Assay Detail
Binding
CHEMBL4153776
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG by electrophysiology assay
32
Total Activities
32
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 |
Target
Voltage-gated inwardly rectifying potassium channel KCNH2 (CHEMBL240) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 32 | 4.85 | 5.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4174323 | — | — | 1 | 5.68 |
| CHEMBL4164430 | — | — | 1 | 5.24 |
| CHEMBL4160664 | — | — | 1 | 5.05 |
| CHEMBL4168290 | — | — | 1 | 5.05 |
| CHEMBL4169828 | — | — | 1 | 4.96 |
| CHEMBL3960323 | — | — | 1 | 4.85 |
| CHEMBL4172761 | — | — | 1 | 4.85 |
| CHEMBL4176135 | — | — | 1 | 4.82 |
| CHEMBL4170883 | — | — | 1 | 4.82 |
| CHEMBL3972724 | — | — | 1 | 4.75 |
| CHEMBL4161022 | — | — | 1 | 4.75 |
| CHEMBL3898577 | — | — | 1 | 4.66 |
| CHEMBL4164853 | — | — | 1 | 4.64 |
| CHEMBL4175071 | — | — | 1 | 4.62 |
| CHEMBL3890490 | — | — | 1 | 4.57 |
| CHEMBL4171264 | — | — | 1 | 4.57 |
| CHEMBL4162952 | — | — | 1 | 4.57 |
| CHEMBL3960662 | — | — | 1 | - |
| CHEMBL3986918 | — | — | 1 | - |
| CHEMBL3946515 | — | — | 1 | - |
| CHEMBL4167508 | — | — | 1 | - |
| CHEMBL3889770 | — | — | 1 | - |
| CHEMBL4111966 | — | — | 1 | - |
| CHEMBL3950905 | — | — | 1 | - |
| CHEMBL3936943 | — | — | 1 | - |
| CHEMBL3979811 | — | — | 1 | - |
| CHEMBL3954517 | — | — | 1 | - |
| CHEMBL3958682 | — | — | 1 | - |
| CHEMBL3936734 | — | — | 1 | - |
| CHEMBL3924247 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4174323 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL4164430 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL4160664 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL4168290 | — | IC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL4169828 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL3960323 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL4172761 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL4176135 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL4170883 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL3972724 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL4161022 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL3898577 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL4164853 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL4175071 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL4171264 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL4162952 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL3890490 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL4171626 | — | IC50 | > | 33000.0 | nM | - |
| CHEMBL4173181 | — | IC50 | > | 33000.0 | nM | - |
| CHEMBL3924247 | — | IC50 | > | 33000.0 | nM | - |
| CHEMBL3936734 | — | IC50 | > | 33000.0 | nM | - |
| CHEMBL3958682 | — | IC50 | > | 33000.0 | nM | - |
| CHEMBL3954517 | — | IC50 | > | 33000.0 | nM | - |
| CHEMBL3979811 | — | IC50 | > | 33000.0 | nM | - |
| CHEMBL3936943 | — | IC50 | > | 33000.0 | nM | - |
| CHEMBL3950905 | — | IC50 | > | 33000.0 | nM | - |
| CHEMBL4111966 | — | IC50 | > | 33000.0 | nM | - |
| CHEMBL3889770 | — | IC50 | > | 33000.0 | nM | - |
| CHEMBL4167508 | — | IC50 | > | 33000.0 | nM | - |
| CHEMBL3946515 | — | IC50 | > | 33000.0 | nM | - |
| CHEMBL3986918 | — | IC50 | > | 33000.0 | nM | - |
| CHEMBL3960662 | — | IC50 | > | 33000.0 | nM | - |