Assay Detail
Binding
CHEMBL822346
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Binding affinity for mutant rat GABA-A receptor alpha-4-(his)-beta-2-gamma-2 subunits expressed in HEK293 cells
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | HEK293 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
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 | 5 | 7.65 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL407 | FLUMAZENIL | 4.0 | 1 | 9.22 |
| CHEMBL6597 | Ro-154513 | — | 1 | 8.15 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 7.64 |
| CHEMBL911 | ZOLPIDEM | 4.0 | 1 | 7.12 |
| CHEMBL13662 | CI-218872 | — | 1 | 6.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL407 | FLUMAZENIL | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL6597 | Ro-154513 | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL12 | DIAZEPAM | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL911 | ZOLPIDEM | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL13662 | CI-218872 | Ki | = | 720.0 | nM | 6.14 |