Assay Detail
Binding
CHEMBL861815
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]Flumazenil from human GABA-Aalpha1 receptor plus beta-2-gamma-2 expressed in HEK293 cells
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
GABA A receptor alpha-1/beta-1/gamma-2 (CHEMBL2111392) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
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 | 5 | 8.20 | 9.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL381059 | — | — | 1 | 9.57 |
| CHEMBL206071 | — | — | 1 | 8.39 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 7.92 |
| CHEMBL205257 | — | — | 1 | 7.85 |
| CHEMBL911 | ZOLPIDEM | 4.0 | 1 | 7.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL381059 | — | Ki | = | 0.27 | nM | 9.57 |
| CHEMBL206071 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL12 | DIAZEPAM | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL205257 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL911 | ZOLPIDEM | Ki | = | 53.0 | nM | 7.28 |