Assay Detail
Binding
CHEMBL648135
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Displacement of [3H]- flunitrazepam from rat GABA-A benzodiazepine receptor
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
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 | 8.65 | 9.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3084321 | — | — | 1 | 9.21 |
| CHEMBL3350338 | — | — | 1 | 9.19 |
| CHEMBL142750 | — | — | 1 | 9.06 |
| CHEMBL163684 | — | — | 1 | 8.62 |
| CHEMBL166357 | — | — | 1 | 8.55 |
| CHEMBL49888 | — | — | 1 | 8.37 |
| CHEMBL48924 | — | — | 1 | 8.32 |
| CHEMBL166267 | — | — | 1 | 8.29 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 8.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3084321 | — | Ki | = | 0.62 | nM | 9.21 |
| CHEMBL3350338 | — | Ki | = | 0.65 | nM | 9.19 |
| CHEMBL142750 | — | Ki | = | 0.87 | nM | 9.06 |
| CHEMBL163684 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL166357 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL49888 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL48924 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL166267 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL12 | DIAZEPAM | Ki | = | 6.0 | nM | 8.22 |