The tyrosine kinase expressed in hepatocellular carcinoma (TEC) family comprises five non-receptor tyrosine kinases – BTK, ITK, BMX, TXK, and TEC – with key roles in immune signalling. Although BTK and ITK have been extensively studied, selective inhibitors for TEC, TXK, and BMX remain scarce. Recently, we identified 7-azaindole-based covalent BMX inhibitors with potent inhibitory activity and robust cellular target engagement but limited selectivity across TEC family members, especially BTK. He
Riding toward Selectivity: Optimization of Covalent 7-Azaindole-Based BMX Kinase Inhibitors
Xiaojun Julia Liang·Matthias Gehringer·Thales Kronenberger·Ekaterina Shevchenko·Alexander Rasch·Benedict‐Tilman Berger·Martin P. Schwalm·Lena M. Berger·Andreas Krämer·Ricardo A. M. Serafim·Michael Förster·A. Chaikuad·María Laura Bolognesi·Susanne Müller·Antti Poso·Stefan Laufer·Stefan Knapp·Claudia Albertini
