Pexidartinib
Sign in to save this workspacePrimary targets: FMS · FDA status: FDA Approved
Selectivity scorecard
KISS
99.49
Gini
0.631
CATDS
0.029
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 Pexidartinib. Strongest target: FMS at 97.5% inhibition.
Accessible data table
| Rank | Target | Inhibition % | Residual activity % |
|---|---|---|---|
| 1 | FMS | 97.5% | 2.5% |
| 2 | C_KIT | 95.2% | 4.8% |
| 3 | AURORA_B | 80.3% | 19.7% |
| 4 | FLT3 | 79.3% | 20.7% |
| 5 | DDR2 | 63.2% | 36.8% |
| 6 | RET | 62.9% | 37.1% |
| 7 | PDGFRB | 62.4% | 37.6% |
| 8 | DDR1 | 60.0% | 40.0% |
| 9 | LCK | 51.9% | 48.1% |
| 10 | TRKC | 46.5% | 53.5% |
| 11 | AURORA_A | 43.9% | 56.1% |
| 12 | LRRK2 | 40.4% | 59.6% |
| 13 | FGFR2 | 39.9% | 60.1% |
| 14 | TRKB | 36.7% | 63.3% |
| 15 | RIPK4 | 35.5% | 64.5% |
| 16 | MUSK | 35.1% | 64.9% |
| 17 | LKB1 | 34.4% | 65.6% |
| 18 | MLK2_MAP3K10 | 34.3% | 65.7% |
| 19 | MAK | 31.7% | 68.3% |
| 20 | FGFR1 | 30.2% | 69.8% |
Selectivity landscape
Where Pexidartinib sits in the 92-drug selectivity landscape (KISS vs Gini). The highlighted point is Pexidartinib.
Atlas insights for Pexidartinib
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 | 1078.02 | |
| ALLOGRAFT_REJECTION | 2486.27 | |
| ANDROGEN_RESPONSE | 617.63 | |
| ANGIOGENESIS | 566.43 | |
| APICAL_JUNCTION | 3241.38 | |
| APICAL_SURFACE | 346.37 | |
| APOPTOSIS | 2520.24 | |
| BILE_ACID_METABOLISM | 403.50 | |
| CHOLESTEROL_HOMEOSTASIS | 488.42 | |
| COAGULATION | 378.01 | |
| COMPLEMENT | 1655.49 | |
| DNA_REPAIR | 571.02 | |
| E2F_TARGETS | 1800.76 | |
| EPITHELIAL_MESENCHYMAL_TRANSITION | 740.83 | |
| ESTROGEN_RESPONSE_EARLY | 1214.54 | |
| ESTROGEN_RESPONSE_LATE | 1269.39 | |
| FATTY_ACID_METABOLISM | 371.06 | |
| G2M_CHECKPOINT | 1859.90 | |
| GLYCOLYSIS | 1079.90 | |
| HEDGEHOG_SIGNALING | 351.25 | |
| HEME_METABOLISM | 777.02 | |
| HYPOXIA | 1539.77 | |
| IL2_STAT5_SIGNALING | 988.17 | |
| IL6_JAK_STAT3_SIGNALING | 1760.46 | |
| INFLAMMATORY_RESPONSE | 1538.26 | |
| INTERFERON_ALPHA_RESPONSE | 254.76 | |
| INTERFERON_GAMMA_RESPONSE | 2056.33 | |
| KRAS_SIGNALING_DN | 299.05 | |
| KRAS_SIGNALING_UP | 1152.46 | |
| MITOTIC_SPINDLE | 2279.43 | |
| MTORC1_SIGNALING | 1445.03 | |
| MYC_TARGETS_V1 | 1239.14 | |
| MYC_TARGETS_V2 | 239.39 | |
| MYOGENESIS | 1218.32 | |
| NOTCH_SIGNALING | 123.00 | |
| OXIDATIVE_PHOSPHORYLATION | 775.21 | |
| P53_PATHWAY | 1256.42 | |
| PANCREAS_BETA_CELLS | 163.22 | |
| PEROXISOME | 533.35 | |
| PI3K_AKT_MTOR_SIGNALING | 3307.01 | |
| PROTEIN_SECRETION | 722.16 | |
| REACTIVE_OXYGEN_SPECIES_PATHWAY | 141.57 | |
| SPERMATOGENESIS | 567.81 | |
| TGF_BETA_SIGNALING | 734.07 | |
| TNFA_SIGNALING_VIA_NFKB | 1742.10 | |
| UNFOLDED_PROTEIN_RESPONSE | 664.49 | |
| UV_RESPONSE_DN | 1664.43 | |
| UV_RESPONSE_UP | 1243.73 | |
| WNT_BETA_CATENIN_SIGNALING | 756.10 | |
| XENOBIOTIC_METABOLISM | 756.57 |
Hallmarks-of-Cancer reach
Anti-tumor matches — the "ideal patient" search
| Sample | Cancer type | cos to ideal |
|---|---|---|
| EPT0291 | EPN | 0.854 |
| SRR23303752 | — | 0.848 |
| aMVAC.P_005_TURBT_S223 | — | 0.831 |
| SRR12202498 | — | 0.829 |
| TCGA-CF-A5U8-01A-11R-A28M-07 | — | 0.829 |
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