Assay Detail
Binding
CHEMBL2032591
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human Erg expressed in HEK293 cells assessed as rubidium efflux after 4 hrs by atomic absorbance spectrometric analysis
6
Total Activities
6
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
Discovery of a novel melanin concentrating hormone receptor 1 (MCHR1) antagonist with reduced hERG inhibition.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 6.48 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1922270 | — | — | 1 | 7.52 |
| CHEMBL17157 | TERFENADINE | 4.0 | 1 | 7.25 |
| CHEMBL2032047 | — | — | 1 | 6.52 |
| CHEMBL914 | FEXOFENADINE | 4.0 | 1 | 4.64 |
| CHEMBL2032048 | — | — | 1 | - |
| CHEMBL2032049 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1922270 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL17157 | TERFENADINE | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL2032047 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL914 | FEXOFENADINE | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL2032048 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL2032049 | — | IC50 | > | 5000.0 | nM | - |