Assay Detail
Binding
CHEMBL862974
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Displacement of [3H]flumazenil from GABA-A receptor in rat cortical membranes
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Membrane |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore modeling.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 29 | 7.46 | 10.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL380906 | — | — | 1 | 10.32 |
| CHEMBL425590 | — | — | 1 | 9.77 |
| CHEMBL204566 | — | — | 1 | 9.59 |
| CHEMBL205536 | — | — | 1 | 9.27 |
| CHEMBL381059 | — | — | 1 | 8.85 |
| CHEMBL206068 | — | — | 1 | 8.74 |
| CHEMBL206591 | — | — | 1 | 7.89 |
| CHEMBL202969 | — | — | 1 | 7.82 |
| CHEMBL205257 | — | — | 1 | 7.80 |
| CHEMBL381491 | — | — | 1 | 7.77 |
| CHEMBL202724 | — | — | 1 | 7.72 |
| CHEMBL206540 | — | — | 1 | 7.70 |
| CHEMBL206071 | — | — | 1 | 7.55 |
| CHEMBL377719 | — | — | 1 | 7.55 |
| CHEMBL205252 | — | — | 1 | 7.46 |
| CHEMBL205456 | — | — | 1 | 7.27 |
| CHEMBL382363 | — | — | 1 | 7.11 |
| CHEMBL383080 | — | — | 1 | 7.04 |
| CHEMBL207752 | — | — | 1 | 6.91 |
| CHEMBL206122 | — | — | 1 | 6.68 |
| CHEMBL205724 | — | — | 1 | 6.67 |
| CHEMBL425049 | — | — | 1 | 6.53 |
| CHEMBL203439 | — | — | 1 | 6.06 |
| CHEMBL205528 | — | — | 1 | 5.58 |
| CHEMBL206762 | — | — | 1 | 5.38 |
| CHEMBL205159 | — | — | 1 | 5.18 |
| CHEMBL377064 | — | — | 1 | 5.15 |
| CHEMBL203223 | — | — | 1 | - |
| CHEMBL377939 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL380906 | — | Ki | = | 0.048 | nM | 10.32 |
| CHEMBL425590 | — | Ki | = | 0.17 | nM | 9.77 |
| CHEMBL204566 | — | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL205536 | — | Ki | = | 0.54 | nM | 9.27 |
| CHEMBL381059 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL206068 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL206591 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL202969 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL205257 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL381491 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL202724 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL206540 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL206071 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL377719 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL205252 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL205456 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL382363 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL383080 | — | Ki | = | 92.0 | nM | 7.04 |
| CHEMBL207752 | — | Ki | = | 122.0 | nM | 6.91 |
| CHEMBL206122 | — | Ki | = | 208.0 | nM | 6.68 |
| CHEMBL205724 | — | Ki | = | 214.0 | nM | 6.67 |
| CHEMBL425049 | — | Ki | = | 295.0 | nM | 6.53 |
| CHEMBL203439 | — | Ki | = | 870.0 | nM | 6.06 |
| CHEMBL205528 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL206762 | — | Ki | = | 4200.0 | nM | 5.38 |
| CHEMBL205159 | — | Ki | = | 6580.0 | nM | 5.18 |
| CHEMBL377064 | — | Ki | = | 7130.0 | nM | 5.15 |
| CHEMBL203223 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL377939 | — | Ki | > | 10000.0 | nM | - |