Assay Detail
Binding
CHEMBL829845
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-Ro- 15-1788 from human gamma-aminobutyric-acid GABA-A receptor alpha-5-beta-3-gamma-2 expressed in L(tk-) cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
GABA-A receptor; alpha-5/beta-3/gamma-2 (CHEMBL2094122) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 4 | 8.28 | 9.18 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL306422 | — | — | 1 | 9.18 |
| CHEMBL363211 | — | — | 1 | 8.85 |
| CHEMBL17468 | — | — | 1 | 8.66 |
| CHEMBL451 | CHLORDIAZEPOXIDE | 4.0 | 1 | 6.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL306422 | — | Ki | = | 0.66 | nM | 9.18 |
| CHEMBL363211 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL17468 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL451 | CHLORDIAZEPOXIDE | Ki | = | 368.0 | nM | 6.43 |