Assay Detail
Binding
CHEMBL680684
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Inhibition of [35S]TBPS binding to GABA-A receptor rat whole brain membranes
10
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Brain membranes |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Novel water soluble 2,6-dimethoxyphenyl ester derivatives with intravenous anaesthetic activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 4.46 | 5.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL526 | PROPOFOL | 4.0 | 1 | 5.09 |
| CHEMBL13254 | ORG-24447 | — | 1 | 4.53 |
| CHEMBL58242 | — | — | 3 | 4.49 |
| CHEMBL294239 | — | — | 3 | 4.46 |
| CHEMBL58044 | — | — | 2 | 4.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL526 | PROPOFOL | IC50 | = | 8100.0 | nM | 5.09 |
| CHEMBL13254 | ORG-24447 | IC50 | = | 29300.0 | nM | 4.53 |
| CHEMBL58242 | — | IC50 | = | 32500.0 | nM | 4.49 |
| CHEMBL294239 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL58044 | — | IC50 | = | 34900.0 | nM | 4.46 |
| CHEMBL294239 | — | IC50 | = | 35800.0 | nM | 4.45 |
| CHEMBL58242 | — | IC50 | = | 69500.0 | nM | 4.16 |
| CHEMBL294239 | — | IC50 | = | 98300.0 | nM | 4.01 |
| CHEMBL58242 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL58044 | — | IC50 | > | 100000.0 | nM | - |