Assay Detail
Binding
CHEMBL650178
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In vitro inhibition of binding to the benzodiazepine receptor in rat cerebral cortical membrane using [3H]diazepam as radioligand
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| 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 novel 3-substituted beta-carbolines as benzodiazepine receptor ligands: probing the benzodiazepine receptor pharmacophore.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.77 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL301605 | — | — | 1 | 8.40 |
| CHEMBL453066 | BETA-CCM | — | 1 | 8.30 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 8.22 |
| CHEMBL53651 | — | — | 1 | 8.10 |
| CHEMBL52750 | — | — | 1 | 7.96 |
| CHEMBL299250 | — | — | 1 | 7.62 |
| CHEMBL298561 | — | — | 1 | 7.35 |
| CHEMBL54968 | — | — | 1 | 6.97 |
| CHEMBL54228 | — | — | 1 | 6.91 |
| CHEMBL53229 | — | — | 1 | 6.90 |
| CHEMBL55630 | — | — | 1 | 6.01 |
| CHEMBL299060 | — | — | 1 | 5.93 |
| CHEMBL275224 | NORHARMANE | — | 1 | 5.79 |
| CHEMBL53230 | — | — | 1 | 5.72 |
| CHEMBL299662 | — | — | 1 | 5.40 |
| CHEMBL416152 | — | — | 1 | 4.88 |
| CHEMBL54381 | — | — | 1 | 4.60 |
| CHEMBL12239 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL301605 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL453066 | BETA-CCM | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL12 | DIAZEPAM | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL53651 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL52750 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL299250 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL298561 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL54968 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL54228 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL53229 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL55630 | — | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL299060 | — | IC50 | = | 1163.0 | nM | 5.93 |
| CHEMBL275224 | NORHARMANE | IC50 | = | 1620.0 | nM | 5.79 |
| CHEMBL53230 | — | IC50 | = | 1920.0 | nM | 5.72 |
| CHEMBL299662 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL416152 | — | IC50 | = | 13200.0 | nM | 4.88 |
| CHEMBL54381 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL12239 | — | IC50 | > | 50000.0 | nM | - |