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BI 605906

2D structure
Target IKBKB 
Targeted domain Kinase domain (active site)
Mode of action Inhibitor (ATP competitive)
Control BI-5026
Recommended cellular usage concentration ≤ 5 µM
In vivo use Yes
Donated by Boehringer Ingelheim


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 % Ctrl
Off-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 µM
Closest off-target in the PDSP scan is SLC6A3 (Ki = 4270.71 nM).