Assay Detail
Binding
CHEMBL653130
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In vitro inhibition of [3H]diazepam binding to rat cerebral cortical membrane benzodiazepine receptors
24
Total Activities
22
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
Biomimetic approach to potential benzodiazepine receptor agonists and antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 24 | 5.18 | 7.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL307061 | — | — | 1 | 7.00 |
| CHEMBL11709 | — | — | 1 | 6.00 |
| CHEMBL453066 | BETA-CCM | — | 1 | 6.00 |
| CHEMBL273491 | — | — | 1 | 5.41 |
| CHEMBL153069 | — | — | 1 | 5.00 |
| CHEMBL156897 | CANTHIN-6-ONE | — | 1 | 5.00 |
| CHEMBL154343 | — | — | 1 | 5.00 |
| CHEMBL346663 | — | — | 1 | 4.95 |
| CHEMBL416152 | — | — | 1 | 4.88 |
| CHEMBL152492 | — | — | 1 | 4.50 |
| CHEMBL11863 | — | — | 1 | 4.24 |
| CHEMBL346218 | — | — | 1 | 4.17 |
| CHEMBL154573 | — | — | 1 | - |
| CHEMBL152548 | — | — | 1 | - |
| CHEMBL440184 | — | — | 1 | - |
| CHEMBL417982 | — | — | 1 | - |
| CHEMBL154813 | — | — | 1 | - |
| CHEMBL346949 | — | — | 1 | - |
| CHEMBL152662 | — | — | 1 | - |
| CHEMBL357950 | — | — | 2 | - |
| CHEMBL273939 | — | — | 1 | - |
| CHEMBL152566 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL307061 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL453066 | BETA-CCM | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL11709 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL273491 | — | Ki | = | 3890.0 | nM | 5.41 |
| CHEMBL153069 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL156897 | CANTHIN-6-ONE | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL154343 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL346663 | — | Ki | = | 11200.0 | nM | 4.95 |
| CHEMBL416152 | — | Ki | = | 13200.0 | nM | 4.88 |
| CHEMBL152492 | — | Ki | = | 32000.0 | nM | 4.50 |
| CHEMBL11863 | — | Ki | = | 58000.0 | nM | 4.24 |
| CHEMBL346218 | — | Ki | = | 68000.0 | nM | 4.17 |
| CHEMBL152566 | — | Ki | > | 50000.0 | nM | - |
| CHEMBL273939 | — | Ki | > | 50000.0 | nM | - |
| CHEMBL357950 | — | Ki | > | 50000.0 | nM | - |
| CHEMBL152662 | — | Ki | > | 50000.0 | nM | - |
| CHEMBL154573 | — | Ki | > | 50000.0 | nM | - |
| CHEMBL346949 | — | Ki | > | 50000.0 | nM | - |
| CHEMBL152566 | — | Ki | > | 50000.0 | nM | - |
| CHEMBL417982 | — | Ki | = | 1470000.0 | nM | - |
| CHEMBL357950 | — | Ki | > | 50000.0 | nM | - |
| CHEMBL440184 | — | Ki | = | 750000.0 | nM | - |
| CHEMBL152548 | — | Ki | > | 50000.0 | nM | - |
| CHEMBL154813 | — | Ki | > | 50000.0 | nM | - |