Assay Detail
Binding
CHEMBL3395250
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-flumazenil from benzodiazepine receptor in Sprague-Dawley rat brain cortical membranes incubated for 35 mins
14
Total Activities
7
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Novel agonists of benzodiazepine receptors: design, synthesis, binding assay and pharmacological evaluation of 1,2,4-triazolo[1,5-a]pyrimidinone and 3-amino-1,2,4-triazole derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 8.75 | 9.17 |
| Ki | 7 | 8.96 | 9.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3394789 | — | — | 2 | 9.38 |
| CHEMBL3394790 | — | — | 2 | 9.28 |
| CHEMBL3394788 | — | — | 2 | 9.01 |
| CHEMBL3394792 | — | — | 2 | 8.86 |
| CHEMBL3394787 | — | — | 2 | 8.84 |
| CHEMBL12 | DIAZEPAM | 4.0 | 2 | 8.81 |
| CHEMBL3394791 | — | — | 2 | 8.56 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3394789 | — | Ki | = | 0.42 | nM | 9.38 |
| CHEMBL3394790 | — | Ki | = | 0.53 | nM | 9.28 |
| CHEMBL3394789 | — | IC50 | = | 0.68 | nM | 9.17 |
| CHEMBL3394790 | — | IC50 | = | 0.87 | nM | 9.06 |
| CHEMBL3394788 | — | Ki | = | 0.97 | nM | 9.01 |
| CHEMBL3394792 | — | Ki | = | 1.37 | nM | 8.86 |
| CHEMBL3394787 | — | Ki | = | 1.46 | nM | 8.84 |
| CHEMBL12 | DIAZEPAM | Ki | = | 1.53 | nM | 8.81 |
| CHEMBL3394788 | — | IC50 | = | 1.59 | nM | 8.80 |
| CHEMBL3394792 | — | IC50 | = | 2.24 | nM | 8.65 |
| CHEMBL3394787 | — | IC50 | = | 2.39 | nM | 8.62 |
| CHEMBL12 | DIAZEPAM | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL3394791 | — | Ki | = | 2.73 | nM | 8.56 |
| CHEMBL3394791 | — | IC50 | = | 4.45 | nM | 8.35 |