Darovasertib
Sign in to save this workspacePrimary targets: PKCA, PKCB1, PKCB2, PKCD, PKCEPSILON, PKCETA, PKCG, PKCIOTA, PKCMU_PRKD1, PKCNU_PRKD3, PKCTHETA, PKCZETA · FDA status: Phase III FDA Trials
Selectivity scorecard
KISS
96.99
Gini
0.719
CATDS
0.019
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 Darovasertib. Strongest target: PKCD at 99.9% inhibition.
Accessible data table
| Rank | Target | Inhibition % | Residual activity % |
|---|---|---|---|
| 1 | PKCD | 99.9% | 0.1% |
| 2 | PKCTHETA | 99.9% | 0.1% |
| 3 | PKCEPSILON | 99.8% | 0.2% |
| 4 | PKCETA | 99.8% | 0.2% |
| 5 | PKCB2 | 99.5% | 0.5% |
| 6 | PKCB1 | 99.0% | 1.0% |
| 7 | PKCG | 97.7% | 2.3% |
| 8 | PKCA | 97.5% | 2.5% |
| 9 | DMPK2 | 97.2% | 2.8% |
| 10 | TRKC | 94.5% | 5.5% |
| 11 | MRCKB_CDC42BPB | 91.2% | 8.8% |
| 12 | MSK2_RPS6KA4 | 91.0% | 9.0% |
| 13 | TRKB | 88.9% | 11.1% |
| 14 | ERBB2_HER2 | 87.7% | 12.3% |
| 15 | GCK_MAP4K2 | 80.0% | 20.1% |
| 16 | MLCK2_MYLK2 | 79.6% | 20.4% |
| 17 | PKN2_PRK2 | 79.3% | 20.7% |
| 18 | MRCKA_CDC42BPA | 75.1% | 24.9% |
| 19 | STK21_CIT | 73.4% | 26.6% |
| 20 | PKCNU_PRKD3 | 72.8% | 27.2% |
Selectivity landscape
Where Darovasertib sits in the 92-drug selectivity landscape (KISS vs Gini). The highlighted point is Darovasertib.
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