AF40431 is the first reported small-molecule ligand of sortilin (IC50: 4.4 µM; Kd: 0.7 µM). AF40431 is bound in the neurotensin-binding site of sortilin.
VGD020 is a CD4 and sortilin inhibitor. It displayed activity for sortilin down-modulation and reduction of progranulin-induced breast cancer stem cell propagation.