Assay Detail
Functional
CHEMBL700530
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Whole-cell patch-clamp on recombinant mouse KCNQ2 channels expressed in HEK 293 cells at -40 mV
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Potassium voltage-gated channel subfamily KQT member 2 (CHEMBL2985) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
(S)-N-[1-(4-cyclopropylmethyl-3,4-dihydro-2H-benzo[1,4]oxazin-6-yl)-ethyl]-3-(2-fluoro-phenyl)-acrylamide is a potent and efficacious KCNQ2 opener which inhibits induced hyperexcitability of rat hippocampal neurons.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 6 | 6.17 | 7.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL176931 | — | — | 1 | 7.22 |
| CHEMBL174891 | — | — | 1 | 6.70 |
| CHEMBL407861 | — | — | 1 | 6.03 |
| CHEMBL41355 | EZOGABINE | 4.0 | 1 | 5.89 |
| CHEMBL368956 | — | — | 1 | 5.70 |
| CHEMBL317935 | — | — | 1 | 5.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL176931 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL174891 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL407861 | — | EC50 | = | 940.0 | nM | 6.03 |
| CHEMBL41355 | EZOGABINE | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL368956 | — | EC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL317935 | — | EC50 | = | 3280.0 | nM | 5.48 |