Assay Detail
Binding
CHEMBL650881
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In vitro displacement of [3H]diazepam from GABA-A benzodiazepine receptor in rat cerebral cortex
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| 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 6-substituted beta-carbolines that behave as benzodiazepine receptor antagonists or inverse agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 6.91 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL268262 | — | — | 1 | 8.00 |
| CHEMBL165794 | — | — | 1 | 7.30 |
| CHEMBL11863 | — | — | 1 | 7.24 |
| CHEMBL166270 | — | — | 1 | 7.12 |
| CHEMBL54968 | — | — | 1 | 6.97 |
| CHEMBL164120 | — | — | 1 | 5.89 |
| CHEMBL417982 | — | — | 1 | 5.83 |
| CHEMBL165021 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL268262 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL165794 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL11863 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL166270 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL54968 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL164120 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL417982 | — | IC50 | = | 1470.0 | nM | 5.83 |
| CHEMBL165021 | — | IC50 | > | 5000.0 | nM | - |