Background:

XMD17-109 is a new inhibitor of ERK5, IC50 value in HeLa cell is 0.09 ± 0.03 μM, and in vitro, Enzymatic IC50 value is 0.162 ± 0.006 μM.

XMD17-109 is capable of inhibiting the ERK5 autophosphorylation in cells.[1]

Through intravenous injection and oral delivery of XMD17-109 in mice, the pharmacokinetic properties of this compound?are as bellows: the T1/2 (half time)?is 8.2?h, the plasma clearance is 8.64 mL/min/Kg (data of intravenous injection), the AUC (area under the curve) of oral delivery is 15745?h*ng/mL and the oral bioavailability is 90%.

Reference:
1.  Deng, X., et al., Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones. European Journal of Medicinal Chemistry, 2013. 70: p. 758-767.