Assay Detail
Binding
CHEMBL682712
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-2-beta-3-gamma-2 receptor subunits expressed in Xenopus oocytes
11
Total Activities
11
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-2/beta-3/gamma-2 (CHEMBL2094130) ↗| 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 | 11 | 7.82 | 9.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL306422 | — | — | 1 | 9.24 |
| CHEMBL68684 | — | — | 1 | 8.82 |
| CHEMBL68490 | — | — | 1 | 8.80 |
| CHEMBL69605 | — | — | 1 | 8.55 |
| CHEMBL17468 | — | — | 1 | 7.96 |
| CHEMBL305068 | — | — | 1 | 7.77 |
| CHEMBL68712 | — | — | 1 | 7.34 |
| CHEMBL62630 | — | — | 1 | 7.20 |
| CHEMBL303718 | — | — | 1 | 7.07 |
| CHEMBL307230 | — | — | 1 | 6.96 |
| CHEMBL451 | CHLORDIAZEPOXIDE | 4.0 | 1 | 6.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL306422 | — | Ki | = | 0.58 | nM | 9.24 |
| CHEMBL68684 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL68490 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL69605 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL17468 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL305068 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL68712 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL62630 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL303718 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL307230 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL451 | CHLORDIAZEPOXIDE | Ki | = | 460.0 | nM | 6.34 |