Discovery of VU6015929: a selective discoidin domain receptor 1/2 (DDR1/2) inhibitor to explore the role of DDR1 in antifibrotic therapy
DE Jeffries, CM Borza, AL Blobaum… - ACS Medicinal …, 2019 - ACS Publications
DE Jeffries, CM Borza, AL Blobaum, A Pozzi, CW Lindsley
ACS Medicinal Chemistry Letters, 2019•ACS PublicationsHerein, we report the discovery of a potent and selective dual DDR1/2 inhibitor, 7e
(VU6015929), displaying low cytotoxicity, good kinome selectivity, and possessing an
acceptable in vitro DMPK profile with good rodent in vivo pharmacokinetics. VU6015929
potently blocks collagen-induced DDR1 activation and collagen-IV production, suggesting
DDR1 inhibition as an exciting target for antifibrotic therapy.
(VU6015929), displaying low cytotoxicity, good kinome selectivity, and possessing an
acceptable in vitro DMPK profile with good rodent in vivo pharmacokinetics. VU6015929
potently blocks collagen-induced DDR1 activation and collagen-IV production, suggesting
DDR1 inhibition as an exciting target for antifibrotic therapy.
Herein, we report the discovery of a potent and selective dual DDR1/2 inhibitor, 7e (VU6015929), displaying low cytotoxicity, good kinome selectivity, and possessing an acceptable in vitro DMPK profile with good rodent in vivo pharmacokinetics. VU6015929 potently blocks collagen-induced DDR1 activation and collagen-IV production, suggesting DDR1 inhibition as an exciting target for antifibrotic therapy.
ACS Publications