Assay Detail
Binding
CHEMBL680690
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibition of [35S]TBPS binding to gamma-aminobutyric-acid A receptor in rat brain cortical membranes in the presence of 5 uM GABA.
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| 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
3 alpha-Hydroxy-3 beta-(phenylethynyl)-5 beta-pregnan-20-ones: synthesis and pharmacological activity of neuroactive steroids with high affinity for GABAA receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 7.06 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3138009 | — | — | 1 | 8.00 |
| CHEMBL3138300 | — | — | 1 | 7.92 |
| CHEMBL3138433 | — | — | 1 | 7.92 |
| CHEMBL3138003 | — | — | 1 | 7.58 |
| CHEMBL3137972 | — | — | 1 | 7.43 |
| CHEMBL3137986 | — | — | 1 | 7.41 |
| CHEMBL3138291 | — | — | 1 | 7.40 |
| CHEMBL3138013 | — | — | 1 | 7.38 |
| CHEMBL3138006 | — | — | 1 | 7.38 |
| CHEMBL3138295 | — | — | 1 | 7.27 |
| CHEMBL3138020 | — | — | 1 | 7.26 |
| CHEMBL3138022 | — | — | 1 | 7.25 |
| CHEMBL3138298 | — | — | 1 | 7.22 |
| CHEMBL3138007 | — | — | 1 | 7.17 |
| CHEMBL3138021 | — | — | 1 | 7.16 |
| CHEMBL3138397 | — | — | 1 | 7.08 |
| CHEMBL3138288 | — | — | 1 | 7.03 |
| CHEMBL3138289 | — | — | 1 | 7.00 |
| CHEMBL3138023 | — | — | 1 | 6.96 |
| CHEMBL3138296 | — | — | 1 | 6.88 |
| CHEMBL3138025 | — | — | 1 | 6.82 |
| CHEMBL3138019 | — | — | 1 | 6.77 |
| CHEMBL3138286 | — | — | 1 | 6.72 |
| CHEMBL3138008 | — | — | 1 | 6.54 |
| CHEMBL3138024 | — | — | 1 | 6.42 |
| CHEMBL3138299 | — | — | 1 | 6.38 |
| CHEMBL3138394 | — | — | 1 | 5.75 |
| CHEMBL3138292 | — | — | 1 | 5.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3138009 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3138300 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3138433 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3138003 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3137972 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL3137986 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3138291 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3138013 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL3138006 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL3138295 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL3138020 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL3138022 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL3138298 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3138007 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL3138021 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3138397 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL3138288 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL3138289 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3138023 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3138296 | — | IC50 | = | 131.0 | nM | 6.88 |
| CHEMBL3138025 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3138019 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3138286 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3138008 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL3138024 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL3138299 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL3138394 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL3138292 | — | IC50 | = | 2300.0 | nM | 5.64 |