Assay Detail
Binding
CHEMBL678744
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Binding affinity for human GABA-A receptor alpha-5--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 | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
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 | 8.98 | 9.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6597 | Ro-154513 | — | 1 | 9.59 |
| CHEMBL58757 | — | — | 1 | 9.40 |
| CHEMBL6655 | — | — | 1 | 9.30 |
| CHEMBL286594 | — | — | 1 | 9.30 |
| CHEMBL57655 | — | — | 1 | 8.96 |
| CHEMBL58385 | — | — | 1 | 8.82 |
| CHEMBL58570 | — | — | 1 | 8.77 |
| CHEMBL59180 | — | — | 1 | 8.77 |
| CHEMBL300840 | — | — | 1 | 8.58 |
| CHEMBL59181 | — | — | 1 | 8.30 |
| CHEMBL432104 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6597 | Ro-154513 | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL58757 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL6655 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL286594 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL57655 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL58385 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL58570 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL59180 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL300840 | — | Ki | = | 2.61 | nM | 8.58 |
| CHEMBL59181 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL432104 | — | Ki | > | 300.0 | nM | - |