Assay Detail
Binding
CHEMBL4354740
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human KCNQ2/3 expressed in HEK293 cells by FLIPR based thallium influx assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Voltage-gated potassium channel, KQT; KCNQ2(Kv7.2)/KCNQ3(Kv7.3) (CHEMBL2221348) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Design and evaluation of pyrazolopyrimidines as KCNQ channel modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 24 | 6.50 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4549421 | — | — | 1 | 7.30 |
| CHEMBL4516269 | — | — | 1 | 7.30 |
| CHEMBL4584469 | — | — | 1 | 7.16 |
| CHEMBL4460237 | — | — | 1 | 7.16 |
| CHEMBL4455848 | — | — | 1 | 7.10 |
| CHEMBL4448080 | — | — | 1 | 6.89 |
| CHEMBL4473937 | — | — | 1 | 6.85 |
| CHEMBL4556856 | — | — | 1 | 6.85 |
| CHEMBL4466756 | — | — | 1 | 6.85 |
| CHEMBL4436737 | — | — | 1 | 6.75 |
| CHEMBL4447300 | — | — | 1 | 6.72 |
| CHEMBL4462345 | — | — | 1 | 6.54 |
| CHEMBL4451236 | — | — | 1 | 6.51 |
| CHEMBL2147028 | — | — | 1 | 6.39 |
| CHEMBL255044 | FLUPIRTINE | 4.0 | 1 | 6.25 |
| CHEMBL4558921 | — | — | 1 | 6.23 |
| CHEMBL4456339 | — | — | 1 | 6.04 |
| CHEMBL4592138 | — | — | 1 | 6.00 |
| CHEMBL4448774 | — | — | 1 | 5.93 |
| CHEMBL4468366 | — | — | 1 | 5.64 |
| CHEMBL41355 | EZOGABINE | 4.0 | 1 | 5.36 |
| CHEMBL2147029 | — | — | 1 | 5.17 |
| CHEMBL4582071 | — | — | 1 | - |
| CHEMBL4554176 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4549421 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4516269 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4584469 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4460237 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4455848 | — | EC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4448080 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4473937 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4556856 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4466756 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4436737 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4447300 | — | EC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4462345 | — | EC50 | = | 290.0 | nM | 6.54 |
| CHEMBL4451236 | — | EC50 | = | 310.0 | nM | 6.51 |
| CHEMBL2147028 | — | EC50 | = | 410.0 | nM | 6.39 |
| CHEMBL255044 | FLUPIRTINE | EC50 | = | 560.0 | nM | 6.25 |
| CHEMBL4558921 | — | EC50 | = | 590.0 | nM | 6.23 |
| CHEMBL4456339 | — | EC50 | = | 910.0 | nM | 6.04 |
| CHEMBL4592138 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4448774 | — | EC50 | = | 1170.0 | nM | 5.93 |
| CHEMBL4468366 | — | EC50 | = | 2310.0 | nM | 5.64 |
| CHEMBL41355 | EZOGABINE | EC50 | = | 4380.0 | nM | 5.36 |
| CHEMBL2147029 | — | EC50 | = | 6800.0 | nM | 5.17 |
| CHEMBL4582071 | — | EC50 | > | 32000.0 | nM | - |
| CHEMBL4554176 | — | EC50 | > | 32000.0 | nM | - |