Assay Detail
Binding
CHEMBL955806
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Inhibition of c-Kit by TR-FRET assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 | 19 | 7.74 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL494821 | — | — | 1 | 9.00 |
| CHEMBL496494 | — | — | 1 | 8.68 |
| CHEMBL493986 | — | — | 1 | 8.21 |
| CHEMBL498557 | — | — | 1 | 8.10 |
| CHEMBL497343 | — | — | 1 | 8.00 |
| CHEMBL525744 | — | — | 1 | 7.89 |
| CHEMBL497958 | — | — | 1 | 7.85 |
| CHEMBL504805 | — | — | 1 | 7.85 |
| CHEMBL506033 | — | — | 1 | 7.77 |
| CHEMBL496713 | — | — | 1 | 7.77 |
| CHEMBL496505 | — | — | 1 | 7.70 |
| CHEMBL522905 | — | — | 1 | 7.70 |
| CHEMBL525893 | — | — | 1 | 7.66 |
| CHEMBL497957 | — | — | 1 | 7.40 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 7.28 |
| CHEMBL497754 | — | — | 1 | 7.22 |
| CHEMBL496916 | — | — | 1 | 7.19 |
| CHEMBL487431 | — | — | 1 | 7.11 |
| CHEMBL523741 | — | — | 1 | 6.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL494821 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL496494 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL493986 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL498557 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL497343 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL525744 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL497958 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL504805 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL506033 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL496713 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL496505 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL522905 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL525893 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL497957 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL941 | IMATINIB | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL497754 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL496916 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL487431 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL523741 | — | IC50 | = | 210.0 | nM | 6.68 |