Alpelisib
Sign in to save this workspacePrimary targets: PI3K · FDA status: FDA Approved
Selectivity scorecard
KISS
97.22
Gini
0.720
CATDS
0.021
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 Alpelisib. Strongest target: RET at 99.6% inhibition.
Accessible data table
| Rank | Target | Inhibition % | Residual activity % |
|---|---|---|---|
| 1 | RET | 99.6% | 0.4% |
| 2 | TRKB | 99.3% | 0.7% |
| 3 | TRKC | 99.3% | 0.7% |
| 4 | FGFR2 | 98.9% | 1.1% |
| 5 | FGFR1 | 98.7% | 1.3% |
| 6 | FGFR3 | 98.6% | 1.4% |
| 7 | TRKA | 97.5% | 2.5% |
| 8 | ROS_ROS1 | 97.1% | 2.9% |
| 9 | FGFR4 | 96.8% | 3.2% |
| 10 | JAK2 | 96.6% | 3.4% |
| 11 | JAK1 | 92.2% | 7.8% |
| 12 | DDR1 | 87.6% | 12.4% |
| 13 | FLT3 | 82.6% | 17.4% |
| 14 | EGFR | 81.3% | 18.7% |
| 15 | ALK | 80.7% | 19.3% |
| 16 | TXK | 80.0% | 20.0% |
| 17 | ERBB4_HER4 | 70.6% | 29.4% |
| 18 | MUSK | 70.2% | 29.8% |
| 19 | BMX_ETK | 68.9% | 31.1% |
| 20 | BLK | 67.4% | 32.6% |
Selectivity landscape
Where Alpelisib sits in the 92-drug selectivity landscape (KISS vs Gini). The highlighted point is Alpelisib.
Atlas insights for Alpelisib
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 | 2032.76 | |
| ALLOGRAFT_REJECTION | 6218.84 | |
| ANDROGEN_RESPONSE | 1460.57 | |
| ANGIOGENESIS | 1006.98 | |
| APICAL_JUNCTION | 6335.32 | |
| APICAL_SURFACE | 744.57 | |
| APOPTOSIS | 4379.85 | |
| BILE_ACID_METABOLISM | 705.82 | |
| CHOLESTEROL_HOMEOSTASIS | 1142.83 | |
| COAGULATION | 612.24 | |
| COMPLEMENT | 3657.82 | |
| DNA_REPAIR | 1378.33 | |
| E2F_TARGETS | 3023.74 | |
| EPITHELIAL_MESENCHYMAL_TRANSITION | 1141.85 | |
| ESTROGEN_RESPONSE_EARLY | 1890.31 | |
| ESTROGEN_RESPONSE_LATE | 1995.20 | |
| FATTY_ACID_METABOLISM | 876.20 | |
| G2M_CHECKPOINT | 2932.76 | |
| GLYCOLYSIS | 2036.19 | |
| HEDGEHOG_SIGNALING | 503.26 | |
| HEME_METABOLISM | 1232.53 | |
| HYPOXIA | 2881.05 | |
| IL2_STAT5_SIGNALING | 2256.89 | |
| IL6_JAK_STAT3_SIGNALING | 5610.91 | |
| INFLAMMATORY_RESPONSE | 3633.52 | |
| INTERFERON_ALPHA_RESPONSE | 736.05 | |
| INTERFERON_GAMMA_RESPONSE | 5517.56 | |
| KRAS_SIGNALING_DN | 577.70 | |
| KRAS_SIGNALING_UP | 2330.14 | |
| MITOTIC_SPINDLE | 3918.92 | |
| MTORC1_SIGNALING | 2553.28 | |
| MYC_TARGETS_V1 | 2257.38 | |
| MYC_TARGETS_V2 | 467.58 | |
| MYOGENESIS | 1904.54 | |
| NOTCH_SIGNALING | 164.81 | |
| OXIDATIVE_PHOSPHORYLATION | 1453.45 | |
| P53_PATHWAY | 2073.67 | |
| PANCREAS_BETA_CELLS | 155.21 | |
| PEROXISOME | 803.31 | |
| PI3K_AKT_MTOR_SIGNALING | 7164.44 | |
| PROTEIN_SECRETION | 1639.77 | |
| REACTIVE_OXYGEN_SPECIES_PATHWAY | 290.52 | |
| SPERMATOGENESIS | 967.91 | |
| TGF_BETA_SIGNALING | 1301.04 | |
| TNFA_SIGNALING_VIA_NFKB | 3226.13 | |
| UNFOLDED_PROTEIN_RESPONSE | 1019.88 | |
| UV_RESPONSE_DN | 3139.27 | |
| UV_RESPONSE_UP | 2334.10 | |
| WNT_BETA_CATENIN_SIGNALING | 1274.96 | |
| XENOBIOTIC_METABOLISM | 1514.99 |
Hallmarks-of-Cancer reach
Anti-tumor matches — the "ideal patient" search
| Sample | Cancer type | cos to ideal |
|---|---|---|
| EPT0291 | EPN | 0.837 |
| SRR23303752 | — | 0.831 |
| SRR10899984 | — | 0.830 |
| TCGA-FD-A43X-01A-11R-A23W-07 | — | 0.820 |
| aMVAC.P_005_TURBT_S223 | — | 0.820 |
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