Afatinib
Sign in to save this workspacePrimary targets: EGFR, ERBB2_HER2, ERBB4_HER4 · FDA status: FDA Approved
Selectivity scorecard
KISS
98.50
Gini
0.709
CATDS
0.020
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 Afatinib. Strongest target: ERBB4_HER4 at 100.0% inhibition.
Accessible data table
| Rank | Target | Inhibition % | Residual activity % |
|---|---|---|---|
| 1 | ERBB4_HER4 | 100.0% | 0.0% |
| 2 | EGFR | 100.0% | 0.0% |
| 3 | ERBB2_HER2 | 98.9% | 1.1% |
| 4 | BLK | 96.8% | 3.2% |
| 5 | TXK | 93.0% | 7.0% |
| 6 | EPHA6 | 93.0% | 7.0% |
| 7 | BTK | 88.6% | 11.4% |
| 8 | DDR1 | 87.5% | 12.5% |
| 9 | LCK | 83.5% | 16.4% |
| 10 | C_MER | 82.8% | 17.2% |
| 11 | LYN | 78.7% | 21.3% |
| 12 | P38A_MAPK14 | 78.1% | 21.9% |
| 13 | IRAK1 | 72.1% | 27.9% |
| 14 | ABL1 | 67.1% | 32.9% |
| 15 | HCK | 66.5% | 33.5% |
| 16 | C_MET | 65.7% | 34.3% |
| 17 | DYRK2 | 62.6% | 37.4% |
| 18 | PEAK1 | 59.8% | 40.2% |
| 19 | FGR | 59.2% | 40.8% |
| 20 | ITK | 58.7% | 41.3% |
Selectivity landscape
Where Afatinib sits in the 92-drug selectivity landscape (KISS vs Gini). The highlighted point is Afatinib.
Atlas insights for Afatinib
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 | 1973.02 | |
| ALLOGRAFT_REJECTION | 7007.21 | |
| ANDROGEN_RESPONSE | 1489.93 | |
| ANGIOGENESIS | 1139.15 | |
| APICAL_JUNCTION | 6861.03 | |
| APICAL_SURFACE | 645.30 | |
| APOPTOSIS | 5118.75 | |
| BILE_ACID_METABOLISM | 759.65 | |
| CHOLESTEROL_HOMEOSTASIS | 1119.55 | |
| COAGULATION | 735.61 | |
| COMPLEMENT | 4273.72 | |
| DNA_REPAIR | 1716.00 | |
| E2F_TARGETS | 3286.68 | |
| EPITHELIAL_MESENCHYMAL_TRANSITION | 1588.46 | |
| ESTROGEN_RESPONSE_EARLY | 2177.97 | |
| ESTROGEN_RESPONSE_LATE | 2154.03 | |
| FATTY_ACID_METABOLISM | 537.06 | |
| G2M_CHECKPOINT | 3162.63 | |
| GLYCOLYSIS | 2096.77 | |
| HEDGEHOG_SIGNALING | 890.04 | |
| HEME_METABOLISM | 1404.86 | |
| HYPOXIA | 3257.16 | |
| IL2_STAT5_SIGNALING | 2444.18 | |
| IL6_JAK_STAT3_SIGNALING | 3577.80 | |
| INFLAMMATORY_RESPONSE | 3936.83 | |
| INTERFERON_ALPHA_RESPONSE | 642.70 | |
| INTERFERON_GAMMA_RESPONSE | 4825.33 | |
| KRAS_SIGNALING_DN | 710.51 | |
| KRAS_SIGNALING_UP | 2729.41 | |
| MITOTIC_SPINDLE | 4868.24 | |
| MTORC1_SIGNALING | 2983.34 | |
| MYC_TARGETS_V1 | 2312.72 | |
| MYC_TARGETS_V2 | 457.28 | |
| MYOGENESIS | 2413.94 | |
| NOTCH_SIGNALING | 311.65 | |
| OXIDATIVE_PHOSPHORYLATION | 951.74 | |
| P53_PATHWAY | 2912.78 | |
| PANCREAS_BETA_CELLS | 255.82 | |
| PEROXISOME | 845.03 | |
| PI3K_AKT_MTOR_SIGNALING | 6298.78 | |
| PROTEIN_SECRETION | 1503.15 | |
| REACTIVE_OXYGEN_SPECIES_PATHWAY | 470.07 | |
| SPERMATOGENESIS | 985.46 | |
| TGF_BETA_SIGNALING | 1356.07 | |
| TNFA_SIGNALING_VIA_NFKB | 3441.26 | |
| UNFOLDED_PROTEIN_RESPONSE | 799.51 | |
| UV_RESPONSE_DN | 3159.56 | |
| UV_RESPONSE_UP | 2749.54 | |
| WNT_BETA_CATENIN_SIGNALING | 1543.47 | |
| XENOBIOTIC_METABOLISM | 1505.81 |
Hallmarks-of-Cancer reach
Anti-tumor matches — the "ideal patient" search
| Sample | Cancer type | cos to ideal |
|---|---|---|
| EPT0291 | EPN | 0.845 |
| SRR23303752 | — | 0.839 |
| SRR10899984 | — | 0.830 |
| TCGA-CF-A5U8-01A-11R-A28M-07 | — | 0.828 |
| aMVAC.P_005_TURBT_S223 | — | 0.826 |
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