Gilteritinib
Sign in to save this workspacePrimary targets: FLT3 · FDA status: FDA Approved
Selectivity scorecard
KISS
88.97
Gini
0.506
CATDS
0.007
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 Gilteritinib. Strongest target: RET at 100.0% inhibition.
Accessible data table
| Rank | Target | Inhibition % | Residual activity % |
|---|---|---|---|
| 1 | RET | 100.0% | 0.0% |
| 2 | TYK1_LTK | 99.7% | 0.3% |
| 3 | ROS_ROS1 | 99.6% | 0.4% |
| 4 | ALK | 99.5% | 0.5% |
| 5 | FLT3 | 99.2% | 0.8% |
| 6 | TRKC | 99.0% | 1.0% |
| 7 | TNIK | 98.8% | 1.2% |
| 8 | AXL | 98.7% | 1.3% |
| 9 | FLT4_VEGFR3 | 98.5% | 1.5% |
| 10 | C_MER | 98.4% | 1.6% |
| 11 | LOK_STK10 | 98.3% | 1.7% |
| 12 | MLK3_MAP3K11 | 97.4% | 2.6% |
| 13 | LRRK2 | 97.2% | 2.8% |
| 14 | STK22D_TSSK1 | 96.8% | 3.2% |
| 15 | DDR2 | 96.7% | 3.3% |
| 16 | BRK | 96.6% | 3.4% |
| 17 | HPK1_MAP4K1 | 96.6% | 3.4% |
| 18 | FGR | 95.8% | 4.2% |
| 19 | DDR1 | 95.7% | 4.3% |
| 20 | MINK_MINK1 | 95.7% | 4.3% |
Selectivity landscape
Where Gilteritinib sits in the 92-drug selectivity landscape (KISS vs Gini). The highlighted point is Gilteritinib.
Atlas insights for Gilteritinib
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 | 3664.21 | |
| ALLOGRAFT_REJECTION | 13029.26 | |
| ANDROGEN_RESPONSE | 2998.28 | |
| ANGIOGENESIS | 2332.46 | |
| APICAL_JUNCTION | 13769.90 | |
| APICAL_SURFACE | 1361.08 | |
| APOPTOSIS | 9591.22 | |
| BILE_ACID_METABOLISM | 1394.29 | |
| CHOLESTEROL_HOMEOSTASIS | 1894.57 | |
| COAGULATION | 1534.25 | |
| COMPLEMENT | 7813.82 | |
| DNA_REPAIR | 2783.93 | |
| E2F_TARGETS | 6803.45 | |
| EPITHELIAL_MESENCHYMAL_TRANSITION | 3241.14 | |
| ESTROGEN_RESPONSE_EARLY | 4856.85 | |
| ESTROGEN_RESPONSE_LATE | 4486.52 | |
| FATTY_ACID_METABOLISM | 1127.12 | |
| G2M_CHECKPOINT | 6729.63 | |
| GLYCOLYSIS | 4128.09 | |
| HEDGEHOG_SIGNALING | 1630.81 | |
| HEME_METABOLISM | 2832.71 | |
| HYPOXIA | 5607.72 | |
| IL2_STAT5_SIGNALING | 4227.49 | |
| IL6_JAK_STAT3_SIGNALING | 7985.80 | |
| INFLAMMATORY_RESPONSE | 7288.40 | |
| INTERFERON_ALPHA_RESPONSE | 1106.85 | |
| INTERFERON_GAMMA_RESPONSE | 9390.61 | |
| KRAS_SIGNALING_DN | 1603.41 | |
| KRAS_SIGNALING_UP | 5046.30 | |
| MITOTIC_SPINDLE | 9082.70 | |
| MTORC1_SIGNALING | 5331.62 | |
| MYC_TARGETS_V1 | 4706.14 | |
| MYC_TARGETS_V2 | 1126.54 | |
| MYOGENESIS | 4608.98 | |
| NOTCH_SIGNALING | 461.88 | |
| OXIDATIVE_PHOSPHORYLATION | 1848.69 | |
| P53_PATHWAY | 4949.87 | |
| PANCREAS_BETA_CELLS | 415.18 | |
| PEROXISOME | 1623.67 | |
| PI3K_AKT_MTOR_SIGNALING | 12612.95 | |
| PROTEIN_SECRETION | 2965.66 | |
| REACTIVE_OXYGEN_SPECIES_PATHWAY | 687.17 | |
| SPERMATOGENESIS | 2155.71 | |
| TGF_BETA_SIGNALING | 2757.18 | |
| TNFA_SIGNALING_VIA_NFKB | 6240.22 | |
| UNFOLDED_PROTEIN_RESPONSE | 2406.31 | |
| UV_RESPONSE_DN | 7197.65 | |
| UV_RESPONSE_UP | 5589.43 | |
| WNT_BETA_CATENIN_SIGNALING | 3129.95 | |
| XENOBIOTIC_METABOLISM | 2949.66 |
Hallmarks-of-Cancer reach
Anti-tumor matches — the "ideal patient" search
| Sample | Cancer type | cos to ideal |
|---|---|---|
| EPT0291 | EPN | 0.844 |
| SRR23303752 | — | 0.837 |
| TCGA-CF-A5U8-01A-11R-A28M-07 | — | 0.830 |
| aMVAC.P_005_TURBT_S223 | — | 0.826 |
| SRR10899984 | — | 0.824 |
Annotations
Sign in to read and post annotations.
Loading…