Gefitinib
Sign in to save this workspacePrimary targets: EGFR · FDA status: FDA Approved
Selectivity scorecard
KISS
99.25
Gini
0.650
CATDS
0.022
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 Gefitinib. Strongest target: EGFR at 99.9% inhibition.
Accessible data table
| Rank | Target | Inhibition % | Residual activity % |
|---|---|---|---|
| 1 | EGFR | 99.9% | 0.1% |
| 2 | ERBB4_HER4 | 96.8% | 3.2% |
| 3 | ERBB2_HER2 | 92.2% | 7.8% |
| 4 | DDR1 | 88.3% | 11.7% |
| 5 | LYN | 80.1% | 19.9% |
| 6 | LOK_STK10 | 79.2% | 20.8% |
| 7 | EPHA6 | 77.4% | 22.6% |
| 8 | LCK | 71.4% | 28.6% |
| 9 | RIPK3 | 71.4% | 28.6% |
| 10 | MNK1 | 68.7% | 31.3% |
| 11 | FLT3 | 62.7% | 37.3% |
| 12 | IRAK1 | 62.4% | 37.6% |
| 13 | SIK2 | 61.4% | 38.6% |
| 14 | SIK1 | 57.7% | 42.3% |
| 15 | RIPK2 | 57.5% | 42.5% |
| 16 | MNK2 | 54.3% | 45.7% |
| 17 | HIPK4 | 50.4% | 49.6% |
| 18 | BLK | 49.4% | 50.6% |
| 19 | MEK5 | 48.5% | 51.5% |
| 20 | P38A_MAPK14 | 47.5% | 52.5% |
Selectivity landscape
Where Gefitinib sits in the 92-drug selectivity landscape (KISS vs Gini). The highlighted point is Gefitinib.
Atlas insights for Gefitinib
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 | 1865.47 | |
| ALLOGRAFT_REJECTION | 5591.30 | |
| ANDROGEN_RESPONSE | 1461.87 | |
| ANGIOGENESIS | 920.45 | |
| APICAL_JUNCTION | 6060.96 | |
| APICAL_SURFACE | 526.47 | |
| APOPTOSIS | 4714.86 | |
| BILE_ACID_METABOLISM | 773.95 | |
| CHOLESTEROL_HOMEOSTASIS | 1000.63 | |
| COAGULATION | 604.08 | |
| COMPLEMENT | 3618.17 | |
| DNA_REPAIR | 1344.71 | |
| E2F_TARGETS | 3360.77 | |
| EPITHELIAL_MESENCHYMAL_TRANSITION | 1472.96 | |
| ESTROGEN_RESPONSE_EARLY | 2011.81 | |
| ESTROGEN_RESPONSE_LATE | 1910.00 | |
| FATTY_ACID_METABOLISM | 621.38 | |
| G2M_CHECKPOINT | 2959.58 | |
| GLYCOLYSIS | 2071.72 | |
| HEDGEHOG_SIGNALING | 702.91 | |
| HEME_METABOLISM | 1304.71 | |
| HYPOXIA | 3032.00 | |
| IL2_STAT5_SIGNALING | 2040.22 | |
| IL6_JAK_STAT3_SIGNALING | 3034.55 | |
| INFLAMMATORY_RESPONSE | 3366.51 | |
| INTERFERON_ALPHA_RESPONSE | 560.56 | |
| INTERFERON_GAMMA_RESPONSE | 4099.81 | |
| KRAS_SIGNALING_DN | 702.58 | |
| KRAS_SIGNALING_UP | 2388.80 | |
| MITOTIC_SPINDLE | 4126.69 | |
| MTORC1_SIGNALING | 2767.33 | |
| MYC_TARGETS_V1 | 2265.53 | |
| MYC_TARGETS_V2 | 429.66 | |
| MYOGENESIS | 2126.69 | |
| NOTCH_SIGNALING | 272.02 | |
| OXIDATIVE_PHOSPHORYLATION | 1076.54 | |
| P53_PATHWAY | 2553.39 | |
| PANCREAS_BETA_CELLS | 195.28 | |
| PEROXISOME | 822.04 | |
| PI3K_AKT_MTOR_SIGNALING | 5721.43 | |
| PROTEIN_SECRETION | 1375.13 | |
| REACTIVE_OXYGEN_SPECIES_PATHWAY | 390.24 | |
| SPERMATOGENESIS | 1014.10 | |
| TGF_BETA_SIGNALING | 1279.77 | |
| TNFA_SIGNALING_VIA_NFKB | 3038.83 | |
| UNFOLDED_PROTEIN_RESPONSE | 703.02 | |
| UV_RESPONSE_DN | 3038.91 | |
| UV_RESPONSE_UP | 2519.77 | |
| WNT_BETA_CATENIN_SIGNALING | 1526.11 | |
| XENOBIOTIC_METABOLISM | 1388.27 |
Anti-tumor matches — the "ideal patient" search
| Sample | Cancer type | cos to ideal |
|---|---|---|
| EPT0291 | EPN | 0.851 |
| SRR23303752 | — | 0.846 |
| TCGA-CF-A5U8-01A-11R-A28M-07 | — | 0.831 |
| SRR12202498 | — | 0.831 |
| aMVAC.P_005_TURBT_S223 | — | 0.831 |
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