Selumetinib
Sign in to save this workspacePrimary targets: MEK1, MEK2 · FDA status: FDA Approved
Selectivity scorecard
KISS
100.00
Gini
0.640
CATDS
0.032
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 Selumetinib. Strongest target: MEK1 at 54.4% inhibition.
Accessible data table
| Rank | Target | Inhibition % | Residual activity % |
|---|---|---|---|
| 1 | MEK1 | 54.4% | 45.6% |
| 2 | MEK2 | 33.0% | 67.0% |
| 3 | SYK | 29.1% | 70.9% |
| 4 | MEKK3 | 26.3% | 73.7% |
| 5 | CK1A1 | 25.8% | 74.2% |
| 6 | AKT3 | 25.5% | 74.5% |
| 7 | ERK1 | 24.5% | 75.5% |
| 8 | STK33 | 22.7% | 77.3% |
| 9 | PRKX | 20.0% | 80.0% |
| 10 | CDK17_CYCLIN_Y(PCTK2) | 18.6% | 81.4% |
| 11 | ALK4_ACVR1B | 17.9% | 82.1% |
| 12 | GLK_MAP4K3 | 17.2% | 82.8% |
| 13 | TYRO3_SKY | 17.1% | 82.9% |
| 14 | CDK1_CYCLIN_A | 16.0% | 84.0% |
| 15 | MEKK6 | 15.9% | 84.1% |
| 16 | NEK9 | 15.7% | 84.3% |
| 17 | EPHA6 | 15.7% | 84.3% |
| 18 | RAF1 | 15.3% | 84.7% |
| 19 | AURORA_A | 15.3% | 84.7% |
| 20 | RIPK4 | 14.2% | 85.8% |
Selectivity landscape
Where Selumetinib sits in the 92-drug selectivity landscape (KISS vs Gini). The highlighted point is Selumetinib.
Atlas insights for Selumetinib
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 | 428.83 | |
| ALLOGRAFT_REJECTION | 856.94 | |
| ANDROGEN_RESPONSE | 313.16 | |
| ANGIOGENESIS | 106.15 | |
| APICAL_JUNCTION | 959.65 | |
| APICAL_SURFACE | 118.35 | |
| APOPTOSIS | 1027.53 | |
| BILE_ACID_METABOLISM | 147.19 | |
| CHOLESTEROL_HOMEOSTASIS | 114.72 | |
| COAGULATION | 224.93 | |
| COMPLEMENT | 657.33 | |
| DNA_REPAIR | 258.11 | |
| E2F_TARGETS | 946.78 | |
| EPITHELIAL_MESENCHYMAL_TRANSITION | 363.31 | |
| ESTROGEN_RESPONSE_EARLY | 552.03 | |
| ESTROGEN_RESPONSE_LATE | 438.97 | |
| FATTY_ACID_METABOLISM | 76.74 | |
| G2M_CHECKPOINT | 822.96 | |
| GLYCOLYSIS | 403.27 | |
| HEDGEHOG_SIGNALING | 66.71 | |
| HEME_METABOLISM | 480.52 | |
| HYPOXIA | 613.88 | |
| IL2_STAT5_SIGNALING | 416.73 | |
| IL6_JAK_STAT3_SIGNALING | 608.59 | |
| INFLAMMATORY_RESPONSE | 818.24 | |
| INTERFERON_ALPHA_RESPONSE | 128.43 | |
| INTERFERON_GAMMA_RESPONSE | 810.90 | |
| KRAS_SIGNALING_DN | 182.79 | |
| KRAS_SIGNALING_UP | 459.89 | |
| MITOTIC_SPINDLE | 836.35 | |
| MTORC1_SIGNALING | 607.91 | |
| MYC_TARGETS_V1 | 684.09 | |
| MYC_TARGETS_V2 | 226.01 | |
| MYOGENESIS | 525.66 | |
| NOTCH_SIGNALING | 94.70 | |
| OXIDATIVE_PHOSPHORYLATION | 159.92 | |
| P53_PATHWAY | 608.03 | |
| PANCREAS_BETA_CELLS | 124.26 | |
| PEROXISOME | 155.10 | |
| PI3K_AKT_MTOR_SIGNALING | 1220.57 | |
| PROTEIN_SECRETION | 183.54 | |
| REACTIVE_OXYGEN_SPECIES_PATHWAY | 59.56 | |
| SPERMATOGENESIS | 415.20 | |
| TGF_BETA_SIGNALING | 342.89 | |
| TNFA_SIGNALING_VIA_NFKB | 869.01 | |
| UNFOLDED_PROTEIN_RESPONSE | 317.38 | |
| UV_RESPONSE_DN | 631.97 | |
| UV_RESPONSE_UP | 463.85 | |
| WNT_BETA_CATENIN_SIGNALING | 317.57 | |
| XENOBIOTIC_METABOLISM | 257.27 |
Hallmarks-of-Cancer reach
Anti-tumor matches — the "ideal patient" search
| Sample | Cancer type | cos to ideal |
|---|---|---|
| EPT0291 | EPN | 0.872 |
| TCGA-CF-A5U8-01A-11R-A28M-07 | — | 0.857 |
| SRR12202498 | — | 0.847 |
| SRR1443713 | GTEX | 0.847 |
| SRR23303752 | — | 0.844 |
Annotations
Sign in to read and post annotations.
Loading…