Table 2.
Kinase Inhibitor | target | binding and kinase inhibition (nM, cell-free unless otherwise noted) |
---|---|---|
UNC202511 | MERTK | Kd: 0.74 IC50 (in cell): 1 μM |
dasatinib23,12 | BCR-Abl | Kd: Src 0.07; Abl 0.03 IC50 (μM): Src; 0.2, Abl 0.03, Lyn 0.6, Btk 1.5 |
BI253613 | PLK1–3 | IC50: PLK1 5.01; PLK2 19.4; PLK3 9.37 |
nilotinib14 | BCR-Abl | IC50 (in cell): 20 – 60 |
spebrutinib15 | Btk | IC50: < 0.5 |
crizotinib16 | ALK | IC50 (in cells): 24 |
erlotinib17 | EGFR | IC50: 2 |
Ibrutinib7 | Btk | IC50: 68 |
gefitinib18 | EGFR | IC50 (in cells): 33 |
vemurafenib19 | BRAFV600E | IC50 (in cells): 64 – 110 |
afatinib20 | EGFR, HER2 | IC50 (in cell): 0.35 – 0.34 μM |