Neratinib
Sign in to save this workspacePrimary targets: ERBB2_HER2 · FDA status: FDA Approved
Selectivity scorecard
KISS
93.18
Gini
0.597
CATDS
0.010
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 Neratinib. Strongest target: EGFR at 100.0% inhibition.
Accessible data table
| Rank | Target | Inhibition % | Residual activity % |
|---|---|---|---|
| 1 | EGFR | 100.0% | 0.0% |
| 2 | ERBB4_HER4 | 99.7% | 0.3% |
| 3 | ERBB2_HER2 | 99.7% | 0.3% |
| 4 | GLK_MAP4K3 | 99.7% | 0.3% |
| 5 | LCK | 99.3% | 0.7% |
| 6 | STK25_YSK1 | 99.2% | 0.8% |
| 7 | KHS_MAP4K5 | 99.0% | 1.0% |
| 8 | TNIK | 98.9% | 1.1% |
| 9 | MST4 | 98.7% | 1.3% |
| 10 | MST3_STK24 | 98.3% | 1.7% |
| 11 | MINK_MINK1 | 98.3% | 1.7% |
| 12 | BLK | 98.2% | 1.8% |
| 13 | HGK_MAP4K4 | 98.1% | 1.9% |
| 14 | C_MER | 97.8% | 2.2% |
| 15 | HPK1_MAP4K1 | 97.7% | 2.4% |
| 16 | SIK1 | 96.4% | 3.6% |
| 17 | AXL | 96.3% | 3.7% |
| 18 | ACK1 | 95.2% | 4.8% |
| 19 | JAK3 | 95.2% | 4.8% |
| 20 | YES_YES1 | 94.3% | 5.7% |
Selectivity landscape
Where Neratinib sits in the 92-drug selectivity landscape (KISS vs Gini). The highlighted point is Neratinib.
Atlas insights for Neratinib
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 | 3363.92 | |
| ALLOGRAFT_REJECTION | 10281.37 | |
| ANDROGEN_RESPONSE | 2559.43 | |
| ANGIOGENESIS | 1912.07 | |
| APICAL_JUNCTION | 10610.46 | |
| APICAL_SURFACE | 1207.99 | |
| APOPTOSIS | 8484.15 | |
| BILE_ACID_METABOLISM | 1254.55 | |
| CHOLESTEROL_HOMEOSTASIS | 1487.09 | |
| COAGULATION | 1228.69 | |
| COMPLEMENT | 6300.72 | |
| DNA_REPAIR | 2449.26 | |
| E2F_TARGETS | 6666.69 | |
| EPITHELIAL_MESENCHYMAL_TRANSITION | 3107.01 | |
| ESTROGEN_RESPONSE_EARLY | 3743.02 | |
| ESTROGEN_RESPONSE_LATE | 3433.41 | |
| FATTY_ACID_METABOLISM | 776.54 | |
| G2M_CHECKPOINT | 6883.18 | |
| GLYCOLYSIS | 2989.13 | |
| HEDGEHOG_SIGNALING | 1171.45 | |
| HEME_METABOLISM | 2520.72 | |
| HYPOXIA | 5068.07 | |
| IL2_STAT5_SIGNALING | 3892.12 | |
| IL6_JAK_STAT3_SIGNALING | 5358.57 | |
| INFLAMMATORY_RESPONSE | 6297.44 | |
| INTERFERON_ALPHA_RESPONSE | 1157.08 | |
| INTERFERON_GAMMA_RESPONSE | 7392.84 | |
| KRAS_SIGNALING_DN | 1164.51 | |
| KRAS_SIGNALING_UP | 3974.38 | |
| MITOTIC_SPINDLE | 8433.22 | |
| MTORC1_SIGNALING | 4811.23 | |
| MYC_TARGETS_V1 | 4369.56 | |
| MYC_TARGETS_V2 | 1120.21 | |
| MYOGENESIS | 3836.68 | |
| NOTCH_SIGNALING | 424.95 | |
| OXIDATIVE_PHOSPHORYLATION | 1478.90 | |
| P53_PATHWAY | 5002.62 | |
| PANCREAS_BETA_CELLS | 498.51 | |
| PEROXISOME | 1217.78 | |
| PI3K_AKT_MTOR_SIGNALING | 9836.72 | |
| PROTEIN_SECRETION | 2089.82 | |
| REACTIVE_OXYGEN_SPECIES_PATHWAY | 733.72 | |
| SPERMATOGENESIS | 2198.08 | |
| TGF_BETA_SIGNALING | 2518.73 | |
| TNFA_SIGNALING_VIA_NFKB | 5974.27 | |
| UNFOLDED_PROTEIN_RESPONSE | 1827.82 | |
| UV_RESPONSE_DN | 5609.67 | |
| UV_RESPONSE_UP | 4032.62 | |
| WNT_BETA_CATENIN_SIGNALING | 2712.34 | |
| XENOBIOTIC_METABOLISM | 2344.91 |
Hallmarks-of-Cancer reach
Anti-tumor matches — the "ideal patient" search
| Sample | Cancer type | cos to ideal |
|---|---|---|
| EPT0291 | EPN | 0.858 |
| TCGA-CF-A5U8-01A-11R-A28M-07 | — | 0.849 |
| SRR23303752 | — | 0.842 |
| SRR12202498 | — | 0.838 |
| aMVAC.P_005_TURBT_S223 | — | 0.834 |
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