Identified kinase targets of dasatinib, nilotinib and imatinib
| Gene name . | Description . | IPI-ID . | Dasatinib . | Nilotinib . | Imatinib . | |||
|---|---|---|---|---|---|---|---|---|
| Unique peptides, no. . | SC,% . | Unique peptides, no. . | SC, % . | Unique peptides, no. . | SC, % . | |||
| BCR-ABL | BCR-ABL fusion protein | — | 57 | 31.9 | 15 | 6.8 | 9 | 4.2 |
| -BCR-ABL | BCR/ABL1 fusion protein (fragment) | IPI00784719 | 2 | 16.9 | — | — | — | — |
| -BCR | Breakpoint cluster region | IPI00472302 | 31 | 29.8 | 5 | 4.7 | 6 | 5.2 |
| -ABL1 | Abelson tyrosine kinase | IPI00221171 | 27 | 28.5 | 10 | 9.3 | 3 | 2.3 |
| BTK | Tyrosine-protein kinase BTK | IPI00029132 | 41/20 | 70.5/36.9 | — | — | — | — |
| CSK | Tyrosine-protein kinase CSK | IPI00013212 | 26/21 | 59.3/55.1 | — | — | — | — |
| MAP3K4 | Mitogen-activated protein kinase kinase kinase 4 | IPI00186536 | 24 | 16.9 | — | — | — | — |
| DDR1 | Discoidin domain receptor 1 | IPI00219996 | 23 | 27.3 | 15 | 17.0 | — | — |
| GAK | Cyclin G–associated kinase | IPI00298949 | 22 | 19.5 | — | — | — | — |
| TEC | Tyrosine-protein kinase TEC | IPI00000878 | 21 | 32.3 | — | — | — | — |
| ABL2 | Tyrosine-protein kinase ABL2 | IPI00329488 | 21 | 19.3 | 13 | 11.3 | — | — |
| LYN | Tyrosine-protein kinase LYN | IPI00298625 | 14/20 | 33.0/46.9 | — | — | — | — |
| MAPK14 | p38α | IPI00002857 | 14/15 | 43.1/43.6 | — | — | — | — |
| EPHB6 | Ephrin type-B receptor 6 precursor | IPI00005222 | 14 | 17.7 | — | — | — | — |
| YES1 | Proto-oncogene tyrosine-protein kinase YES | IPI00013981 | 13/10 | 23.4/17.5 | — | — | — | — |
| EPHB4 | Ephrin type-B receptor 4 precursor | IPI00289342 | 12/5 | 13.3/5.0 | — | — | — | — |
| ZAK | Mitogen-activated protein kinase kinase kinase MLT | IPI00029643 | 11 | 29.7 | — | — | — | — |
| SNF1LK2 | Serine/threonine-protein kinase SNF1-like kinase 2 (QIK) | IPI00465291 | 10 | 10.7 | — | — | — | — |
| FYN | Tyrosine-protein kinase FYN | IPI00640091 | 9/7 | 15.9/13.3 | — | — | — | — |
| SRC | Proto-oncogene tyrosine-protein kinase SRC | IPI00328867 | 8/18 | 14.0/40.4 | — | — | — | — |
| RIPK2 | Receptor-interacting serine/threonine-protein kinase 2 | IPI00021917 | 5/2 | 10.6/4.3 | — | — | — | — |
| MAP3K1 | Mitogen-activated protein kinase kinase kinase 1 | IPI00012318 | 5 | 3.8 | — | — | — | — |
| FRK | Tyrosine-protein kinase FRK | IPI00000885 | 4/2 | 7.3/3.2 | — | — | — | — |
| EPHB2 | Ephrin type-B receptor 2 precursor | IPI00219421 | 4 | 4.5 | — | — | — | — |
| FGR | Proto-oncogene tyrosine-protein kinase FGR | IPI00016871 | 3/24 | 4.5/50.5 | — | — | — | — |
| TYK2 | Nonreceptor tyrosine-protein kinase TYK2 | IPI00022353 | 3 | 2.5 | — | — | — | — |
| HCK | Tyrosine-protein kinase HCK | IPI00029769 | —/23 | —/56.0 | — | — | — | — |
| BMX | Tyrosine-protein kinase BMX | IPI00020899 | —/11 | —/20.1 | — | — | — | — |
| ILK | Integrin-linked protein kinase | IPI00013219 | —/9 | —/23.0 | — | — | — | — |
| MAP3K3 | Mitogen-activated protein kinase kinase kinase 3 | IPI00181703 | —/5 | —/11.4 | — | — | — | — |
| LCK | Proto-oncogene tyrosine-protein kinase LCK | IPI00555672 | —/3 | —/5.6 | — | — | — | — |
| LIMK2 | LIM domain kinase 2 | IPI00100853 | —/2 | —/4.1 | — | — | — | — |
| SYK | Spleen tyrosine kinase | IPI00018597 | —/2 | —/3.3 | — | — | — | — |
| Gene name . | Description . | IPI-ID . | Dasatinib . | Nilotinib . | Imatinib . | |||
|---|---|---|---|---|---|---|---|---|
| Unique peptides, no. . | SC,% . | Unique peptides, no. . | SC, % . | Unique peptides, no. . | SC, % . | |||
| BCR-ABL | BCR-ABL fusion protein | — | 57 | 31.9 | 15 | 6.8 | 9 | 4.2 |
| -BCR-ABL | BCR/ABL1 fusion protein (fragment) | IPI00784719 | 2 | 16.9 | — | — | — | — |
| -BCR | Breakpoint cluster region | IPI00472302 | 31 | 29.8 | 5 | 4.7 | 6 | 5.2 |
| -ABL1 | Abelson tyrosine kinase | IPI00221171 | 27 | 28.5 | 10 | 9.3 | 3 | 2.3 |
| BTK | Tyrosine-protein kinase BTK | IPI00029132 | 41/20 | 70.5/36.9 | — | — | — | — |
| CSK | Tyrosine-protein kinase CSK | IPI00013212 | 26/21 | 59.3/55.1 | — | — | — | — |
| MAP3K4 | Mitogen-activated protein kinase kinase kinase 4 | IPI00186536 | 24 | 16.9 | — | — | — | — |
| DDR1 | Discoidin domain receptor 1 | IPI00219996 | 23 | 27.3 | 15 | 17.0 | — | — |
| GAK | Cyclin G–associated kinase | IPI00298949 | 22 | 19.5 | — | — | — | — |
| TEC | Tyrosine-protein kinase TEC | IPI00000878 | 21 | 32.3 | — | — | — | — |
| ABL2 | Tyrosine-protein kinase ABL2 | IPI00329488 | 21 | 19.3 | 13 | 11.3 | — | — |
| LYN | Tyrosine-protein kinase LYN | IPI00298625 | 14/20 | 33.0/46.9 | — | — | — | — |
| MAPK14 | p38α | IPI00002857 | 14/15 | 43.1/43.6 | — | — | — | — |
| EPHB6 | Ephrin type-B receptor 6 precursor | IPI00005222 | 14 | 17.7 | — | — | — | — |
| YES1 | Proto-oncogene tyrosine-protein kinase YES | IPI00013981 | 13/10 | 23.4/17.5 | — | — | — | — |
| EPHB4 | Ephrin type-B receptor 4 precursor | IPI00289342 | 12/5 | 13.3/5.0 | — | — | — | — |
| ZAK | Mitogen-activated protein kinase kinase kinase MLT | IPI00029643 | 11 | 29.7 | — | — | — | — |
| SNF1LK2 | Serine/threonine-protein kinase SNF1-like kinase 2 (QIK) | IPI00465291 | 10 | 10.7 | — | — | — | — |
| FYN | Tyrosine-protein kinase FYN | IPI00640091 | 9/7 | 15.9/13.3 | — | — | — | — |
| SRC | Proto-oncogene tyrosine-protein kinase SRC | IPI00328867 | 8/18 | 14.0/40.4 | — | — | — | — |
| RIPK2 | Receptor-interacting serine/threonine-protein kinase 2 | IPI00021917 | 5/2 | 10.6/4.3 | — | — | — | — |
| MAP3K1 | Mitogen-activated protein kinase kinase kinase 1 | IPI00012318 | 5 | 3.8 | — | — | — | — |
| FRK | Tyrosine-protein kinase FRK | IPI00000885 | 4/2 | 7.3/3.2 | — | — | — | — |
| EPHB2 | Ephrin type-B receptor 2 precursor | IPI00219421 | 4 | 4.5 | — | — | — | — |
| FGR | Proto-oncogene tyrosine-protein kinase FGR | IPI00016871 | 3/24 | 4.5/50.5 | — | — | — | — |
| TYK2 | Nonreceptor tyrosine-protein kinase TYK2 | IPI00022353 | 3 | 2.5 | — | — | — | — |
| HCK | Tyrosine-protein kinase HCK | IPI00029769 | —/23 | —/56.0 | — | — | — | — |
| BMX | Tyrosine-protein kinase BMX | IPI00020899 | —/11 | —/20.1 | — | — | — | — |
| ILK | Integrin-linked protein kinase | IPI00013219 | —/9 | —/23.0 | — | — | — | — |
| MAP3K3 | Mitogen-activated protein kinase kinase kinase 3 | IPI00181703 | —/5 | —/11.4 | — | — | — | — |
| LCK | Proto-oncogene tyrosine-protein kinase LCK | IPI00555672 | —/3 | —/5.6 | — | — | — | — |
| LIMK2 | LIM domain kinase 2 | IPI00100853 | —/2 | —/4.1 | — | — | — | — |
| SYK | Spleen tyrosine kinase | IPI00018597 | —/2 | —/3.3 | — | — | — | — |
Proteins are sorted by decreasing peptide counts. The BCR-ABL fusion protein, which as a whole is not represented by an IPI-ID, is split into its components BCR and ABL1, as well as a short peptide sequence characteristic of the fusion region of BCR-ABL. The listed BCR-ABL parameters were determined by combination of the separate component parameters. Unique peptides are the number of all unique peptides observed for a particular protein. The listed sequence coverage (SC) is based on these unique peptides. Imatinib has been italicized to reflect the lower potency of c-imatinib3 compared with imatinib.
IPI-ID indicates IPI protein database entries to which identified peptides were assigned; SC, sequence coverage; and —, no entry.