Assay Detail
Binding
CHEMBL899077
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Inhibition of RET kinase in Sf9 cells
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | Sf9 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Proto-oncogene tyrosine-protein kinase receptor Ret (CHEMBL2041) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The discovery of substituted 4-(3-hydroxyanilino)-quinolines as potent RET kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 7.41 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL237347 | GW559768X | — | 1 | 8.52 |
| CHEMBL237344 | — | — | 1 | 8.22 |
| CHEMBL237128 | — | — | 1 | 7.60 |
| CHEMBL237127 | — | — | 1 | 7.60 |
| CHEMBL399208 | — | — | 1 | 7.47 |
| CHEMBL395358 | — | — | 1 | 7.12 |
| CHEMBL237126 | — | — | 1 | 7.12 |
| CHEMBL237345 | — | — | 1 | 7.10 |
| CHEMBL237557 | — | — | 1 | 7.07 |
| CHEMBL395359 | — | — | 1 | 7.05 |
| CHEMBL237346 | — | — | 1 | 7.02 |
| CHEMBL392856 | — | — | 1 | 7.00 |
| CHEMBL236928 | — | — | 1 | - |
| CHEMBL393115 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL237347 | GW559768X | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL237344 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL237128 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL237127 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL399208 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL395358 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL237126 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL237345 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL237557 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL395359 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL237346 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL392856 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL236928 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL393115 | — | IC50 | > | 1000.0 | nM | - |