Assay Detail
Binding
CHEMBL654242
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]flunitrazepam binding to benzodiazepine receptor in bovine brain membrane
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Bos taurus |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL2094107) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Bos taurus |
Publication
Synthesis, binding studies, and structure-activity relationships of 1-aryl-and 2-aryl[1]benzopyranopyrazol-4-ones, central benzodiazepine receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 5.87 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 7.60 |
| CHEMBL100796 | — | — | 1 | 7.19 |
| CHEMBL321131 | — | — | 1 | 7.05 |
| CHEMBL313280 | — | — | 1 | 7.00 |
| CHEMBL90142 | — | — | 1 | 6.55 |
| CHEMBL412610 | — | — | 1 | 6.52 |
| CHEMBL330598 | — | — | 1 | 6.50 |
| CHEMBL102240 | — | — | 1 | 6.20 |
| CHEMBL101286 | — | — | 1 | 6.16 |
| CHEMBL103836 | — | — | 1 | 6.12 |
| CHEMBL412671 | — | — | 1 | 6.12 |
| CHEMBL451 | CHLORDIAZEPOXIDE | 4.0 | 1 | 6.10 |
| CHEMBL102251 | — | — | 1 | 6.00 |
| CHEMBL101071 | — | — | 1 | 5.89 |
| CHEMBL317599 | — | — | 1 | 5.70 |
| CHEMBL323108 | — | — | 1 | 5.52 |
| CHEMBL102071 | — | — | 1 | 5.51 |
| CHEMBL103918 | — | — | 1 | 5.47 |
| CHEMBL318534 | — | — | 1 | 5.30 |
| CHEMBL103762 | — | — | 1 | 5.10 |
| CHEMBL103889 | — | — | 1 | 4.80 |
| CHEMBL99633 | — | — | 1 | 4.80 |
| CHEMBL317685 | — | — | 1 | 4.60 |
| CHEMBL316613 | — | — | 1 | 4.52 |
| CHEMBL327492 | — | — | 1 | 4.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL12 | DIAZEPAM | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL100796 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL321131 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL313280 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL90142 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL412610 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL330598 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL102240 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL101286 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL103836 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL412671 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL451 | CHLORDIAZEPOXIDE | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL102251 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL101071 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL317599 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL323108 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL102071 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL103918 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL318534 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL103762 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL103889 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL99633 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL317685 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL316613 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL327492 | — | IC50 | = | 43000.0 | nM | 4.37 |