Assay Detail
Binding
CHEMBL839964
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Displacement of [3H]flumazenil from bovine benzodiazepine receptor GABA-A channel of brain membranes
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Bos taurus |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL2093872) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Homo sapiens |
Publication
High affinity central benzodiazepine receptor ligands: synthesis and biological evaluation of a series of phenyltriazolobenzotriazindione derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 7.63 | 9.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL452 | CLONAZEPAM | 4.0 | 1 | 9.07 |
| CHEMBL407 | FLUMAZENIL | 4.0 | 1 | 9.05 |
| CHEMBL372281 | — | — | 1 | 8.55 |
| CHEMBL191088 | — | — | 1 | 8.22 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 8.00 |
| CHEMBL192554 | — | — | 1 | 7.96 |
| CHEMBL192555 | — | — | 1 | 7.66 |
| CHEMBL371834 | — | — | 1 | 7.42 |
| CHEMBL192198 | — | — | 1 | 7.27 |
| CHEMBL191978 | — | — | 1 | 7.25 |
| CHEMBL193141 | — | — | 1 | 6.77 |
| CHEMBL192615 | — | — | 1 | 6.73 |
| CHEMBL193203 | — | — | 1 | 6.65 |
| CHEMBL190768 | — | — | 1 | 6.21 |
| CHEMBL193230 | — | — | 1 | - |
| CHEMBL365808 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL452 | CLONAZEPAM | Ki | = | 0.85 | nM | 9.07 |
| CHEMBL407 | FLUMAZENIL | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL372281 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL191088 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL12 | DIAZEPAM | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL192554 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL192555 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL371834 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL192198 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL191978 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL193141 | — | Ki | = | 169.0 | nM | 6.77 |
| CHEMBL192615 | — | Ki | = | 185.0 | nM | 6.73 |
| CHEMBL193203 | — | Ki | = | 224.0 | nM | 6.65 |
| CHEMBL190768 | — | Ki | = | 616.0 | nM | 6.21 |
| CHEMBL193230 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL365808 | — | Ki | > | 10000.0 | nM | - |