Assay Detail
Binding
CHEMBL3756073
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human Ret Y791F mutant by radiometric assay in presence of [gamma-33P]-ATP
3
Total Activities
3
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
A Pyrazolo[3,4-d]pyrimidin-4-amine Derivative Containing an Isoxazole Moiety Is a Selective and Potent Inhibitor of RET Gatekeeper Mutants.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 8.17 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3753341 | — | — | 1 | 8.52 |
| CHEMBL2105717 | CABOZANTINIB | 4.0 | 1 | 8.15 |
| CHEMBL2058538 | — | — | 1 | 7.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3753341 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2105717 | CABOZANTINIB | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2058538 | — | IC50 | = | 14.0 | nM | 7.85 |