Umbralisib — mesenchymal druggability
Inhibition of Umbralisib across the 47 mesenchymal-specific kinases of Table S9 (1 µM single dose). Weighted inhibition 15.4% · mean inhibition 13.9% · 2/47 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 |
|---|---|---|---|---|---|
| JAK1 | JAK1 | 3.6 | 96.4 | 1.17 | Upregulated |
| DDR2 | DDR2 | 20.2 | 79.8 | 3.68 | Upregulated |
| ABL2_ARG | ABL2 | 44.2 | 55.8 | 1.66 | Upregulated |
| EPHA2 | EPHA2 | 49.0 | 51.0 | 1.22 | Upregulated |
| PDGFRB | PDGFRB | 53.4 | 46.6 | 3.93 | Upregulated |
| PDGFRA | PDGFRA | 61.7 | 38.3 | 2.74 | Upregulated |
| EPHB2 | EPHB2 | 62.9 | 37.1 | 1.15 | Upregulated |
| EPHA4 | EPHA4 | 67.6 | 32.4 | 1.10 | Upregulated |
| FGFR1 | FGFR1 | 73.1 | 26.9 | 2.73 | Upregulated |
| AKT3 | AKT3 | 74.1 | 25.9 | 2.59 | Upregulated |
| EPHA5 | EPHA5 | 80.4 | 19.6 | 1.50 | Upregulated |
| PKCA | PRKCA | 80.6 | 19.4 | 2.09 | Upregulated |
| FYN | FYN | 83.8 | 16.2 | 1.85 | Upregulated |
| ZIPK_DAPK3 | DAPK3 | 86.9 | 13.1 | 1.16 | Upregulated |
| HGK_MAP4K4 | MAP4K4 | 88.0 | 12.0 | 1.66 | Upregulated |
| BMPR2 | BMPR2 | 89.3 | 10.7 | 1.10 | Upregulated |
| PLK2 | PLK2 | 90.8 | 9.2 | 2.42 | Upregulated |
| ARK5_NUAK1 | NUAK1 | 93.0 | 7.0 | 1.97 | Upregulated |
| NEK7 | NEK7 | 93.5 | 6.5 | 1.54 | Upregulated |
| ALK5_TGFBR1 | TGFBR1 | 93.5 | 6.5 | 1.12 | Upregulated |
| DRAK1_STK17A | STK17A | 93.6 | 6.4 | 1.98 | Upregulated |
| NEK6 | NEK6 | 94.4 | 5.6 | 1.67 | Upregulated |
| TGFBR2 | TGFBR2 | 95.1 | 4.9 | 2.39 | Upregulated |
| LIMK1 | LIMK1 | 95.7 | 4.3 | 1.10 | Upregulated |
| CAMK1A | CAMK1 | 97.1 | 2.9 | 1.86 | Upregulated |
| STK32B_YANK2 | STK32B | 97.1 | 2.9 | 1.72 | Upregulated |
| ALK2_ACVR1 | ACVR1 | 97.1 | 2.9 | 1.66 | Upregulated |
| DYRK3 | DYRK3 | 97.6 | 2.4 | 1.57 | Upregulated |
| LATS2 | LATS2 | 97.7 | 2.3 | 1.37 | Upregulated |
| CAMK4 | CAMK4 | 98.0 | 2.0 | 1.06 | Upregulated |
| RSK3 | RPS6KA2 | 98.3 | 1.7 | 1.66 | Upregulated |
| C_MET | MET | 98.5 | 1.5 | 1.20 | Upregulated |
| EGFR | EGFR | 98.8 | 1.2 | 1.50 | Upregulated |
| CDK15_CYCLIN_A2 | CDK15 | 98.9 | 1.1 | 2.05 | Upregulated |
| HIPK2 | HIPK2 | 99.0 | 1.0 | 1.12 | Upregulated |
| CAMK2D | CAMK2D | 99.8 | 0.2 | 1.19 | Upregulated |
| MEKK3 | MAP3K3 | 100.0 | 0.0 | 1.03 | Upregulated |
| MLCK_MYLK | MYLK | 100.0 | 0.0 | 4.25 | Upregulated |
| TIE2_TEK | TEK | 100.0 | 0.0 | 1.16 | Upregulated |
| PKCMU_PRKD1 | PRKD1 | 100.0 | 0.0 | 2.02 | Upregulated |
| PKCNU_PRKD3 | PRKD3 | 100.0 | 0.0 | 1.04 | Upregulated |
| DCAMKL2 | DCLK2 | 100.0 | 0.0 | 1.52 | Upregulated |
| DLK_MAP3K12 | MAP3K12 | 100.0 | 0.0 | 1.29 | Upregulated |
| AXL | AXL | 100.0 | 0.0 | 5.65 | Upregulated |
| PEAK1 | PEAK1 | 100.0 | 0.0 | 1.59 | Upregulated |
| PKACB | PRKACB | 100.0 | 0.0 | 1.25 | Upregulated |
| SGK1 | SGK1 | 100.0 | 0.0 | 2.88 | Upregulated |