Lapatinib
Sign in to save this workspacePrimary targets: EGFR, ERBB2_HER2 · FDA status: FDA Approved
Selectivity scorecard
KISS
99.25
Gini
0.616
CATDS
0.038
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 Lapatinib. Strongest target: EGFR at 99.2% inhibition.
Accessible data table
| Rank | Target | Inhibition % | Residual activity % |
|---|---|---|---|
| 1 | EGFR | 99.2% | 0.8% |
| 2 | ERBB4_HER4 | 97.8% | 2.2% |
| 3 | ERBB2_HER2 | 95.8% | 4.2% |
| 4 | RIPK3 | 52.5% | 47.5% |
| 5 | SLK_STK2 | 51.5% | 48.5% |
| 6 | ARAF | 47.3% | 52.7% |
| 7 | CAMKK2 | 37.0% | 63.0% |
| 8 | PKMYT1 | 31.1% | 68.9% |
| 9 | BRK | 30.3% | 69.7% |
| 10 | RAF1 | 29.6% | 70.4% |
| 11 | RIPK4 | 28.9% | 71.1% |
| 12 | ERN1_IRE1 | 28.5% | 71.5% |
| 13 | TRPM7_CHAK1 | 25.7% | 74.3% |
| 14 | TLK1 | 25.0% | 75.0% |
| 15 | PKCNU_PRKD3 | 21.9% | 78.1% |
| 16 | PDK2_PDHK2 | 21.4% | 78.6% |
| 17 | HASPIN | 20.8% | 79.2% |
| 18 | NEK8 | 20.0% | 80.0% |
| 19 | IKKA_CHUK | 20.0% | 80.0% |
| 20 | TTBK2 | 19.9% | 80.1% |
Selectivity landscape
Where Lapatinib sits in the 92-drug selectivity landscape (KISS vs Gini). The highlighted point is Lapatinib.
Atlas insights for Lapatinib
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 | 743.50 | |
| ALLOGRAFT_REJECTION | 1754.48 | |
| ANDROGEN_RESPONSE | 932.20 | |
| ANGIOGENESIS | 440.61 | |
| APICAL_JUNCTION | 2549.03 | |
| APICAL_SURFACE | 304.79 | |
| APOPTOSIS | 2061.13 | |
| BILE_ACID_METABOLISM | 351.20 | |
| CHOLESTEROL_HOMEOSTASIS | 641.95 | |
| COAGULATION | 216.00 | |
| COMPLEMENT | 1573.72 | |
| DNA_REPAIR | 604.51 | |
| E2F_TARGETS | 1699.92 | |
| EPITHELIAL_MESENCHYMAL_TRANSITION | 608.31 | |
| ESTROGEN_RESPONSE_EARLY | 931.96 | |
| ESTROGEN_RESPONSE_LATE | 701.63 | |
| FATTY_ACID_METABOLISM | 230.56 | |
| G2M_CHECKPOINT | 1128.32 | |
| GLYCOLYSIS | 878.12 | |
| HEDGEHOG_SIGNALING | 289.22 | |
| HEME_METABOLISM | 431.90 | |
| HYPOXIA | 1353.29 | |
| IL2_STAT5_SIGNALING | 759.91 | |
| IL6_JAK_STAT3_SIGNALING | 1276.08 | |
| INFLAMMATORY_RESPONSE | 1602.76 | |
| INTERFERON_ALPHA_RESPONSE | 305.36 | |
| INTERFERON_GAMMA_RESPONSE | 1659.72 | |
| KRAS_SIGNALING_DN | 412.48 | |
| KRAS_SIGNALING_UP | 1046.42 | |
| MITOTIC_SPINDLE | 1721.46 | |
| MTORC1_SIGNALING | 1124.19 | |
| MYC_TARGETS_V1 | 1255.14 | |
| MYC_TARGETS_V2 | 243.81 | |
| MYOGENESIS | 951.93 | |
| NOTCH_SIGNALING | 192.31 | |
| OXIDATIVE_PHOSPHORYLATION | 376.39 | |
| P53_PATHWAY | 963.67 | |
| PANCREAS_BETA_CELLS | 83.69 | |
| PEROXISOME | 247.21 | |
| PI3K_AKT_MTOR_SIGNALING | 2335.20 | |
| PROTEIN_SECRETION | 782.94 | |
| REACTIVE_OXYGEN_SPECIES_PATHWAY | 174.95 | |
| SPERMATOGENESIS | 557.46 | |
| TGF_BETA_SIGNALING | 573.39 | |
| TNFA_SIGNALING_VIA_NFKB | 1438.95 | |
| UNFOLDED_PROTEIN_RESPONSE | 389.51 | |
| UV_RESPONSE_DN | 1149.86 | |
| UV_RESPONSE_UP | 1065.53 | |
| WNT_BETA_CATENIN_SIGNALING | 777.88 | |
| XENOBIOTIC_METABOLISM | 654.40 |
Hallmarks-of-Cancer reach
Anti-tumor matches — the "ideal patient" search
| Sample | Cancer type | cos to ideal |
|---|---|---|
| EPT0291 | EPN | 0.869 |
| SRR23303752 | — | 0.854 |
| TCGA-CF-A5U8-01A-11R-A28M-07 | — | 0.850 |
| aMVAC.P_005_TURBT_S223 | — | 0.844 |
| SRR12202498 | — | 0.842 |
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