UniProt P00533 · PDB · AlphaFold · Substrate: pEY + Mn · Clone: cytoplasmic (aa 668-1210)
Top inhibitors
| # | Drug | Inhibition | Residual | KISS | Gini |
|---|---|---|---|---|---|
| 1 | Lazertinib | 100.0% | 0.0% | 97.47 | 0.674 |
| 2 | Neratinib | 100.0% | 0.0% | 93.18 | 0.597 |
| 3 | Mobocertinib | 100.0% | 0.0% | 97.22 | 0.757 |
| 4 | Afatinib | 100.0% | 0.0% | 98.50 | 0.709 |
| 5 | Gefitinib | 99.9% | 0.1% | 99.25 | 0.650 |
| 6 | Dacomitinib | 99.8% | 0.2% | 97.99 | 0.664 |
| 7 | Erlotinib | 99.4% | 0.6% | 99.75 | 0.695 |
| 8 | Ibrutinib | 99.3% | 0.7% | 94.74 | 0.723 |
| 9 | Vandetanib | 99.3% | 0.7% | 95.74 | 0.723 |
| 10 | Bosutinib | 99.3% | 0.7% | 87.22 | 0.555 |
| 11 | Lapatinib | 99.2% | 0.8% | 99.25 | 0.616 |
| 12 | Pralsetinib | 99.1% | 0.9% | 93.43 | 0.643 |
| 13 | Osimertinib | 99.1% | 0.9% | 97.24 | 0.733 |
| 14 | Brigatinib | 98.5% | 1.5% | 82.96 | 0.513 |
| 15 | Canertinib | 98.4% | 1.6% | 96.49 | 0.671 |
| 16 | Dasatinib | 97.9% | 2.1% | 87.97 | 0.699 |
| 17 | Fostamatinib | 97.8% | 2.2% | 96.74 | 0.613 |
| 18 | Defactinib | 94.6% | 5.4% | 92.68 | 0.450 |
| 19 | Gilteritinib | 91.0% | 9.0% | 88.97 | 0.506 |
| 20 | Zanubrutinib | 88.2% | 11.8% | 98.24 | 0.788 |
Paralog block
No paralog group registered for this kinase.
EMT expression
- Mesenchymal log2(TPM+1): 4.62
- Epithelial log2(TPM+1): 3.13
- Fold change: 1.50
- Status: Upregulated
Selectivity landscape vs inhibition on EGFR
Each point is one of the 92 approved drugs; color = inhibition % on EGFR.
Mutation lollipop
Cancer-associated mutations plotted by residue position. Marker size + color scale with the number of distinct cancer reports.
Variants (64)
EGFR (A763_Y764insFHEA)
indel
EGFR (A763_Y764insFQEA)
indel
EGFR (A767_S768insTLA)
indel
EGFR (C775S/T790M/L858R)
compound
EGFR (C797A)
point
EGFR (C797G/L858R)
compound
EGFR (C797S)
point
EGFR (C797S/L858R)
compound
EGFR (D761Y)
point
EGFR (D770GY)
point
EGFR (D770_N771insG)
indel
EGFR (D770_N771insNPG)
indel
EGFR (D770_N771insNPG/T790M)
compound
EGFR (G719C)
point
EGFR (G719D)
point
EGFR (G719S)
point
EGFR (K716A)
point
EGFR (K716A/C797S/L858R)
compound
EGFR (K716A/T790M/C797S/L858R)
compound
EGFR (K716Q/L718Q)
compound
EGFR (K728A)
point
EGFR (K728A/T790M/C797S/L858R)
point
EGFR (L718Q)
point
EGFR (L747S)
point
EGFR (L792F)
point
EGFR (L792F/L858R)
compound
EGFR (L792H)
point
EGFR (L792H/C797S/L858R)
compound
EGFR (L792H/L858R)
compound
EGFR (L858R)
point
EGFR (L861Q)
point
EGFR (N771_P772insH)
indel
EGFR (N771_P772insN)
indel
EGFR (R999A)
point
EGFR (S768I)
point
EGFR (T790M)
point
EGFR (T790M/C797G/L858R)
compound
EGFR (T790M/C797S)
compound
EGFR (T790M/C797S/L858R)
compound
EGFR (T790M/L792F/C797S/L858R)
compound
EGFR (T790M/L792F/L858R)
compound
EGFR (T790M/L792H/C797S/L858R)
compound
EGFR (T790M/L792H/L858R)
compound
EGFR (T790M/L858R)
compound
EGFR (V769_D770insGE)
indel
EGFR (V948R)
point
EGFR (d746)
point
EGFR (d746-750)
unknown
EGFR (d746-750/C775S/T790M/L858R)
compound
EGFR (d746-750/C797A)
compound
EGFR (d746-750/C797S)
compound
EGFR (d746-750/G724S)
compound
EGFR (d746-750/S768I)
compound
EGFR (d746-750/T790M)
point
EGFR (d746-750/T790M/C797S)
compound
EGFR (d746-750/T790M/C797S/L858R)
compound
EGFR (d746-750/T790M/L792F)
compound
EGFR (d746-750/T790M/L792H)
compound
EGFR (d746-750/T790M/L798I)
compound
EGFR (d746-750/T790M/L858R)
compound
EGFR (d747-749)
indel
EGFR (d747-749/A750P)
point
EGFR (d747-752/P753S)
point
EGFR (d752-759)
unknown
Mutation × cancer associations
| Mutation | Cancer | Organ | Source |
|---|---|---|---|
| A750P | carcinoma_lung | Lung | ref |
| A750P | lymphoid_neoplasm_haematopoietic_and_lymphoid_tissue | Blood/Lymphatic System | ref |
| A763 | carcinoma_lung | Lung | ref |
| A767 | carcinoma_lung | Lung | ref |
| A767 | glioma_central_nervous_system | Brain/CNS | ref |
| A767 | carcinoma_liver | Liver | ref |
| A767 | carcinoma_NS | Other | ref |
| A767 | LIHC | Liver | ref |
| A767 | LUAD | Lung | ref |
| C797G | carcinoma_lung | Lung | ref |
| C797A | carcinoma_lung | Lung | ref |
| C797S | carcinoma_lung | Lung | ref |
| D761Y | other_lung | Lung | ref |
| D761Y | carcinoma_lung | Lung | ref |
| D770 | carcinoma_lung | Lung | ref |
| D770 | carcinoma_endometrium | Uterus | ref |
| D770 | thymic_carcinoma_thymus | Thyroid | ref |
| D770 | fibrous_hamartoma_of_infancy_soft_tissue | Soft Tissue | ref |
| D770 | carcinoma_urinary_tract | Bladder | ref |
| D770 | glioma_central_nervous_system | Brain/CNS | ref |
| D770 | carcinoma_upper_aerodigestive_tract | Brain/CNS | ref |
| D770GY | glioma_central_nervous_system | Brain/CNS | ref |
| D770GY | carcinoma_upper_aerodigestive_tract | Brain/CNS | ref |
| G719C | carcinoma_lung | Lung | ref |
| G719C | mesothelioma_pleura | Lung | ref |
| G719C | carcinoma_NS | Other | ref |
| G719C | glioma_central_nervous_system | Brain/CNS | ref |
| G719C | malignant_melanoma_NS | Skin | ref |
| G719C | other_lung | Lung | ref |
| G719C | GBM-US | Brain/CNS | ref |
Showing 30 of 161 associations.
3D structure
Embedded NGL viewer pulls a representative PDB entry (or AlphaFold model if no experimental structure is registered). Heavy bundle — loaded only on demand.
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