Apatinib
Sign in to save this workspacePrimary targets: KDR_VEGFR2 · FDA status: NMPA Approved
Selectivity scorecard
KISS
97.73
Gini
0.704
CATDS
0.022
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 Apatinib. Strongest target: RAF1 at 100.0% inhibition.
Accessible data table
| Rank | Target | Inhibition % | Residual activity % |
|---|---|---|---|
| 1 | RAF1 | 100.0% | 0.0% |
| 2 | C_KIT | 98.9% | 1.1% |
| 3 | FMS | 97.8% | 2.2% |
| 4 | FLT1_VEGFR1 | 95.6% | 4.4% |
| 5 | YSK4_MAP3K19 | 95.3% | 4.7% |
| 6 | BRAF | 94.1% | 5.9% |
| 7 | KDR_VEGFR2 | 92.3% | 7.7% |
| 8 | FLT4_VEGFR3 | 90.8% | 9.2% |
| 9 | ARAF | 90.7% | 9.3% |
| 10 | JAK1 | 88.7% | 11.3% |
| 11 | LYN | 82.3% | 17.7% |
| 12 | TAOK2_TAO1 | 81.5% | 18.6% |
| 13 | RET | 81.1% | 18.9% |
| 14 | DDR2 | 80.9% | 19.1% |
| 15 | PDGFRB | 80.9% | 19.1% |
| 16 | LCK | 71.8% | 28.2% |
| 17 | ZAK_MLTK | 71.1% | 28.9% |
| 18 | HIPK4 | 70.8% | 29.2% |
| 19 | ABL2_ARG | 65.4% | 34.6% |
| 20 | JAK2 | 65.3% | 34.7% |
Selectivity landscape
Where Apatinib sits in the 92-drug selectivity landscape (KISS vs Gini). The highlighted point is Apatinib.
Atlas insights for Apatinib
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 | 1807.53 | |
| ALLOGRAFT_REJECTION | 5296.23 | |
| ANDROGEN_RESPONSE | 723.40 | |
| ANGIOGENESIS | 820.54 | |
| APICAL_JUNCTION | 5706.96 | |
| APICAL_SURFACE | 586.03 | |
| APOPTOSIS | 3734.49 | |
| BILE_ACID_METABOLISM | 461.52 | |
| CHOLESTEROL_HOMEOSTASIS | 566.65 | |
| COAGULATION | 635.26 | |
| COMPLEMENT | 3080.44 | |
| DNA_REPAIR | 800.12 | |
| E2F_TARGETS | 2540.09 | |
| EPITHELIAL_MESENCHYMAL_TRANSITION | 994.35 | |
| ESTROGEN_RESPONSE_EARLY | 1886.59 | |
| ESTROGEN_RESPONSE_LATE | 1624.68 | |
| FATTY_ACID_METABOLISM | 376.56 | |
| G2M_CHECKPOINT | 2479.88 | |
| GLYCOLYSIS | 1451.23 | |
| HEDGEHOG_SIGNALING | 528.46 | |
| HEME_METABOLISM | 1339.99 | |
| HYPOXIA | 2182.46 | |
| IL2_STAT5_SIGNALING | 2065.76 | |
| IL6_JAK_STAT3_SIGNALING | 3898.34 | |
| INFLAMMATORY_RESPONSE | 3394.06 | |
| INTERFERON_ALPHA_RESPONSE | 695.59 | |
| INTERFERON_GAMMA_RESPONSE | 3996.85 | |
| KRAS_SIGNALING_DN | 524.97 | |
| KRAS_SIGNALING_UP | 2199.89 | |
| MITOTIC_SPINDLE | 3201.98 | |
| MTORC1_SIGNALING | 2044.51 | |
| MYC_TARGETS_V1 | 1995.06 | |
| MYC_TARGETS_V2 | 453.28 | |
| MYOGENESIS | 1544.77 | |
| NOTCH_SIGNALING | 83.78 | |
| OXIDATIVE_PHOSPHORYLATION | 754.71 | |
| P53_PATHWAY | 1745.17 | |
| PANCREAS_BETA_CELLS | 120.79 | |
| PEROXISOME | 489.86 | |
| PI3K_AKT_MTOR_SIGNALING | 5775.16 | |
| PROTEIN_SECRETION | 1122.07 | |
| REACTIVE_OXYGEN_SPECIES_PATHWAY | 219.76 | |
| SPERMATOGENESIS | 1183.35 | |
| TGF_BETA_SIGNALING | 860.42 | |
| TNFA_SIGNALING_VIA_NFKB | 2760.38 | |
| UNFOLDED_PROTEIN_RESPONSE | 771.61 | |
| UV_RESPONSE_DN | 3031.79 | |
| UV_RESPONSE_UP | 2014.42 | |
| WNT_BETA_CATENIN_SIGNALING | 907.08 | |
| XENOBIOTIC_METABOLISM | 947.62 |
Hallmarks-of-Cancer reach
Anti-tumor matches — the "ideal patient" search
| Sample | Cancer type | cos to ideal |
|---|---|---|
| SRR23303752 | — | 0.824 |
| EPT0291 | EPN | 0.823 |
| TCGA-CF-A5U8-01A-11R-A28M-07 | — | 0.814 |
| TCGA-FD-A43X-01A-11R-A23W-07 | — | 0.811 |
| SRR10899984 | — | 0.808 |
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