Paxalisib
Sign in to save this workspacePrimary targets: PI3K, MTOR_FRAP1 · FDA status: FDA Phase III Trials to begin
Selectivity scorecard
KISS
99.75
Gini
0.609
CATDS
0.039
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 Paxalisib. Strongest target: CHK1 at 95.2% inhibition.
Accessible data table
| Rank | Target | Inhibition % | Residual activity % |
|---|---|---|---|
| 1 | CHK1 | 95.2% | 4.8% |
| 2 | MTOR_FRAP1 | 81.2% | 18.8% |
| 3 | RAF1 | 54.2% | 45.8% |
| 4 | MLK2_MAP3K10 | 46.7% | 53.3% |
| 5 | YES_YES1 | 42.8% | 57.2% |
| 6 | MLK3_MAP3K11 | 38.6% | 61.4% |
| 7 | CAMK2D | 35.8% | 64.2% |
| 8 | RSK3 | 34.1% | 65.9% |
| 9 | LCK | 29.5% | 70.5% |
| 10 | BTK | 27.1% | 72.9% |
| 11 | CDK3_CYCLIN_C | 26.6% | 73.4% |
| 12 | HCK | 26.0% | 74.0% |
| 13 | CAMK2A | 24.1% | 75.9% |
| 14 | PAK4 | 22.5% | 77.5% |
| 15 | SYK | 22.3% | 77.7% |
| 16 | FLT3 | 20.6% | 79.4% |
| 17 | BLK | 20.2% | 79.8% |
| 18 | FYN | 20.2% | 79.8% |
| 19 | TXK | 19.4% | 80.6% |
| 20 | FGR | 19.1% | 80.9% |
Selectivity landscape
Where Paxalisib sits in the 92-drug selectivity landscape (KISS vs Gini). The highlighted point is Paxalisib.
Atlas insights for Paxalisib
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 | 745.70 | |
| ALLOGRAFT_REJECTION | 2390.81 | |
| ANDROGEN_RESPONSE | 606.71 | |
| ANGIOGENESIS | 353.86 | |
| APICAL_JUNCTION | 2577.67 | |
| APICAL_SURFACE | 229.23 | |
| APOPTOSIS | 2057.03 | |
| BILE_ACID_METABOLISM | 244.06 | |
| CHOLESTEROL_HOMEOSTASIS | 189.79 | |
| COAGULATION | 292.51 | |
| COMPLEMENT | 1339.28 | |
| DNA_REPAIR | 480.73 | |
| E2F_TARGETS | 1541.35 | |
| EPITHELIAL_MESENCHYMAL_TRANSITION | 758.09 | |
| ESTROGEN_RESPONSE_EARLY | 1149.86 | |
| ESTROGEN_RESPONSE_LATE | 995.17 | |
| FATTY_ACID_METABOLISM | 169.10 | |
| G2M_CHECKPOINT | 1535.35 | |
| GLYCOLYSIS | 807.77 | |
| HEDGEHOG_SIGNALING | 229.55 | |
| HEME_METABOLISM | 734.20 | |
| HYPOXIA | 1028.06 | |
| IL2_STAT5_SIGNALING | 834.55 | |
| IL6_JAK_STAT3_SIGNALING | 1242.79 | |
| INFLAMMATORY_RESPONSE | 1543.51 | |
| INTERFERON_ALPHA_RESPONSE | 239.30 | |
| INTERFERON_GAMMA_RESPONSE | 1556.32 | |
| KRAS_SIGNALING_DN | 415.65 | |
| KRAS_SIGNALING_UP | 945.85 | |
| MITOTIC_SPINDLE | 1782.87 | |
| MTORC1_SIGNALING | 1201.41 | |
| MYC_TARGETS_V1 | 1025.64 | |
| MYC_TARGETS_V2 | 301.77 | |
| MYOGENESIS | 1044.22 | |
| NOTCH_SIGNALING | 96.72 | |
| OXIDATIVE_PHOSPHORYLATION | 271.91 | |
| P53_PATHWAY | 935.42 | |
| PANCREAS_BETA_CELLS | 97.96 | |
| PEROXISOME | 384.77 | |
| PI3K_AKT_MTOR_SIGNALING | 2468.76 | |
| PROTEIN_SECRETION | 617.96 | |
| REACTIVE_OXYGEN_SPECIES_PATHWAY | 159.59 | |
| SPERMATOGENESIS | 506.39 | |
| TGF_BETA_SIGNALING | 577.74 | |
| TNFA_SIGNALING_VIA_NFKB | 1515.64 | |
| UNFOLDED_PROTEIN_RESPONSE | 527.68 | |
| UV_RESPONSE_DN | 1433.89 | |
| UV_RESPONSE_UP | 1044.80 | |
| WNT_BETA_CATENIN_SIGNALING | 700.39 | |
| XENOBIOTIC_METABOLISM | 566.37 |
Hallmarks-of-Cancer reach
Anti-tumor matches — the "ideal patient" search
| Sample | Cancer type | cos to ideal |
|---|---|---|
| EPT0291 | EPN | 0.848 |
| TCGA-CF-A5U8-01A-11R-A28M-07 | — | 0.840 |
| SRR23303752 | — | 0.838 |
| SRR12202498 | — | 0.826 |
| aMVAC.P_005_TURBT_S223 | — | 0.825 |
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