Assay Detail
Binding
CHEMBL4200456
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Inhibition of ATM autophosphorylation at Ser1981 residue in human HT-29 cells measured after 1 hr by Hoechst staining based fluorescence assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HT-29 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of a Series of 3-Cinnoline Carboxamides as Orally Bioavailable, Highly Potent, and Selective ATM Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.90 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4210045 | — | — | 1 | 9.30 |
| CHEMBL4212961 | — | — | 1 | 9.05 |
| CHEMBL4208569 | — | — | 1 | 8.96 |
| CHEMBL4213503 | — | — | 1 | 8.74 |
| CHEMBL4217549 | — | — | 1 | 8.72 |
| CHEMBL4218854 | — | — | 1 | 8.55 |
| CHEMBL4213919 | — | — | 1 | 8.41 |
| CHEMBL4217902 | — | — | 1 | 8.41 |
| CHEMBL4215266 | — | — | 1 | 8.00 |
| CHEMBL4166405 | — | — | 1 | 7.48 |
| CHEMBL4205148 | — | — | 1 | 7.46 |
| CHEMBL4216325 | — | — | 1 | 7.36 |
| CHEMBL4218734 | — | — | 1 | 7.34 |
| CHEMBL4205675 | — | — | 1 | 7.31 |
| CHEMBL4217379 | — | — | 1 | 7.21 |
| CHEMBL4209427 | — | — | 1 | 6.85 |
| CHEMBL4210849 | — | — | 1 | 6.58 |
| CHEMBL4205554 | — | — | 1 | 6.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4210045 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4212961 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL4208569 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4213503 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4217549 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4218854 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL4213919 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL4217902 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL4215266 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4166405 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4205148 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4216325 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4218734 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL4205675 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4217379 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL4209427 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4210849 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL4205554 | — | IC50 | = | 330.0 | nM | 6.48 |