Assay Detail
Binding
CHEMBL940929
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]bufuralol from hERG channel expressed in HEK293 cells
16
Total Activities
14
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 | Intermediate |
Target
Voltage-gated inwardly rectifying potassium channel KCNH2 (CHEMBL240) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of (-)-6-[2-[4-(3-fluorophenyl)-4-hydroxy-1-piperidinyl]-1-hydroxyethyl]-3,4-dihydro-2(1H)-quinolinone--a potent NR2B-selective N-methyl D-aspartate (NMDA) antagonist for the treatment of pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 5.18 | 5.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL246635 | — | — | 1 | 5.80 |
| CHEMBL401407 | — | — | 1 | 5.62 |
| CHEMBL246634 | — | — | 1 | 5.58 |
| CHEMBL246816 | — | — | 1 | 5.51 |
| CHEMBL247840 | — | — | 1 | 5.48 |
| CHEMBL246815 | — | — | 1 | 5.13 |
| CHEMBL404851 | — | — | 1 | 5.07 |
| CHEMBL246819 | — | — | 3 | 5.01 |
| CHEMBL404852 | — | — | 1 | 5.00 |
| CHEMBL17350 | TRAXOPRODIL | 2.0 | 1 | 5.00 |
| CHEMBL246818 | — | — | 1 | 4.96 |
| CHEMBL246817 | — | — | 1 | 4.80 |
| CHEMBL247842 | — | — | 1 | - |
| CHEMBL247841 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL246635 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL401407 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL246634 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL246816 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL247840 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL246815 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL404851 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL246819 | — | IC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL404852 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL17350 | TRAXOPRODIL | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL246818 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL246819 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL246817 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL246819 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL247842 | — | IC50 | < | 1000.0 | nM | - |
| CHEMBL247841 | — | IC50 | < | 1500.0 | nM | - |