Assay Detail
Binding
CHEMBL4839289
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG stably expressed in CHO-K1 cells at -90 mV holding potential by automated Q-patch clamp method
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| 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
Structure-Activity Relationship Studies Reveal New Astemizole Analogues Active against <i>Plasmodium falciparum</i> In Vitro.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 6.65 | 8.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL296419 | ASTEMIZOLE | 4.0 | 1 | 8.38 |
| CHEMBL4870175 | — | — | 1 | 7.30 |
| CHEMBL4867115 | — | — | 1 | 7.30 |
| CHEMBL4868736 | — | — | 1 | 7.05 |
| CHEMBL4847937 | — | — | 1 | 6.96 |
| CHEMBL6966 | VERAPAMIL | 4.0 | 1 | 6.70 |
| CHEMBL4868855 | — | — | 1 | 6.39 |
| CHEMBL4870498 | — | — | 1 | 6.01 |
| CHEMBL4856218 | — | — | 1 | 5.38 |
| CHEMBL4853871 | — | — | 1 | 5.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL296419 | ASTEMIZOLE | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL4870175 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4867115 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4868736 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL4847937 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL6966 | VERAPAMIL | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4868855 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL4870498 | — | IC50 | = | 970.0 | nM | 6.01 |
| CHEMBL4856218 | — | IC50 | = | 4160.0 | nM | 5.38 |
| CHEMBL4853871 | — | IC50 | = | 8610.0 | nM | 5.07 |