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.
Atlas insights for Darovasertib
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 | 1132.36 | |
| ALLOGRAFT_REJECTION | 2147.23 | |
| ANDROGEN_RESPONSE | 1077.79 | |
| ANGIOGENESIS | 265.79 | |
| APICAL_JUNCTION | 2066.98 | |
| APICAL_SURFACE | 243.98 | |
| APOPTOSIS | 3234.09 | |
| BILE_ACID_METABOLISM | 427.77 | |
| CHOLESTEROL_HOMEOSTASIS | 299.70 | |
| COAGULATION | 247.56 | |
| COMPLEMENT | 1463.03 | |
| DNA_REPAIR | 838.70 | |
| E2F_TARGETS | 2927.46 | |
| EPITHELIAL_MESENCHYMAL_TRANSITION | 1013.79 | |
| ESTROGEN_RESPONSE_EARLY | 1512.98 | |
| ESTROGEN_RESPONSE_LATE | 1319.83 | |
| FATTY_ACID_METABOLISM | 260.00 | |
| G2M_CHECKPOINT | 3107.83 | |
| GLYCOLYSIS | 1148.96 | |
| HEDGEHOG_SIGNALING | 386.79 | |
| HEME_METABOLISM | 1165.44 | |
| HYPOXIA | 2198.27 | |
| IL2_STAT5_SIGNALING | 1507.68 | |
| IL6_JAK_STAT3_SIGNALING | 1302.14 | |
| INFLAMMATORY_RESPONSE | 1788.94 | |
| INTERFERON_ALPHA_RESPONSE | 284.02 | |
| INTERFERON_GAMMA_RESPONSE | 1992.57 | |
| KRAS_SIGNALING_DN | 456.08 | |
| KRAS_SIGNALING_UP | 970.63 | |
| MITOTIC_SPINDLE | 2290.57 | |
| MTORC1_SIGNALING | 1581.48 | |
| MYC_TARGETS_V1 | 1543.31 | |
| MYC_TARGETS_V2 | 522.05 | |
| MYOGENESIS | 1863.73 | |
| NOTCH_SIGNALING | 264.16 | |
| OXIDATIVE_PHOSPHORYLATION | 295.27 | |
| P53_PATHWAY | 2095.29 | |
| PANCREAS_BETA_CELLS | 349.93 | |
| PEROXISOME | 561.43 | |
| PI3K_AKT_MTOR_SIGNALING | 3457.13 | |
| PROTEIN_SECRETION | 566.79 | |
| REACTIVE_OXYGEN_SPECIES_PATHWAY | 208.65 | |
| SPERMATOGENESIS | 764.87 | |
| TGF_BETA_SIGNALING | 1164.63 | |
| TNFA_SIGNALING_VIA_NFKB | 2514.93 | |
| UNFOLDED_PROTEIN_RESPONSE | 661.82 | |
| UV_RESPONSE_DN | 2074.38 | |
| UV_RESPONSE_UP | 1302.31 | |
| WNT_BETA_CATENIN_SIGNALING | 1147.95 | |
| XENOBIOTIC_METABOLISM | 574.47 |
Hallmarks-of-Cancer reach
Anti-tumor matches — the "ideal patient" search
| Sample | Cancer type | cos to ideal |
|---|---|---|
| EPT0291 | EPN | 0.863 |
| TCGA-CF-A5U8-01A-11R-A28M-07 | — | 0.852 |
| SRR12202498 | — | 0.836 |
| SRR1443713 | GTEX | 0.835 |
| b6a7e87e-2674-4a48-a3c2-c8a9806762b5 | — | 0.830 |
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