Assay Detail
Binding
CHEMBL679468
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Binding affinity for recombinant rat GABA-A receptor alpha-1-beta-2-gamma-2 subunits expressed in HEK293 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 | Autocuration |
Target
GABA-A receptor; alpha-1/beta-2/gamma-2 (CHEMBL2095167) ↗| 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 | 7.72 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL104568 | — | — | 1 | 8.15 |
| CHEMBL322313 | — | — | 1 | 8.00 |
| CHEMBL440150 | — | — | 1 | 8.00 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 7.85 |
| CHEMBL322697 | — | — | 1 | 7.64 |
| CHEMBL107227 | — | — | 1 | 7.60 |
| CHEMBL911 | ZOLPIDEM | 4.0 | 1 | 7.57 |
| CHEMBL107447 | — | — | 1 | 7.37 |
| CHEMBL106051 | — | — | 1 | 7.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL104568 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL322313 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL440150 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL12 | DIAZEPAM | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL322697 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL107227 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL911 | ZOLPIDEM | Ki | = | 26.7 | nM | 7.57 |
| CHEMBL107447 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL106051 | — | Ki | = | 47.0 | nM | 7.33 |