gomisin G, schisandrin, schisandrin C, schisanhenol, schisantherin A and schisantherin B. These lignans were further identified by LC-ESI-MS in the isolated fraction revealing AChE inhibition. Moreover three other lignans: γ-schisandrin, schisandrin B and gomisin J were tentatively identified by LC-ESI-MS.