BAY-885
Probe criteria
| Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) | Surpasses criterion: MAPK7 inhibition (@ 250 μM ATP), IC50= 35 nM |
| Selectivity within target family: > 30-fold | Surpasses criterion: Selectivity against Eurofins kinase panel at 1 μM (350 kinases were tested). Residual kinase activity below 50% reported for FER (h): 38%, EPHB3 (h): 42%, EPHA5 (h): 57%. For other kinases, residual activity reported ≥ 80%. |
| Selectivity outside target family | Clean PDSP scan with one exception for SIGMAR1 (Ki = 2502.07 nM) |
| On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 | Surpasses criterion: active in cellular mechanistic luciferase assay (IC50 =115 nM) demonstrating on-target cell activity |
| Control compound (100 times less potent than the probe) | Surpasses criterion: BAY-693 with biochemical activity IC50 = 6.4 µM and cellular on target activity IC50 = 11 µM)Clean PDSP scan with exception for SIGMAR1 (Ki = 2368.65 nM) and TMEM97 (Ki =4903.43 nM) |