Assay Detail
Functional
CHEMBL2169533
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at KCNQ2 expressed in CHO cells incubated for 3 mins by automated patch clamp assay
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Potassium voltage-gated channel subfamily KQT member 2 (CHEMBL2476) ↗| Type | SINGLE PROTEIN |
| 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 | 34 | 6.18 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2164048 | — | — | 1 | 7.16 |
| CHEMBL2163658 | — | — | 1 | 6.92 |
| CHEMBL2164068 | — | — | 1 | 6.89 |
| CHEMBL1464225 | — | — | 1 | 6.79 |
| CHEMBL2164062 | — | — | 1 | 6.77 |
| CHEMBL2163667 | — | — | 1 | 6.68 |
| CHEMBL2163659 | — | — | 1 | 6.62 |
| CHEMBL2164049 | — | — | 1 | 6.58 |
| CHEMBL2163662 | — | — | 1 | 6.55 |
| CHEMBL2164054 | — | — | 1 | 6.50 |
| CHEMBL2164066 | — | — | 1 | 6.48 |
| CHEMBL2164055 | — | — | 1 | 6.48 |
| CHEMBL2164064 | — | — | 1 | 6.44 |
| CHEMBL2163661 | — | — | 1 | 6.42 |
| CHEMBL2163657 | — | — | 1 | 6.41 |
| CHEMBL2163664 | — | — | 1 | 6.36 |
| CHEMBL2164069 | — | — | 1 | 6.33 |
| CHEMBL1412066 | — | — | 1 | 5.88 |
| CHEMBL2164053 | — | — | 1 | 5.65 |
| CHEMBL2163655 | — | — | 1 | 5.48 |
| CHEMBL2164052 | — | — | 1 | 5.46 |
| CHEMBL2163350 | — | — | 1 | 5.28 |
| CHEMBL2163673 | — | — | 1 | 4.90 |
| CHEMBL2163686 | — | — | 1 | 4.82 |
| CHEMBL2164061 | — | — | 1 | 4.69 |
| CHEMBL2163665 | — | — | 1 | - |
| CHEMBL2163671 | — | — | 1 | - |
| CHEMBL2164060 | — | — | 1 | - |
| CHEMBL2164058 | — | — | 1 | - |
| CHEMBL2164057 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2164048 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL2163658 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL2164068 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL1464225 | — | IC50 | = | 163.0 | nM | 6.79 |
| CHEMBL2164062 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL2163667 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL2163659 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL2164049 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL2163662 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL2164054 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL2164066 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL2164055 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL2164064 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL2163661 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL2163657 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL2163664 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL2164069 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL1412066 | — | IC50 | = | 1320.0 | nM | 5.88 |
| CHEMBL2164053 | — | IC50 | = | 2220.0 | nM | 5.65 |
| CHEMBL2163655 | — | IC50 | = | 3310.0 | nM | 5.48 |
| CHEMBL2164052 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL2163350 | — | IC50 | = | 5270.0 | nM | 5.28 |
| CHEMBL2163673 | — | IC50 | = | 12670.0 | nM | 4.90 |
| CHEMBL2163686 | — | IC50 | = | 14990.0 | nM | 4.82 |
| CHEMBL2164061 | — | IC50 | = | 20230.0 | nM | 4.69 |
| CHEMBL2163665 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2163671 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2164060 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2164058 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2164057 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2164056 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2163675 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2163679 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2163680 | — | IC50 | > | 30000.0 | nM | - |