BI 605906
Probe criteria
| Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) | Surpasses criterion: IKBKB: IC50 = 49 nM |
| Selectivity within target family: > 30-fold | Surpasses criterion: 3 hits out of 397 kinases; Dose response measurements: GAK IC50 = 188 nM; AAK1 IC50 = 272 nM; IRAK3 IC50 = 921 nM; NanoBRET (SGC-FFM): GAK IC50 = 6.5 μM; AAK1 IC50 = 7.0 μM; IRAK3 IC50 > 20 μM |
| Selectivity outside target family | Surpasses criterion: Panlabs panel: human PDE3A 31 % Ctrl at 10 µM; all other targets >50 % CtrlOff-targets in the PDSP scan are DRD2 Ki = 341.44 nM, DRD3 Ki = 428.07 nM, GABA/PBR Ki = 2622.51 nM. |
| On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 | Surpasses criterion: EC50 = 0.9 µM (Inhibition of phospho-IκBα in HeLa cells); EC50 = 0.7 µM (Inhibition of expression of ICAM1 in HeLa cells) |
| Control compound (100 times less potent than the probe) | Surpasses criterion: BI-5026: IKBKB IC50 > 10 µMClosest off-target in the PDSP scan is SLC6A3 (Ki = 4270.71 nM). |