Alpelisib — mesenchymal druggability
Inhibition of Alpelisib across the 47 mesenchymal-specific kinases of Table S9 (1 µM single dose). Weighted inhibition 16.6% · mean inhibition 14.1% · 3/47 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 |
|---|---|---|---|---|---|
| FGFR1 | FGFR1 | 1.3 | 98.7 | 2.73 | Upregulated |
| JAK1 | JAK1 | 7.8 | 92.2 | 1.17 | Upregulated |
| EGFR | EGFR | 18.7 | 81.3 | 1.50 | Upregulated |
| ARK5_NUAK1 | NUAK1 | 41.0 | 59.0 | 1.97 | Upregulated |
| DDR2 | DDR2 | 44.7 | 55.3 | 3.68 | Upregulated |
| LIMK1 | LIMK1 | 49.7 | 50.3 | 1.10 | Upregulated |
| PDGFRB | PDGFRB | 61.0 | 39.0 | 3.93 | Upregulated |
| AXL | AXL | 77.0 | 23.0 | 5.65 | Upregulated |
| BMPR2 | BMPR2 | 81.0 | 19.0 | 1.10 | Upregulated |
| FYN | FYN | 81.1 | 18.9 | 1.85 | Upregulated |
| ABL2_ARG | ABL2 | 87.3 | 12.7 | 1.66 | Upregulated |
| RSK3 | RPS6KA2 | 88.5 | 11.5 | 1.66 | Upregulated |
| PDGFRA | PDGFRA | 88.9 | 11.1 | 2.74 | Upregulated |
| PKCMU_PRKD1 | PRKD1 | 89.4 | 10.6 | 2.02 | Upregulated |
| TGFBR2 | TGFBR2 | 90.3 | 9.8 | 2.39 | Upregulated |
| PKACB | PRKACB | 90.7 | 9.3 | 1.25 | Upregulated |
| CAMK4 | CAMK4 | 91.1 | 8.9 | 1.06 | Upregulated |
| CDK15_CYCLIN_A2 | CDK15 | 92.5 | 7.5 | 2.05 | Upregulated |
| DYRK3 | DYRK3 | 94.5 | 5.5 | 1.57 | Upregulated |
| NEK7 | NEK7 | 94.6 | 5.4 | 1.54 | Upregulated |
| MEKK3 | MAP3K3 | 94.6 | 5.4 | 1.03 | Upregulated |
| PKCA | PRKCA | 94.7 | 5.3 | 2.09 | Upregulated |
| PLK2 | PLK2 | 95.6 | 4.4 | 2.42 | Upregulated |
| HGK_MAP4K4 | MAP4K4 | 96.6 | 3.4 | 1.66 | Upregulated |
| HIPK2 | HIPK2 | 97.4 | 2.6 | 1.12 | Upregulated |
| NEK6 | NEK6 | 97.5 | 2.5 | 1.67 | Upregulated |
| MLCK_MYLK | MYLK | 97.8 | 2.2 | 4.25 | Upregulated |
| SGK1 | SGK1 | 98.2 | 1.8 | 2.88 | Upregulated |
| AKT3 | AKT3 | 98.2 | 1.8 | 2.59 | Upregulated |
| CAMK2D | CAMK2D | 98.7 | 1.3 | 1.19 | Upregulated |
| PKCNU_PRKD3 | PRKD3 | 98.8 | 1.2 | 1.04 | Upregulated |
| EPHA5 | EPHA5 | 99.2 | 0.8 | 1.50 | Upregulated |
| C_MET | MET | 99.2 | 0.8 | 1.20 | Upregulated |
| EPHA4 | EPHA4 | 99.9 | 0.1 | 1.10 | Upregulated |
| CAMK1A | CAMK1 | 100.0 | 0.0 | 1.86 | Upregulated |
| ALK5_TGFBR1 | TGFBR1 | 100.0 | 0.0 | 1.12 | Upregulated |
| DRAK1_STK17A | STK17A | 100.0 | 0.0 | 1.98 | Upregulated |
| ALK2_ACVR1 | ACVR1 | 100.0 | 0.0 | 1.66 | Upregulated |
| TIE2_TEK | TEK | 100.0 | 0.0 | 1.16 | Upregulated |
| ZIPK_DAPK3 | DAPK3 | 100.0 | 0.0 | 1.16 | Upregulated |
| EPHB2 | EPHB2 | 100.0 | 0.0 | 1.15 | Upregulated |
| EPHA2 | EPHA2 | 100.0 | 0.0 | 1.22 | Upregulated |
| DLK_MAP3K12 | MAP3K12 | 100.0 | 0.0 | 1.29 | Upregulated |
| LATS2 | LATS2 | 100.0 | 0.0 | 1.37 | Upregulated |
| PEAK1 | PEAK1 | 100.0 | 0.0 | 1.59 | Upregulated |
| DCAMKL2 | DCLK2 | 100.0 | 0.0 | 1.52 | Upregulated |
| STK32B_YANK2 | STK32B | 100.0 | 0.0 | 1.72 | Upregulated |