Assay Detail
Binding
CHEMBL652451
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]flunitrazepam from GABA-A benzodiazepine receptor of rat cortical membranes
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Membrane |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
High-affinity alpha-aminobutyric acid A/benzodiazepine ligands: synthesis and structure-activity relationship studies of a new series of tetracyclic imidazoquinoxalines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 8.23 | 9.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL142750 | — | — | 1 | 9.06 |
| CHEMBL15093 | PNU-91571 | — | 1 | 9.00 |
| CHEMBL143864 | — | — | 1 | 8.92 |
| CHEMBL279867 | PANADIPLON | 2.0 | 1 | 8.80 |
| CHEMBL423925 | — | — | 1 | 8.70 |
| CHEMBL142329 | — | — | 1 | 8.59 |
| CHEMBL357637 | — | — | 1 | 8.43 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 8.31 |
| CHEMBL140631 | — | — | 1 | 8.14 |
| CHEMBL343489 | — | — | 1 | 8.00 |
| CHEMBL141243 | — | — | 1 | 7.72 |
| CHEMBL343688 | — | — | 1 | 7.68 |
| CHEMBL142792 | — | — | 1 | 7.60 |
| CHEMBL264999 | — | — | 1 | 6.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL142750 | — | Ki | = | 0.87 | nM | 9.06 |
| CHEMBL15093 | PNU-91571 | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL143864 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL279867 | PANADIPLON | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL423925 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL142329 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL357637 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL12 | DIAZEPAM | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL140631 | — | Ki | = | 7.3 | nM | 8.14 |
| CHEMBL343489 | — | Ki | = | 9.9 | nM | 8.00 |
| CHEMBL141243 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL343688 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL142792 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL264999 | — | Ki | = | 579.0 | nM | 6.24 |