Assay Detail
Binding
CHEMBL5263769
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Displacement of [35S]-TBPS from rat synaptosomes GABAA receptor incubated for 90 mins by liquid scintillation counting method
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Synaptosome |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Breakthroughs in neuroactive steroid drug discovery.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 6.88 | 7.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5285617 | — | — | 1 | 7.14 |
| CHEMBL207538 | BREXANOLONE | 4.0 | 1 | 7.07 |
| CHEMBL260226 | — | — | 1 | 7.03 |
| CHEMBL5275473 | — | — | 1 | 6.85 |
| CHEMBL259201 | — | — | 1 | 6.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5285617 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL207538 | BREXANOLONE | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL260226 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL5275473 | — | IC50 | = | 141.0 | nM | 6.85 |
| CHEMBL259201 | — | IC50 | = | 490.0 | nM | 6.31 |