Wichur et al. designed a series of 1-(phenylsulfonyl)-1H-indole-based multifunctional ligands targeting cholinesterases and 5-HT6 receptors with anti-aggregation properties against amyloid-beta (Aβ) and tau [177], both of which are critical in Alzheimer’s disease progression. Here, BCHE is linked to early-onset autosomal dominant Alzheimer disease.