Tepotinib
Sign in to save this workspacePrimary targets: C_MET · FDA status: FDA Approved
Selectivity scorecard
KISS
99.75
Gini
0.727
CATDS
0.042
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 Tepotinib. Strongest target: C_MET at 95.2% inhibition.
Accessible data table
| Rank | Target | Inhibition % | Residual activity % |
|---|---|---|---|
| 1 | C_MET | 95.2% | 4.8% |
| 2 | TRKC | 86.2% | 13.8% |
| 3 | IRAK4 | 72.7% | 27.3% |
| 4 | IRAK1 | 72.6% | 27.4% |
| 5 | FGFR2 | 72.6% | 27.4% |
| 6 | AXL | 69.6% | 30.4% |
| 7 | FGFR1 | 62.3% | 37.7% |
| 8 | MELK | 50.4% | 49.6% |
| 9 | FGFR3 | 49.8% | 50.2% |
| 10 | FGFR4 | 49.2% | 50.8% |
| 11 | TRKB | 33.1% | 66.9% |
| 12 | STK39_STLK3 | 30.5% | 69.5% |
| 13 | FLT4_VEGFR3 | 28.5% | 71.5% |
| 14 | FLT1_VEGFR1 | 28.2% | 71.8% |
| 15 | BMPR2 | 25.1% | 74.9% |
| 16 | ALK | 24.9% | 75.1% |
| 17 | LYN | 24.9% | 75.1% |
| 18 | CAMK1G | 23.4% | 76.6% |
| 19 | LCK | 19.9% | 80.1% |
| 20 | GSK3B | 18.7% | 81.3% |
Selectivity landscape
Where Tepotinib sits in the 92-drug selectivity landscape (KISS vs Gini). The highlighted point is Tepotinib.
Atlas insights for Tepotinib
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 | 737.96 | |
| ALLOGRAFT_REJECTION | 1938.38 | |
| ANDROGEN_RESPONSE | 682.09 | |
| ANGIOGENESIS | 314.24 | |
| APICAL_JUNCTION | 2189.69 | |
| APICAL_SURFACE | 222.84 | |
| APOPTOSIS | 2110.72 | |
| BILE_ACID_METABOLISM | 295.92 | |
| CHOLESTEROL_HOMEOSTASIS | 327.49 | |
| COAGULATION | 235.70 | |
| COMPLEMENT | 1275.25 | |
| DNA_REPAIR | 701.15 | |
| E2F_TARGETS | 1823.46 | |
| EPITHELIAL_MESENCHYMAL_TRANSITION | 521.96 | |
| ESTROGEN_RESPONSE_EARLY | 841.90 | |
| ESTROGEN_RESPONSE_LATE | 905.18 | |
| FATTY_ACID_METABOLISM | 310.95 | |
| G2M_CHECKPOINT | 1885.24 | |
| GLYCOLYSIS | 912.22 | |
| HEDGEHOG_SIGNALING | 133.01 | |
| HEME_METABOLISM | 639.29 | |
| HYPOXIA | 1214.53 | |
| IL2_STAT5_SIGNALING | 816.55 | |
| IL6_JAK_STAT3_SIGNALING | 1532.50 | |
| INFLAMMATORY_RESPONSE | 1138.22 | |
| INTERFERON_ALPHA_RESPONSE | 201.58 | |
| INTERFERON_GAMMA_RESPONSE | 1821.90 | |
| KRAS_SIGNALING_DN | 248.18 | |
| KRAS_SIGNALING_UP | 732.25 | |
| MITOTIC_SPINDLE | 1606.16 | |
| MTORC1_SIGNALING | 1130.81 | |
| MYC_TARGETS_V1 | 1163.26 | |
| MYC_TARGETS_V2 | 281.03 | |
| MYOGENESIS | 858.63 | |
| NOTCH_SIGNALING | 91.90 | |
| OXIDATIVE_PHOSPHORYLATION | 561.40 | |
| P53_PATHWAY | 1211.04 | |
| PANCREAS_BETA_CELLS | 146.10 | |
| PEROXISOME | 372.77 | |
| PI3K_AKT_MTOR_SIGNALING | 2803.44 | |
| PROTEIN_SECRETION | 549.46 | |
| REACTIVE_OXYGEN_SPECIES_PATHWAY | 178.27 | |
| SPERMATOGENESIS | 427.03 | |
| TGF_BETA_SIGNALING | 829.05 | |
| TNFA_SIGNALING_VIA_NFKB | 1398.94 | |
| UNFOLDED_PROTEIN_RESPONSE | 391.70 | |
| UV_RESPONSE_DN | 1451.33 | |
| UV_RESPONSE_UP | 854.74 | |
| WNT_BETA_CATENIN_SIGNALING | 688.12 | |
| XENOBIOTIC_METABOLISM | 510.18 |
Anti-tumor matches — the "ideal patient" search
| Sample | Cancer type | cos to ideal |
|---|---|---|
| EPT0291 | EPN | 0.859 |
| TCGA-CF-A5U8-01A-11R-A28M-07 | — | 0.835 |
| SRR12202498 | — | 0.832 |
| SRR1443713 | GTEX | 0.832 |
| aMVAC.P_005_TURBT_S223 | — | 0.832 |
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