Assay Detail
Binding
CHEMBL654240
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Inhibition of [3H]flunitrazepam binding to GABA-A central Benzodiazepine receptor of bovine brain membranes
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Bos taurus |
| Subcellular | Brain membranes |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL2094107) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Bos taurus |
Publication
Specific inhibition of benzodiazepine receptor binding by some N-(indol-3-ylglyoxylyl)amino acid derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 5.38 | 7.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL13209 | NITRAZEPAM | 3.0 | 1 | 7.42 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 7.39 |
| CHEMBL314045 | — | — | 1 | 6.70 |
| CHEMBL84859 | — | — | 1 | 6.30 |
| CHEMBL451 | CHLORDIAZEPOXIDE | 4.0 | 1 | 5.96 |
| CHEMBL147766 | — | — | 1 | 5.70 |
| CHEMBL85966 | — | — | 1 | 5.32 |
| CHEMBL148451 | — | — | 1 | 5.27 |
| CHEMBL82672 | — | — | 1 | 5.21 |
| CHEMBL146364 | — | — | 1 | 4.70 |
| CHEMBL146082 | — | — | 1 | 4.66 |
| CHEMBL82675 | — | — | 1 | 4.66 |
| CHEMBL146415 | — | — | 1 | 4.42 |
| CHEMBL146094 | — | — | 1 | 4.22 |
| CHEMBL145854 | — | — | 1 | 4.12 |
| CHEMBL148040 | — | — | 1 | 4.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL13209 | NITRAZEPAM | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL12 | DIAZEPAM | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL314045 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL84859 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL451 | CHLORDIAZEPOXIDE | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL147766 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL85966 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL148451 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL82672 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL146364 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL146082 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL82675 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL146415 | — | IC50 | = | 38000.0 | nM | 4.42 |
| CHEMBL146094 | — | IC50 | = | 60000.0 | nM | 4.22 |
| CHEMBL145854 | — | IC50 | = | 75000.0 | nM | 4.12 |
| CHEMBL148040 | — | IC50 | = | 80000.0 | nM | 4.10 |