Assay Detail
Binding
CHEMBL650878
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]diazepam binding to GABA-A benzodiazepine receptor of rat brain
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 8.10 | 8.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL13280 | FLUNITRAZEPAM | 4.0 | 1 | 8.77 |
| CHEMBL452 | CLONAZEPAM | 4.0 | 1 | 8.77 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 8.15 |
| CHEMBL13095 | RO-054520 | — | 1 | 7.62 |
| CHEMBL73096 | — | — | 1 | 7.19 |
| CHEMBL306760 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL13280 | FLUNITRAZEPAM | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL452 | CLONAZEPAM | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL12 | DIAZEPAM | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL13095 | RO-054520 | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL73096 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL306760 | — | IC50 | > | 100000.0 | nM | - |