Selpercatinib
Sign in to save this workspacePrimary targets: RET · FDA status: FDA Approved
Selectivity scorecard
KISS
96.72
Gini
0.635
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 Selpercatinib. Strongest target: RET at 100.0% inhibition.
Accessible data table
| Rank | Target | Inhibition % | Residual activity % |
|---|---|---|---|
| 1 | RET | 100.0% | 0.0% |
| 2 | FLT4_VEGFR3 | 98.9% | 1.1% |
| 3 | C_KIT | 98.7% | 1.3% |
| 4 | FLT1_VEGFR1 | 96.2% | 3.8% |
| 5 | FLT3 | 96.1% | 3.9% |
| 6 | KDR_VEGFR2 | 95.9% | 4.1% |
| 7 | FGFR2 | 95.0% | 5.0% |
| 8 | JAK2 | 93.8% | 6.2% |
| 9 | EPHB1 | 93.6% | 6.4% |
| 10 | EPHA6 | 93.0% | 7.0% |
| 11 | FMS | 92.8% | 7.2% |
| 12 | DDR2 | 92.2% | 7.8% |
| 13 | AURORA_C | 90.4% | 9.6% |
| 14 | PLK4_SAK | 89.2% | 10.8% |
| 15 | FGFR1 | 87.4% | 12.6% |
| 16 | LCK | 87.3% | 12.7% |
| 17 | FGFR3 | 86.6% | 13.4% |
| 18 | LYN | 86.4% | 13.6% |
| 19 | CHK2 | 86.3% | 13.7% |
| 20 | AURORA_B | 86.1% | 13.9% |
Selectivity landscape
Where Selpercatinib sits in the 92-drug selectivity landscape (KISS vs Gini). The highlighted point is Selpercatinib.
Atlas insights for Selpercatinib
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 | 2785.31 | |
| ALLOGRAFT_REJECTION | 8179.99 | |
| ANDROGEN_RESPONSE | 1574.36 | |
| ANGIOGENESIS | 1414.60 | |
| APICAL_JUNCTION | 8730.56 | |
| APICAL_SURFACE | 861.56 | |
| APOPTOSIS | 6494.21 | |
| BILE_ACID_METABOLISM | 882.64 | |
| CHOLESTEROL_HOMEOSTASIS | 1041.86 | |
| COAGULATION | 1138.60 | |
| COMPLEMENT | 4804.29 | |
| DNA_REPAIR | 1835.53 | |
| E2F_TARGETS | 4349.33 | |
| EPITHELIAL_MESENCHYMAL_TRANSITION | 1807.27 | |
| ESTROGEN_RESPONSE_EARLY | 2836.51 | |
| ESTROGEN_RESPONSE_LATE | 3172.24 | |
| FATTY_ACID_METABOLISM | 887.94 | |
| G2M_CHECKPOINT | 4735.17 | |
| GLYCOLYSIS | 2743.76 | |
| HEDGEHOG_SIGNALING | 1093.11 | |
| HEME_METABOLISM | 2214.39 | |
| HYPOXIA | 4141.03 | |
| IL2_STAT5_SIGNALING | 3126.65 | |
| IL6_JAK_STAT3_SIGNALING | 5809.79 | |
| INFLAMMATORY_RESPONSE | 4404.01 | |
| INTERFERON_ALPHA_RESPONSE | 757.65 | |
| INTERFERON_GAMMA_RESPONSE | 6280.04 | |
| KRAS_SIGNALING_DN | 670.28 | |
| KRAS_SIGNALING_UP | 3181.05 | |
| MITOTIC_SPINDLE | 5660.25 | |
| MTORC1_SIGNALING | 3666.55 | |
| MYC_TARGETS_V1 | 2919.59 | |
| MYC_TARGETS_V2 | 620.72 | |
| MYOGENESIS | 2791.32 | |
| NOTCH_SIGNALING | 259.13 | |
| OXIDATIVE_PHOSPHORYLATION | 1521.45 | |
| P53_PATHWAY | 3543.54 | |
| PANCREAS_BETA_CELLS | 434.07 | |
| PEROXISOME | 1088.23 | |
| PI3K_AKT_MTOR_SIGNALING | 9011.44 | |
| PROTEIN_SECRETION | 1776.13 | |
| REACTIVE_OXYGEN_SPECIES_PATHWAY | 513.63 | |
| SPERMATOGENESIS | 1403.29 | |
| TGF_BETA_SIGNALING | 2010.50 | |
| TNFA_SIGNALING_VIA_NFKB | 4462.51 | |
| UNFOLDED_PROTEIN_RESPONSE | 1365.51 | |
| UV_RESPONSE_DN | 4630.46 | |
| UV_RESPONSE_UP | 3087.00 | |
| WNT_BETA_CATENIN_SIGNALING | 1746.30 | |
| XENOBIOTIC_METABOLISM | 1725.22 |
Hallmarks-of-Cancer reach
Anti-tumor matches — the "ideal patient" search
| Sample | Cancer type | cos to ideal |
|---|---|---|
| EPT0291 | EPN | 0.842 |
| SRR23303752 | — | 0.837 |
| SRR10899984 | — | 0.826 |
| aMVAC.P_005_TURBT_S223 | — | 0.825 |
| TCGA-CF-A5U8-01A-11R-A28M-07 | — | 0.824 |
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