Entrectinib
Sign in to save this workspacePrimary targets: TRKA · FDA status: FDA Approved
Selectivity scorecard
KISS
93.69
Gini
0.671
CATDS
0.013
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 Entrectinib. Strongest target: HASPIN at 100.0% inhibition.
Accessible data table
| Rank | Target | Inhibition % | Residual activity % |
|---|---|---|---|
| 1 | HASPIN | 100.0% | 0.0% |
| 2 | TRKB | 99.8% | 0.2% |
| 3 | RET | 99.6% | 0.4% |
| 4 | ROS_ROS1 | 99.3% | 0.7% |
| 5 | TXK | 99.1% | 0.9% |
| 6 | TRKA | 99.0% | 1.0% |
| 7 | JAK2 | 99.0% | 1.0% |
| 8 | TRKC | 98.8% | 1.2% |
| 9 | ALK | 98.8% | 1.2% |
| 10 | TYK2 | 97.9% | 2.1% |
| 11 | IRR_INSRR | 97.5% | 2.5% |
| 12 | ACK1 | 97.3% | 2.7% |
| 13 | TYK1_LTK | 97.3% | 2.7% |
| 14 | HPK1_MAP4K1 | 96.3% | 3.7% |
| 15 | FLT3 | 96.1% | 3.9% |
| 16 | DDR1 | 96.0% | 4.0% |
| 17 | MUSK | 95.9% | 4.1% |
| 18 | FGR | 95.4% | 4.6% |
| 19 | BTK | 95.1% | 4.9% |
| 20 | ARK5_NUAK1 | 93.5% | 6.5% |
Selectivity landscape
Where Entrectinib sits in the 92-drug selectivity landscape (KISS vs Gini). The highlighted point is Entrectinib.
Atlas insights for Entrectinib
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 | 2728.55 | |
| ALLOGRAFT_REJECTION | 10338.30 | |
| ANDROGEN_RESPONSE | 1520.35 | |
| ANGIOGENESIS | 1499.80 | |
| APICAL_JUNCTION | 9114.00 | |
| APICAL_SURFACE | 1048.14 | |
| APOPTOSIS | 5910.18 | |
| BILE_ACID_METABOLISM | 885.59 | |
| CHOLESTEROL_HOMEOSTASIS | 1100.03 | |
| COAGULATION | 1165.08 | |
| COMPLEMENT | 5255.90 | |
| DNA_REPAIR | 1532.42 | |
| E2F_TARGETS | 3455.77 | |
| EPITHELIAL_MESENCHYMAL_TRANSITION | 1651.19 | |
| ESTROGEN_RESPONSE_EARLY | 2705.02 | |
| ESTROGEN_RESPONSE_LATE | 2652.04 | |
| FATTY_ACID_METABOLISM | 949.90 | |
| G2M_CHECKPOINT | 4026.00 | |
| GLYCOLYSIS | 2663.18 | |
| HEDGEHOG_SIGNALING | 773.84 | |
| HEME_METABOLISM | 1766.03 | |
| HYPOXIA | 3485.82 | |
| IL2_STAT5_SIGNALING | 3324.22 | |
| IL6_JAK_STAT3_SIGNALING | 6902.58 | |
| INFLAMMATORY_RESPONSE | 5227.25 | |
| INTERFERON_ALPHA_RESPONSE | 916.09 | |
| INTERFERON_GAMMA_RESPONSE | 7138.96 | |
| KRAS_SIGNALING_DN | 907.69 | |
| KRAS_SIGNALING_UP | 3380.41 | |
| MITOTIC_SPINDLE | 5689.90 | |
| MTORC1_SIGNALING | 3664.44 | |
| MYC_TARGETS_V1 | 2622.89 | |
| MYC_TARGETS_V2 | 832.59 | |
| MYOGENESIS | 2731.68 | |
| NOTCH_SIGNALING | 98.60 | |
| OXIDATIVE_PHOSPHORYLATION | 1450.01 | |
| P53_PATHWAY | 2999.58 | |
| PANCREAS_BETA_CELLS | 165.93 | |
| PEROXISOME | 1085.73 | |
| PI3K_AKT_MTOR_SIGNALING | 9342.75 | |
| PROTEIN_SECRETION | 1677.02 | |
| REACTIVE_OXYGEN_SPECIES_PATHWAY | 473.34 | |
| SPERMATOGENESIS | 1420.84 | |
| TGF_BETA_SIGNALING | 1634.21 | |
| TNFA_SIGNALING_VIA_NFKB | 4033.59 | |
| UNFOLDED_PROTEIN_RESPONSE | 1393.21 | |
| UV_RESPONSE_DN | 4527.23 | |
| UV_RESPONSE_UP | 3405.42 | |
| WNT_BETA_CATENIN_SIGNALING | 1425.61 | |
| XENOBIOTIC_METABOLISM | 2171.96 |
Hallmarks-of-Cancer reach
Anti-tumor matches — the "ideal patient" search
| Sample | Cancer type | cos to ideal |
|---|---|---|
| EPT0291 | EPN | 0.818 |
| SRR23303752 | — | 0.818 |
| SRR10899984 | — | 0.817 |
| TCGA-FD-A43X-01A-11R-A23W-07 | — | 0.807 |
| TCGA-CF-A5U8-01A-11R-A28M-07 | — | 0.803 |
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