Assay Detail
Binding
CHEMBL650876
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Inhibition of [3H]-diazepam binding to GABA-A benzodiazepine receptor of rat cerebral cortical membranes
10
Total Activities
10
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
Synthesis of 7,12-dihydropyrido[3,4-b:5,4-b']diindoles. A novel class of rigid, planar benzodiazepine receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.33 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL301605 | — | — | 1 | 8.40 |
| CHEMBL79945 | — | — | 1 | 8.15 |
| CHEMBL141039 | — | — | 1 | 8.10 |
| CHEMBL439945 | — | — | 1 | 8.00 |
| CHEMBL311747 | — | — | 1 | 7.92 |
| CHEMBL310167 | — | — | 1 | 7.80 |
| CHEMBL78650 | — | — | 1 | 7.10 |
| CHEMBL302056 | — | — | 1 | 6.15 |
| CHEMBL343107 | — | — | 1 | 6.05 |
| CHEMBL312333 | — | — | 1 | 5.67 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL301605 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL79945 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL141039 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL439945 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL311747 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL310167 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL78650 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL302056 | — | IC50 | = | 715.0 | nM | 6.15 |
| CHEMBL343107 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL312333 | — | IC50 | = | 2150.0 | nM | 5.67 |