Assay Detail
Binding
CHEMBL4040853
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [35S]TBPS from GABA-A receptor in Sprague-Dawley rat cerebral cortex cell membranes after 90 mins in presence of GABA by liquid scintillation counting
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Neuroactive Steroids. 2. 3α-Hydroxy-3β-methyl-21-(4-cyano-1H-pyrazol-1'-yl)-19-nor-5β-pregnan-20-one (SAGE-217): A Clinical Next Generation Neuroactive Steroid Positive Allosteric Modulator of the (γ-Aminobutyric Acid)A Receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 7.57 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4105630 | ZURANOLONE | 4.0 | 1 | 8.15 |
| CHEMBL4103751 | — | — | 1 | 8.10 |
| CHEMBL3427532 | — | — | 1 | 7.96 |
| CHEMBL4085062 | — | — | 1 | 7.89 |
| CHEMBL4073780 | — | — | 1 | 7.89 |
| CHEMBL4084134 | — | — | 1 | 7.80 |
| CHEMBL4104908 | — | — | 1 | 7.77 |
| CHEMBL4091891 | — | — | 1 | 7.75 |
| CHEMBL4062424 | — | — | 1 | 7.68 |
| CHEMBL207538 | BREXANOLONE | 4.0 | 1 | 7.66 |
| CHEMBL4081622 | — | — | 1 | 7.55 |
| CHEMBL3427530 | — | — | 1 | 7.52 |
| CHEMBL4100583 | — | — | 1 | 7.44 |
| CHEMBL4103198 | — | — | 1 | 7.35 |
| CHEMBL4073679 | — | — | 1 | 7.31 |
| CHEMBL4071062 | — | — | 1 | 7.19 |
| CHEMBL4072311 | — | — | 1 | 7.11 |
| CHEMBL4078922 | — | — | 1 | 7.10 |
| CHEMBL4098519 | — | — | 1 | 6.60 |
| CHEMBL4080678 | — | — | 1 | - |
| CHEMBL4099623 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4105630 | ZURANOLONE | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4103751 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3427532 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4085062 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4073780 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4084134 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4104908 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4091891 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4062424 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL207538 | BREXANOLONE | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4081622 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3427530 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4100583 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4103198 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4073679 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4071062 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL4072311 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL4078922 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4098519 | — | IC50 | = | 251.0 | nM | 6.60 |
| CHEMBL4080678 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4099623 | — | IC50 | > | 3000.0 | nM | - |