Assay Detail
Binding
CHEMBL954625
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]flumazenil from rat GABA-A alpha-1-beta-2-gamma-2 receptor expressed in HEK293 cells
20
Total Activities
20
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 | Autocuration |
Target
GABA-A receptor; alpha-1/beta-2/gamma-2 (CHEMBL2095167) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Identification of anxiolytic/nonsedative agents among indol-3-ylglyoxylamides acting as functionally selective agonists at the gamma-aminobutyric acid-A (GABAA) alpha2 benzodiazepine receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 7.00 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL521901 | — | — | 1 | 8.05 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 7.96 |
| CHEMBL75456 | — | — | 1 | 7.85 |
| CHEMBL74302 | — | — | 1 | 7.80 |
| CHEMBL495634 | — | — | 1 | 7.55 |
| CHEMBL75306 | — | — | 1 | 7.38 |
| CHEMBL911 | ZOLPIDEM | 4.0 | 1 | 7.30 |
| CHEMBL306310 | — | — | 1 | 6.71 |
| CHEMBL495615 | — | — | 1 | 6.71 |
| CHEMBL495616 | — | — | 1 | 6.70 |
| CHEMBL495592 | — | — | 1 | 6.65 |
| CHEMBL127135 | — | — | 1 | 6.61 |
| CHEMBL495635 | — | — | 1 | 6.61 |
| CHEMBL307139 | — | — | 1 | 6.53 |
| CHEMBL75406 | — | — | 1 | 5.94 |
| CHEMBL522716 | — | — | 1 | 5.69 |
| CHEMBL496228 | — | — | 1 | - |
| CHEMBL522059 | — | — | 1 | - |
| CHEMBL522888 | — | — | 1 | - |
| CHEMBL339918 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL521901 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL12 | DIAZEPAM | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL75456 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL74302 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL495634 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL75306 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL911 | ZOLPIDEM | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL306310 | — | Ki | = | 195.0 | nM | 6.71 |
| CHEMBL495615 | — | Ki | = | 195.0 | nM | 6.71 |
| CHEMBL495616 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL495592 | — | Ki | = | 225.0 | nM | 6.65 |
| CHEMBL127135 | — | Ki | = | 245.0 | nM | 6.61 |
| CHEMBL495635 | — | Ki | = | 246.0 | nM | 6.61 |
| CHEMBL307139 | — | Ki | = | 293.0 | nM | 6.53 |
| CHEMBL75406 | — | Ki | = | 1150.0 | nM | 5.94 |
| CHEMBL522716 | — | Ki | = | 2049.0 | nM | 5.69 |
| CHEMBL496228 | — | Ki | - | — | - | |
| CHEMBL522059 | — | Ki | - | — | - | |
| CHEMBL522888 | — | Ki | - | — | - | |
| CHEMBL339918 | — | Ki | - | — | - |