Description: ARUK3001185 (Compound 8l) is a potent, selective, orally active, and brain-penetrant Notum inhibitor (IC50 = 6.7 nM), suitable for oral dosing in rodent models of disease [1]. Target: Others. Smiles: C(F)(F)(F)C1=C(Cl)C(=CC=C1Cl)N2C=CN=N2

ARUK3001185 is an inhibitor of palmitoleoyl-protein carboxylesterase NOTUM (IC50 = 6.7 nM), an enzyme involved in the deacylation of Wnt. It is selective for NOTUM over a panel of 39 serine hydrolases and 485 kinases, including casein kinase 1 (CK1) and glycogen synthase kinase 3 (GSK3), at 10 µM and a panel of 47...