Assay Detail
Binding
CHEMBL648141
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Binding affinity for Diazepam-Insensitive fraction of GABA-A benzodiazepine receptors
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Synthesis and evaluation of imidazo[1,5-a][1,4]benzodiazepine esters with high affinities and selectivities at "diazepam-insensitive" benzodiazepine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 7.79 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6659 | — | — | 1 | 8.82 |
| CHEMBL415293 | — | — | 1 | 8.77 |
| CHEMBL269366 | RO-194603 | — | 1 | 8.59 |
| CHEMBL6814 | — | — | 1 | 8.57 |
| CHEMBL6861 | — | — | 1 | 8.06 |
| CHEMBL6862 | — | — | 1 | 7.48 |
| CHEMBL6752 | — | — | 1 | 7.28 |
| CHEMBL7069 | — | — | 1 | 6.91 |
| CHEMBL266943 | — | — | 1 | 6.91 |
| CHEMBL6793 | — | — | 1 | 6.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6659 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL415293 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL269366 | RO-194603 | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL6814 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL6861 | — | Ki | = | 8.8 | nM | 8.06 |
| CHEMBL6862 | — | Ki | = | 33.3 | nM | 7.48 |
| CHEMBL6752 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL7069 | — | Ki | = | 122.6 | nM | 6.91 |
| CHEMBL266943 | — | Ki | = | 123.5 | nM | 6.91 |
| CHEMBL6793 | — | Ki | = | 299.6 | nM | 6.52 |