Assay Detail
Binding
CHEMBL955811
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Inhibition of Src 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 | Expert |
Target
Proto-oncogene tyrosine-protein kinase Src (CHEMBL267) ↗| 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 | 6.35 | 7.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL496494 | — | — | 1 | 7.44 |
| CHEMBL497958 | — | — | 1 | 7.37 |
| CHEMBL497343 | — | — | 1 | 7.11 |
| CHEMBL506033 | — | — | 1 | 6.82 |
| CHEMBL496713 | — | — | 1 | 6.77 |
| CHEMBL522905 | — | — | 1 | 6.58 |
| CHEMBL496916 | — | — | 1 | 6.57 |
| CHEMBL496505 | — | — | 1 | 6.41 |
| CHEMBL497754 | — | — | 1 | 6.41 |
| CHEMBL493986 | — | — | 1 | 6.40 |
| CHEMBL498557 | — | — | 1 | 6.12 |
| CHEMBL494821 | — | — | 1 | 6.10 |
| CHEMBL504805 | — | — | 1 | 6.07 |
| CHEMBL523741 | — | — | 1 | 6.00 |
| CHEMBL525744 | — | — | 1 | 5.85 |
| CHEMBL487431 | — | — | 1 | 5.30 |
| CHEMBL497957 | — | — | 1 | 4.60 |
| CHEMBL525893 | — | — | 1 | - |
| CHEMBL941 | IMATINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL496494 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL497958 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL497343 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL506033 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL496713 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL522905 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL496916 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL496505 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL497754 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL493986 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL498557 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL494821 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL504805 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL523741 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL525744 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL487431 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL497957 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL525893 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL941 | IMATINIB | IC50 | > | 25000.0 | nM | - |