Tenalisib
Sign in to save this workspacePrimary targets: PI3K · FDA status: FDA Phase I Trials Completed
Selectivity scorecard
KISS
97.98
Gini
0.702
CATDS
0.027
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 Tenalisib. Strongest target: RET at 98.5% inhibition.
Accessible data table
| Rank | Target | Inhibition % | Residual activity % |
|---|---|---|---|
| 1 | RET | 98.5% | 1.5% |
| 2 | TRKC | 98.1% | 1.9% |
| 3 | FGFR3 | 98.0% | 2.0% |
| 4 | JAK1 | 96.4% | 3.6% |
| 5 | FGFR2 | 96.0% | 4.0% |
| 6 | TRKB | 95.3% | 4.7% |
| 7 | JAK2 | 93.8% | 6.2% |
| 8 | FGFR1 | 93.2% | 6.8% |
| 9 | ROS_ROS1 | 87.4% | 12.6% |
| 10 | FGFR4 | 83.9% | 16.1% |
| 11 | FLT3 | 76.8% | 23.2% |
| 12 | DDR1 | 73.4% | 26.6% |
| 13 | TRKA | 59.0% | 41.0% |
| 14 | JAK3 | 55.1% | 44.9% |
| 15 | LIMK1 | 54.4% | 45.6% |
| 16 | TYK2 | 52.3% | 47.7% |
| 17 | MLK3_MAP3K11 | 52.0% | 48.0% |
| 18 | FLT4_VEGFR3 | 48.7% | 51.3% |
| 19 | ALK | 45.2% | 54.8% |
| 20 | C_SRC | 39.0% | 61.0% |
Selectivity landscape
Where Tenalisib sits in the 92-drug selectivity landscape (KISS vs Gini). The highlighted point is Tenalisib.
Atlas insights for Tenalisib
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 | 1528.50 | |
| ALLOGRAFT_REJECTION | 4353.88 | |
| ANDROGEN_RESPONSE | 1066.97 | |
| ANGIOGENESIS | 607.60 | |
| APICAL_JUNCTION | 4329.63 | |
| APICAL_SURFACE | 508.09 | |
| APOPTOSIS | 3100.67 | |
| BILE_ACID_METABOLISM | 442.95 | |
| CHOLESTEROL_HOMEOSTASIS | 582.90 | |
| COAGULATION | 382.96 | |
| COMPLEMENT | 2297.19 | |
| DNA_REPAIR | 883.19 | |
| E2F_TARGETS | 2424.90 | |
| EPITHELIAL_MESENCHYMAL_TRANSITION | 969.55 | |
| ESTROGEN_RESPONSE_EARLY | 1426.21 | |
| ESTROGEN_RESPONSE_LATE | 1612.06 | |
| FATTY_ACID_METABOLISM | 662.60 | |
| G2M_CHECKPOINT | 2474.95 | |
| GLYCOLYSIS | 1482.22 | |
| HEDGEHOG_SIGNALING | 335.53 | |
| HEME_METABOLISM | 943.81 | |
| HYPOXIA | 1952.64 | |
| IL2_STAT5_SIGNALING | 1666.06 | |
| IL6_JAK_STAT3_SIGNALING | 4453.47 | |
| INFLAMMATORY_RESPONSE | 2545.10 | |
| INTERFERON_ALPHA_RESPONSE | 560.07 | |
| INTERFERON_GAMMA_RESPONSE | 4130.28 | |
| KRAS_SIGNALING_DN | 335.77 | |
| KRAS_SIGNALING_UP | 1551.88 | |
| MITOTIC_SPINDLE | 2571.15 | |
| MTORC1_SIGNALING | 1755.14 | |
| MYC_TARGETS_V1 | 1591.81 | |
| MYC_TARGETS_V2 | 359.56 | |
| MYOGENESIS | 1388.05 | |
| NOTCH_SIGNALING | 98.07 | |
| OXIDATIVE_PHOSPHORYLATION | 1161.41 | |
| P53_PATHWAY | 1423.36 | |
| PANCREAS_BETA_CELLS | 147.88 | |
| PEROXISOME | 571.88 | |
| PI3K_AKT_MTOR_SIGNALING | 5643.91 | |
| PROTEIN_SECRETION | 1112.30 | |
| REACTIVE_OXYGEN_SPECIES_PATHWAY | 156.37 | |
| SPERMATOGENESIS | 890.19 | |
| TGF_BETA_SIGNALING | 932.70 | |
| TNFA_SIGNALING_VIA_NFKB | 2470.50 | |
| UNFOLDED_PROTEIN_RESPONSE | 839.67 | |
| UV_RESPONSE_DN | 2282.40 | |
| UV_RESPONSE_UP | 1525.27 | |
| WNT_BETA_CATENIN_SIGNALING | 948.78 | |
| XENOBIOTIC_METABOLISM | 886.71 |
Hallmarks-of-Cancer reach
Anti-tumor matches — the "ideal patient" search
| Sample | Cancer type | cos to ideal |
|---|---|---|
| EPT0291 | EPN | 0.834 |
| SRR23303752 | — | 0.824 |
| SRR10899984 | — | 0.823 |
| TCGA-FD-A43X-01A-11R-A23W-07 | — | 0.818 |
| TCGA-CF-A5U8-01A-11R-A28M-07 | — | 0.814 |
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