Assay Detail
Binding
CHEMBL4766673
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human RET using KKKSPGEYVNIEFG as substrate incubated for 15 mins followed by Mg/ATP addition and measured after 40 mins by [gamma-33P]-ATP assay
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Proto-oncogene tyrosine-protein kinase receptor Ret (CHEMBL2041) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structural optimization and structure-activity relationship studies of N-phenyl-7,8-dihydro-6H-pyrimido[5,4-b][1,4]oxazin-4-amine derivatives as a new class of inhibitors of RET and its drug resistance mutants.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 6.74 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 8.05 |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 8.05 |
| CHEMBL4779887 | — | — | 1 | 8.00 |
| CHEMBL4793380 | — | — | 1 | 8.00 |
| CHEMBL4789515 | — | — | 1 | 8.00 |
| CHEMBL2105717 | CABOZANTINIB | 4.0 | 1 | 7.89 |
| CHEMBL4784865 | — | — | 1 | 7.68 |
| CHEMBL4784000 | — | — | 1 | 7.66 |
| CHEMBL4797687 | — | — | 1 | 7.60 |
| CHEMBL4798046 | — | — | 1 | 7.30 |
| CHEMBL4794949 | — | — | 1 | 7.11 |
| CHEMBL4797171 | — | — | 1 | 6.75 |
| CHEMBL4793991 | — | — | 1 | 6.64 |
| CHEMBL4793949 | — | — | 1 | 6.51 |
| CHEMBL4786825 | — | — | 1 | 6.49 |
| CHEMBL4798842 | — | — | 1 | 6.49 |
| CHEMBL4789912 | — | — | 1 | 6.11 |
| CHEMBL4786580 | — | — | 1 | 6.06 |
| CHEMBL4798574 | — | — | 1 | 6.03 |
| CHEMBL4792943 | — | — | 1 | 5.97 |
| CHEMBL4797671 | — | — | 1 | 5.83 |
| CHEMBL4794893 | — | — | 1 | 5.65 |
| CHEMBL4796114 | — | — | 1 | 5.51 |
| CHEMBL4783259 | — | — | 1 | 5.50 |
| CHEMBL4781910 | — | — | 1 | 5.17 |
| CHEMBL4779377 | — | — | 1 | 5.06 |
| CHEMBL4794285 | — | — | 1 | - |
| CHEMBL4788477 | — | — | 1 | - |
| CHEMBL4781659 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1336 | SORAFENIB | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL24828 | VANDETANIB | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4779887 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4793380 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4789515 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2105717 | CABOZANTINIB | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4784865 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4784000 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4797687 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4798046 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4794949 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL4797171 | — | IC50 | = | 177.0 | nM | 6.75 |
| CHEMBL4793991 | — | IC50 | = | 227.0 | nM | 6.64 |
| CHEMBL4793949 | — | IC50 | = | 306.0 | nM | 6.51 |
| CHEMBL4786825 | — | IC50 | = | 324.0 | nM | 6.49 |
| CHEMBL4798842 | — | IC50 | = | 322.0 | nM | 6.49 |
| CHEMBL4789912 | — | IC50 | = | 781.0 | nM | 6.11 |
| CHEMBL4786580 | — | IC50 | = | 865.0 | nM | 6.06 |
| CHEMBL4798574 | — | IC50 | = | 944.0 | nM | 6.03 |
| CHEMBL4792943 | — | IC50 | = | 1071.0 | nM | 5.97 |
| CHEMBL4797671 | — | IC50 | = | 1474.0 | nM | 5.83 |
| CHEMBL4794893 | — | IC50 | = | 2223.0 | nM | 5.65 |
| CHEMBL4796114 | — | IC50 | = | 3073.0 | nM | 5.51 |
| CHEMBL4783259 | — | IC50 | = | 3154.0 | nM | 5.50 |
| CHEMBL4781910 | — | IC50 | = | 6811.0 | nM | 5.17 |
| CHEMBL4779377 | — | IC50 | = | 8766.0 | nM | 5.06 |
| CHEMBL4794285 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4788477 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4781659 | — | IC50 | > | 10000.0 | nM | - |