Assay Detail
Binding
CHEMBL824049
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Binding affinity for mutant rat GABA-A receptor alpha-6-(his,thr,gly,val)beta2gamma2 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 | Expert |
Target
GABA A receptor alpha-6/beta-2/gamma-2 (CHEMBL2111365) ↗| 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 | 7.03 | 8.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 8.68 |
| CHEMBL407 | FLUMAZENIL | 4.0 | 1 | 7.48 |
| CHEMBL13662 | CI-218872 | — | 1 | 6.11 |
| CHEMBL911 | ZOLPIDEM | 4.0 | 1 | 5.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL12 | DIAZEPAM | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL407 | FLUMAZENIL | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL13662 | CI-218872 | Ki | = | 780.0 | nM | 6.11 |
| CHEMBL911 | ZOLPIDEM | Ki | = | 1400.0 | nM | 5.85 |