ChE/Aβ1-42-IN-1 (compound 28) is a potent ChE and Aβ 1-42 aggregation inhibitor with IC 50 s of 0.062, 0.767 and 1.227 µM for AChE , BuChE and Aβ 1-42 aggregation, respectively. ChE/β1-42-IN-1 shows excellent BBB penetration. ChE/Aβ1-42-IN-1 is a potent multi-targeted anti-Alzheimer's agent.