Assay Detail
Binding
CHEMBL4153771
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ATR in human HT29 cells assessed as decrease in Chk1 phosphorylation at Ser 345 preincubated for 1 hr followed by 4NQO addition and measured after 1 hr by Hoechst 33342 dye-based immunofluorescence assay
40
Total Activities
40
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
The Identification of Potent, Selective, and Orally Available Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase: The Discovery of AZD0156 (8-{6-[3-(Dimethylamino)propoxy]pyridin-3-yl}-3-methyl-1-(tetrahydro-2 H-pyran-4-yl)-1,3-dihydro-2 H-imidazo[4,5- c]quinolin-2-one).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 40 | 5.74 | 7.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4159181 | — | — | 1 | 7.29 |
| CHEMBL4169828 | — | — | 1 | 7.06 |
| CHEMBL4163629 | — | — | 1 | 5.70 |
| CHEMBL4174323 | — | — | 1 | 5.51 |
| CHEMBL3954517 | — | — | 1 | 5.36 |
| CHEMBL3960662 | — | — | 1 | 5.21 |
| CHEMBL4162142 | — | — | 1 | 5.00 |
| CHEMBL4164853 | — | — | 1 | 4.82 |
| CHEMBL4167508 | — | — | 1 | - |
| CHEMBL4164430 | — | — | 1 | - |
| CHEMBL3946515 | — | — | 1 | - |
| CHEMBL4172819 | — | — | 1 | - |
| CHEMBL4170883 | — | — | 1 | - |
| CHEMBL3898577 | — | — | 1 | - |
| CHEMBL3950905 | — | — | 1 | - |
| CHEMBL4173181 | — | — | 1 | - |
| CHEMBL4172761 | — | — | 1 | - |
| CHEMBL4161022 | — | — | 1 | - |
| CHEMBL4171626 | — | — | 1 | - |
| CHEMBL4159593 | — | — | 1 | - |
| CHEMBL4111966 | — | — | 1 | - |
| CHEMBL3890490 | — | — | 1 | - |
| CHEMBL3972724 | — | — | 1 | - |
| CHEMBL4176012 | — | — | 1 | - |
| CHEMBL4173494 | — | — | 1 | - |
| CHEMBL3960323 | — | — | 1 | - |
| CHEMBL3936943 | — | — | 1 | - |
| CHEMBL3979811 | — | — | 1 | - |
| CHEMBL3958682 | — | — | 1 | - |
| CHEMBL3889770 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4159181 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL4169828 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL4163629 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL4174323 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL3954517 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL3960662 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL4162142 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4164853 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL3950905 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3924247 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4173181 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4172761 | — | IC50 | > | 16000.0 | nM | - |
| CHEMBL4161022 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4171626 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4164430 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4175071 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3936734 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3986918 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4162952 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4167277 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4176135 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4168290 | — | IC50 | > | 28000.0 | nM | - |
| CHEMBL4160664 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4171264 | — | IC50 | > | 26000.0 | nM | - |
| CHEMBL3898577 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4170883 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4172819 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3946515 | — | IC50 | > | 29000.0 | nM | - |
| CHEMBL4167508 | — | IC50 | > | 13000.0 | nM | - |
| CHEMBL4159593 | — | IC50 | > | 27600.0 | nM | - |
| CHEMBL4111966 | — | IC50 | > | 23000.0 | nM | - |
| CHEMBL3890490 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3972724 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4176012 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4173494 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3960323 | — | IC50 | > | 2600.0 | nM | - |
| CHEMBL3936943 | — | IC50 | > | 24000.0 | nM | - |
| CHEMBL3979811 | — | IC50 | > | 24000.0 | nM | - |
| CHEMBL3958682 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3889770 | — | IC50 | > | 30000.0 | nM | - |