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.
Atlas insights for Regorafenib
Pathway-space view of what this drug actually does, drawn from the Pathway Atlas.
On-target vs off-target shadow
On-target0%
Off-target100%
Ghost (2nd-order)0%
| Pathway | Composition | Total |Π| |
|---|---|---|
| ADIPOGENESIS | 1741.58 | |
| ALLOGRAFT_REJECTION | 4249.73 | |
| ANDROGEN_RESPONSE | 910.69 | |
| ANGIOGENESIS | 856.72 | |
| APICAL_JUNCTION | 5645.74 | |
| APICAL_SURFACE | 430.59 | |
| APOPTOSIS | 3932.90 | |
| BILE_ACID_METABOLISM | 570.99 | |
| CHOLESTEROL_HOMEOSTASIS | 867.60 | |
| COAGULATION | 565.87 | |
| COMPLEMENT | 2902.84 | |
| DNA_REPAIR | 1173.10 | |
| E2F_TARGETS | 2921.10 | |
| EPITHELIAL_MESENCHYMAL_TRANSITION | 1152.33 | |
| ESTROGEN_RESPONSE_EARLY | 1948.50 | |
| ESTROGEN_RESPONSE_LATE | 1780.08 | |
| FATTY_ACID_METABOLISM | 662.29 | |
| G2M_CHECKPOINT | 2987.32 | |
| GLYCOLYSIS | 1762.36 | |
| HEDGEHOG_SIGNALING | 684.08 | |
| HEME_METABOLISM | 1204.92 | |
| HYPOXIA | 2354.61 | |
| IL2_STAT5_SIGNALING | 1677.32 | |
| IL6_JAK_STAT3_SIGNALING | 2806.09 | |
| INFLAMMATORY_RESPONSE | 2497.29 | |
| INTERFERON_ALPHA_RESPONSE | 469.14 | |
| INTERFERON_GAMMA_RESPONSE | 3069.14 | |
| KRAS_SIGNALING_DN | 577.49 | |
| KRAS_SIGNALING_UP | 1998.53 | |
| MITOTIC_SPINDLE | 3802.07 | |
| MTORC1_SIGNALING | 2037.22 | |
| MYC_TARGETS_V1 | 2306.51 | |
| MYC_TARGETS_V2 | 469.30 | |
| MYOGENESIS | 1642.72 | |
| NOTCH_SIGNALING | 173.55 | |
| OXIDATIVE_PHOSPHORYLATION | 1144.29 | |
| P53_PATHWAY | 2031.38 | |
| PANCREAS_BETA_CELLS | 211.15 | |
| PEROXISOME | 720.89 | |
| PI3K_AKT_MTOR_SIGNALING | 5748.87 | |
| PROTEIN_SECRETION | 1113.23 | |
| REACTIVE_OXYGEN_SPECIES_PATHWAY | 307.28 | |
| SPERMATOGENESIS | 959.09 | |
| TGF_BETA_SIGNALING | 1200.37 | |
| TNFA_SIGNALING_VIA_NFKB | 2542.31 | |
| UNFOLDED_PROTEIN_RESPONSE | 827.68 | |
| UV_RESPONSE_DN | 2995.06 | |
| UV_RESPONSE_UP | 1909.21 | |
| WNT_BETA_CATENIN_SIGNALING | 1306.14 | |
| XENOBIOTIC_METABOLISM | 1036.20 |
Hallmarks-of-Cancer reach
Anti-tumor matches — the "ideal patient" search
| Sample | Cancer type | cos to ideal |
|---|---|---|
| EPT0291 | EPN | 0.840 |
| SRR23303752 | — | 0.835 |
| aMVAC.P_005_TURBT_S223 | — | 0.821 |
| TCGA-CF-A5U8-01A-11R-A28M-07 | — | 0.819 |
| SRR12202498 | — | 0.814 |
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