TABLE 1

BTK and TEC selectivity based on biochemical functional and kinetic analyses

DrugIC50 (nM) ± S.D.IC50 RatioKi (nM) ± S.D.Kinact (s−1) ± S.D.Kinact/Ki (nM−1*s−1) ± S.D.Ratio of Kinact/Ki
BTKTECTEC/BTKBTKTECBTKTECBTKTECBTK/TEC
Ibrutinib0.24 ± 0.20.24 ± 0.210.95 ± 0.0091.8 ± 0.050.011 ± 0.00040.013 ± 0.00050.012 ± 0.00060.008 ± 0.00041.5
Acalabrutinib2.3 ± 1.69.7 ± 2.64.28.7 ± 0.5160 ± 370.0021 ± 0.00040.012 ± 0.0010.00024 ± 0.000030.00008 ± 0.000013.0