Assay Detail
Binding
CHEMBL3859699
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG
4
Total Activities
4
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
Design, Synthesis, and Biological Evaluation of Novel Tetrahydroprotoberberine Derivatives (THPBs) as Selective α1A-Adrenoceptor Antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 5.36 | 6.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL473 | DOFETILIDE | 4.0 | 1 | 6.70 |
| CHEMBL24778 | SILODOSIN | 4.0 | 1 | 5.09 |
| CHEMBL3892879 | — | — | 1 | 4.88 |
| CHEMBL3916182 | — | — | 1 | 4.78 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL473 | DOFETILIDE | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL24778 | SILODOSIN | IC50 | = | 8200.0 | nM | 5.09 |
| CHEMBL3892879 | — | IC50 | = | 13200.0 | nM | 4.88 |
| CHEMBL3916182 | — | IC50 | = | 16500.0 | nM | 4.78 |