Rabusertib
Sign in to save this workspacePrimary targets: CHK1 · FDA status: FDA trials Discontinued after Phase II
Selectivity scorecard
KISS
98.74
Gini
0.687
CATDS
0.025
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 Rabusertib. Strongest target: CHK1 at 99.4% inhibition.
Accessible data table
| Rank | Target | Inhibition % | Residual activity % |
|---|---|---|---|
| 1 | CHK1 | 99.4% | 0.6% |
| 2 | RAF1 | 95.6% | 4.4% |
| 3 | CAMK2A | 92.0% | 8.0% |
| 4 | RSK3 | 91.1% | 8.9% |
| 5 | CAMK2D | 90.9% | 9.1% |
| 6 | RSK4 | 84.3% | 15.8% |
| 7 | CDK3_CYCLIN_C | 80.3% | 19.7% |
| 8 | RSK2 | 76.2% | 23.8% |
| 9 | TRKC | 75.2% | 24.8% |
| 10 | RSK1 | 74.3% | 25.7% |
| 11 | SIK2 | 72.1% | 27.9% |
| 12 | FLT3 | 71.2% | 28.8% |
| 13 | TNIK | 57.8% | 42.2% |
| 14 | BRSK2 | 56.9% | 43.1% |
| 15 | MEK5 | 53.9% | 46.1% |
| 16 | AMPK(A2_B2_G2) | 48.0% | 52.0% |
| 17 | LOK_STK10 | 47.4% | 52.6% |
| 18 | MSSK1_STK23 | 44.1% | 55.9% |
| 19 | AMPK(A2_B2_G1) | 41.9% | 58.1% |
| 20 | BRAF | 41.1% | 58.9% |
Selectivity landscape
Where Rabusertib sits in the 92-drug selectivity landscape (KISS vs Gini). The highlighted point is Rabusertib.
Atlas insights for Rabusertib
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 | 1037.82 | |
| ALLOGRAFT_REJECTION | 1753.24 | |
| ANDROGEN_RESPONSE | 819.33 | |
| ANGIOGENESIS | 323.73 | |
| APICAL_JUNCTION | 2448.05 | |
| APICAL_SURFACE | 159.13 | |
| APOPTOSIS | 3096.42 | |
| BILE_ACID_METABOLISM | 451.83 | |
| CHOLESTEROL_HOMEOSTASIS | 386.09 | |
| COAGULATION | 129.57 | |
| COMPLEMENT | 1335.97 | |
| DNA_REPAIR | 468.98 | |
| E2F_TARGETS | 2513.30 | |
| EPITHELIAL_MESENCHYMAL_TRANSITION | 1332.27 | |
| ESTROGEN_RESPONSE_EARLY | 1907.59 | |
| ESTROGEN_RESPONSE_LATE | 1437.23 | |
| FATTY_ACID_METABOLISM | 239.25 | |
| G2M_CHECKPOINT | 2143.87 | |
| GLYCOLYSIS | 1188.30 | |
| HEDGEHOG_SIGNALING | 367.82 | |
| HEME_METABOLISM | 730.36 | |
| HYPOXIA | 1510.91 | |
| IL2_STAT5_SIGNALING | 715.96 | |
| IL6_JAK_STAT3_SIGNALING | 880.63 | |
| INFLAMMATORY_RESPONSE | 1617.41 | |
| INTERFERON_ALPHA_RESPONSE | 239.45 | |
| INTERFERON_GAMMA_RESPONSE | 1166.42 | |
| KRAS_SIGNALING_DN | 841.67 | |
| KRAS_SIGNALING_UP | 767.54 | |
| MITOTIC_SPINDLE | 2266.07 | |
| MTORC1_SIGNALING | 1432.00 | |
| MYC_TARGETS_V1 | 1342.06 | |
| MYC_TARGETS_V2 | 457.98 | |
| MYOGENESIS | 1644.85 | |
| NOTCH_SIGNALING | 147.38 | |
| OXIDATIVE_PHOSPHORYLATION | 466.96 | |
| P53_PATHWAY | 1254.14 | |
| PANCREAS_BETA_CELLS | 112.05 | |
| PEROXISOME | 722.16 | |
| PI3K_AKT_MTOR_SIGNALING | 2893.43 | |
| PROTEIN_SECRETION | 972.61 | |
| REACTIVE_OXYGEN_SPECIES_PATHWAY | 85.69 | |
| SPERMATOGENESIS | 644.24 | |
| TGF_BETA_SIGNALING | 1006.15 | |
| TNFA_SIGNALING_VIA_NFKB | 1888.87 | |
| UNFOLDED_PROTEIN_RESPONSE | 739.05 | |
| UV_RESPONSE_DN | 2080.22 | |
| UV_RESPONSE_UP | 1359.14 | |
| WNT_BETA_CATENIN_SIGNALING | 1297.29 | |
| XENOBIOTIC_METABOLISM | 664.78 |
Hallmarks-of-Cancer reach
Anti-tumor matches — the "ideal patient" search
| Sample | Cancer type | cos to ideal |
|---|---|---|
| EPT0291 | EPN | 0.845 |
| SRR23303752 | — | 0.829 |
| TCGA-CF-A5U8-01A-11R-A28M-07 | — | 0.827 |
| b6a7e87e-2674-4a48-a3c2-c8a9806762b5 | — | 0.817 |
| aMVAC.P_005_TURBT_S223 | — | 0.816 |
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