Assay Detail
Binding
CHEMBL650681
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Inhibition of [3H]Ro-151788 binding to GABA-A central benzodiazepine receptor of bovine brain membranes
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Bos taurus |
| Subcellular | Brain membranes |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL2094107) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Bos taurus |
Publication
Synthesis and benzodiazepine receptor affinity of pyrazolo[1,5-a]pyrimidine derivatives. 3. New 6-(3-thienyl) series as alpha 1 selective ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 7.79 | 8.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL104568 | — | — | 1 | 8.41 |
| CHEMBL322313 | — | — | 1 | 8.24 |
| CHEMBL440150 | — | — | 1 | 8.06 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 8.00 |
| CHEMBL107227 | — | — | 1 | 7.52 |
| CHEMBL109114 | — | — | 1 | 7.51 |
| CHEMBL106051 | — | — | 1 | 7.40 |
| CHEMBL105873 | — | — | 1 | 7.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL104568 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL322313 | — | Ki | = | 5.8 | nM | 8.24 |
| CHEMBL440150 | — | Ki | = | 8.8 | nM | 8.06 |
| CHEMBL12 | DIAZEPAM | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL107227 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL109114 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL106051 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL105873 | — | Ki | = | 73.0 | nM | 7.14 |