Assay Detail
Binding
CHEMBL828720
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [35S]TBPS from picrotoxin site of 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. 10. The effect of methyl group substitution at the C-6 and C-7 positions on the GABA modulatory and anesthetic actions of (3alpha,5alpha)- and (3alpha,5beta)-3-hydroxypregnan-20-one.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 6.15 | 8.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3138080 | — | — | 1 | 8.24 |
| CHEMBL3138334 | — | — | 1 | 7.35 |
| CHEMBL210952 | ELTANOLONE | 2.0 | 1 | 7.15 |
| CHEMBL207538 | BREXANOLONE | 4.0 | 1 | 7.13 |
| CHEMBL3138079 | — | — | 1 | 5.98 |
| CHEMBL3138338 | — | — | 1 | 5.91 |
| CHEMBL3138408 | — | — | 1 | 5.91 |
| CHEMBL3138332 | — | — | 1 | 5.53 |
| CHEMBL3138076 | — | — | 1 | 5.51 |
| CHEMBL3138075 | — | — | 1 | 5.22 |
| CHEMBL3138323 | — | — | 1 | 4.97 |
| CHEMBL3138081 | — | — | 1 | 4.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3138080 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL3138334 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL210952 | ELTANOLONE | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL207538 | BREXANOLONE | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL3138079 | — | IC50 | = | 1040.0 | nM | 5.98 |
| CHEMBL3138338 | — | IC50 | = | 1240.0 | nM | 5.91 |
| CHEMBL3138408 | — | IC50 | = | 1240.0 | nM | 5.91 |
| CHEMBL3138332 | — | IC50 | = | 2940.0 | nM | 5.53 |
| CHEMBL3138076 | — | IC50 | = | 3080.0 | nM | 5.51 |
| CHEMBL3138075 | — | IC50 | = | 5990.0 | nM | 5.22 |
| CHEMBL3138323 | — | IC50 | = | 10800.0 | nM | 4.97 |
| CHEMBL3138081 | — | IC50 | = | 12000.0 | nM | 4.92 |