Assay Detail
Binding
CHEMBL649962
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In vitro inhibition of [3H]flunitrazepam binding to GABA-A receptor of rat cerebral cortex membranes
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cerebral cortex |
| Subcellular | Membrane |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Synthesis and benzodiazepine receptor affinities of rigid analogues of 3-carboxy-beta-carbolines: demonstration that the benzodiazepine receptor recognizes preferentially the s-cis conformation of the 3-carboxy group.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.78 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL53232 | — | — | 1 | 8.96 |
| CHEMBL453066 | BETA-CCM | — | 1 | 8.46 |
| CHEMBL301120 | — | — | 1 | 8.18 |
| CHEMBL11709 | — | — | 1 | 8.15 |
| CHEMBL51381 | — | — | 1 | 7.57 |
| CHEMBL295716 | — | — | 1 | 7.38 |
| CHEMBL50695 | — | — | 1 | 6.82 |
| CHEMBL429711 | — | — | 1 | 6.71 |
| CHEMBL54087 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL53232 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL453066 | BETA-CCM | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL301120 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL11709 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL51381 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL295716 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL50695 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL429711 | — | IC50 | = | 197.0 | nM | 6.71 |
| CHEMBL54087 | — | IC50 | > | 10000.0 | nM | - |