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Sign in to save this workspacePrimary targets: CK1EPSILON, PI3K · FDA status: FDA Approval Withdrawn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.
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 |
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