Multitarget AD inhibitor-1 is a reversible and selective inhibitor of butyrylcholinesterase (BuChE) with IC50 values of 7.22 µM for human BuChE (hBuChE) and 1.55 µM for equine serum BuChE (eqBuChE). It also exhibits inhibitory activity towards beta-secretase (IC50 41.60 µM), amyloid beta aggregation (IC50 3.09 µM), and tau aggregation. As a diphenylpropylamine derivative, Multitarget AD inhibitor-1 is promising for research into multifunctional, disease-modifying treatments for Alzheimers disease.