Assay Detail
Binding
CHEMBL680435
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-3-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-3/beta-3/gamma-2 (CHEMBL2094120) ↗| 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 | 8.04 | 9.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL306422 | — | — | 1 | 9.21 |
| CHEMBL307111 | — | — | 1 | 9.10 |
| CHEMBL68684 | — | — | 1 | 9.02 |
| CHEMBL68490 | — | — | 1 | 8.89 |
| CHEMBL69605 | — | — | 1 | 8.28 |
| CHEMBL305068 | — | — | 1 | 8.12 |
| CHEMBL17468 | — | — | 1 | 8.00 |
| CHEMBL68712 | — | — | 1 | 7.60 |
| CHEMBL62630 | — | — | 1 | 7.40 |
| CHEMBL303718 | — | — | 1 | 7.39 |
| CHEMBL307230 | — | — | 1 | 7.32 |
| CHEMBL451 | CHLORDIAZEPOXIDE | 4.0 | 1 | 6.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL306422 | — | Ki | = | 0.61 | nM | 9.21 |
| CHEMBL307111 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL68684 | — | Ki | = | 0.96 | nM | 9.02 |
| CHEMBL68490 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL69605 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL305068 | — | Ki | = | 7.6 | nM | 8.12 |
| CHEMBL17468 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL68712 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL62630 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL303718 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL307230 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL451 | CHLORDIAZEPOXIDE | Ki | = | 740.0 | nM | 6.13 |