TABLE 2 

IC50 determination on cysteine kinases with a cysteine in the same position as Cys481 in BTK

Kinasei+3 ResidueIC50
1237
nM
BTKAsn5.1 ± 1.01.5 ± 0.22.3 ± 0.51.6 ± 0.2
TECAsn126 ± 1110 ± 216 ± 441 ± 3
ITKAsp>10004.9 ± 1.224 ± 252 ± 5
BMXAsn46 ± 120.8 ± 0.11.6 ± 0.43.3 ± 0.4
TXKAsn368 ± 1412.0 ± 0.39.1 ± 2.77.6 ± 2.4
EGFRAsp>10005.3 ± 1.3199 ± 3520 ± 5
ERBB2Asp∼10006.4 ± 1.8>100013 ± 3
ERBB4Glu16 ± 53.4 ± 1.449 ± 125.3 ± 0.5
BLKAsp>10000.1 ± 0.0131 ± 2719 ± 4
JAK3Asp>100032 ± 155.4 ± 1.1>1000
  • BTK and ITK kinase activity was measured using the IMAP assay. For BMX, TXK, EGFR, ERBB2, ERBB4, BLK, and JAK3, kinase activity was measured at Thermo Fisher using the Z′-LYTE assay. TEC kinase activity was determined in a LanthaScreen assay. Results are mean ± S.D. of at least three independent experiments.