Assay Detail
Binding
CHEMBL822942
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Binding affinity for mutant rat GABA-A receptor alpha-1-(arg)-beta-2-gamma-2 subunits expressed in HEK293 cells
4
Total Activities
4
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 | 4 | 7.85 | 8.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6597 | Ro-154513 | — | 1 | 8.72 |
| CHEMBL407 | FLUMAZENIL | 4.0 | 1 | 6.97 |
| CHEMBL13662 | CI-218872 | — | 1 | - |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6597 | Ro-154513 | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL407 | FLUMAZENIL | Ki | = | 106.0 | nM | 6.97 |
| CHEMBL13662 | CI-218872 | Ki | > | 10000.0 | nM | - |
| CHEMBL12 | DIAZEPAM | Ki | > | 10000.0 | nM | - |