Assay Detail
Binding
CHEMBL649963
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibitory concentration of compound against benzodiazepine receptor from rat cerebral cortex using [3H]- flunitrazepam was evaluated
21
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cerebral cortex |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Synthesis of benzo-fused benzodiazepines employed as probes of the agonist pharmacophore of benzodiazepine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 7.42 | 8.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL443823 | — | — | 1 | 8.44 |
| CHEMBL1518572 | — | — | 1 | 8.30 |
| CHEMBL12 | DIAZEPAM | 4.0 | 2 | 8.22 |
| CHEMBL356411 | — | — | 1 | 7.85 |
| CHEMBL346836 | — | — | 1 | 7.62 |
| CHEMBL150639 | — | — | 1 | 7.40 |
| CHEMBL163225 | — | — | 1 | 7.26 |
| CHEMBL350394 | — | — | 1 | 6.92 |
| CHEMBL445131 | — | — | 1 | 6.82 |
| CHEMBL352086 | — | — | 1 | 6.58 |
| CHEMBL351067 | — | — | 1 | 6.50 |
| CHEMBL163081 | — | — | 1 | 6.40 |
| CHEMBL350651 | — | — | 1 | - |
| CHEMBL355155 | — | — | 1 | - |
| CHEMBL349234 | — | — | 1 | - |
| CHEMBL349688 | — | — | 1 | - |
| CHEMBL165276 | — | — | 1 | - |
| CHEMBL350120 | — | — | 1 | - |
| CHEMBL164865 | — | — | 1 | - |
| CHEMBL165386 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL443823 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL1518572 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL12 | DIAZEPAM | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL12 | DIAZEPAM | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL356411 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL346836 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL150639 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL163225 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL350394 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL445131 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL352086 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL351067 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL163081 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL350651 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL349234 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL355155 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL349688 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL165276 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL350120 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL164865 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL165386 | — | IC50 | > | 1000.0 | nM | - |