Assay Detail
Binding
CHEMBL676825
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity for human GABA-A receptor alpha-1-beta-2-gamma-2 expressed in L(tk-) cell membranes
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
GABA-A receptor; alpha-1/beta-2/gamma-2 (CHEMBL2095172) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Synthesis and pharmacological properties of novel 8-substituted imidazobenzodiazepines: high-affinity, selective probes for alpha 5-containing GABAA receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 7.71 | 8.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6597 | Ro-154513 | — | 1 | 8.48 |
| CHEMBL57655 | — | — | 1 | 8.42 |
| CHEMBL59180 | — | — | 1 | 8.00 |
| CHEMBL6655 | — | — | 1 | 7.94 |
| CHEMBL58570 | — | — | 1 | 7.83 |
| CHEMBL58385 | — | — | 1 | 7.69 |
| CHEMBL58757 | — | — | 1 | 7.57 |
| CHEMBL286594 | — | — | 1 | 7.55 |
| CHEMBL59181 | — | — | 1 | 6.92 |
| CHEMBL300840 | — | — | 1 | 6.71 |
| CHEMBL432104 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6597 | Ro-154513 | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL57655 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL59180 | — | Ki | = | 10.1 | nM | 8.00 |
| CHEMBL6655 | — | Ki | = | 11.4 | nM | 7.94 |
| CHEMBL58570 | — | Ki | = | 14.8 | nM | 7.83 |
| CHEMBL58385 | — | Ki | = | 20.4 | nM | 7.69 |
| CHEMBL58757 | — | Ki | = | 26.9 | nM | 7.57 |
| CHEMBL286594 | — | Ki | = | 28.4 | nM | 7.55 |
| CHEMBL59181 | — | Ki | = | 121.1 | nM | 6.92 |
| CHEMBL300840 | — | Ki | = | 197.0 | nM | 6.71 |
| CHEMBL432104 | — | Ki | > | 300.0 | nM | - |