Assay Detail
Binding
CHEMBL955807
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Inhibition of SCF-induced phosphorylation of c-Kit in MO7e cells by TR-FRET assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | MO7e |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Mast/stem cell growth factor receptor Kit (CHEMBL1936) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of aryl aminoquinazoline pyridones as potent, selective, and orally efficacious inhibitors of receptor tyrosine kinase c-Kit.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 7.62 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL497957 | — | — | 1 | 7.92 |
| CHEMBL522905 | — | — | 1 | 7.85 |
| CHEMBL496494 | — | — | 1 | 7.80 |
| CHEMBL525893 | — | — | 1 | 7.80 |
| CHEMBL497343 | — | — | 1 | 7.75 |
| CHEMBL497958 | — | — | 1 | 7.75 |
| CHEMBL506033 | — | — | 1 | 7.75 |
| CHEMBL498557 | — | — | 1 | 7.75 |
| CHEMBL497754 | — | — | 1 | 7.66 |
| CHEMBL496916 | — | — | 1 | 7.55 |
| CHEMBL504805 | — | — | 1 | 7.55 |
| CHEMBL496505 | — | — | 1 | 7.51 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 7.34 |
| CHEMBL496713 | — | — | 1 | 7.17 |
| CHEMBL525744 | — | — | 1 | 7.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL497957 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL522905 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL496494 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL525893 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL497343 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL497958 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL506033 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL498557 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL497754 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL496916 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL504805 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL496505 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL941 | IMATINIB | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL496713 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL525744 | — | IC50 | = | 72.0 | nM | 7.14 |