Assay Detail
Binding
CHEMBL648133
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Displacement of [3H]flunitrazepam from diazepam-sensitive GABA-A benzodiazepine receptor of rat cerebellar membrane
12
Total Activities
12
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 | 12 | 8.05 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL46547 | SARMAZENIL | 2.0 | 1 | 9.70 |
| CHEMBL54069 | — | — | 1 | 9.40 |
| CHEMBL267665 | RO-147437 | — | 1 | 8.89 |
| CHEMBL301513 | — | — | 1 | 8.82 |
| CHEMBL6597 | Ro-154513 | — | 1 | 8.28 |
| CHEMBL145300 | — | — | 1 | 8.27 |
| CHEMBL415290 | Ro-151310 | — | 1 | 8.27 |
| CHEMBL300027 | — | — | 1 | 8.12 |
| CHEMBL52934 | — | — | 1 | 7.86 |
| CHEMBL53425 | — | — | 1 | 7.05 |
| CHEMBL53119 | — | — | 1 | 6.04 |
| CHEMBL291473 | — | — | 1 | 5.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL46547 | SARMAZENIL | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL54069 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL267665 | RO-147437 | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL301513 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL6597 | Ro-154513 | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL145300 | — | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL415290 | Ro-151310 | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL300027 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL52934 | — | Ki | = | 13.7 | nM | 7.86 |
| CHEMBL53425 | — | Ki | = | 88.4 | nM | 7.05 |
| CHEMBL53119 | — | Ki | = | 907.0 | nM | 6.04 |
| CHEMBL291473 | — | Ki | = | 1209.0 | nM | 5.92 |