Assay Detail
Binding
CHEMBL1111366
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]Flumazenil from cloned human GABA alpha-2-beta-3-gamma-2 receptor expressed in HEK293 cells
6
Total Activities
6
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-2/beta-3/gamma-2 (CHEMBL2094130) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
The discovery and unique pharmacological profile of RO4938581 and RO4882224 as potent and selective GABAA alpha5 inverse agonists for the treatment of cognitive dysfunction.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 7.08 | 7.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1077391 | — | — | 1 | 7.62 |
| CHEMBL1078985 | — | — | 1 | 7.62 |
| CHEMBL1080412 | — | — | 1 | 7.09 |
| CHEMBL1078580 | — | — | 1 | 6.73 |
| CHEMBL1080588 | — | — | 1 | 6.73 |
| CHEMBL1077381 | — | — | 1 | 6.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1077391 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL1078985 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL1080412 | — | Ki | = | 81.0 | nM | 7.09 |
| CHEMBL1078580 | — | Ki | = | 186.0 | nM | 6.73 |
| CHEMBL1080588 | — | Ki | = | 185.0 | nM | 6.73 |
| CHEMBL1077381 | — | Ki | = | 219.0 | nM | 6.66 |