Assay Detail
Binding
CHEMBL818517
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]flumazenil binding to rat alpha-5-beta-3-gamma-2 GABA-A receptor subunits expressed in HEK293 cells
6
Total Activities
6
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 | Expert |
Target
GABA A receptor alpha-5/beta-3/gamma-2 (CHEMBL2111374) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Novel N-(arylalkyl)indol-3-ylglyoxylylamides targeted as ligands of the benzodiazepine receptor: synthesis, biological evaluation, and molecular modeling analysis of the structure-activity relationships.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 6.45 | 7.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL74302 | — | — | 1 | 7.24 |
| CHEMBL521901 | — | — | 1 | 7.02 |
| CHEMBL75306 | — | — | 1 | 6.90 |
| CHEMBL75456 | — | — | 1 | 6.62 |
| CHEMBL495592 | — | — | 1 | 5.67 |
| CHEMBL75406 | — | — | 1 | 5.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL74302 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL521901 | — | Ki | = | 95.0 | nM | 7.02 |
| CHEMBL75306 | — | Ki | = | 126.0 | nM | 6.90 |
| CHEMBL75456 | — | Ki | = | 239.0 | nM | 6.62 |
| CHEMBL495592 | — | Ki | = | 2160.0 | nM | 5.67 |
| CHEMBL75406 | — | Ki | = | 5500.0 | nM | 5.26 |