Assay Detail
Binding
CHEMBL954626
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Displacement of [3H]flumazenil from rat GABA-A alpha-2-beta-2-gamma-2 receptor expressed in HEK293 cells
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Gamma-aminobutyric acid receptor subunit alpha-2 (CHEMBL341) ↗| Type | SINGLE PROTEIN |
| 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 | 19 | 6.34 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 7.82 |
| CHEMBL521901 | — | — | 1 | 7.07 |
| CHEMBL127135 | — | — | 1 | 6.93 |
| CHEMBL75456 | — | — | 1 | 6.92 |
| CHEMBL74302 | — | — | 1 | 6.68 |
| CHEMBL495634 | — | — | 1 | 6.64 |
| CHEMBL495616 | — | — | 1 | 6.29 |
| CHEMBL495635 | — | — | 1 | 6.16 |
| CHEMBL911 | ZOLPIDEM | 4.0 | 1 | 6.12 |
| CHEMBL495615 | — | — | 1 | 6.09 |
| CHEMBL75406 | — | — | 1 | 5.81 |
| CHEMBL75306 | — | — | 1 | 5.78 |
| CHEMBL306310 | — | — | 1 | 5.71 |
| CHEMBL307139 | — | — | 1 | 5.53 |
| CHEMBL495592 | — | — | 1 | 5.51 |
| CHEMBL522888 | — | — | 1 | - |
| CHEMBL522059 | — | — | 1 | - |
| CHEMBL496228 | — | — | 1 | - |
| CHEMBL339918 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL12 | DIAZEPAM | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL521901 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL127135 | — | Ki | = | 118.0 | nM | 6.93 |
| CHEMBL75456 | — | Ki | = | 121.0 | nM | 6.92 |
| CHEMBL74302 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL495634 | — | Ki | = | 231.0 | nM | 6.64 |
| CHEMBL495616 | — | Ki | = | 513.0 | nM | 6.29 |
| CHEMBL495635 | — | Ki | = | 690.0 | nM | 6.16 |
| CHEMBL911 | ZOLPIDEM | Ki | = | 765.0 | nM | 6.12 |
| CHEMBL495615 | — | Ki | = | 810.0 | nM | 6.09 |
| CHEMBL75406 | — | Ki | = | 1550.0 | nM | 5.81 |
| CHEMBL75306 | — | Ki | = | 1645.0 | nM | 5.78 |
| CHEMBL306310 | — | Ki | = | 1950.0 | nM | 5.71 |
| CHEMBL307139 | — | Ki | = | 2980.0 | nM | 5.53 |
| CHEMBL495592 | — | Ki | = | 3100.0 | nM | 5.51 |
| CHEMBL522888 | — | Ki | - | — | - | |
| CHEMBL522059 | — | Ki | - | — | - | |
| CHEMBL496228 | — | Ki | - | — | - | |
| CHEMBL339918 | — | Ki | - | — | - |