Assay Detail
Binding
CHEMBL651481
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]- Ro.15-1788 from GABA-A central Benzodiazepine receptor (BzR) of Bovine cerebral cortex membrane
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Bos taurus |
| Tissue | Cerebral cortex |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL2094107) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Bos taurus |
Publication
3-Aryl-[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-ones: tricyclic heteroaromatic derivatives as a new class of benzodiazepine receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 7.53 | 10.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL407 | FLUMAZENIL | 4.0 | 1 | 10.05 |
| CHEMBL452 | CLONAZEPAM | 4.0 | 1 | 9.07 |
| CHEMBL269112 | — | — | 1 | 7.89 |
| CHEMBL7698 | — | — | 1 | 7.36 |
| CHEMBL7113 | — | — | 1 | 7.28 |
| CHEMBL7608 | — | — | 1 | 7.25 |
| CHEMBL7327 | — | — | 1 | 7.13 |
| CHEMBL7953 | — | — | 1 | 6.97 |
| CHEMBL7614 | — | — | 1 | 6.94 |
| CHEMBL7334 | — | — | 1 | 6.77 |
| CHEMBL7909 | — | — | 1 | 6.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL407 | FLUMAZENIL | Ki | = | 0.09 | nM | 10.05 |
| CHEMBL452 | CLONAZEPAM | Ki | = | 0.85 | nM | 9.07 |
| CHEMBL269112 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL7698 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL7113 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL7608 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL7327 | — | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL7953 | — | Ki | = | 107.0 | nM | 6.97 |
| CHEMBL7614 | — | Ki | = | 115.0 | nM | 6.94 |
| CHEMBL7334 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL7909 | — | Ki | = | 860.0 | nM | 6.07 |