Umbralisib
Sign in to save this workspacePrimary targets: CK1EPSILON, PI3K · FDA status: FDA Approval Withdrawn
Selectivity scorecard
KISS
98.74
Gini
0.670
CATDS
0.023
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 Umbralisib. Strongest target: RAF1 at 99.8% inhibition.
Accessible data table
| Rank | Target | Inhibition % | Residual activity % |
|---|---|---|---|
| 1 | RAF1 | 99.8% | 0.2% |
| 2 | JAK1 | 96.4% | 3.6% |
| 3 | JAK2 | 96.2% | 3.8% |
| 4 | YSK4_MAP3K19 | 95.9% | 4.1% |
| 5 | C_KIT | 94.5% | 5.5% |
| 6 | ARAF | 84.9% | 15.1% |
| 7 | DDR2 | 79.8% | 20.2% |
| 8 | TAOK2_TAO1 | 75.4% | 24.6% |
| 9 | FMS | 74.9% | 25.1% |
| 10 | ZAK_MLTK | 71.9% | 28.1% |
| 11 | KDR_VEGFR2 | 67.8% | 32.2% |
| 12 | JAK3 | 67.1% | 32.9% |
| 13 | HIPK4 | 67.0% | 33.0% |
| 14 | LYN | 65.5% | 34.5% |
| 15 | BRAF | 65.3% | 34.7% |
| 16 | TYK2 | 62.2% | 37.8% |
| 17 | LCK | 61.9% | 38.1% |
| 18 | FLT4_VEGFR3 | 57.8% | 42.2% |
| 19 | ABL2_ARG | 55.8% | 44.2% |
| 20 | CK1EPSILON | 55.6% | 44.4% |
Selectivity landscape
Where Umbralisib sits in the 92-drug selectivity landscape (KISS vs Gini). The highlighted point is Umbralisib.
Atlas insights for Umbralisib
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 | 1763.20 | |
| ALLOGRAFT_REJECTION | 4950.79 | |
| ANDROGEN_RESPONSE | 546.73 | |
| ANGIOGENESIS | 584.31 | |
| APICAL_JUNCTION | 4681.50 | |
| APICAL_SURFACE | 538.39 | |
| APOPTOSIS | 3432.81 | |
| BILE_ACID_METABOLISM | 432.74 | |
| CHOLESTEROL_HOMEOSTASIS | 531.33 | |
| COAGULATION | 579.40 | |
| COMPLEMENT | 2790.18 | |
| DNA_REPAIR | 737.85 | |
| E2F_TARGETS | 2560.85 | |
| EPITHELIAL_MESENCHYMAL_TRANSITION | 910.82 | |
| ESTROGEN_RESPONSE_EARLY | 1951.95 | |
| ESTROGEN_RESPONSE_LATE | 1745.23 | |
| FATTY_ACID_METABOLISM | 372.57 | |
| G2M_CHECKPOINT | 2408.55 | |
| GLYCOLYSIS | 1303.62 | |
| HEDGEHOG_SIGNALING | 382.38 | |
| HEME_METABOLISM | 1323.40 | |
| HYPOXIA | 2099.72 | |
| IL2_STAT5_SIGNALING | 2067.77 | |
| IL6_JAK_STAT3_SIGNALING | 4102.41 | |
| INFLAMMATORY_RESPONSE | 3360.77 | |
| INTERFERON_ALPHA_RESPONSE | 735.16 | |
| INTERFERON_GAMMA_RESPONSE | 4216.01 | |
| KRAS_SIGNALING_DN | 471.61 | |
| KRAS_SIGNALING_UP | 1935.77 | |
| MITOTIC_SPINDLE | 2731.14 | |
| MTORC1_SIGNALING | 1804.75 | |
| MYC_TARGETS_V1 | 1906.85 | |
| MYC_TARGETS_V2 | 499.02 | |
| MYOGENESIS | 1448.65 | |
| NOTCH_SIGNALING | 110.14 | |
| OXIDATIVE_PHOSPHORYLATION | 647.11 | |
| P53_PATHWAY | 1768.52 | |
| PANCREAS_BETA_CELLS | 125.77 | |
| PEROXISOME | 462.23 | |
| PI3K_AKT_MTOR_SIGNALING | 5104.11 | |
| PROTEIN_SECRETION | 905.11 | |
| REACTIVE_OXYGEN_SPECIES_PATHWAY | 200.96 | |
| SPERMATOGENESIS | 1233.69 | |
| TGF_BETA_SIGNALING | 913.38 | |
| TNFA_SIGNALING_VIA_NFKB | 2857.10 | |
| UNFOLDED_PROTEIN_RESPONSE | 817.99 | |
| UV_RESPONSE_DN | 2775.34 | |
| UV_RESPONSE_UP | 1931.49 | |
| WNT_BETA_CATENIN_SIGNALING | 945.51 | |
| XENOBIOTIC_METABOLISM | 751.62 |
Hallmarks-of-Cancer reach
Anti-tumor matches — the "ideal patient" search
| Sample | Cancer type | cos to ideal |
|---|---|---|
| EPT0291 | EPN | 0.836 |
| SRR23303752 | — | 0.828 |
| TCGA-CF-A5U8-01A-11R-A28M-07 | — | 0.822 |
| SRR10899984 | — | 0.819 |
| TCGA-FD-A43X-01A-11R-A23W-07 | — | 0.818 |
Annotations
Sign in to read and post annotations.
Loading…