Defactinib
Sign in to save this workspacePrimary targets: FAK_PTK2 · FDA status: FDA Approved
Selectivity scorecard
KISS
92.68
Gini
0.450
CATDS
0.006
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 Defactinib. Strongest target: ERBB4_HER4 at 99.6% inhibition.
Accessible data table
| Rank | Target | Inhibition % | Residual activity % |
|---|---|---|---|
| 1 | ERBB4_HER4 | 99.6% | 0.4% |
| 2 | FAK_PTK2 | 98.5% | 1.5% |
| 3 | CLK1 | 97.9% | 2.1% |
| 4 | CDK5_P25 | 96.8% | 3.2% |
| 5 | MLK3_MAP3K11 | 96.4% | 3.6% |
| 6 | GSK3B | 96.3% | 3.7% |
| 7 | CDK1_CYCLIN_A | 96.3% | 3.7% |
| 8 | LRRK2 | 95.8% | 4.2% |
| 9 | JAK2 | 95.3% | 4.7% |
| 10 | MUSK | 95.2% | 4.8% |
| 11 | TYK2 | 95.0% | 5.0% |
| 12 | YSK4_MAP3K19 | 94.9% | 5.1% |
| 13 | EGFR | 94.6% | 5.4% |
| 14 | FLT3 | 94.6% | 5.4% |
| 15 | CLK2 | 94.5% | 5.5% |
| 16 | CDK9_CYCLIN_K | 93.7% | 6.3% |
| 17 | JAK1 | 93.7% | 6.3% |
| 18 | CDK3_CYCLIN_E | 92.6% | 7.4% |
| 19 | CDK2_CYCLIN_E | 92.6% | 7.4% |
| 20 | MLK1_MAP3K9 | 92.2% | 7.8% |
Selectivity landscape
Where Defactinib sits in the 92-drug selectivity landscape (KISS vs Gini). The highlighted point is Defactinib.
Atlas insights for Defactinib
Pathway-space view of what this drug actually does, drawn from the Pathway Atlas.
Hallmarks-of-Cancer reach
Anti-tumor matches — the "ideal patient" search
| Sample | Cancer type | cos to ideal |
|---|---|---|
| EPT0291 | EPN | 0.879 |
| TCGA-CF-A5U8-01A-11R-A28M-07 | — | 0.864 |
| SRR12202498 | — | 0.851 |
| aMVAC.P_005_TURBT_S223 | — | 0.846 |
| SRR1443713 | GTEX | 0.846 |
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