Assay Detail
Binding
CHEMBL650084
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In vitro inhibition of binding to GABA-A central benzodiazepine-receptor of rat brain
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
2-Arylpyrazolo[4,3-c]quinolin-3-ones: novel agonist, partial agonist, and antagonist of benzodiazepines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 9.23 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3144739 | — | — | 1 | 10.00 |
| CHEMBL19732 | CGS-8216 | — | 1 | 9.40 |
| CHEMBL20042 | CGS-9896 | — | 1 | 9.22 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 8.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3144739 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL19732 | CGS-8216 | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL20042 | CGS-9896 | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL12 | DIAZEPAM | IC50 | = | 5.0 | nM | 8.30 |