Assay Detail
Binding
CHEMBL647210
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Binding affinity for Diazepam-Sensitive fraction of GABA-A benzodiazepine receptors
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| 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 | 16 | 8.21 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL407 | FLUMAZENIL | 4.0 | 1 | 9.10 |
| CHEMBL6752 | — | — | 1 | 9.05 |
| CHEMBL173082 | — | — | 1 | 9.05 |
| CHEMBL7298 | — | — | 1 | 8.96 |
| CHEMBL268626 | — | — | 1 | 8.85 |
| CHEMBL6421 | — | — | 1 | 8.68 |
| CHEMBL6814 | — | — | 1 | 8.43 |
| CHEMBL415293 | — | — | 1 | 8.40 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 8.18 |
| CHEMBL6659 | — | — | 1 | 8.15 |
| CHEMBL6861 | — | — | 1 | 7.98 |
| CHEMBL6862 | — | — | 1 | 7.61 |
| CHEMBL7069 | — | — | 1 | 7.57 |
| CHEMBL266943 | — | — | 1 | 7.53 |
| CHEMBL269705 | RO-145975 | — | 1 | 7.14 |
| CHEMBL6826 | — | — | 1 | 6.74 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL407 | FLUMAZENIL | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL6752 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL173082 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL7298 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL268626 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL6421 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL6814 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL415293 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL12 | DIAZEPAM | Ki | = | 6.6 | nM | 8.18 |
| CHEMBL6659 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL6861 | — | Ki | = | 10.5 | nM | 7.98 |
| CHEMBL6862 | — | Ki | = | 24.8 | nM | 7.61 |
| CHEMBL7069 | — | Ki | = | 26.9 | nM | 7.57 |
| CHEMBL266943 | — | Ki | = | 29.8 | nM | 7.53 |
| CHEMBL269705 | RO-145975 | Ki | = | 72.0 | nM | 7.14 |
| CHEMBL6826 | — | Ki | = | 184.0 | nM | 6.74 |