Assay Detail
Binding
CHEMBL685342
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Binding affinity for recombinant rat GABA-A receptor alpha-5-beta-3-gamma-2 subunits expressed in HEK 293 cells
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | HEK293 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Expert |
Target
GABA A receptor alpha-5/beta-3/gamma-2 (CHEMBL2111374) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
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 | 9 | 6.84 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 7.96 |
| CHEMBL440150 | — | — | 1 | 7.66 |
| CHEMBL106051 | — | — | 1 | 6.81 |
| CHEMBL322313 | — | — | 1 | 6.68 |
| CHEMBL107227 | — | — | 1 | 6.68 |
| CHEMBL322697 | — | — | 1 | 6.65 |
| CHEMBL104568 | — | — | 1 | 6.13 |
| CHEMBL107447 | — | — | 1 | 6.13 |
| CHEMBL911 | ZOLPIDEM | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL12 | DIAZEPAM | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL440150 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL106051 | — | Ki | = | 156.0 | nM | 6.81 |
| CHEMBL322313 | — | Ki | = | 207.0 | nM | 6.68 |
| CHEMBL107227 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL322697 | — | Ki | = | 223.0 | nM | 6.65 |
| CHEMBL104568 | — | Ki | = | 740.0 | nM | 6.13 |
| CHEMBL107447 | — | Ki | = | 737.0 | nM | 6.13 |
| CHEMBL911 | ZOLPIDEM | Ki | > | 10000.0 | nM | - |