Assay Detail
Binding
CHEMBL681947
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3S]-tert-butylbicyclophosphorothionate (TBPS) from Gamma-aminobutyric acid A (GABA-A) receptor of rat brain membranes
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| 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
Neurosteroid analogues. 8. Structure-activity studies of N-acylated 17a-aza-D-homosteroid analogues of the anesthetic steroids (3alpha, 5alpha)- and (3alpha,5beta)-3-hydroxypregnan-20-one.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 6.46 | 7.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1256760 | — | — | 1 | 7.41 |
| CHEMBL108614 | — | — | 1 | 7.35 |
| CHEMBL210952 | ELTANOLONE | 2.0 | 1 | 7.15 |
| CHEMBL207538 | BREXANOLONE | 4.0 | 1 | 7.13 |
| CHEMBL3140372 | — | — | 1 | 6.92 |
| CHEMBL107932 | — | — | 1 | 6.70 |
| CHEMBL111792 | — | — | 1 | 6.37 |
| CHEMBL325363 | — | — | 1 | 6.26 |
| CHEMBL107980 | — | — | 1 | 6.03 |
| CHEMBL421415 | — | — | 1 | 5.58 |
| CHEMBL432604 | — | — | 1 | 5.46 |
| CHEMBL321866 | — | — | 1 | 5.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1256760 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL108614 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL210952 | ELTANOLONE | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL207538 | BREXANOLONE | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL3140372 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL107932 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL111792 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL325363 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL107980 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL421415 | — | IC50 | = | 2610.0 | nM | 5.58 |
| CHEMBL432604 | — | IC50 | = | 3470.0 | nM | 5.46 |
| CHEMBL321866 | — | IC50 | = | 6220.0 | nM | 5.21 |