Trametinib
Sign in to save this workspacePrimary targets: MEK1, MEK2 · FDA status: FDA Approved
Selectivity scorecard
KISS
99.50
Gini
0.718
CATDS
0.056
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 Trametinib. Strongest target: MEK1 at 98.7% inhibition.
Accessible data table
| Rank | Target | Inhibition % | Residual activity % |
|---|---|---|---|
| 1 | MEK1 | 98.7% | 1.3% |
| 2 | MEK2 | 93.1% | 6.9% |
| 3 | PDK2_PDHK2 | 40.0% | 60.0% |
| 4 | CAMKK2 | 36.6% | 63.4% |
| 5 | PKG2_PRKG2 | 25.7% | 74.3% |
| 6 | ITK | 24.4% | 75.6% |
| 7 | COT1_MAP3K8 | 24.1% | 75.9% |
| 8 | CDK6_CYCLIN_D3 | 23.3% | 76.7% |
| 9 | MUSK | 22.8% | 77.2% |
| 10 | GSK3A | 21.5% | 78.5% |
| 11 | AURORA_C | 20.4% | 79.6% |
| 12 | TTBK2 | 20.1% | 79.9% |
| 13 | LYN | 19.0% | 81.0% |
| 14 | PHKG2 | 18.4% | 81.6% |
| 15 | CK1D | 18.4% | 81.6% |
| 16 | STK39_STLK3 | 18.0% | 82.0% |
| 17 | PLK3 | 17.6% | 82.4% |
| 18 | P38A_MAPK14 | 17.3% | 82.7% |
| 19 | MEKK3 | 17.2% | 82.8% |
| 20 | EPHA4 | 16.5% | 83.5% |
Selectivity landscape
Where Trametinib sits in the 92-drug selectivity landscape (KISS vs Gini). The highlighted point is Trametinib.
Atlas insights for Trametinib
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 | 349.52 | |
| ALLOGRAFT_REJECTION | 1114.86 | |
| ANDROGEN_RESPONSE | 418.09 | |
| ANGIOGENESIS | 174.48 | |
| APICAL_JUNCTION | 1176.64 | |
| APICAL_SURFACE | 89.22 | |
| APOPTOSIS | 1142.09 | |
| BILE_ACID_METABOLISM | 160.69 | |
| CHOLESTEROL_HOMEOSTASIS | 204.72 | |
| COAGULATION | 81.53 | |
| COMPLEMENT | 660.34 | |
| DNA_REPAIR | 339.64 | |
| E2F_TARGETS | 1059.56 | |
| EPITHELIAL_MESENCHYMAL_TRANSITION | 408.07 | |
| ESTROGEN_RESPONSE_EARLY | 541.59 | |
| ESTROGEN_RESPONSE_LATE | 508.54 | |
| FATTY_ACID_METABOLISM | 138.56 | |
| G2M_CHECKPOINT | 829.20 | |
| GLYCOLYSIS | 459.07 | |
| HEDGEHOG_SIGNALING | 133.67 | |
| HEME_METABOLISM | 275.15 | |
| HYPOXIA | 600.86 | |
| IL2_STAT5_SIGNALING | 446.68 | |
| IL6_JAK_STAT3_SIGNALING | 587.03 | |
| INFLAMMATORY_RESPONSE | 715.51 | |
| INTERFERON_ALPHA_RESPONSE | 125.61 | |
| INTERFERON_GAMMA_RESPONSE | 826.06 | |
| KRAS_SIGNALING_DN | 242.75 | |
| KRAS_SIGNALING_UP | 451.05 | |
| MITOTIC_SPINDLE | 879.73 | |
| MTORC1_SIGNALING | 510.10 | |
| MYC_TARGETS_V1 | 602.39 | |
| MYC_TARGETS_V2 | 171.67 | |
| MYOGENESIS | 550.14 | |
| NOTCH_SIGNALING | 111.95 | |
| OXIDATIVE_PHOSPHORYLATION | 130.97 | |
| P53_PATHWAY | 585.69 | |
| PANCREAS_BETA_CELLS | 43.27 | |
| PEROXISOME | 157.55 | |
| PI3K_AKT_MTOR_SIGNALING | 1292.05 | |
| PROTEIN_SECRETION | 276.99 | |
| REACTIVE_OXYGEN_SPECIES_PATHWAY | 39.48 | |
| SPERMATOGENESIS | 364.28 | |
| TGF_BETA_SIGNALING | 353.53 | |
| TNFA_SIGNALING_VIA_NFKB | 731.87 | |
| UNFOLDED_PROTEIN_RESPONSE | 220.04 | |
| UV_RESPONSE_DN | 622.37 | |
| UV_RESPONSE_UP | 520.71 | |
| WNT_BETA_CATENIN_SIGNALING | 534.04 | |
| XENOBIOTIC_METABOLISM | 262.45 |
Hallmarks-of-Cancer reach
Anti-tumor matches — the "ideal patient" search
| Sample | Cancer type | cos to ideal |
|---|---|---|
| EPT0291 | EPN | 0.865 |
| TCGA-CF-A5U8-01A-11R-A28M-07 | — | 0.852 |
| SRR12202498 | — | 0.832 |
| SRR23303752 | — | 0.829 |
| aMVAC.P_005_TURBT_S223 | — | 0.829 |
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