Assay Detail
Binding
CHEMBL823756
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity for rat GABA-A receptor alpha-3-beta-2-gamma-2 subunits expressed in HEK293 cells
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | HEK293 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Expert |
Target
GABA A receptor alpha-3/beta-2/gamma-2 (CHEMBL2111343) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Four amino acid exchanges convert a diazepam-insensitive, inverse agonist-preferring GABAA receptor into a diazepam-preferring GABAA receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 7.65 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL407 | FLUMAZENIL | 4.0 | 1 | 9.22 |
| CHEMBL344859 | — | — | 1 | 8.40 |
| CHEMBL6597 | Ro-154513 | — | 1 | 8.30 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 7.77 |
| CHEMBL911 | ZOLPIDEM | 4.0 | 1 | 6.40 |
| CHEMBL13662 | CI-218872 | — | 1 | 5.79 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL407 | FLUMAZENIL | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL344859 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL6597 | Ro-154513 | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL12 | DIAZEPAM | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL911 | ZOLPIDEM | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL13662 | CI-218872 | Ki | = | 1620.0 | nM | 5.79 |