Assay Detail
Binding
CHEMBL942241
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Displacement of [3H]Ro-151788 from benzodiazepine binding site of GABAA alpha-2-beta-2-gamma-2 receptor expressed in HEK293T cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HEK-293T |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
GABA A receptor alpha-2/beta-2/gamma-2 (CHEMBL2111413) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Structural requirements for eszopiclone and zolpidem binding to the gamma-aminobutyric acid type-A (GABAA) receptor are different.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 4 | 7.19 | 8.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL407 | FLUMAZENIL | 4.0 | 1 | 8.24 |
| CHEMBL1522 | ESZOPICLONE | 4.0 | 1 | 6.94 |
| CHEMBL911 | ZOLPIDEM | 4.0 | 1 | 6.39 |
| CHEMBL6597 | Ro-154513 | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL407 | FLUMAZENIL | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL1522 | ESZOPICLONE | Ki | = | 114.0 | nM | 6.94 |
| CHEMBL911 | ZOLPIDEM | Ki | = | 408.0 | nM | 6.39 |
| CHEMBL6597 | Ro-154513 | Ki | - | — | - |