1258292-64-6

GDC-046 is a potent, selective, and orally bioavailable TYK2 inhibitor with Kis of 4.8, 0.7, 0.7, and 0.4 nM for TYK2, JAK1, JAK2, and JAK3, respectively[1].

Tyk2: 4.8 nM (Ki); JAK1: 0.7 nM (Ki); JAK2: 0.7 nM (Ki); JAK3: 0.4 nM (Ki)

[1] Jun Liang, et al. Lead Optimization of a 4-aminopyridine Benzamide Scaffold to Identify Potent, Selective, and Orally Bioavailable TYK2 Inhibitors. J Med Chem. 2013 Jun 13;56(11):4521-36. DOI:10.1021/jm400266t