BAY-876
| Target | SLC2A1 |
| Mode of action | Inhibitor |
| Control | BAY-588 |
| Recommended cellular usage concentration | 0.1 - 75 nM |
| In vivo use | yes |
| Donated by | Bayer |
Probe criteria
| Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) | IC50 = 2 nM (Inhibition of glucose uptake measured by measuring ATP levels using CellTiter-Glo Luminescent Cell viability assay) |
| Selectivity within target family: > 30-fold | Surpasses criterion: closest is SLC2A4 which is >100x less selective (IC50 = 270 nM); IC50 SLC2A2 = 9.4 µM; IC50 SLC2A3 = 1.6 µM |
| Selectivity outside target family | Closest off-targets: ADORA3 (IC50 = 1.14 µM); PTGER4 (IC50 = 1.12 µM) (Eurofins panel #68, others > 5 µM); clean for 18 tested kinases (all > 20 µM) ; Clean PDSP scan with the closest hit on HTR2 (pKi = 5.1) |
| On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 | IC50 = 3.2 nM (glucose uptake assay in HeLa-MaTu cell line) |
| Control compound (100 times less potent than the probe) | Surpasses criterion: IC50 SLC2A1 = 1.2 μM; clean PDSP scan |