Tucatinib
Sign in to save this workspacePrimary targets: ERBB2_HER2 · FDA status: FDA Approved
Selectivity scorecard
KISS
99.75
Gini
0.652
CATDS
0.054
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 Tucatinib. Strongest target: JAK1 at 92.7% inhibition.
Accessible data table
| Rank | Target | Inhibition % | Residual activity % |
|---|---|---|---|
| 1 | JAK1 | 92.7% | 7.3% |
| 2 | RIPK4 | 36.0% | 64.0% |
| 3 | JAK2 | 33.6% | 66.4% |
| 4 | TYK2 | 29.5% | 70.5% |
| 5 | AURORA_A | 28.4% | 71.6% |
| 6 | STK38_NDR1 | 20.5% | 79.5% |
| 7 | COT1_MAP3K8 | 18.9% | 81.1% |
| 8 | CDK1_CYCLIN_E | 17.7% | 82.3% |
| 9 | MEKK6 | 17.6% | 82.4% |
| 10 | PKCIOTA | 17.3% | 82.7% |
| 11 | WNK3 | 17.2% | 82.8% |
| 12 | TRKB | 16.4% | 83.6% |
| 13 | CDK4_CYCLIN_D1 | 16.4% | 83.6% |
| 14 | CDK4_CYCLIN_D3 | 15.6% | 84.4% |
| 15 | LRRK2 | 15.0% | 85.0% |
| 16 | TAOK3_JIK | 14.8% | 85.2% |
| 17 | FAK_PTK2 | 14.6% | 85.4% |
| 18 | CDK1_CYCLIN_B | 14.3% | 85.7% |
| 19 | CAMK4 | 14.1% | 85.9% |
| 20 | AURORA_B | 13.7% | 86.3% |
Selectivity landscape
Where Tucatinib sits in the 92-drug selectivity landscape (KISS vs Gini). The highlighted point is Tucatinib.
Atlas insights for Tucatinib
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 | 664.16 | |
| ALLOGRAFT_REJECTION | 1655.75 | |
| ANDROGEN_RESPONSE | 282.49 | |
| ANGIOGENESIS | 157.30 | |
| APICAL_JUNCTION | 1328.70 | |
| APICAL_SURFACE | 226.76 | |
| APOPTOSIS | 1353.80 | |
| BILE_ACID_METABOLISM | 131.97 | |
| CHOLESTEROL_HOMEOSTASIS | 131.40 | |
| COAGULATION | 137.52 | |
| COMPLEMENT | 867.13 | |
| DNA_REPAIR | 317.71 | |
| E2F_TARGETS | 1107.69 | |
| EPITHELIAL_MESENCHYMAL_TRANSITION | 369.72 | |
| ESTROGEN_RESPONSE_EARLY | 752.95 | |
| ESTROGEN_RESPONSE_LATE | 682.10 | |
| FATTY_ACID_METABOLISM | 119.03 | |
| G2M_CHECKPOINT | 1080.11 | |
| GLYCOLYSIS | 460.30 | |
| HEDGEHOG_SIGNALING | 80.74 | |
| HEME_METABOLISM | 500.33 | |
| HYPOXIA | 770.76 | |
| IL2_STAT5_SIGNALING | 975.34 | |
| IL6_JAK_STAT3_SIGNALING | 1857.53 | |
| INFLAMMATORY_RESPONSE | 1429.49 | |
| INTERFERON_ALPHA_RESPONSE | 340.98 | |
| INTERFERON_GAMMA_RESPONSE | 1862.29 | |
| KRAS_SIGNALING_DN | 185.12 | |
| KRAS_SIGNALING_UP | 650.38 | |
| MITOTIC_SPINDLE | 955.95 | |
| MTORC1_SIGNALING | 628.03 | |
| MYC_TARGETS_V1 | 741.47 | |
| MYC_TARGETS_V2 | 185.54 | |
| MYOGENESIS | 709.02 | |
| NOTCH_SIGNALING | 70.40 | |
| OXIDATIVE_PHOSPHORYLATION | 177.46 | |
| P53_PATHWAY | 776.27 | |
| PANCREAS_BETA_CELLS | 80.33 | |
| PEROXISOME | 180.18 | |
| PI3K_AKT_MTOR_SIGNALING | 1738.77 | |
| PROTEIN_SECRETION | 335.65 | |
| REACTIVE_OXYGEN_SPECIES_PATHWAY | 91.04 | |
| SPERMATOGENESIS | 433.32 | |
| TGF_BETA_SIGNALING | 366.95 | |
| TNFA_SIGNALING_VIA_NFKB | 1238.69 | |
| UNFOLDED_PROTEIN_RESPONSE | 414.10 | |
| UV_RESPONSE_DN | 922.16 | |
| UV_RESPONSE_UP | 719.42 | |
| WNT_BETA_CATENIN_SIGNALING | 468.28 | |
| XENOBIOTIC_METABOLISM | 230.78 |
Hallmarks-of-Cancer reach
Anti-tumor matches — the "ideal patient" search
| Sample | Cancer type | cos to ideal |
|---|---|---|
| EPT0291 | EPN | 0.853 |
| TCGA-CF-A5U8-01A-11R-A28M-07 | — | 0.840 |
| TCGA-CV-7424-01A-11R-2081-07 | — | 0.838 |
| SRR10899984 | — | 0.838 |
| C3L-03726 | — | 0.835 |
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