Assay Detail
Binding
CHEMBL976274
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Inhibition of human Src kinase by TR-FRET assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Proto-oncogene tyrosine-protein kinase Src (CHEMBL267) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Novel N9-arenethenyl purines as potent dual Src/Abl tyrosine kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 8.01 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL459877 | — | — | 1 | 9.05 |
| CHEMBL460074 | — | — | 1 | 8.89 |
| CHEMBL451790 | — | — | 1 | 8.85 |
| CHEMBL528330 | — | — | 1 | 8.75 |
| CHEMBL454873 | — | — | 1 | 8.43 |
| CHEMBL454872 | — | — | 1 | 8.40 |
| CHEMBL454611 | — | — | 1 | 8.26 |
| CHEMBL520540 | — | — | 1 | 8.18 |
| CHEMBL488840 | — | — | 1 | 8.08 |
| CHEMBL452563 | — | — | 1 | 7.77 |
| CHEMBL488658 | — | — | 1 | 7.50 |
| CHEMBL510891 | — | — | 1 | 6.90 |
| CHEMBL454868 | — | — | 1 | 6.70 |
| CHEMBL488659 | — | — | 1 | 6.42 |
| CHEMBL509002 | — | — | 1 | - |
| CHEMBL455384 | — | — | 1 | - |
| CHEMBL509941 | — | — | 1 | - |
| CHEMBL454358 | — | — | 1 | - |
| CHEMBL516498 | — | — | 1 | - |
| CHEMBL461767 | — | — | 1 | - |
| CHEMBL461768 | — | — | 1 | - |
| CHEMBL510893 | — | — | 1 | - |
| CHEMBL518166 | — | — | 1 | - |
| CHEMBL517256 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL459877 | — | IC50 | = | 0.89 | nM | 9.05 |
| CHEMBL460074 | — | IC50 | = | 1.29 | nM | 8.89 |
| CHEMBL451790 | — | IC50 | = | 1.43 | nM | 8.85 |
| CHEMBL528330 | — | IC50 | = | 1.78 | nM | 8.75 |
| CHEMBL454873 | — | IC50 | = | 3.74 | nM | 8.43 |
| CHEMBL454872 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL454611 | — | IC50 | = | 5.56 | nM | 8.26 |
| CHEMBL520540 | — | IC50 | = | 6.58 | nM | 8.18 |
| CHEMBL488840 | — | IC50 | = | 8.31 | nM | 8.08 |
| CHEMBL452563 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL488658 | — | IC50 | = | 31.8 | nM | 7.50 |
| CHEMBL510891 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL454868 | — | IC50 | = | 198.0 | nM | 6.70 |
| CHEMBL488659 | — | IC50 | = | 376.0 | nM | 6.42 |
| CHEMBL509002 | — | IC50 | < | 0.46 | nM | - |
| CHEMBL455384 | — | IC50 | < | 0.46 | nM | - |
| CHEMBL509941 | — | IC50 | < | 0.23 | nM | - |
| CHEMBL454358 | — | IC50 | < | 0.23 | nM | - |
| CHEMBL516498 | — | IC50 | < | 0.46 | nM | - |
| CHEMBL461767 | — | IC50 | < | 0.46 | nM | - |
| CHEMBL461768 | — | IC50 | < | 0.46 | nM | - |
| CHEMBL510893 | — | IC50 | < | 0.46 | nM | - |
| CHEMBL518166 | — | IC50 | < | 0.46 | nM | - |
| CHEMBL517256 | — | IC50 | < | 0.46 | nM | - |