Assay Detail
Binding
CHEMBL4774539
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG stably expressed in HEK293 cells by whole-cell manual patch clamp method
8
Total Activities
8
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
Design, synthesis and biological evaluation of diamino substituted cyclobut-3-ene-1,2-dione derivatives for the treatment of drug-resistant tuberculosis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.89 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL473 | DOFETILIDE | 4.0 | 1 | 7.89 |
| CHEMBL4799560 | — | — | 1 | - |
| CHEMBL4785407 | — | — | 1 | - |
| CHEMBL4101131 | — | — | 1 | - |
| CHEMBL4776524 | — | — | 1 | - |
| CHEMBL4784832 | — | — | 1 | - |
| CHEMBL4779974 | — | — | 1 | - |
| CHEMBL4788475 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL473 | DOFETILIDE | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4799560 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4785407 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4101131 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4776524 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4784832 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4779974 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4788475 | — | IC50 | > | 10000.0 | nM | - |