Assay Detail
Binding
CHEMBL4040856
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Positive allosteric modulation of GABAA receptor alpha4beta3delta (unknown origin) expressed in CHO cells assessed as potentiation of GABA-mediated increase in channel current under holding potential at -80 mV preincubated for 30 secs followed by GABA stimulation for 2 secs by manual patch clamp assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Gamma-aminobutyric acid receptor subunit alpha-4/beta3/delta (CHEMBL3430899) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
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 |
|---|---|---|---|
| EC50 | 21 | 6.27 | 7.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL207538 | BREXANOLONE | 4.0 | 1 | 7.12 |
| CHEMBL4073780 | — | — | 1 | 6.96 |
| CHEMBL4062424 | — | — | 1 | 6.72 |
| CHEMBL3427532 | — | — | 1 | 6.62 |
| CHEMBL4105630 | ZURANOLONE | 4.0 | 1 | 6.52 |
| CHEMBL4084134 | — | — | 1 | 6.24 |
| CHEMBL4085062 | — | — | 1 | 6.13 |
| CHEMBL3427530 | — | — | 1 | 5.91 |
| CHEMBL4073679 | — | — | 1 | 5.87 |
| CHEMBL4103751 | — | — | 1 | 5.80 |
| CHEMBL4080678 | — | — | 1 | 5.70 |
| CHEMBL4081622 | — | — | 1 | 5.69 |
| CHEMBL4098519 | — | — | 1 | - |
| CHEMBL4072311 | — | — | 1 | - |
| CHEMBL4104908 | — | — | 1 | - |
| CHEMBL4100583 | — | — | 1 | - |
| CHEMBL4099623 | — | — | 1 | - |
| CHEMBL4071062 | — | — | 1 | - |
| CHEMBL4091891 | — | — | 1 | - |
| CHEMBL4078922 | — | — | 1 | - |
| CHEMBL4103198 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL207538 | BREXANOLONE | EC50 | = | 75.5 | nM | 7.12 |
| CHEMBL4073780 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4062424 | — | EC50 | = | 192.0 | nM | 6.72 |
| CHEMBL3427532 | — | EC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4105630 | ZURANOLONE | EC50 | = | 299.0 | nM | 6.52 |
| CHEMBL4084134 | — | EC50 | = | 577.0 | nM | 6.24 |
| CHEMBL4085062 | — | EC50 | = | 744.0 | nM | 6.13 |
| CHEMBL3427530 | — | EC50 | = | 1242.0 | nM | 5.91 |
| CHEMBL4073679 | — | EC50 | = | 1355.0 | nM | 5.87 |
| CHEMBL4103751 | — | EC50 | = | 1601.0 | nM | 5.80 |
| CHEMBL4080678 | — | EC50 | = | 2012.0 | nM | 5.70 |
| CHEMBL4081622 | — | EC50 | = | 2052.0 | nM | 5.69 |
| CHEMBL4098519 | — | EC50 | - | — | - | |
| CHEMBL4072311 | — | EC50 | - | — | - | |
| CHEMBL4104908 | — | EC50 | - | — | - | |
| CHEMBL4100583 | — | EC50 | - | — | - | |
| CHEMBL4099623 | — | EC50 | - | — | - | |
| CHEMBL4071062 | — | EC50 | - | — | - | |
| CHEMBL4091891 | — | EC50 | - | — | - | |
| CHEMBL4078922 | — | EC50 | - | — | - | |
| CHEMBL4103198 | — | EC50 | - | — | - |