Assay Detail
Binding
CHEMBL653049
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In vitro displacement of [3H]flunitrazepam from GABA-A central benzodiazepine receptor of rat cerebral cortex membranes
8
Total Activities
8
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
Synthetic routes to 4-amino-3-carboxy-beta-carboline derivatives: incidental formation of novel furo[3,4-c]-beta-carbolin-2-ones displaying high affinities for the benzodiazepine receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.88 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL305360 | — | — | 1 | 9.70 |
| CHEMBL453066 | BETA-CCM | — | 1 | 8.70 |
| CHEMBL59724 | — | — | 1 | 7.92 |
| CHEMBL291395 | — | — | 1 | 7.70 |
| CHEMBL61911 | — | — | 1 | 7.70 |
| CHEMBL60349 | — | — | 1 | 7.33 |
| CHEMBL292101 | — | — | 1 | 7.16 |
| CHEMBL293340 | — | — | 1 | 6.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL305360 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL453066 | BETA-CCM | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL59724 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL291395 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL61911 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL60349 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL292101 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL293340 | — | IC50 | = | 150.0 | nM | 6.82 |