Assay Detail
Binding
CHEMBL652730
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Inhibition of specific binding of 1.5 nM [3H]diazepam to rat brain benzodiazepine receptors
28
Total Activities
28
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
Benzodiazepine receptor binding activity of 8-substituted-9-(3-substituted-benzyl)-6-(dimethylamino)-9H-purines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 6.00 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 8.22 |
| CHEMBL56243 | — | — | 1 | 7.96 |
| CHEMBL61684 | — | — | 1 | 7.60 |
| CHEMBL293038 | — | — | 1 | 7.47 |
| CHEMBL60919 | — | — | 1 | 6.96 |
| CHEMBL292555 | — | — | 1 | 6.96 |
| CHEMBL292062 | — | — | 1 | 6.89 |
| CHEMBL293203 | — | — | 1 | 6.72 |
| CHEMBL451 | CHLORDIAZEPOXIDE | 4.0 | 1 | 6.70 |
| CHEMBL292295 | — | — | 1 | 6.44 |
| CHEMBL60774 | — | — | 1 | 6.22 |
| CHEMBL60940 | — | — | 1 | 6.08 |
| CHEMBL7344 | — | — | 1 | 6.05 |
| CHEMBL293769 | — | — | 1 | 6.00 |
| CHEMBL291875 | — | — | 1 | 5.82 |
| CHEMBL292401 | — | — | 1 | 5.75 |
| CHEMBL60971 | — | — | 1 | 5.52 |
| CHEMBL293221 | — | — | 1 | 5.28 |
| CHEMBL303518 | — | — | 1 | 5.27 |
| CHEMBL302878 | — | — | 1 | 5.24 |
| CHEMBL439754 | — | — | 1 | 5.14 |
| CHEMBL62399 | — | — | 1 | 5.10 |
| CHEMBL60841 | — | — | 1 | 5.07 |
| CHEMBL59453 | — | — | 1 | 5.05 |
| CHEMBL6889 | — | — | 1 | 4.89 |
| CHEMBL292728 | — | — | 1 | 4.77 |
| CHEMBL294070 | — | — | 1 | 4.37 |
| CHEMBL293865 | — | — | 1 | 4.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL12 | DIAZEPAM | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL56243 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL61684 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL293038 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL60919 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL292555 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL292062 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL293203 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL451 | CHLORDIAZEPOXIDE | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL292295 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL60774 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL60940 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL7344 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL293769 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL291875 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL292401 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL60971 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL293221 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL303518 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL302878 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL439754 | — | IC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL62399 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL60841 | — | IC50 | = | 8500.0 | nM | 5.07 |
| CHEMBL59453 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL6889 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL292728 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL294070 | — | IC50 | = | 43000.0 | nM | 4.37 |
| CHEMBL293865 | — | IC50 | = | 47000.0 | nM | 4.33 |