Assay Detail
Binding
CHEMBL650287
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Displacement of [3H]- Diazepam from GABA-A Benzodiazepine receptor of rat forebrain
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Synthesis and benzodiazepine binding activity of a series of novel [1,2,4]triazolo[1,5-c]quinazolin-5(6H)-ones.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.16 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL330116 | — | — | 1 | 8.40 |
| CHEMBL318552 | — | — | 1 | 8.00 |
| CHEMBL329300 | — | — | 1 | 7.00 |
| CHEMBL317375 | — | — | 1 | 6.89 |
| CHEMBL330209 | — | — | 1 | 6.70 |
| CHEMBL432061 | — | — | 1 | 6.70 |
| CHEMBL318288 | — | — | 1 | 6.46 |
| CHEMBL329504 | — | — | 1 | - |
| CHEMBL97928 | — | — | 1 | - |
| CHEMBL319071 | — | — | 1 | - |
| CHEMBL327283 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL330116 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL318552 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL329300 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL317375 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL330209 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL432061 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL318288 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL329504 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL97928 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL319071 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL327283 | — | IC50 | > | 1000.0 | nM | - |