Assay Detail
Binding
CHEMBL650833
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Inhibition of [3H]-Ro- 15-1788 binding to GABA-A benzodiazepine receptor in rat brain membrane
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| 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
Computer-aided molecular modeling, synthesis, and biological evaluation of 8-(benzyloxy)-2-phenylpyrazolo[4,3-c]quinoline as a novel benzodiazepine receptor agonist ligand.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 8.54 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL10483 | — | — | 1 | 9.30 |
| CHEMBL3144700 | — | — | 1 | 9.17 |
| CHEMBL3144823 | — | — | 1 | 9.13 |
| CHEMBL1518572 | — | — | 1 | 9.00 |
| CHEMBL3144860 | — | — | 1 | 8.43 |
| CHEMBL11709 | — | — | 1 | 8.30 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 7.69 |
| CHEMBL3144703 | — | — | 1 | 7.28 |
| CHEMBL3144702 | — | — | 1 | - |
| CHEMBL3144699 | — | — | 1 | - |
| CHEMBL3144701 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL10483 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3144700 | — | IC50 | = | 0.68 | nM | 9.17 |
| CHEMBL3144823 | — | IC50 | = | 0.74 | nM | 9.13 |
| CHEMBL1518572 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3144860 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL11709 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL12 | DIAZEPAM | IC50 | = | 20.6 | nM | 7.69 |
| CHEMBL3144703 | — | IC50 | = | 52.3 | nM | 7.28 |
| CHEMBL3144702 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL3144699 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3144701 | — | IC50 | > | 1000.0 | nM | - |