EMT / mesenchymal druggability
Table S9 profiles all 92 clinical kinase inhibitors against 47 mesenchymal-specific kinases at a single 1 µM dose — the druggable TGF-β/BMP receptor module (ALK5/TGFBR1, TGFBR2, BMPR2, ACVR1) plus AXL, MET, DDR2, PDGFRA/B, FGFR1, EPHA2, NUAK1, LATS2 and PEAK1. Values are residual activity % (0–100, lower = stronger inhibition); inhibition % = 100 − residual. Drugs are ranked by weighted inhibition — each kinase’s inhibition weighted by its Table S8 mesenchymal fold-change — so coverage of the most mesenchymal-enriched kinases counts for more than the naive S9 Avg.
92 inhibitors ranked by mesenchymal-program coverage
Strong inhibition counts kinases at ≤ 35% residual activity, the same single-dose hit cut used elsewhere on the platform.
Most mesenchymal-enriched targets in the program
Expression weights are the Table S8 mesenchymal/epithelial fold-change.
| Kinase (RBC label) | HGNC | Fold-change (mes/epi) | Status |
|---|---|---|---|
| AXL | AXL | 5.65 | Upregulated |
| MLCK_MYLK | MYLK | 4.25 | Upregulated |
| PDGFRB | PDGFRB | 3.93 | Upregulated |
| DDR2 | DDR2 | 3.68 | Upregulated |
| SGK1 | SGK1 | 2.88 | Upregulated |
| PDGFRA | PDGFRA | 2.74 | Upregulated |
| FGFR1 | FGFR1 | 2.73 | Upregulated |
| AKT3 | AKT3 | 2.59 | Upregulated |