Assay Detail
Binding
CHEMBL768693
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Effective concentration against Potassium voltage gated channel KQT-like subfamily, member 2 expressed in HEK 293 cells
2
Total Activities
2
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 | Expert |
Target
Potassium voltage-gated channel subfamily KQT member 2 (CHEMBL2476) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Fluorine substitution can block CYP3A4 metabolism-dependent inhibition: identification of (S)-N-[1-(4-fluoro-3- morpholin-4-ylphenyl)ethyl]-3- (4-fluorophenyl)acrylamide as an orally bioavailable KCNQ2 opener devoid of CYP3A4 metabolism-dependent inhibition.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 2 | 5.72 | 5.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL100379 | — | — | 1 | 5.92 |
| CHEMBL317935 | — | — | 1 | 5.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL100379 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL317935 | — | EC50 | = | 3000.0 | nM | 5.52 |