BAY-474
| Target | MET |
| Targeted domain | Kinase domain (active site) |
| Mode of action | Inhibitor (type 1, ATP competitive) |
| Control | BAY-827 |
| Recommended cellular usage concentration | 0.001 - 1 µM |
| In vivo use | yes |
| Donated by | Bayer |
Probe criteria
| Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) | Surpasses criterion: Biochemical MET assay: IC50 < 1 nM |
| Selectivity within target family: > 30-fold | Surpasses criterion: selectivity > 1000 fold vs all other kinases (Millipore panel (214 at 1 µM), IC50 > 10 µM) except for RPS6KA3 (RSK2) with IC50 = 0.9 µM |
| Selectivity outside target family | Surpasses criterion: Eurofins-Panlabs radioligand binding assay (68) at 10 µM: cleanClean PDSP scan |
| On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 | Surpasses criterion: Mechanistic cellular assay (p-c-Met, MKN-45 cells): IC50 2.9 nM; Cellular proliferation assays: two-digit nanomolar IC90 |
| Control compound (100 times less potent than the probe) | Surpasses criterion: BAY-827 with 4 orders of magnitude less in vitro potency (IC50 = 11 µM) Shows activity on HTR6 (pKi = 6.2) in the GPCR scan. For others check the PDSP scan data. |