Assay Detail
Binding
CHEMBL822941
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Binding affinity for rat GABA-A receptor alpha-1-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 | Autocuration |
Target
GABA-A receptor; alpha-1/beta-2/gamma-2 (CHEMBL2095167) ↗| 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 | 8.12 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL407 | FLUMAZENIL | 4.0 | 1 | 9.30 |
| CHEMBL344859 | — | — | 1 | 9.10 |
| CHEMBL6597 | Ro-154513 | — | 1 | 7.82 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 7.80 |
| CHEMBL911 | ZOLPIDEM | 4.0 | 1 | 7.72 |
| CHEMBL13662 | CI-218872 | — | 1 | 6.97 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL407 | FLUMAZENIL | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL344859 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL6597 | Ro-154513 | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL12 | DIAZEPAM | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL911 | ZOLPIDEM | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL13662 | CI-218872 | Ki | = | 108.0 | nM | 6.97 |