Regorafenib
Sign in to save this workspacePrimary targets: FLT1_VEGFR1, FLT4_VEGFR3, KDR_VEGFR2 · FDA status: FDA Approved
Selectivity scorecard
KISS
95.99
Gini
0.719
CATDS
0.019
Computed from wild-type kinome inhibition at 1 μM. Gini reproduces the published values within tolerance; KISS and CATDS are computed but pending reconciliation with the paper's reference code.
Polypharmacology radar
Top 20 strongest-inhibited wild-type kinases for Regorafenib. Strongest target: RAF1 at 99.9% inhibition.
Accessible data table
| Rank | Target | Inhibition % | Residual activity % |
|---|---|---|---|
| 1 | RAF1 | 99.9% | 0.1% |
| 2 | ARAF | 98.8% | 1.2% |
| 3 | RET | 98.7% | 1.3% |
| 4 | BRAF | 98.3% | 1.7% |
| 5 | HIPK4 | 98.0% | 2.0% |
| 6 | DDR2 | 97.6% | 2.4% |
| 7 | FMS | 97.4% | 2.6% |
| 8 | PDGFRA | 96.7% | 3.3% |
| 9 | PDGFRB | 95.4% | 4.6% |
| 10 | YSK4_MAP3K19 | 95.4% | 4.6% |
| 11 | DDR1 | 92.7% | 7.3% |
| 12 | FLT4_VEGFR3 | 92.2% | 7.8% |
| 13 | RIPK3 | 91.9% | 8.1% |
| 14 | FLT1_VEGFR1 | 91.8% | 8.2% |
| 15 | KDR_VEGFR2 | 91.7% | 8.3% |
| 16 | ZAK_MLTK | 90.7% | 9.3% |
| 17 | ERK7_MAPK15 | 89.7% | 10.3% |
| 18 | FGFR2 | 77.9% | 22.1% |
| 19 | MUSK | 76.8% | 23.1% |
| 20 | EPHA6 | 75.5% | 24.5% |
Selectivity landscape
Where Regorafenib sits in the 92-drug selectivity landscape (KISS vs Gini). The highlighted point is Regorafenib.
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