UniProt P07949 · PDB · AlphaFold · Substrate: TRK-C derived peptide · Clone: cytoplasmic (aa 658-1114)
Top inhibitors
| # | Drug | Inhibition | Residual | KISS | Gini |
|---|---|---|---|---|---|
| 1 | Pralsetinib | 100.0% | 0.0% | 93.43 | 0.643 |
| 2 | Ponatinib | 100.0% | 0.0% | 78.23 | 0.534 |
| 3 | Gilteritinib | 100.0% | 0.0% | 88.97 | 0.506 |
| 4 | Selpercatinib | 100.0% | 0.0% | 96.72 | 0.635 |
| 5 | Nintedanib | 100.0% | 0.0% | 90.23 | 0.608 |
| 6 | Fedratinib | 99.9% | 0.1% | 96.21 | 0.576 |
| 7 | Tivozanib | 99.7% | 0.3% | 92.42 | 0.673 |
| 8 | Alpelisib | 99.6% | 0.4% | 97.22 | 0.720 |
| 9 | Entrectinib | 99.6% | 0.4% | 93.69 | 0.671 |
| 10 | Lenvatinib | 98.8% | 1.2% | 97.74 | 0.726 |
| 11 | Regorafenib | 98.7% | 1.3% | 95.99 | 0.719 |
| 12 | Vandetanib | 98.6% | 1.4% | 95.74 | 0.723 |
| 13 | Tenalisib | 98.5% | 1.5% | 97.98 | 0.702 |
| 14 | Alectinib | 97.8% | 2.2% | 95.49 | 0.651 |
| 15 | Futibatinib | 97.7% | 2.3% | 98.48 | 0.718 |
| 16 | Cabozantinib | 97.5% | 2.5% | 92.73 | 0.751 |
| 17 | Sunitinib | 97.2% | 2.8% | 91.73 | 0.524 |
| 18 | Brigatinib | 94.9% | 5.1% | 82.96 | 0.513 |
| 19 | Erdafitinib | 94.7% | 5.3% | 95.71 | 0.737 |
| 20 | Sorafenib | 94.0% | 6.0% | 96.72 | 0.776 |
Paralog block
No paralog group registered for this kinase.
EMT expression
- Mesenchymal log2(TPM+1): 0.26
- Epithelial log2(TPM+1): 1.05
- Fold change: -0.80
- Status: No significant change
Selectivity landscape vs inhibition on RET
Each point is one of the 92 approved drugs; color = inhibition % on RET.
Mutation lollipop
Cancer-associated mutations plotted by residue position. Marker size + color scale with the number of distinct cancer reports.
Variants (28)
RET (A883F)
point
RET (E732K)
point
RET (E762Q)
point
RET (G691S)
point
RET (G810C)
point
RET (G810R)
point
RET (G810S)
point
RET (G810S/M918T)
compound
RET (L730I)
point
RET (L730M)
point
RET (L790F)
point
RET (M918T)
point
RET (R749T)
point
RET (R813Q)
point
RET (R912P)
point
RET (S891A)
point
RET (S904A)
point
RET (S904F)
point
RET (V738A)
point
RET (V778I)
point
RET (V804E)
point
RET (V804L)
point
RET (V804M)
point
RET (V804M/G810S)
compound
RET (Y791F)
point
RET (Y806C)
point
RET (Y806H)
point
RET (Y806N)
point
Mutation × cancer associations
| Mutation | Cancer | Organ | Source |
|---|---|---|---|
| A883F | carcinoma_thyroid | Thyroid | ref |
| G691S | carcinoma_breast | Breast | ref |
| G691S | haemangioblastoma_soft_tissue | Soft Tissue | ref |
| G691S | meningioma_meninges | Brain/CNS | ref |
| G691S | carcinoma_lung | Lung | ref |
| G691S | carcinoma_large_intestine | Large Intestine | ref |
| G691S | pheochromocytoma_adrenal_gland | Adrenal | ref |
| G691S | haematopoietic_neoplasm_haematopoietic_and_lymphoid_tissue | Blood/Lymphatic System | ref |
| G691S | BRCA-KR | Breast | ref |
| G691S | LAML-KR | Blood/Lymphatic System | ref |
| G691S | LUSC-KR | Blood/Lymphatic System | ref |
| G810C | carcinoma_lung | Lung | ref |
| G810C | carcinoma_thyroid | Thyroid | ref |
| G810R | carcinoma_lung | Lung | ref |
| G810R | carcinoma_thyroid | Thyroid | ref |
| G810S | carcinoma_lung | Lung | ref |
| G810S | carcinoma_thyroid | Thyroid | ref |
| L730I | carcinoma_thyroid | Thyroid | ref |
| M918T | carcinoma_thyroid | Thyroid | ref |
| M918T | pheochromocytoma_adrenal_gland | Adrenal | ref |
| M918T | carcinoma_breast | Breast | ref |
| M918T | carcinoma_biliary_tract | Biliary Tract | ref |
| M918T | PCPG | Adrenal | ref |
| E732K | carcinoma_lung | Lung | ref |
| E732K | carcinoma_thyroid | Thyroid | ref |
| S891A | carcinoma_thyroid | Thyroid | ref |
| S904F | carcinoma_large_intestine | Large Intestine | ref |
| V778I | carcinoma_breast | Breast | ref |
| V778I | BRCA-US | Breast | ref |
| V804M | carcinoma_thyroid | Thyroid | ref |
Showing 30 of 54 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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