Assay Detail
Binding
CHEMBL2330635
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Inhibition of ATR in human HeLa cell nuclear extracts using glutathione S-transferase-p53N66 and ATP as substrate incubated for 10 mins prior to ATP addition measured after 1 hr by ELISA
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 38 | 7.14 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2325703 | — | — | 1 | 8.52 |
| CHEMBL2325705 | — | — | 1 | 8.40 |
| CHEMBL2325711 | — | — | 1 | 8.30 |
| CHEMBL2325697 | — | — | 1 | 8.30 |
| CHEMBL2325699 | — | — | 1 | 8.15 |
| CHEMBL2325704 | — | — | 1 | 8.10 |
| CHEMBL2325720 | — | — | 1 | 8.10 |
| CHEMBL2325706 | — | — | 1 | 8.05 |
| CHEMBL2325708 | — | — | 1 | 7.89 |
| CHEMBL2325439 | — | — | 1 | 7.82 |
| CHEMBL2325440 | — | — | 1 | 7.80 |
| CHEMBL2325695 | — | — | 1 | 7.64 |
| CHEMBL2325718 | — | — | 1 | 7.55 |
| CHEMBL2030442 | — | — | 1 | 7.52 |
| CHEMBL2325712 | — | — | 1 | 7.48 |
| CHEMBL2325709 | — | — | 1 | 7.48 |
| CHEMBL2325696 | — | — | 1 | 7.47 |
| CHEMBL2325438 | — | — | 1 | 7.39 |
| CHEMBL2325710 | — | — | 1 | 7.34 |
| CHEMBL2325707 | — | — | 1 | 7.21 |
| CHEMBL2325724 | — | — | 1 | 7.18 |
| CHEMBL2325715 | — | — | 1 | 6.92 |
| CHEMBL2325716 | — | — | 1 | 6.89 |
| CHEMBL2325726 | — | — | 1 | 6.85 |
| CHEMBL2325698 | — | — | 1 | 6.77 |
| CHEMBL2325717 | — | — | 1 | 6.75 |
| CHEMBL2325701 | — | — | 1 | 6.75 |
| CHEMBL2325721 | — | — | 1 | 6.66 |
| CHEMBL2325723 | — | — | 1 | 6.52 |
| CHEMBL2325713 | — | — | 1 | 6.44 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2325703 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2325705 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2325697 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2325711 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2325699 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2325704 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL2325720 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL2325706 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL2325708 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2325439 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2325440 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL2325695 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL2325718 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL2030442 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2325709 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL2325712 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL2325696 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL2325438 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL2325710 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL2325707 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL2325724 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL2325715 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL2325716 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL2325726 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL2325698 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL2325717 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL2325701 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL2325721 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL2325723 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL2325713 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL2325725 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL2325722 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL2325714 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL2325700 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL2030436 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL2325702 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL2321916 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL2325719 | — | IC50 | - | — | - |