Assay Detail
Binding
CHEMBL4366089
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Inhibition of human ERG expressed in HEK293 cells by whole cell patch clamp method
15
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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
Discovery of a Lead Triphenylethanamine Cholesterol Ester Transfer Protein (CETP) Inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 4.68 | 4.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4439823 | — | — | 1 | 4.96 |
| CHEMBL4552555 | — | — | 1 | 4.92 |
| CHEMBL4545593 | — | — | 1 | 4.89 |
| CHEMBL4468680 | — | — | 1 | 4.80 |
| CHEMBL4436115 | — | — | 1 | 4.66 |
| CHEMBL4457286 | — | — | 1 | 4.36 |
| CHEMBL4452514 | — | — | 1 | 4.20 |
| CHEMBL4448253 | — | — | 2 | - |
| CHEMBL4473304 | — | — | 1 | - |
| CHEMBL4468692 | — | — | 1 | - |
| CHEMBL4574163 | — | — | 1 | - |
| CHEMBL4439856 | — | — | 1 | - |
| CHEMBL4469874 | — | — | 1 | - |
| CHEMBL4475826 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4439823 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL4552555 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL4545593 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL4468680 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL4436115 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL4457286 | — | IC50 | = | 44000.0 | nM | 4.36 |
| CHEMBL4452514 | — | IC50 | = | 63000.0 | nM | 4.20 |
| CHEMBL4448253 | — | IC50 | > | 80000.0 | nM | - |
| CHEMBL4448253 | — | IC50 | > | 80000.0 | nM | - |
| CHEMBL4473304 | — | IC50 | > | 80000.0 | nM | - |
| CHEMBL4468692 | — | IC50 | > | 80000.0 | nM | - |
| CHEMBL4574163 | — | IC50 | > | 80000.0 | nM | - |
| CHEMBL4439856 | — | IC50 | - | — | - | |
| CHEMBL4469874 | — | IC50 | - | — | - | |
| CHEMBL4475826 | — | IC50 | - | — | - |