Assay Detail
Binding
CHEMBL677790
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Displacement of [3H]flunitrazepam from alpha-1-beta-2-gamma-2 GABA-A receptor subunits expressed in Sf9 cell membranes
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | Sf9 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Antagonist, partial agonist, and full agonist imidazo[1,5-a]quinoxaline amides and carbamates acting through the GABAA/benzodiazepine receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 8.94 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL49888 | — | — | 1 | 9.52 |
| CHEMBL354385 | — | — | 1 | 9.52 |
| CHEMBL351822 | — | — | 1 | 9.40 |
| CHEMBL164243 | — | — | 1 | 9.40 |
| CHEMBL165458 | — | — | 1 | 9.22 |
| CHEMBL352676 | — | — | 1 | 9.10 |
| CHEMBL299133 | — | — | 1 | 8.57 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 7.89 |
| CHEMBL6597 | Ro-154513 | — | 1 | 7.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL49888 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL354385 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL351822 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL164243 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL165458 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL352676 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL299133 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL12 | DIAZEPAM | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL6597 | Ro-154513 | Ki | = | 15.0 | nM | 7.82 |