Menu

BAY-7598

2D structure
Target MMP12 
Targeted domain Protease domain
Mode of action Inhibitor
Control BAY-694
Recommended cellular usage concentration < 10 nM
In vivo use Yes
Donated by Bayer


Probe criteria


Inhibitor/agonist potency: goal is < 100 nM (IC50, KD) Surpasses criterion: Biochemical assay (human MMP12): IC50 = 85 pM; Biophysical binding assay (SPR biosensor-based assay): Kd = 0.004 nM
Selectivity within target family: > 30-fold Surpasses criterion: > 100 fold selectivity vs all other human MMPs tested (> 40 fold selectivity of rodent ortholog MMP12 vs all rodent MMPs tested), closest off-targets: MMP10 (IC50 = 13 nM), MMP8 (IC50 = 15 nM)
Selectivity outside target family Surpasses criterion: No relevant activity in panel of 68 off-targets (@ 10 µM compound conc.); clean PDSP scan
Control compound (100 times less potent than the probe) Surpasses criterion: BAY-694: >> 1,000 times less in biochemical assay (IC50 = 80 nM); clean PDSP scan