Assay Detail
Binding
CHEMBL648132
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Displacement of [3H]flunitrazepam from diazepam-insensitive GABA-A benzodiazepine receptor of rat cerebellar membrane
13
Total Activities
10
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 structure-activity relationships of 3,5-disubstituted 4,5-dihydro-6H-imidazo[1,5-a][1,4]benzodiazepin-6-ones at diazepam-sensitive and diazepam-insensitive benzodiazepine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 7.46 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL52934 | — | — | 2 | 8.85 |
| CHEMBL6597 | Ro-154513 | — | 1 | 8.51 |
| CHEMBL53425 | — | — | 2 | 8.14 |
| CHEMBL415290 | Ro-151310 | — | 1 | 7.77 |
| CHEMBL46547 | SARMAZENIL | 2.0 | 1 | 7.70 |
| CHEMBL54069 | — | — | 1 | 7.70 |
| CHEMBL301513 | — | — | 1 | 6.95 |
| CHEMBL145300 | — | — | 1 | 6.90 |
| CHEMBL300027 | — | — | 2 | 6.74 |
| CHEMBL267665 | RO-147437 | — | 1 | 6.67 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL52934 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL6597 | Ro-154513 | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL53425 | — | Ki | = | 7.3 | nM | 8.14 |
| CHEMBL52934 | — | Ki | = | 10.9 | nM | 7.96 |
| CHEMBL415290 | Ro-151310 | Ki | = | 16.9 | nM | 7.77 |
| CHEMBL46547 | SARMAZENIL | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL54069 | — | Ki | = | 20.2 | nM | 7.70 |
| CHEMBL301513 | — | Ki | = | 112.0 | nM | 6.95 |
| CHEMBL53425 | — | Ki | = | 115.0 | nM | 6.94 |
| CHEMBL145300 | — | Ki | = | 127.0 | nM | 6.90 |
| CHEMBL300027 | — | Ki | = | 184.0 | nM | 6.74 |
| CHEMBL267665 | RO-147437 | Ki | = | 214.0 | nM | 6.67 |
| CHEMBL300027 | — | Ki | = | 761.0 | nM | 6.12 |