Assay Detail
Functional
CHEMBL2169529
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at KCNQ1/E1 expressed in CHO cells incubated for 3 mins by automated patch clamp assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | CHO |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Voltage-gated potassium channel, IKs; KCNQ1(Kv7.1)/KCNE1(MinK) (CHEMBL2221347) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Discovery of a series of 2-phenyl-N-(2-(pyrrolidin-1-yl)phenyl)acetamides as novel molecular switches that modulate modes of K(v)7.2 (KCNQ2) channel pharmacology: identification of (S)-2-phenyl-N-(2-(pyrrolidin-1-yl)phenyl)butanamide (ML252) as a potent, brain penetrant K(v)7.2 channel inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 1 | 5.09 | 5.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2164048 | — | — | 1 | 5.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2164048 | — | IC50 | = | 8120.0 | nM | 5.09 |