VU6015929

VU6015929 (Compound 7e; 4-100 nM; 24 hours; HEK293-DDR1b cells) treatment inhibits collagen I-induced DDR1 phosphorylation in a dose dependent manner. Analysis of the phosphorylated DDR1/total DDR1 ratio reveals an IC ₅₀ for VU6015929 of 0.7078 nM.

VU6015929 (Compound 7e) is further evaluated in a rat IV (0.5 mg/kg)/PO (3 mg/kg) PK study in a 10% EtOH/40% PEG400/50% saline vehicle. VU6015929 displays a good in vitro:in vivo correlation (IVIC), with moderate in vivo clearance (CL _p = 34.2 mL/min/kg), an ~3 hour half-life, moderate volume of distribution at steady state (V _ss = 4.3 L/kg) and 12.5% oral bioavailability with a rapid T _max (0.75 hr).