Assay Detail
Binding
CHEMBL955810
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Inhibition of Lck 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 |
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 | 6.27 | 8.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL496494 | — | — | 1 | 8.14 |
| CHEMBL493986 | — | — | 1 | 7.72 |
| CHEMBL497343 | — | — | 1 | 6.96 |
| CHEMBL506033 | — | — | 1 | 6.82 |
| CHEMBL496713 | — | — | 1 | 6.64 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 6.50 |
| CHEMBL522905 | — | — | 1 | 6.47 |
| CHEMBL496916 | — | — | 1 | 6.39 |
| CHEMBL497754 | — | — | 1 | 6.32 |
| CHEMBL494821 | — | — | 1 | 6.24 |
| CHEMBL496505 | — | — | 1 | 6.24 |
| CHEMBL497958 | — | — | 1 | 6.13 |
| CHEMBL498557 | — | — | 1 | 5.92 |
| CHEMBL504805 | — | — | 1 | 5.77 |
| CHEMBL523741 | — | — | 1 | 5.77 |
| CHEMBL525744 | — | — | 1 | 5.75 |
| CHEMBL487431 | — | — | 1 | 5.72 |
| CHEMBL525893 | — | — | 1 | 5.11 |
| CHEMBL497957 | — | — | 1 | 4.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL496494 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL493986 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL497343 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL506033 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL496713 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL941 | IMATINIB | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL522905 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL496916 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL497754 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL494821 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL496505 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL497958 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL498557 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL504805 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL523741 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL525744 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL487431 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL525893 | — | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL497957 | — | IC50 | = | 25000.0 | nM | 4.60 |