BAY-7598
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 |