Fedratinib — mesenchymal druggability
Inhibition of Fedratinib across the 47 mesenchymal-specific kinases of Table S9 (1 µM single dose). Weighted inhibition 35.4% · mean inhibition 29.9% · 9/47 kinases inhibited to ≤ 35% residual activity.
Strongest inhibition shown left. Inhibition % = 100 − residual activity %.
Per-kinase profile
| Kinase (RBC label) | HGNC | Residual % | Inhibition % | Mes/epi fold-change | Status |
|---|---|---|---|---|---|
| ZIPK_DAPK3 | DAPK3 | 2.3 | 97.7 | 1.16 | Upregulated |
| JAK1 | JAK1 | 5.8 | 94.2 | 1.17 | Upregulated |
| ARK5_NUAK1 | NUAK1 | 6.5 | 93.5 | 1.97 | Upregulated |
| DDR2 | DDR2 | 11.7 | 88.3 | 3.68 | Upregulated |
| FYN | FYN | 16.5 | 83.5 | 1.85 | Upregulated |
| ABL2_ARG | ABL2 | 22.8 | 77.2 | 1.66 | Upregulated |
| AXL | AXL | 23.7 | 76.3 | 5.65 | Upregulated |
| FGFR1 | FGFR1 | 27.2 | 72.8 | 2.73 | Upregulated |
| ALK2_ACVR1 | ACVR1 | 30.6 | 69.3 | 1.66 | Upregulated |
| PDGFRB | PDGFRB | 36.8 | 63.2 | 3.93 | Upregulated |
| PDGFRA | PDGFRA | 50.5 | 49.5 | 2.74 | Upregulated |
| PKCA | PRKCA | 55.3 | 44.7 | 2.09 | Upregulated |
| CAMK2D | CAMK2D | 55.5 | 44.5 | 1.19 | Upregulated |
| TGFBR2 | TGFBR2 | 58.9 | 41.1 | 2.39 | Upregulated |
| MLCK_MYLK | MYLK | 61.2 | 38.8 | 4.25 | Upregulated |
| DCAMKL2 | DCLK2 | 66.4 | 33.6 | 1.52 | Upregulated |
| EPHA2 | EPHA2 | 67.1 | 32.9 | 1.22 | Upregulated |
| LIMK1 | LIMK1 | 70.6 | 29.4 | 1.10 | Upregulated |
| LATS2 | LATS2 | 75.3 | 24.7 | 1.37 | Upregulated |
| PKCMU_PRKD1 | PRKD1 | 77.9 | 22.1 | 2.02 | Upregulated |
| BMPR2 | BMPR2 | 78.5 | 21.5 | 1.10 | Upregulated |
| CAMK1A | CAMK1 | 81.3 | 18.7 | 1.86 | Upregulated |
| PKACB | PRKACB | 82.4 | 17.6 | 1.25 | Upregulated |
| MEKK3 | MAP3K3 | 82.5 | 17.5 | 1.03 | Upregulated |
| RSK3 | RPS6KA2 | 82.8 | 17.2 | 1.66 | Upregulated |
| EGFR | EGFR | 85.9 | 14.1 | 1.50 | Upregulated |
| EPHB2 | EPHB2 | 86.1 | 13.9 | 1.15 | Upregulated |
| TIE2_TEK | TEK | 86.5 | 13.5 | 1.16 | Upregulated |
| CAMK4 | CAMK4 | 89.3 | 10.7 | 1.06 | Upregulated |
| EPHA5 | EPHA5 | 89.7 | 10.3 | 1.50 | Upregulated |
| PKCNU_PRKD3 | PRKD3 | 89.8 | 10.2 | 1.04 | Upregulated |
| EPHA4 | EPHA4 | 91.9 | 8.1 | 1.10 | Upregulated |
| CDK15_CYCLIN_A2 | CDK15 | 92.2 | 7.8 | 2.05 | Upregulated |
| PLK2 | PLK2 | 92.8 | 7.2 | 2.42 | Upregulated |
| DRAK1_STK17A | STK17A | 93.2 | 6.8 | 1.98 | Upregulated |
| C_MET | MET | 93.6 | 6.4 | 1.20 | Upregulated |
| HGK_MAP4K4 | MAP4K4 | 94.1 | 5.9 | 1.66 | Upregulated |
| AKT3 | AKT3 | 95.1 | 4.9 | 2.59 | Upregulated |
| NEK7 | NEK7 | 96.4 | 3.6 | 1.54 | Upregulated |
| NEK6 | NEK6 | 96.5 | 3.5 | 1.67 | Upregulated |
| DYRK3 | DYRK3 | 96.7 | 3.3 | 1.57 | Upregulated |
| HIPK2 | HIPK2 | 97.2 | 2.8 | 1.12 | Upregulated |
| SGK1 | SGK1 | 97.6 | 2.4 | 2.88 | Upregulated |
| DLK_MAP3K12 | MAP3K12 | 100.0 | 0.0 | 1.29 | Upregulated |
| ALK5_TGFBR1 | TGFBR1 | 100.0 | 0.0 | 1.12 | Upregulated |
| PEAK1 | PEAK1 | 100.0 | 0.0 | 1.59 | Upregulated |
| STK32B_YANK2 | STK32B | 100.0 | 0.0 | 1.72 | Upregulated |