CDD-1115 (CDD1115) is a potent, selective inhibitor of BMP type 2 receptor BMPR2 with IC50 of 1.8 nM and Kiapp of 6.2 nM.
CDD-1115 showed weak inhibition (>250 nM) of ALK1 and ALK2 (>100-fold over BMPR2) and poor inhibition (>1000 nM) of ALK3, ALK5, ALK6, and TGFBR2 (>555-fold over BMPR2) and was inactive in inhibiting ALK4, ACVR2A, and ACVR2B.
CDD-1115 inhibited BMP-mediated gene expression in mammalian cell cultures, suppressed BRE-reporter activity in a luciferase reporter (293T-BRE-Luc) assays with IC50 of 24.1 uM.
CDD-1115 exhibited poor half-life in mouse and human liver microsomes.
