Assay Detail
Binding
CHEMBL4478166
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Inhibition of ATM (unknown origin) using p53 as substrate incubated for 30 mins followed by substrate addition measured after 2 hrs in presence of ATP by HTRF method
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Novel 3-Quinoline Carboxamides as Potent, Selective, and Orally Bioavailable Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 8.35 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4166405 | — | — | 1 | 9.22 |
| CHEMBL2140173 | — | — | 1 | 9.10 |
| CHEMBL4565988 | — | — | 1 | 8.70 |
| CHEMBL4593348 | — | — | 1 | 8.10 |
| CHEMBL2143829 | — | — | 1 | 7.68 |
| CHEMBL4527822 | — | — | 1 | 7.31 |
| CHEMBL4218734 | — | — | 1 | - |
| CHEMBL222102 | KU-55933 | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4166405 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL2140173 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4565988 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4593348 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL2143829 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4527822 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4218734 | — | IC50 | < | 1.2 | nM | - |
| CHEMBL222102 | KU-55933 | IC50 | < | 2.0 | nM | - |