Assay Detail
Binding
CHEMBL682082
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-Ro- 15-1788 from human GABA-A alpha-5-beta-3-gamma-2 receptor subunits expressed in Xenopus oocytes
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Oocyte |
| 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
Selective, orally active gamma-aminobutyric acidA alpha5 receptor inverse agonists as cognition enhancers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 8.58 | 9.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL68684 | — | — | 1 | 9.21 |
| CHEMBL306422 | — | — | 1 | 9.18 |
| CHEMBL68490 | — | — | 1 | 9.10 |
| CHEMBL307111 | — | — | 1 | 9.06 |
| CHEMBL305068 | — | — | 1 | 8.96 |
| CHEMBL69605 | — | — | 1 | 8.70 |
| CHEMBL17468 | — | — | 1 | 8.64 |
| CHEMBL68712 | — | — | 1 | 8.54 |
| CHEMBL62630 | — | — | 1 | 8.51 |
| CHEMBL307230 | — | — | 1 | 8.43 |
| CHEMBL303718 | — | — | 1 | 8.34 |
| CHEMBL451 | CHLORDIAZEPOXIDE | 4.0 | 1 | 6.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL68684 | — | Ki | = | 0.62 | nM | 9.21 |
| CHEMBL306422 | — | Ki | = | 0.66 | nM | 9.18 |
| CHEMBL68490 | — | Ki | = | 0.79 | nM | 9.10 |
| CHEMBL307111 | — | Ki | = | 0.87 | nM | 9.06 |
| CHEMBL305068 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL69605 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL17468 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL68712 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL62630 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL307230 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL303718 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL451 | CHLORDIAZEPOXIDE | Ki | = | 520.0 | nM | 6.28 |