UniProt P04049 · PDB · AlphaFold · Substrate: MEK1 (K97R) · Clone: catalytic (aa306-648)
Top inhibitors
| # | Drug | Inhibition | Residual | KISS | Gini |
|---|---|---|---|---|---|
| 1 | Apatinib | 100.0% | 0.0% | 97.73 | 0.704 |
| 2 | Ponatinib | 100.0% | 0.0% | 78.23 | 0.534 |
| 3 | Ripretinib | 100.0% | 0.0% | 92.95 | 0.674 |
| 4 | Sorafenib | 100.0% | 0.0% | 96.72 | 0.776 |
| 5 | Regorafenib | 99.9% | 0.1% | 95.99 | 0.719 |
| 6 | Upadacitinib | 99.9% | 0.1% | 97.98 | 0.663 |
| 7 | Umbralisib | 99.8% | 0.2% | 98.74 | 0.670 |
| 8 | Dabrafenib | 99.8% | 0.2% | 94.74 | 0.633 |
| 9 | Encorafenib | 99.7% | 0.3% | 98.50 | 0.755 |
| 10 | Nilotinib | 98.3% | 1.7% | 96.49 | 0.765 |
| 11 | Rabusertib | 95.6% | 4.4% | 98.74 | 0.687 |
| 12 | Pazopanib | 95.5% | 4.5% | 97.49 | 0.672 |
| 13 | Vemurafenib | 95.2% | 4.8% | 96.49 | 0.598 |
| 14 | Dasatinib | 74.3% | 25.7% | 87.97 | 0.699 |
| 15 | Imatinib | 74.0% | 26.0% | 99.00 | 0.718 |
| 16 | Tivozanib | 67.6% | 32.4% | 92.42 | 0.673 |
| 17 | Erdafitinib | 61.4% | 38.6% | 95.71 | 0.737 |
| 18 | Paxalisib | 54.2% | 45.8% | 99.75 | 0.609 |
| 19 | Repotrectinib | 51.6% | 48.4% | 84.21 | 0.608 |
| 20 | Ibrutinib | 37.5% | 62.5% | 94.74 | 0.723 |
Paralog block
ARAF, BRAF, RAF1
EMT expression
- Mesenchymal log2(TPM+1): 5.79
- Epithelial log2(TPM+1): 5.52
- Fold change: 0.27
- Status: No significant change
Selectivity landscape vs inhibition on RAF1
Each point is one of the 92 approved drugs; color = inhibition % on RAF1.
Mutation lollipop
Cancer-associated mutations plotted by residue position. Marker size + color scale with the number of distinct cancer reports.
Variants (1)
Mutation × cancer associations
| Mutation | Cancer | Organ | Source |
|---|---|---|---|
| R391W | carcinoid-endocrine_tumour_lung | Lung | ref |
| R391W | lymphoid_neoplasm_haematopoietic_and_lymphoid_tissue | Blood/Lymphatic System | ref |
| R391W | malignant_melanoma_skin | Skin | ref |
| R391W | CLLE-ES | Blood/Lymphatic System | ref |
| R391W | KIRP-US | Kidney | ref |
| R391W | KIRP | Kidney | ref |
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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