Assay Detail
Binding
CHEMBL2444337
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Induction of mouse KCNQ2 expressed in HEK293 cells at -40 mV holding potential by whole-cell patch clamp assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Potassium voltage-gated channel subfamily KQT member 2 (CHEMBL2985) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
Discovery of (S,E)-3-(2-fluorophenyl)-N-(1-(3-(pyridin-3-yloxy)phenyl)ethyl)-acrylamide as a potent and efficacious KCNQ2 (Kv7.2) opener for the treatment of neuropathic pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 9 | 7.43 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2440363 | — | — | 1 | 9.05 |
| CHEMBL401942 | — | — | 1 | 8.62 |
| CHEMBL361184 | — | — | 1 | 8.00 |
| CHEMBL180886 | — | — | 1 | 7.70 |
| CHEMBL176931 | — | — | 1 | 7.22 |
| CHEMBL41355 | EZOGABINE | 4.0 | 1 | 5.89 |
| CHEMBL317935 | — | — | 1 | 5.50 |
| CHEMBL2440364 | — | — | 1 | - |
| CHEMBL2440362 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2440363 | — | EC50 | = | 0.9 | nM | 9.05 |
| CHEMBL401942 | — | EC50 | = | 2.4 | nM | 8.62 |
| CHEMBL361184 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL180886 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL176931 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL41355 | EZOGABINE | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL317935 | — | EC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL2440364 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2440362 | — | EC50 | > | 10000.0 | nM | - |