Assay Detail
Binding
CHEMBL4836452
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Inhibition of RET wild type (unknown origin)
11
Total Activities
11
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
Discovery and optimization of selective RET inhibitors via scaffold hopping.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 8.56 | 9.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4872605 | — | — | 1 | 9.44 |
| CHEMBL4870957 | — | — | 1 | 9.17 |
| CHEMBL4582651 | PRALSETINIB | 4.0 | 1 | 9.11 |
| CHEMBL4845703 | — | — | 1 | 9.05 |
| CHEMBL4861957 | — | — | 1 | 8.95 |
| CHEMBL4846521 | — | — | 1 | 8.89 |
| CHEMBL4859281 | — | — | 1 | 8.86 |
| CHEMBL4875034 | — | — | 1 | 8.80 |
| CHEMBL4862303 | — | — | 1 | 7.72 |
| CHEMBL4848545 | — | — | 1 | 7.13 |
| CHEMBL4859271 | — | — | 1 | 7.03 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4872605 | — | IC50 | = | 0.36 | nM | 9.44 |
| CHEMBL4870957 | — | IC50 | = | 0.68 | nM | 9.17 |
| CHEMBL4582651 | PRALSETINIB | IC50 | = | 0.78 | nM | 9.11 |
| CHEMBL4845703 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL4861957 | — | IC50 | = | 1.12 | nM | 8.95 |
| CHEMBL4846521 | — | IC50 | = | 1.29 | nM | 8.89 |
| CHEMBL4859281 | — | IC50 | = | 1.39 | nM | 8.86 |
| CHEMBL4875034 | — | IC50 | = | 1.58 | nM | 8.80 |
| CHEMBL4862303 | — | IC50 | = | 19.1 | nM | 7.72 |
| CHEMBL4848545 | — | IC50 | = | 73.87 | nM | 7.13 |
| CHEMBL4859271 | — | IC50 | = | 92.99 | nM | 7.03 |