Assay Detail
Binding
CHEMBL654251
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Binding affinity to the benzodiazepine receptor assayed using 0.5 nM [3H]flunitrazapam as radioligand in guinea pig cerebellum
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Cerebellum |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL2093872) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Homo sapiens |
Publication
The discovery of a novel and potent benzodiazepine receptor pharmacophore
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 8.04 | 9.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL309517 | — | — | 1 | 9.80 |
| CHEMBL79037 | — | — | 1 | 9.62 |
| CHEMBL78730 | — | — | 1 | 9.34 |
| CHEMBL76263 | — | — | 1 | 9.31 |
| CHEMBL419096 | — | — | 1 | 9.22 |
| CHEMBL77226 | — | — | 1 | 9.10 |
| CHEMBL444586 | — | — | 1 | 8.96 |
| CHEMBL444050 | — | — | 1 | 8.74 |
| CHEMBL80610 | — | — | 1 | 8.66 |
| CHEMBL75642 | — | — | 1 | 8.55 |
| CHEMBL78768 | — | — | 1 | 8.01 |
| CHEMBL76793 | — | — | 1 | 7.92 |
| CHEMBL310564 | — | — | 1 | 7.89 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 7.85 |
| CHEMBL79166 | — | — | 1 | 7.80 |
| CHEMBL80756 | — | — | 1 | 7.77 |
| CHEMBL78759 | — | — | 1 | 7.75 |
| CHEMBL80609 | — | — | 1 | 7.72 |
| CHEMBL309854 | — | — | 1 | 7.62 |
| CHEMBL80738 | — | — | 1 | 7.57 |
| CHEMBL308096 | — | — | 1 | 7.51 |
| CHEMBL431597 | — | — | 1 | 7.48 |
| CHEMBL77958 | — | — | 1 | 7.26 |
| CHEMBL80189 | — | — | 1 | 7.05 |
| CHEMBL78880 | — | — | 1 | 6.96 |
| CHEMBL76918 | — | — | 1 | 6.68 |
| CHEMBL83597 | — | — | 1 | 5.02 |
| CHEMBL310589 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL309517 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL79037 | — | IC50 | = | 0.24 | nM | 9.62 |
| CHEMBL78730 | — | IC50 | = | 0.46 | nM | 9.34 |
| CHEMBL76263 | — | IC50 | = | 0.49 | nM | 9.31 |
| CHEMBL419096 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL77226 | — | IC50 | = | 0.79 | nM | 9.10 |
| CHEMBL444586 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL444050 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL80610 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL75642 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL78768 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL76793 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL310564 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL12 | DIAZEPAM | IC50 | = | 14.1 | nM | 7.85 |
| CHEMBL79166 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL80756 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL78759 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL80609 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL309854 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL80738 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL308096 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL431597 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL77958 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL80189 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL78880 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL76918 | — | IC50 | = | 209.0 | nM | 6.68 |
| CHEMBL83597 | — | IC50 | = | 9600.0 | nM | 5.02 |
| CHEMBL310589 | — | IC50 | > | 1000.0 | nM | - |