Axitinib
Sign in to save this workspacePrimary targets: FLT1_VEGFR1, KDR_VEGFR2, FLT4_VEGFR3 · FDA status: FDA Approved
Selectivity scorecard
KISS
93.23
Gini
0.688
CATDS
0.012
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 Axitinib. Strongest target: AURORA_A at 100.0% inhibition.
Accessible data table
| Rank | Target | Inhibition % | Residual activity % |
|---|---|---|---|
| 1 | AURORA_A | 100.0% | 0.0% |
| 2 | ABL1 | 99.4% | 0.6% |
| 3 | TNIK | 99.0% | 1.0% |
| 4 | FLT4_VEGFR3 | 98.5% | 1.5% |
| 5 | ABL2_ARG | 98.3% | 1.7% |
| 6 | FLT1_VEGFR1 | 98.1% | 1.9% |
| 7 | KDR_VEGFR2 | 96.9% | 3.1% |
| 8 | FGFR2 | 96.1% | 3.9% |
| 9 | PDGFRA | 96.0% | 4.0% |
| 10 | FMS | 95.2% | 4.8% |
| 11 | AURORA_B | 95.1% | 4.9% |
| 12 | FGFR1 | 94.9% | 5.1% |
| 13 | ROS_ROS1 | 93.7% | 6.3% |
| 14 | AMPK(A1_B2_G2) | 93.7% | 6.3% |
| 15 | AMPK(A1_B2_G3) | 93.6% | 6.4% |
| 16 | MINK_MINK1 | 93.4% | 6.6% |
| 17 | AMPK(A1_B2_G1) | 93.3% | 6.7% |
| 18 | FGFR3 | 93.1% | 6.9% |
| 19 | AMPK(A2_B2_G2) | 93.0% | 7.0% |
| 20 | PDGFRB | 92.9% | 7.1% |
Selectivity landscape
Where Axitinib sits in the 92-drug selectivity landscape (KISS vs Gini). The highlighted point is Axitinib.
Atlas insights for Axitinib
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 | 2116.56 | |
| ALLOGRAFT_REJECTION | 7428.81 | |
| ANDROGEN_RESPONSE | 1307.05 | |
| ANGIOGENESIS | 1437.60 | |
| APICAL_JUNCTION | 7944.24 | |
| APICAL_SURFACE | 860.23 | |
| APOPTOSIS | 6343.31 | |
| BILE_ACID_METABOLISM | 827.68 | |
| CHOLESTEROL_HOMEOSTASIS | 1258.94 | |
| COAGULATION | 850.30 | |
| COMPLEMENT | 4229.88 | |
| DNA_REPAIR | 1424.21 | |
| E2F_TARGETS | 3198.44 | |
| EPITHELIAL_MESENCHYMAL_TRANSITION | 1616.69 | |
| ESTROGEN_RESPONSE_EARLY | 2594.29 | |
| ESTROGEN_RESPONSE_LATE | 2579.14 | |
| FATTY_ACID_METABOLISM | 869.28 | |
| G2M_CHECKPOINT | 3347.80 | |
| GLYCOLYSIS | 2256.79 | |
| HEDGEHOG_SIGNALING | 636.77 | |
| HEME_METABOLISM | 1802.49 | |
| HYPOXIA | 3341.37 | |
| IL2_STAT5_SIGNALING | 2334.08 | |
| IL6_JAK_STAT3_SIGNALING | 4504.90 | |
| INFLAMMATORY_RESPONSE | 3426.59 | |
| INTERFERON_ALPHA_RESPONSE | 730.68 | |
| INTERFERON_GAMMA_RESPONSE | 5098.27 | |
| KRAS_SIGNALING_DN | 774.09 | |
| KRAS_SIGNALING_UP | 2780.26 | |
| MITOTIC_SPINDLE | 5272.44 | |
| MTORC1_SIGNALING | 3005.45 | |
| MYC_TARGETS_V1 | 2193.69 | |
| MYC_TARGETS_V2 | 569.26 | |
| MYOGENESIS | 2464.23 | |
| NOTCH_SIGNALING | 172.57 | |
| OXIDATIVE_PHOSPHORYLATION | 1393.93 | |
| P53_PATHWAY | 2939.43 | |
| PANCREAS_BETA_CELLS | 217.43 | |
| PEROXISOME | 1139.41 | |
| PI3K_AKT_MTOR_SIGNALING | 8166.36 | |
| PROTEIN_SECRETION | 1838.77 | |
| REACTIVE_OXYGEN_SPECIES_PATHWAY | 377.15 | |
| SPERMATOGENESIS | 992.54 | |
| TGF_BETA_SIGNALING | 1633.14 | |
| TNFA_SIGNALING_VIA_NFKB | 3370.13 | |
| UNFOLDED_PROTEIN_RESPONSE | 1138.09 | |
| UV_RESPONSE_DN | 3957.32 | |
| UV_RESPONSE_UP | 2915.49 | |
| WNT_BETA_CATENIN_SIGNALING | 1524.41 | |
| XENOBIOTIC_METABOLISM | 1635.78 |
Hallmarks-of-Cancer reach
Anti-tumor matches — the "ideal patient" search
| Sample | Cancer type | cos to ideal |
|---|---|---|
| SRR23303752 | — | 0.829 |
| EPT0291 | EPN | 0.825 |
| SRR10899984 | — | 0.814 |
| aMVAC.P_005_TURBT_S223 | — | 0.810 |
| SRR12202498 | — | 0.802 |
Annotations
Sign in to read and post annotations.
Loading…