Table 1. Inhibition profiles for reference compounds and clinically relevant kinase inhibitors.
Selected results are illustrated from the profiling of ATP, staurosporine, dasatinib (Sprycel), imatinib (Gleevec), erlotinib (Tarceva), BIRB796, and sorafenib (Nexavar) in HL60 and PC3 proteomes. Data are shown where significant inhibition with the clinically relevant kinase inhibitors was observed. In total, approximately 220 kinases were evaluated for inhibitory activity. See also Supplemental Table S1 and Supplemental Figures S1, S2, and S3.
| Kinase name | ATP Kdapp | staurosporine | dasatinib | erlotinib | BIRB796 | sorafenib | imatinib |
|---|---|---|---|---|---|---|---|
| ABL1/2 | 5.2 | 13 | 0.0067, 0.0034 | >10 | >10 | >10 | 0.21, 0.15 |
| ACK | 22 | 0.062 | 0.033 | >10 | >10 | >10 | >10 |
| AurA/B/C | 9.5 | 0.076 | >10 | 7.4 | >10 | >10 | >10 |
| AurB | 31 | 0.03, 0.012 | >10, >4 | 6.4, 2.6 | >10, >4 | >10, >4 | >10, >4 |
| BRAF | 6.1 | >10 | 3.2 | >10 | >10 | >10 | >10 |
| BTK | 86 | 0.91 | 0.013 | >10 | >10 | >10 | >10 |
| CDK5 | 13 | 0.64 | >10 | >10 | >10 | >10 | 10 |
| CDK8/11 | 19 | 2.2 | >10 | >10 | >10 | >10 | 11 |
| CSK | 17 | 2.9, 2.4 | 0.015, 0.012 | >10 | >10 | >10 | >10 |
| EGFR | 18 | >10 | 4.7, 4.1 | 0.3, 0.19 | >10 | >10 | >10 |
| EphA1 | 1.7 | 4.3 | 0.022 | >10 | >10 | >10 | >10 |
| EphA2 | 22 | 11 | 0.017 | >10 | >10 | >10 | >10 |
| EphB2 | 5.2 | 10 | 0.014 | >10 | >10 | >10 | >10 |
| EphB4 | 8.5 | >10 | 0.0028 | 5.2 | >10 | >10 | >10 |
| FGR | 2.6 | 0.92, 0.37 | 0.0068, 0.0027 | >10, >4 | >10, >4 | >10, >4 | >10, >4 |
| FYN | ND | 0.27, ND | ND | 5.8, ND | ND | >10, ND | ND |
| GCK | 26 | 0.1 | 5 | >10 | >10 | >10 | >10 |
| GCN2 | 92 | 1.3, 1.1 | >10 | 0.76, 0.6 | >10 | >10 | >10 |
| HCK | 10 | 0.43 | 0.015 | >10 | >10 | >10 | >10 |
| ILK | 57 | >10 | 0.24 | 1.1 | >10 | >10 | >10 |
| IRAK3 | 360 | 0.012 | 10 | >10 | >10 | >10 | ND |
| JAK1 (Domain 2) | 1.8 | 0.21, 0.051 | 5.3, 1.3 | >10, >2.5 | >10, >2.5 | >10, >2.5 | >10, >2.5 |
| JNK1/2/3 | 19 | 9.2 | >10 | >10 | 0.087 | >10 | 8.6 |
| JNK2 | ND | 3.1 | >10 | >10 | 0.029 | >10 | 5.3 |
| KHS1 | 9.6 | 0.12 | 0.4 | >10 | >10 | >10 | >10 |
| KHS1/2 | 7.8 | 0.23 | 2.2 | >10 | >10 | >10 | >10 |
| LOK | 12 | 0.012 | 10 | 1.2 | 1 | 5.3 | >10 |
| LYN | 1 | 0.41 | 0.0031 | >10 | >10 | >10 | >10 |
| MAP2K1 | 8.1 | 0.49, 0.2 | 10, 4 | >10, >4 | >10, >4 | ND | >10, >4 |
| MAP2K5 | 2.6 | 2.6, 1.4 | 0.058, 0.037 | 10 | >10 | >10 | >10 |
| MAP3K1 | 64 | 10 | 0.49 | 0.63 | >10 | 0.82 | >10 |
| MAP3K2 | 7.9 | 1 | 6.5 | >10 | >10 | >10 | >10 |
| MAP3K4 | 20 | >10 | 0.51 | >10 | >10 | >10 | >10 |
| MET | 74 | 0.63, 0.67 | >10 | 3.5, 2.4 | >10 | >10 | >10 |
| MINK, HGK, TNIK | 7.6 | 0.11 | >10 | >10 | 1.1 | >10 | >10 |
| MLKL | 150 | >10 | 3.2 | >10 | >10 | >10 | >10 |
| p38a | 570 | >10 | 0.77 | >10 | 0.19 | 2.4 | >10 |
| p38d/g | 300 | 1.3 | >10 | >10 | 0.45 | >10 | >10 |
| PIK3C3 | 97 | >10 | >10 | >10 | >10 | >10 | 9.5 |
| PIP5K2c | 63 | >10 | >10 | 3.7 | >10 | >10 | 1.5 |
| PIP5K3 | 7 | 10 | >10 | >10 | >10 | >10 | 4.2 |
| PYK2 | 70 | 0.2 | >10 | >10 | 9 | >10 | >10 |
| QSK | 20 | 0.12 | 0.39 | >10 | >10 | >10 | >10 |
| SLK | 3.8 | 0.0091 | >10 | 0.58 | >10 | >10 | >10 |
| SRC | 9.8 | 0.89 | 0.0033 | >10 | >10 | >10 | >10 |
| STLK5 | 54 | >10 | 0.64, 0.21 | >10 | >10 | >10 | >10 |
| SYK | 3.2 | 0.045 | 10 | >10 | >10 | >10 | >10 |
| TAO2 | 1.1 | 0.71, 0.46 | >10 | >10 | >10 | 7.1, 2.8 | >10 |
| TEC | ND | >10, ND | 0.55, <0.079 | >10, ND | >10, ND | >10, ND | >10, ND |
| YES | 31 | 1.1 | 0.0032 | >10 | >10 | >10 | >10 |
| ZAK | 19 | 10 | 0.1445 | >10 | 5.4 | 0.103 | >10 |