Assay Detail
Binding
CHEMBL3756067
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human wild type RET by radiometric assay in presence of [gamma-33P]-ATP
21
Total Activities
21
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 | 21 | 6.93 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3753341 | — | — | 1 | 8.85 |
| CHEMBL3753512 | — | — | 1 | 8.70 |
| CHEMBL3751904 | — | — | 1 | 8.30 |
| CHEMBL3752118 | — | — | 1 | 7.57 |
| CHEMBL3752395 | — | — | 1 | 7.39 |
| CHEMBL3753958 | — | — | 1 | 7.39 |
| CHEMBL3752879 | — | — | 1 | 7.28 |
| CHEMBL3752712 | — | — | 1 | 7.17 |
| CHEMBL3754346 | — | — | 1 | 7.13 |
| CHEMBL3753242 | — | — | 1 | 7.02 |
| CHEMBL3754092 | — | — | 1 | 6.82 |
| CHEMBL3754442 | — | — | 1 | 6.72 |
| CHEMBL3751965 | — | — | 1 | 6.68 |
| CHEMBL3752025 | — | — | 1 | 6.67 |
| CHEMBL3753903 | — | — | 1 | 6.62 |
| CHEMBL3753714 | — | — | 1 | 6.62 |
| CHEMBL3752736 | — | — | 1 | 6.23 |
| CHEMBL3754247 | — | — | 1 | 6.04 |
| CHEMBL3752827 | — | — | 1 | 6.04 |
| CHEMBL3753503 | — | — | 1 | 5.31 |
| CHEMBL3754195 | — | — | 1 | 5.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3753341 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3753512 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3751904 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3752118 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3752395 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL3753958 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL3752879 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL3752712 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL3754346 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL3753242 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL3754092 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3754442 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3751965 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL3752025 | — | IC50 | = | 213.0 | nM | 6.67 |
| CHEMBL3753903 | — | IC50 | = | 241.0 | nM | 6.62 |
| CHEMBL3753714 | — | IC50 | = | 241.0 | nM | 6.62 |
| CHEMBL3752736 | — | IC50 | = | 583.0 | nM | 6.23 |
| CHEMBL3754247 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL3752827 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL3753503 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL3754195 | — | IC50 | = | 8330.0 | nM | 5.08 |