Assay Detail
Binding
CHEMBL3223680
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG
15
Total Activities
15
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
Property based optimisation of glucokinase activators discovery of the phase IIb clinical candidate AZD1656
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 4.56 | 5.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3219108 | — | — | 1 | 5.05 |
| CHEMBL3219109 | — | — | 1 | 4.96 |
| CHEMBL3219120 | — | — | 1 | 4.75 |
| CHEMBL3219123 | — | — | 1 | 4.75 |
| CHEMBL3219116 | — | — | 1 | 4.57 |
| CHEMBL3219119 | — | — | 1 | 4.55 |
| CHEMBL3219106 | — | — | 1 | 4.51 |
| CHEMBL3219117 | — | — | 1 | 4.46 |
| CHEMBL3219115 | — | — | 1 | 4.44 |
| CHEMBL3219110 | — | — | 1 | 4.42 |
| CHEMBL3219121 | — | — | 1 | 4.40 |
| CHEMBL3219105 | — | — | 1 | 4.27 |
| CHEMBL3217925 | — | — | 1 | 4.16 |
| CHEMBL3219107 | — | — | 1 | - |
| CHEMBL3219124 | AZD-1656 | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3219108 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL3219109 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL3219120 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL3219123 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL3219116 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL3219119 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL3219106 | — | IC50 | = | 31000.0 | nM | 4.51 |
| CHEMBL3219117 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL3219115 | — | IC50 | = | 36000.0 | nM | 4.44 |
| CHEMBL3219110 | — | IC50 | = | 38000.0 | nM | 4.42 |
| CHEMBL3219121 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL3219105 | — | IC50 | = | 54000.0 | nM | 4.27 |
| CHEMBL3217925 | — | IC50 | = | 70000.0 | nM | 4.16 |
| CHEMBL3219107 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3219124 | AZD-1656 | IC50 | > | 100000.0 | nM | - |