Assay Detail
Binding
CHEMBL4153770
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ATM autophosphorylation at Ser1981 in human HT29 cells preincubated for 1 hr followed by X ray irradiation 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 | 7.92 | 9.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3936943 | — | — | 1 | 9.77 |
| CHEMBL3960323 | — | — | 1 | 9.70 |
| CHEMBL3889770 | — | — | 1 | 9.62 |
| CHEMBL3936734 | — | — | 1 | 9.60 |
| CHEMBL3954517 | — | — | 1 | 9.60 |
| CHEMBL3979811 | — | — | 1 | 9.54 |
| CHEMBL3890490 | — | — | 1 | 9.48 |
| CHEMBL3960662 | — | — | 1 | 9.24 |
| CHEMBL3958682 | — | — | 1 | 9.12 |
| CHEMBL3986918 | — | — | 1 | 9.11 |
| CHEMBL4111966 | — | — | 1 | 9.03 |
| CHEMBL3950905 | — | — | 1 | 8.96 |
| CHEMBL3972724 | — | — | 1 | 8.96 |
| CHEMBL3946515 | — | — | 1 | 8.92 |
| CHEMBL3924247 | — | — | 1 | 8.82 |
| CHEMBL4163629 | — | — | 1 | 8.77 |
| CHEMBL3898577 | — | — | 1 | 8.59 |
| CHEMBL4162142 | — | — | 1 | 8.30 |
| CHEMBL4175071 | — | — | 1 | 8.22 |
| CHEMBL4161022 | — | — | 1 | 8.09 |
| CHEMBL4167277 | — | — | 1 | 8.07 |
| CHEMBL4172819 | — | — | 1 | 7.66 |
| CHEMBL4173181 | — | — | 1 | 7.64 |
| CHEMBL4160664 | — | — | 1 | 7.00 |
| CHEMBL4171626 | — | — | 1 | 6.89 |
| CHEMBL4176135 | — | — | 1 | 6.85 |
| CHEMBL4172761 | — | — | 1 | 6.80 |
| CHEMBL4168290 | — | — | 1 | 6.80 |
| CHEMBL4164430 | — | — | 1 | 6.64 |
| CHEMBL4164853 | — | — | 1 | 6.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3936943 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL3960323 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3889770 | — | IC50 | = | 0.24 | nM | 9.62 |
| CHEMBL3936734 | — | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL3954517 | — | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL3979811 | — | IC50 | = | 0.29 | nM | 9.54 |
| CHEMBL3890490 | — | IC50 | = | 0.33 | nM | 9.48 |
| CHEMBL3960662 | — | IC50 | = | 0.57 | nM | 9.24 |
| CHEMBL3958682 | — | IC50 | = | 0.76 | nM | 9.12 |
| CHEMBL3986918 | — | IC50 | = | 0.78 | nM | 9.11 |
| CHEMBL4111966 | — | IC50 | = | 0.94 | nM | 9.03 |
| CHEMBL3950905 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3972724 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3946515 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3924247 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4163629 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3898577 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL4162142 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4175071 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4161022 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL4167277 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL4172819 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4173181 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4160664 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4171626 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4176135 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4172761 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4168290 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4164430 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4164853 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4171264 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4169828 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL4167508 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL4162952 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL4170883 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL4174323 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL4159181 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4176012 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL4173494 | — | IC50 | > | 28000.0 | nM | - |
| CHEMBL4159593 | — | IC50 | > | 30000.0 | nM | - |