Pralsetinib
Sign in to save this workspacePrimary targets: RET · FDA status: FDA Approved
Selectivity scorecard
KISS
93.43
Gini
0.643
CATDS
0.011
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 Pralsetinib. Strongest target: RET at 100.0% inhibition.
Accessible data table
| Rank | Target | Inhibition % | Residual activity % |
|---|---|---|---|
| 1 | RET | 100.0% | 0.0% |
| 2 | ERBB4_HER4 | 99.7% | 0.3% |
| 3 | TRKC | 99.4% | 0.6% |
| 4 | TRKB | 99.4% | 0.6% |
| 5 | EGFR | 99.1% | 0.9% |
| 6 | JAK1 | 99.1% | 0.9% |
| 7 | JAK2 | 99.1% | 0.9% |
| 8 | TRKA | 98.7% | 1.3% |
| 9 | JAK3 | 98.1% | 1.9% |
| 10 | FLT3 | 97.6% | 2.4% |
| 11 | ERBB2_HER2 | 97.5% | 2.5% |
| 12 | ROS_ROS1 | 97.3% | 2.7% |
| 13 | DDR1 | 96.9% | 3.1% |
| 14 | TYK2 | 96.8% | 3.2% |
| 15 | MLK3_MAP3K11 | 96.5% | 3.5% |
| 16 | FLT4_VEGFR3 | 96.5% | 3.5% |
| 17 | LIMK1 | 96.4% | 3.6% |
| 18 | BLK | 96.1% | 3.9% |
| 19 | DDR2 | 95.9% | 4.1% |
| 20 | C_KIT | 93.8% | 6.2% |
Selectivity landscape
Where Pralsetinib sits in the 92-drug selectivity landscape (KISS vs Gini). The highlighted point is Pralsetinib.
Atlas insights for Pralsetinib
Pathway-space view of what this drug actually does, drawn from the Pathway Atlas.
On-target vs off-target shadow
On-target1%
Off-target99%
Ghost (2nd-order)0%
| Pathway | Composition | Total |Π| |
|---|---|---|
| ADIPOGENESIS | 3617.60 | |
| ALLOGRAFT_REJECTION | 10878.12 | |
| ANDROGEN_RESPONSE | 2594.93 | |
| ANGIOGENESIS | 1755.61 | |
| APICAL_JUNCTION | 11094.57 | |
| APICAL_SURFACE | 1090.24 | |
| APOPTOSIS | 7953.98 | |
| BILE_ACID_METABOLISM | 1078.77 | |
| CHOLESTEROL_HOMEOSTASIS | 1737.81 | |
| COAGULATION | 1300.49 | |
| COMPLEMENT | 6585.18 | |
| DNA_REPAIR | 2305.52 | |
| E2F_TARGETS | 5462.02 | |
| EPITHELIAL_MESENCHYMAL_TRANSITION | 2732.20 | |
| ESTROGEN_RESPONSE_EARLY | 3580.18 | |
| ESTROGEN_RESPONSE_LATE | 3488.19 | |
| FATTY_ACID_METABOLISM | 1139.76 | |
| G2M_CHECKPOINT | 5892.44 | |
| GLYCOLYSIS | 3187.60 | |
| HEDGEHOG_SIGNALING | 1003.38 | |
| HEME_METABOLISM | 2613.11 | |
| HYPOXIA | 4593.44 | |
| IL2_STAT5_SIGNALING | 4064.15 | |
| IL6_JAK_STAT3_SIGNALING | 8317.58 | |
| INFLAMMATORY_RESPONSE | 6604.15 | |
| INTERFERON_ALPHA_RESPONSE | 1256.38 | |
| INTERFERON_GAMMA_RESPONSE | 8788.05 | |
| KRAS_SIGNALING_DN | 945.16 | |
| KRAS_SIGNALING_UP | 4398.07 | |
| MITOTIC_SPINDLE | 7638.67 | |
| MTORC1_SIGNALING | 4372.69 | |
| MYC_TARGETS_V1 | 3895.39 | |
| MYC_TARGETS_V2 | 910.11 | |
| MYOGENESIS | 3489.46 | |
| NOTCH_SIGNALING | 359.35 | |
| OXIDATIVE_PHOSPHORYLATION | 1863.05 | |
| P53_PATHWAY | 4110.22 | |
| PANCREAS_BETA_CELLS | 372.74 | |
| PEROXISOME | 1487.22 | |
| PI3K_AKT_MTOR_SIGNALING | 11204.68 | |
| PROTEIN_SECRETION | 2255.39 | |
| REACTIVE_OXYGEN_SPECIES_PATHWAY | 710.62 | |
| SPERMATOGENESIS | 1788.71 | |
| TGF_BETA_SIGNALING | 2369.43 | |
| TNFA_SIGNALING_VIA_NFKB | 6133.14 | |
| UNFOLDED_PROTEIN_RESPONSE | 1812.68 | |
| UV_RESPONSE_DN | 5683.17 | |
| UV_RESPONSE_UP | 4081.25 | |
| WNT_BETA_CATENIN_SIGNALING | 2293.95 | |
| XENOBIOTIC_METABOLISM | 2249.07 |
Hallmarks-of-Cancer reach
Anti-tumor matches — the "ideal patient" search
| Sample | Cancer type | cos to ideal |
|---|---|---|
| EPT0291 | EPN | 0.847 |
| SRR23303752 | — | 0.840 |
| SRR10899984 | — | 0.836 |
| TCGA-CF-A5U8-01A-11R-A28M-07 | — | 0.833 |
| aMVAC.P_005_TURBT_S223 | — | 0.830 |
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