Assay Detail
Functional
CHEMBL822946
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Potentiation of GABA-activated currents in Xenopus oocytes expressing cloned human alpha-1-beta-2-gamma-2L subunits of GABA-A receptor
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | Oocyte |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
GABA-A receptor; alpha-1/beta-2/gamma-2 (CHEMBL2095172) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Synthesis and in vitro activity of 3 beta-substituted-3 alpha-hydroxypregnan-20-ones: allosteric modulators of the GABAA receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 6 | 6.65 | 6.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3137994 | — | — | 1 | 6.82 |
| CHEMBL207538 | BREXANOLONE | 4.0 | 1 | 6.80 |
| CHEMBL1568698 | GANAXOLONE | 4.0 | 1 | 6.58 |
| CHEMBL3137990 | — | — | 1 | 6.41 |
| CHEMBL3137988 | — | — | 1 | - |
| CHEMBL3137984 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3137994 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL207538 | BREXANOLONE | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL1568698 | GANAXOLONE | EC50 | = | 260.0 | nM | 6.58 |
| CHEMBL3137990 | — | EC50 | = | 390.0 | nM | 6.41 |
| CHEMBL3137988 | — | EC50 | ~ | 20000.0 | nM | - |
| CHEMBL3137984 | — | EC50 | > | 50000.0 | nM | - |