UniProt P15056 · PDB · AlphaFold · Substrate: MEK1 (K97R) · Clone: full-length
Top inhibitors
| # | Drug | Inhibition | Residual | KISS | Gini |
|---|---|---|---|---|---|
| 1 | Ripretinib | 100.0% | 0.0% | 92.95 | 0.674 |
| 2 | Ponatinib | 99.4% | 0.6% | 78.23 | 0.534 |
| 3 | Sorafenib | 98.5% | 1.5% | 96.72 | 0.776 |
| 4 | Dabrafenib | 98.3% | 1.7% | 94.74 | 0.633 |
| 5 | Regorafenib | 98.3% | 1.7% | 95.99 | 0.719 |
| 6 | Encorafenib | 98.0% | 2.0% | 98.50 | 0.755 |
| 7 | Apatinib | 94.1% | 5.9% | 97.73 | 0.704 |
| 8 | Vemurafenib | 92.8% | 7.2% | 96.49 | 0.598 |
| 9 | Nilotinib | 85.8% | 14.2% | 96.49 | 0.765 |
| 10 | Dasatinib | 80.6% | 19.4% | 87.97 | 0.699 |
| 11 | Pazopanib | 79.3% | 20.7% | 97.49 | 0.672 |
| 12 | Umbralisib | 65.3% | 34.7% | 98.74 | 0.670 |
| 13 | Pacritinib | 58.5% | 41.5% | 88.64 | 0.452 |
| 14 | Gedatolisib | 56.5% | 43.5% | 99.75 | 0.611 |
| 15 | Erdafitinib | 54.1% | 45.9% | 95.71 | 0.737 |
| 16 | Upadacitinib | 49.6% | 50.4% | 97.98 | 0.663 |
| 17 | Dacomitinib | 46.6% | 53.4% | 97.99 | 0.664 |
| 18 | Tivozanib | 41.8% | 58.2% | 92.42 | 0.673 |
| 19 | Rabusertib | 41.1% | 58.9% | 98.74 | 0.687 |
| 20 | Canertinib | 40.7% | 59.3% | 96.49 | 0.671 |
Paralog block
ARAF, BRAF, RAF1
EMT expression
- Mesenchymal log2(TPM+1): 2.96
- Epithelial log2(TPM+1): 3.10
- Fold change: -0.15
- Status: No significant change
Selectivity landscape vs inhibition on BRAF
Each point is one of the 92 approved drugs; color = inhibition % on BRAF.
Mutation lollipop
Cancer-associated mutations plotted by residue position. Marker size + color scale with the number of distinct cancer reports.
Variants (11)
Mutation × cancer associations
| Mutation | Cancer | Organ | Source |
|---|---|---|---|
| D485G | carcinoma_lung | Lung | ref |
| D485G | Colon/Colorectal Cancer | Large Intestine | ref |
| P490Y | carcinoma_lung | Lung | ref |
| P490Y | Colon/Colorectal Cancer | Large Intestine | ref |
| R506K | carcinoma_lung | Lung | ref |
| R506K | Colon/Colorectal Cancer | Large Intestine | ref |
| V599E | malignant_melanoma_skin | Skin | ref |
| V599E | carcinoma_thyroid | Thyroid | ref |
| V599E | Colon/Colorectal Cancer | Large Intestine | ref |
| G464V | Breast Cancer | Breast | ref |
| G464V | carcinoma_breast | Breast | ref |
| G464V | carcinoma_lung | Lung | ref |
| G464V | lymphoid_neoplasm_haematopoietic_and_lymphoid_tissue | Blood/Lymphatic System | ref |
| G464V | carcinoma_biliary_tract | Biliary Tract | ref |
| G464V | carcinoma_large_intestine | Large Intestine | ref |
| G464V | carcinoma_ovary | Ovary | ref |
| G464V | BTCA-SG | Biliary Tract | ref |
| G464V | LUAD-US | Lung | ref |
| G464V | LUSC-US | Lung | ref |
| G464V | LUAD | Lung | ref |
| G464V | LUSC | Lung | ref |
| G464V | BRCA | Breast | ref |
| G469A | Lung Cancer | Lung | ref |
| G469A | Myeloma | Blood/Lymphatic System | ref |
| G469A | Unknown | Other | ref |
| G469A | carcinoma_lung | Lung | ref |
| G469A | carcinoma_large_intestine | Large Intestine | ref |
| G469A | carcinoma_oesophagus | Stomach/Digestive Tract | ref |
| G469A | lymphoid_neoplasm_haematopoietic_and_lymphoid_tissue | Blood/Lymphatic System | ref |
| G469A | malignant_melanoma_skin | Skin | ref |
Showing 30 of 156 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.
Annotations
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