Assay Detail
Binding
CHEMBL1034067
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]dofetilide from human ERG expressed in HEK293 cells
11
Total Activities
11
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
1-Amido-1-phenyl-3-piperidinylbutanes - CCR5 antagonists for the treatment of HIV. Part 1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.38 | 8.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL460009 | — | — | 1 | 8.33 |
| CHEMBL460217 | — | — | 1 | 6.93 |
| CHEMBL456019 | — | — | 1 | 6.61 |
| CHEMBL469542 | — | — | 1 | 6.07 |
| CHEMBL459600 | — | — | 1 | 5.78 |
| CHEMBL459598 | — | — | 1 | 5.51 |
| CHEMBL469724 | — | — | 1 | 5.40 |
| CHEMBL516939 | — | — | 1 | - |
| CHEMBL460630 | — | — | 1 | - |
| CHEMBL518794 | — | — | 1 | - |
| CHEMBL459599 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL460009 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL460217 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL456019 | — | IC50 | = | 248.0 | nM | 6.61 |
| CHEMBL469542 | — | IC50 | = | 849.0 | nM | 6.07 |
| CHEMBL459600 | — | IC50 | = | 1650.0 | nM | 5.78 |
| CHEMBL459598 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL469724 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL516939 | — | IC50 | < | 5280.0 | nM | - |
| CHEMBL460630 | — | IC50 | - | — | - | |
| CHEMBL518794 | — | IC50 | - | — | - | |
| CHEMBL459599 | — | IC50 | - | — | - |