Assay Detail
Binding
CHEMBL1027247
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]astemizole from human ERG expressed in HEK293 cells
16
Total Activities
15
Compounds Tested
2
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
Enantiomeric propanolamines as selective N-methyl-D-aspartate 2B receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.18 | 7.16 |
| IC20 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL494504 | — | — | 1 | 7.16 |
| CHEMBL524038 | — | — | 1 | 6.89 |
| CHEMBL492620 | — | — | 1 | 6.77 |
| CHEMBL523167 | — | — | 1 | 6.43 |
| CHEMBL493087 | — | — | 1 | 6.37 |
| CHEMBL492438 | — | — | 2 | 6.14 |
| CHEMBL494105 | — | — | 1 | 6.14 |
| CHEMBL493712 | — | — | 1 | 6.11 |
| CHEMBL495328 | — | — | 1 | 6.08 |
| CHEMBL495114 | — | — | 1 | 5.92 |
| CHEMBL492846 | — | — | 1 | 5.86 |
| CHEMBL523671 | — | — | 1 | 5.79 |
| CHEMBL493078 | — | — | 1 | 5.77 |
| CHEMBL493053 | — | — | 1 | 5.72 |
| CHEMBL494061 | — | — | 1 | 5.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL494504 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL524038 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL492620 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL523167 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL493087 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL492438 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL494105 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL493712 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL495328 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL495114 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL492846 | — | IC50 | = | 1390.0 | nM | 5.86 |
| CHEMBL523671 | — | IC50 | = | 1630.0 | nM | 5.79 |
| CHEMBL493078 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL493053 | — | IC50 | = | 1910.0 | nM | 5.72 |
| CHEMBL494061 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL492438 | — | IC20 | > | 174.0 | nM | - |