Assay Detail
Binding
CHEMBL5609169
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [35S]TBPS binding to GABA-A receptor in Sprague-Dawley rat brain cortical membrane incubated for 90 mins by liquid scintillation spectrometry
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cortex |
| Subcellular | Membrane |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Synthesis and evaluation of neuroactive steroids with novel pharmacophore at C-21 let identify a compound with advantageous PK profile and higher EC<sub>50</sub> and E<sub>max</sub> as PAM on GABAA receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 8.81 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5612974 | — | — | 1 | 9.00 |
| CHEMBL5614143 | — | — | 1 | 9.00 |
| CHEMBL5612574 | — | — | 1 | 9.00 |
| CHEMBL5612649 | — | — | 1 | 8.92 |
| CHEMBL4105630 | ZURANOLONE | 4.0 | 1 | 8.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5612974 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5614143 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5612574 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5612649 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4105630 | ZURANOLONE | IC50 | = | 7.0 | nM | 8.15 |