Assay Detail
Binding
CHEMBL2173630
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG transfected in HEK293 cell membranes by whole cell patch clamp assay
10
Total Activities
10
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
Synthesis and biological evaluation of the 1-arylpyrazole class of σ(1) receptor antagonists: identification of 4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine (S1RA, E-52862).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 5.29 | 5.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2170225 | — | — | 1 | 5.46 |
| CHEMBL2170232 | — | — | 1 | 5.39 |
| CHEMBL2170213 | — | — | 1 | 5.35 |
| CHEMBL2170070 | — | — | 1 | 5.13 |
| CHEMBL2170231 | — | — | 1 | 5.13 |
| CHEMBL2170051 | — | — | 1 | - |
| CHEMBL2170066 | — | — | 1 | - |
| CHEMBL2170063 | — | — | 1 | - |
| CHEMBL2170062 | — | — | 1 | - |
| CHEMBL2170061 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2170225 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL2170232 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL2170213 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL2170070 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL2170231 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL2170051 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2170066 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2170063 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2170062 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2170061 | — | IC50 | > | 10000.0 | nM | - |