Assay Detail
Binding
CHEMBL650877
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Inhibition of [3H]- flunitrazepam binding to GABA-A Benzodiazepine receptor of rat cerebral cortex membranes
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| 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
3-Amino-beta-carboline derivatives and the benzodiazepine receptor. Synthesis of a selective antagonist of the sedative action of diazepam.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.00 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL11709 | — | — | 1 | 8.70 |
| CHEMBL165882 | — | — | 1 | 7.15 |
| CHEMBL353674 | — | — | 1 | 7.10 |
| CHEMBL353967 | — | — | 1 | 6.34 |
| CHEMBL167732 | — | — | 1 | 5.40 |
| CHEMBL353110 | — | — | 1 | 5.33 |
| CHEMBL167052 | — | — | 1 | 5.20 |
| CHEMBL54381 | — | — | 1 | 4.60 |
| CHEMBL165802 | — | — | 1 | 4.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL11709 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL165882 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL353674 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL353967 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL167732 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL353110 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL167052 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL54381 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL165802 | — | IC50 | = | 62000.0 | nM | 4.21 |