Assay Detail
Binding
CHEMBL3756068
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human Ret V804M mutant by radiometric assay in presence of [gamma-33P]-ATP
19
Total Activities
19
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 | 19 | 6.30 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3753341 | — | — | 1 | 8.40 |
| CHEMBL3753512 | — | — | 1 | 7.85 |
| CHEMBL3751904 | — | — | 1 | 7.39 |
| CHEMBL3752118 | — | — | 1 | 6.74 |
| CHEMBL3752712 | — | — | 1 | 6.66 |
| CHEMBL3752395 | — | — | 1 | 6.45 |
| CHEMBL3752879 | — | — | 1 | 6.45 |
| CHEMBL2105717 | CABOZANTINIB | 4.0 | 1 | 6.45 |
| CHEMBL3753958 | — | — | 1 | 6.28 |
| CHEMBL3754346 | — | — | 1 | 6.25 |
| CHEMBL3752025 | — | — | 1 | 6.04 |
| CHEMBL3753242 | — | — | 1 | 6.03 |
| CHEMBL3753903 | — | — | 1 | 5.80 |
| CHEMBL3753714 | — | — | 1 | 5.70 |
| CHEMBL3751965 | — | — | 1 | 5.68 |
| CHEMBL2058538 | — | — | 1 | 5.58 |
| CHEMBL3753503 | — | — | 1 | 5.43 |
| CHEMBL3752736 | — | — | 1 | 5.25 |
| CHEMBL3754247 | — | — | 1 | 5.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3753341 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3753512 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3751904 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL3752118 | — | IC50 | = | 182.0 | nM | 6.74 |
| CHEMBL3752712 | — | IC50 | = | 217.0 | nM | 6.66 |
| CHEMBL3752395 | — | IC50 | = | 355.0 | nM | 6.45 |
| CHEMBL3752879 | — | IC50 | = | 354.0 | nM | 6.45 |
| CHEMBL2105717 | CABOZANTINIB | IC50 | = | 358.0 | nM | 6.45 |
| CHEMBL3753958 | — | IC50 | = | 531.0 | nM | 6.28 |
| CHEMBL3754346 | — | IC50 | = | 557.0 | nM | 6.25 |
| CHEMBL3752025 | — | IC50 | = | 903.0 | nM | 6.04 |
| CHEMBL3753242 | — | IC50 | = | 927.0 | nM | 6.03 |
| CHEMBL3753903 | — | IC50 | = | 1570.0 | nM | 5.80 |
| CHEMBL3753714 | — | IC50 | = | 1990.0 | nM | 5.70 |
| CHEMBL3751965 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL2058538 | — | IC50 | = | 2650.0 | nM | 5.58 |
| CHEMBL3753503 | — | IC50 | = | 3680.0 | nM | 5.43 |
| CHEMBL3752736 | — | IC50 | = | 5680.0 | nM | 5.25 |
| CHEMBL3754247 | — | IC50 | = | 5880.0 | nM | 5.23 |