Erlotinib
Sign in to save this workspacePrimary targets: EGFR · FDA status: FDA Approved
Selectivity scorecard
KISS
99.75
Gini
0.695
CATDS
0.027
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 Erlotinib. Strongest target: EGFR at 99.4% inhibition.
Accessible data table
| Rank | Target | Inhibition % | Residual activity % |
|---|---|---|---|
| 1 | EGFR | 99.4% | 0.6% |
| 2 | LOK_STK10 | 89.5% | 10.5% |
| 3 | DDR1 | 83.5% | 16.5% |
| 4 | ERBB4_HER4 | 77.6% | 22.4% |
| 5 | ERBB2_HER2 | 77.5% | 22.5% |
| 6 | MEK5 | 70.9% | 29.1% |
| 7 | ABL1 | 70.5% | 29.5% |
| 8 | SLK_STK2 | 68.6% | 31.4% |
| 9 | ABL2_ARG | 66.8% | 33.2% |
| 10 | FLT3 | 61.3% | 38.7% |
| 11 | LYN | 59.6% | 40.4% |
| 12 | DDR2 | 51.2% | 48.8% |
| 13 | FGFR2 | 50.7% | 49.3% |
| 14 | EPHA6 | 50.0% | 50.0% |
| 15 | LCK | 49.7% | 50.3% |
| 16 | RET | 49.5% | 50.5% |
| 17 | FLT4_VEGFR3 | 48.7% | 51.3% |
| 18 | BLK | 48.0% | 52.0% |
| 19 | MNK1 | 47.6% | 52.4% |
| 20 | RIPK2 | 44.7% | 55.3% |
Selectivity landscape
Where Erlotinib sits in the 92-drug selectivity landscape (KISS vs Gini). The highlighted point is Erlotinib.
Atlas insights for Erlotinib
Pathway-space view of what this drug actually does, drawn from the Pathway Atlas.
On-target vs off-target shadow
On-target23%
Off-target77%
Ghost (2nd-order)0%
| Pathway | Composition | Total |Π| |
|---|---|---|
| ADIPOGENESIS | 1611.54 | |
| ALLOGRAFT_REJECTION | 4788.67 | |
| ANDROGEN_RESPONSE | 1066.98 | |
| ANGIOGENESIS | 917.28 | |
| APICAL_JUNCTION | 5191.80 | |
| APICAL_SURFACE | 619.01 | |
| APOPTOSIS | 4072.42 | |
| BILE_ACID_METABOLISM | 608.25 | |
| CHOLESTEROL_HOMEOSTASIS | 1194.48 | |
| COAGULATION | 590.95 | |
| COMPLEMENT | 3291.76 | |
| DNA_REPAIR | 1222.00 | |
| E2F_TARGETS | 2637.31 | |
| EPITHELIAL_MESENCHYMAL_TRANSITION | 1051.68 | |
| ESTROGEN_RESPONSE_EARLY | 1628.83 | |
| ESTROGEN_RESPONSE_LATE | 1639.94 | |
| FATTY_ACID_METABOLISM | 472.86 | |
| G2M_CHECKPOINT | 2221.20 | |
| GLYCOLYSIS | 1555.43 | |
| HEDGEHOG_SIGNALING | 524.57 | |
| HEME_METABOLISM | 1132.27 | |
| HYPOXIA | 2495.27 | |
| IL2_STAT5_SIGNALING | 1760.90 | |
| IL6_JAK_STAT3_SIGNALING | 2961.22 | |
| INFLAMMATORY_RESPONSE | 2908.61 | |
| INTERFERON_ALPHA_RESPONSE | 552.46 | |
| INTERFERON_GAMMA_RESPONSE | 3648.11 | |
| KRAS_SIGNALING_DN | 541.14 | |
| KRAS_SIGNALING_UP | 2158.99 | |
| MITOTIC_SPINDLE | 3866.78 | |
| MTORC1_SIGNALING | 2161.48 | |
| MYC_TARGETS_V1 | 1972.43 | |
| MYC_TARGETS_V2 | 377.60 | |
| MYOGENESIS | 1589.58 | |
| NOTCH_SIGNALING | 215.24 | |
| OXIDATIVE_PHOSPHORYLATION | 927.68 | |
| P53_PATHWAY | 2226.60 | |
| PANCREAS_BETA_CELLS | 172.43 | |
| PEROXISOME | 763.22 | |
| PI3K_AKT_MTOR_SIGNALING | 4893.14 | |
| PROTEIN_SECRETION | 1266.35 | |
| REACTIVE_OXYGEN_SPECIES_PATHWAY | 361.24 | |
| SPERMATOGENESIS | 761.26 | |
| TGF_BETA_SIGNALING | 1090.89 | |
| TNFA_SIGNALING_VIA_NFKB | 2450.70 | |
| UNFOLDED_PROTEIN_RESPONSE | 717.38 | |
| UV_RESPONSE_DN | 2521.69 | |
| UV_RESPONSE_UP | 2184.21 | |
| WNT_BETA_CATENIN_SIGNALING | 1240.87 | |
| XENOBIOTIC_METABOLISM | 1219.56 |
Hallmarks-of-Cancer reach
Anti-tumor matches — the "ideal patient" search
| Sample | Cancer type | cos to ideal |
|---|---|---|
| EPT0291 | EPN | 0.850 |
| SRR23303752 | — | 0.848 |
| aMVAC.P_005_TURBT_S223 | — | 0.833 |
| SRR10899984 | — | 0.833 |
| SRR12202498 | — | 0.830 |
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