Assay Detail
Binding
CHEMBL954623
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]flumazenil from Benzodiazepine receptor in bovine cerebral cortex membrane
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Bos taurus |
| Tissue | Cerebral cortex |
| Subcellular | Membrane |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
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 | 18 | 6.93 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 8.00 |
| CHEMBL495634 | — | — | 1 | 7.89 |
| CHEMBL75456 | — | — | 1 | 7.77 |
| CHEMBL74302 | — | — | 1 | 7.68 |
| CHEMBL521901 | — | — | 1 | 7.55 |
| CHEMBL911 | ZOLPIDEM | 4.0 | 1 | 7.29 |
| CHEMBL127135 | — | — | 1 | 7.28 |
| CHEMBL75306 | — | — | 1 | 7.28 |
| CHEMBL75307 | — | — | 1 | 6.93 |
| CHEMBL75289 | — | — | 1 | 6.92 |
| CHEMBL306310 | — | — | 1 | 6.79 |
| CHEMBL495616 | — | — | 1 | 6.75 |
| CHEMBL495615 | — | — | 1 | 6.52 |
| CHEMBL307139 | — | — | 1 | 6.21 |
| CHEMBL495635 | — | — | 1 | 6.20 |
| CHEMBL495592 | — | — | 1 | 6.17 |
| CHEMBL75406 | — | — | 1 | 5.88 |
| CHEMBL522716 | — | — | 1 | 5.67 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL12 | DIAZEPAM | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL495634 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL75456 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL74302 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL521901 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL911 | ZOLPIDEM | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL127135 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL75306 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL75307 | — | Ki | = | 117.0 | nM | 6.93 |
| CHEMBL75289 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL306310 | — | Ki | = | 163.0 | nM | 6.79 |
| CHEMBL495616 | — | Ki | = | 178.0 | nM | 6.75 |
| CHEMBL495615 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL307139 | — | Ki | = | 620.0 | nM | 6.21 |
| CHEMBL495635 | — | Ki | = | 636.0 | nM | 6.20 |
| CHEMBL495592 | — | Ki | = | 675.0 | nM | 6.17 |
| CHEMBL75406 | — | Ki | = | 1307.0 | nM | 5.88 |
| CHEMBL522716 | — | Ki | = | 2160.0 | nM | 5.67 |