Assay Detail
Binding
CHEMBL677024
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Displacement of [3H]Flunitrazepam from GABA-A receptor alpha-1-beta-2-gamma-2 subunits expressed in Sf9 cells
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | Sf9 |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
GABA-A receptor; alpha-1/beta-2/gamma-2 (CHEMBL2095172) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
High-affinity partial agonist imidazo[1,5-a]quinoxaline amides, carbamates, and ureas at the gamma-aminobutyric acid A/benzodiazepine receptor complex.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 8.92 | 9.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL50763 | — | — | 1 | 9.77 |
| CHEMBL290036 | — | — | 1 | 9.52 |
| CHEMBL49888 | — | — | 1 | 9.52 |
| CHEMBL279867 | PANADIPLON | 2.0 | 1 | 8.46 |
| CHEMBL48211 | — | — | 1 | 8.33 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 7.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL50763 | — | Ki | = | 0.17 | nM | 9.77 |
| CHEMBL290036 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL49888 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL279867 | PANADIPLON | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL48211 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL12 | DIAZEPAM | Ki | = | 13.0 | nM | 7.89 |