Canertinib
Sign in to save this workspacePrimary targets: ERBB2_HER2 · FDA status: FDA Trials Discontinued
Selectivity scorecard
KISS
96.49
Gini
0.671
CATDS
0.014
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 Canertinib. Strongest target: TXK at 100.0% inhibition.
Accessible data table
| Rank | Target | Inhibition % | Residual activity % |
|---|---|---|---|
| 1 | TXK | 100.0% | 0.0% |
| 2 | BLK | 99.7% | 0.3% |
| 3 | ERBB4_HER4 | 99.6% | 0.4% |
| 4 | BMX_ETK | 99.4% | 0.6% |
| 5 | ERBB2_HER2 | 99.4% | 0.6% |
| 6 | BTK | 99.3% | 0.7% |
| 7 | JAK3 | 98.9% | 1.1% |
| 8 | DDR1 | 98.5% | 1.5% |
| 9 | EGFR | 98.4% | 1.6% |
| 10 | LCK | 97.7% | 2.3% |
| 11 | ITK | 96.9% | 3.1% |
| 12 | LYN | 95.2% | 4.8% |
| 13 | EPHA6 | 92.1% | 7.9% |
| 14 | ABL1 | 91.6% | 8.4% |
| 15 | RET | 88.0% | 12.1% |
| 16 | YES_YES1 | 87.8% | 12.2% |
| 17 | FGR | 87.3% | 12.7% |
| 18 | RIPK2 | 87.1% | 12.9% |
| 19 | MNK2 | 87.0% | 13.0% |
| 20 | EPHB4 | 86.9% | 13.1% |
Selectivity landscape
Where Canertinib sits in the 92-drug selectivity landscape (KISS vs Gini). The highlighted point is Canertinib.
Atlas insights for Canertinib
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 | 2717.55 | |
| ALLOGRAFT_REJECTION | 9759.94 | |
| ANDROGEN_RESPONSE | 1855.18 | |
| ANGIOGENESIS | 1711.40 | |
| APICAL_JUNCTION | 9865.67 | |
| APICAL_SURFACE | 1047.72 | |
| APOPTOSIS | 7401.29 | |
| BILE_ACID_METABOLISM | 1149.80 | |
| CHOLESTEROL_HOMEOSTASIS | 1689.69 | |
| COAGULATION | 1061.65 | |
| COMPLEMENT | 5881.06 | |
| DNA_REPAIR | 1968.38 | |
| E2F_TARGETS | 4549.25 | |
| EPITHELIAL_MESENCHYMAL_TRANSITION | 2010.04 | |
| ESTROGEN_RESPONSE_EARLY | 3151.17 | |
| ESTROGEN_RESPONSE_LATE | 2930.94 | |
| FATTY_ACID_METABOLISM | 764.76 | |
| G2M_CHECKPOINT | 4702.23 | |
| GLYCOLYSIS | 2521.82 | |
| HEDGEHOG_SIGNALING | 1076.35 | |
| HEME_METABOLISM | 2133.14 | |
| HYPOXIA | 4211.26 | |
| IL2_STAT5_SIGNALING | 3257.72 | |
| IL6_JAK_STAT3_SIGNALING | 4773.45 | |
| INFLAMMATORY_RESPONSE | 5367.50 | |
| INTERFERON_ALPHA_RESPONSE | 938.64 | |
| INTERFERON_GAMMA_RESPONSE | 6483.05 | |
| KRAS_SIGNALING_DN | 958.99 | |
| KRAS_SIGNALING_UP | 3704.83 | |
| MITOTIC_SPINDLE | 6785.69 | |
| MTORC1_SIGNALING | 3881.60 | |
| MYC_TARGETS_V1 | 3128.58 | |
| MYC_TARGETS_V2 | 685.60 | |
| MYOGENESIS | 3159.74 | |
| NOTCH_SIGNALING | 285.54 | |
| OXIDATIVE_PHOSPHORYLATION | 1413.68 | |
| P53_PATHWAY | 4021.11 | |
| PANCREAS_BETA_CELLS | 317.20 | |
| PEROXISOME | 1243.06 | |
| PI3K_AKT_MTOR_SIGNALING | 9077.51 | |
| PROTEIN_SECRETION | 2150.01 | |
| REACTIVE_OXYGEN_SPECIES_PATHWAY | 611.98 | |
| SPERMATOGENESIS | 1285.68 | |
| TGF_BETA_SIGNALING | 1987.40 | |
| TNFA_SIGNALING_VIA_NFKB | 4538.95 | |
| UNFOLDED_PROTEIN_RESPONSE | 1248.65 | |
| UV_RESPONSE_DN | 4865.43 | |
| UV_RESPONSE_UP | 3690.23 | |
| WNT_BETA_CATENIN_SIGNALING | 2174.47 | |
| XENOBIOTIC_METABOLISM | 2179.77 |
Anti-tumor matches — the "ideal patient" search
| Sample | Cancer type | cos to ideal |
|---|---|---|
| EPT0291 | EPN | 0.836 |
| SRR23303752 | — | 0.835 |
| SRR10899984 | — | 0.823 |
| aMVAC.P_005_TURBT_S223 | — | 0.821 |
| TCGA-CF-A5U8-01A-11R-A28M-07 | — | 0.820 |
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