BAY-293
| Target | SOS1 |
| Targeted domain | RAS GEF |
| Mode of action | Inhibitor |
| Control | BAY-294 |
| Recommended cellular usage concentration | 0.02 - 1.1 µM |
| In vivo use | No |
| Donated by | Bayer |
Probe criteria
| Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd>/sub>) | Surpasses criterion: IC50 (SOS1 interaction assay) = 21 nM |
| Selectivity within target family: > 30-fold | Surpasses criterion: GEFs: IC50 > 20000 nM on SOS2 and MCF2L (DBS) |
| Selectivity outside target family | 358 kinases at 1µM compound concentration > 67% remaining activity Lead profiling screen (77 targets): BAY-293 binds to several aminergic GPCRs and transporters Shows activity on various targets in the PDSP scan: Closest off-targets are: HTR2A (Ki = 133.44 nM), ADRA2C (Ki = 130.87 nM), HRH2 (Ki = 139.82 nM), HTR1D (Ki = 181.12 nM), TMEM97 (Ki = 179.81 nM), CHRM1 (Ki = 237.75nM), ADRA1D (Ki = 337.65 nM). |
| On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 | Surpasses criterion: Inhibition of RAS-activation and pERK in cells with IC50 < 1 µM |
| Control compound (100 times less potent than the probe) | Surpasses criterion: IC50 (SOS1 interaction assay) = 2340 nM (> 100 fold); Shows activity on various targets in the PDSP scan: Closest off-targets are: HRH2 (Ki = 21.13 nM), HTR2A (Ki = 69.37 nM), HTR2B (Ki = 74.56 nM), HTR1D (Ki = 93.49 nM) |