Assay Detail
Binding
CHEMBL822944
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]flumazenil binding to rat alpha-1-beta-2-gamma-2 GABA-A receptor subunits expressed in HEK293 cells
7
Total Activities
7
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 | Autocuration |
Target
GABA-A receptor; alpha-1/beta-2/gamma-2 (CHEMBL2095167) ↗| 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 | 7 | 7.19 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL521901 | — | — | 1 | 8.05 |
| CHEMBL75456 | — | — | 1 | 7.85 |
| CHEMBL74302 | — | — | 1 | 7.80 |
| CHEMBL75306 | — | — | 1 | 7.38 |
| CHEMBL495592 | — | — | 1 | 6.65 |
| CHEMBL31796 | — | — | 1 | 6.65 |
| CHEMBL75406 | — | — | 1 | 5.94 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL521901 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL75456 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL74302 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL75306 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL495592 | — | Ki | = | 225.0 | nM | 6.65 |
| CHEMBL31796 | — | Ki | = | 224.0 | nM | 6.65 |
| CHEMBL75406 | — | Ki | = | 1150.0 | nM | 5.94 |