Assay Detail
Binding
CHEMBL952530
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activity at rat wild type GABAA alpha-1-beta-2-gamma-2 receptor expressed in xenopus oocytes assessed as GABA-elicited response by two electrode voltage clamp method relative to control
7
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | Oocyte |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Gamma-aminobutyric acid receptor subunit alpha-1 (CHEMBL1962) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Proximity-accelerated chemical coupling reaction in the benzodiazepine-binding site of gamma-aminobutyric acid type A receptors: superposition of different allosteric modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| max activation | 4 | - | - |
| EC50 | 3 | 7.43 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6597 | Ro-154513 | — | 2 | 8.96 |
| CHEMBL911 | ZOLPIDEM | 4.0 | 2 | 6.72 |
| CHEMBL485829 | — | — | 2 | 6.60 |
| CHEMBL407 | FLUMAZENIL | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6597 | Ro-154513 | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL911 | ZOLPIDEM | EC50 | = | 191.0 | nM | 6.72 |
| CHEMBL485829 | — | EC50 | = | 250.0 | nM | 6.60 |
| CHEMBL911 | ZOLPIDEM | max activation | = | 429.0 | % | - |
| CHEMBL485829 | — | max activation | = | 11.0 | % | - |
| CHEMBL6597 | Ro-154513 | max activation | = | -15.0 | % | - |
| CHEMBL407 | FLUMAZENIL | max activation | = | 12.0 | % | - |