Assay Detail
Binding
CHEMBL650464
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Displacement of [3H]-diazepam from GABA-A benzodiazepine receptor of rat cerebral cortex
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
A new thienylpyrazoloquinoline: a potent and orally active inverse agonist to benzodiazepine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 9.12 | 9.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL19732 | CGS-8216 | — | 1 | 9.66 |
| CHEMBL3144843 | — | — | 1 | 9.50 |
| CHEMBL3144626 | — | — | 1 | 9.49 |
| CHEMBL11709 | — | — | 1 | 8.94 |
| CHEMBL453066 | BETA-CCM | — | 1 | 8.83 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 8.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL19732 | CGS-8216 | Ki | = | 0.221 | nM | 9.66 |
| CHEMBL3144843 | — | Ki | = | 0.316 | nM | 9.50 |
| CHEMBL3144626 | — | Ki | = | 0.32 | nM | 9.49 |
| CHEMBL11709 | — | Ki | = | 1.14 | nM | 8.94 |
| CHEMBL453066 | BETA-CCM | Ki | = | 1.47 | nM | 8.83 |
| CHEMBL12 | DIAZEPAM | Ki | = | 5.02 | nM | 8.30 |