Assay Detail
Binding
CHEMBL2330631
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ATR-mediated CHK1 phosphorylation at serine 345 in human HT29 cells after 1 hr in presence of 4-nitroquinoline 1-oxide
38
Total Activities
38
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 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 | 5.76 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2325697 | — | — | 1 | 7.30 |
| CHEMBL2325705 | — | — | 1 | 6.75 |
| CHEMBL2325703 | — | — | 1 | 6.55 |
| CHEMBL2325699 | — | — | 1 | 6.46 |
| CHEMBL2325704 | — | — | 1 | 6.44 |
| CHEMBL2325706 | — | — | 1 | 6.38 |
| CHEMBL2325439 | — | — | 1 | 6.36 |
| CHEMBL2325720 | — | — | 1 | 6.31 |
| CHEMBL2325711 | — | — | 1 | 6.23 |
| CHEMBL2325440 | — | — | 1 | 6.14 |
| CHEMBL2325708 | — | — | 1 | 6.11 |
| CHEMBL2325695 | — | — | 1 | 6.10 |
| CHEMBL2030442 | — | — | 1 | 5.96 |
| CHEMBL2325724 | — | — | 1 | 5.82 |
| CHEMBL2325712 | — | — | 1 | 5.70 |
| CHEMBL2325718 | — | — | 1 | 5.60 |
| CHEMBL2325709 | — | — | 1 | 5.55 |
| CHEMBL2325710 | — | — | 1 | 5.54 |
| CHEMBL2325707 | — | — | 1 | 5.43 |
| CHEMBL2325696 | — | — | 1 | 5.43 |
| CHEMBL2325698 | — | — | 1 | 5.36 |
| CHEMBL2325721 | — | — | 1 | 5.20 |
| CHEMBL2325723 | — | — | 1 | 5.14 |
| CHEMBL2325717 | — | — | 1 | 5.05 |
| CHEMBL2325438 | — | — | 1 | 5.04 |
| CHEMBL2325716 | — | — | 1 | 4.89 |
| CHEMBL2325726 | — | — | 1 | 4.82 |
| CHEMBL2325715 | — | — | 1 | 4.80 |
| CHEMBL2325725 | — | — | 1 | 4.62 |
| CHEMBL2325722 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2325697 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL2325705 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL2325703 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL2325699 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL2325704 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL2325706 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL2325439 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL2325720 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL2325711 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL2325440 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL2325708 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL2325695 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL2030442 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL2325724 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL2325712 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL2325718 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL2325709 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL2325710 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL2325696 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL2325707 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL2325698 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL2325721 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL2325723 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL2325717 | — | IC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL2325438 | — | IC50 | = | 9200.0 | nM | 5.04 |
| CHEMBL2325716 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL2325726 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL2325715 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL2325725 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL2325722 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2030436 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2325700 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2325701 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2325702 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2325714 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2325719 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2321916 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2325713 | — | IC50 | > | 30000.0 | nM | - |