Assay Detail
Binding
CHEMBL681840
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity for human GABA-A receptor alpha-2-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 | Expert |
Target
GABA A receptor alpha-2/beta-2/gamma-2 (CHEMBL2111413) ↗| 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 | 7.61 | 8.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6597 | Ro-154513 | — | 1 | 8.59 |
| CHEMBL57655 | — | — | 1 | 8.14 |
| CHEMBL6655 | — | — | 1 | 7.97 |
| CHEMBL286594 | — | — | 1 | 7.67 |
| CHEMBL59180 | — | — | 1 | 7.65 |
| CHEMBL58757 | — | — | 1 | 7.58 |
| CHEMBL58385 | — | — | 1 | 7.57 |
| CHEMBL58570 | — | — | 1 | 7.25 |
| CHEMBL300840 | — | — | 1 | 6.85 |
| CHEMBL59181 | — | — | 1 | 6.85 |
| CHEMBL432104 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6597 | Ro-154513 | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL57655 | — | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL6655 | — | Ki | = | 10.7 | nM | 7.97 |
| CHEMBL286594 | — | Ki | = | 21.4 | nM | 7.67 |
| CHEMBL59180 | — | Ki | = | 22.2 | nM | 7.65 |
| CHEMBL58757 | — | Ki | = | 26.3 | nM | 7.58 |
| CHEMBL58385 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL58570 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL300840 | — | Ki | = | 142.6 | nM | 6.85 |
| CHEMBL59181 | — | Ki | = | 141.9 | nM | 6.85 |
| CHEMBL432104 | — | Ki | > | 300.0 | nM | - |