Skip to main content
. 2024 May 7;67(10):8122–8140. doi: 10.1021/acs.jmedchem.4c00220

Table 5. Selectivity of Selected BTK Inhibitors over Kinases with a Reactive Cysteine at the 481 Position.

      compound
  amino acid @484 position tolebrutinib (2) Kd [nM] evobrutinib (4) Kd [nM] 10Kd [nM] 25Kd [nM] 27Kd [nM]
BTK Kd [nM] Asn 1.4 4.6 0.6 0.63 0.31
Kinase with Cys481   Fold Selectivity for BTK (off-target kinase Kd/BTK Kd)
BMX Asn 3 4 43 43 14
TEC Asn 1 <1 9 9 7
TXK Asn 5 37 27 27 6
JAK3 Asp 847 1217 157 157 390
BLK Asp 3 133 460 460 839
ITK Asp 671 587 1200 1206 274
EGFR Asp 9 2000 >10 000 >10 000 9355
ERBB2 Asp 2 1152 >10 000 >10 000 7419
ERBB4 Glu 4 137 700 714 7741