Assay Detail
Binding
CHEMBL3430052
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]TBPS from GABAA receptor in Sprague-Dawley rat brain cortical membrane after 90 mins by liquid scintillation spectrometry
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL2093872) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Homo sapiens |
Publication
Neuroactive Steroids. 1. Positive Allosteric Modulators of the (γ-Aminobutyric Acid)A Receptor: Structure-Activity Relationships of Heterocyclic Substitution at C-21.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 7.35 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3427535 | — | — | 1 | 8.22 |
| CHEMBL3427547 | — | — | 1 | 8.22 |
| CHEMBL3427532 | — | — | 1 | 7.96 |
| CHEMBL3427539 | — | — | 1 | 7.96 |
| CHEMBL3427540 | — | — | 1 | 7.82 |
| CHEMBL3427543 | — | — | 1 | 7.80 |
| CHEMBL3427542 | — | — | 1 | 7.80 |
| CHEMBL3427544 | — | — | 1 | 7.77 |
| CHEMBL3427531 | — | — | 1 | 7.68 |
| CHEMBL207538 | BREXANOLONE | 4.0 | 1 | 7.66 |
| CHEMBL3427545 | — | — | 1 | 7.62 |
| CHEMBL3427537 | — | — | 1 | 7.62 |
| CHEMBL3427548 | — | — | 1 | 7.60 |
| CHEMBL3427533 | — | — | 1 | 7.57 |
| CHEMBL3427526 | — | — | 1 | 7.51 |
| CHEMBL3427530 | — | — | 1 | 7.50 |
| CHEMBL3427546 | — | — | 1 | 7.48 |
| CHEMBL3427541 | — | — | 1 | 7.38 |
| CHEMBL1568698 | GANAXOLONE | 4.0 | 1 | 7.38 |
| CHEMBL3427538 | — | — | 1 | 7.30 |
| CHEMBL3427523 | — | — | 1 | 7.27 |
| CHEMBL3427528 | — | — | 1 | 7.26 |
| CHEMBL3427536 | — | — | 1 | 7.16 |
| CHEMBL3427519 | — | — | 1 | 7.13 |
| CHEMBL3427524 | — | — | 1 | 6.99 |
| CHEMBL3427522 | — | — | 1 | 6.97 |
| CHEMBL3427534 | — | — | 1 | 6.85 |
| CHEMBL3427521 | — | — | 1 | 6.83 |
| CHEMBL3427525 | — | — | 1 | 6.76 |
| CHEMBL3427527 | — | — | 1 | 6.67 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3427535 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3427547 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3427532 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3427539 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3427540 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3427543 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3427542 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3427544 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3427531 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL207538 | BREXANOLONE | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3427545 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3427537 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3427548 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3427533 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3427526 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL3427530 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3427546 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL3427541 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL1568698 | GANAXOLONE | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL3427538 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3427523 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL3427528 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL3427536 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL3427519 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL3427524 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL3427522 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL3427534 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3427521 | — | IC50 | = | 149.0 | nM | 6.83 |
| CHEMBL3427525 | — | IC50 | = | 174.0 | nM | 6.76 |
| CHEMBL3427527 | — | IC50 | = | 214.0 | nM | 6.67 |
| CHEMBL3427529 | — | IC50 | = | 1289.0 | nM | 5.89 |
| CHEMBL3427520 | — | IC50 | = | 2886.0 | nM | 5.54 |