Assay Detail
Binding
CHEMBL650465
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity against benzodiazepine (BZ) receptor by displacing [3H]diazepam in cerebral cortex of Wistar rats
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Thienylpyrazoloquinolines: potent agonists and inverse agonists to benzodiazepine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 36 | 8.63 | 9.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL19732 | CGS-8216 | — | 1 | 9.66 |
| CHEMBL3144626 | — | — | 1 | 9.49 |
| CHEMBL3144843 | — | — | 1 | 9.49 |
| CHEMBL3144616 | — | — | 1 | 9.43 |
| CHEMBL3144847 | — | — | 1 | 9.42 |
| CHEMBL3144612 | — | — | 1 | 9.39 |
| CHEMBL3144747 | — | — | 1 | 9.39 |
| CHEMBL3144614 | — | — | 1 | 9.32 |
| CHEMBL3144622 | — | — | 1 | 9.20 |
| CHEMBL3144618 | — | — | 1 | 9.19 |
| CHEMBL3144833 | — | — | 1 | 9.19 |
| CHEMBL3144755 | — | — | 1 | 9.14 |
| CHEMBL3144746 | — | — | 1 | 9.14 |
| CHEMBL3144740 | — | — | 1 | 9.14 |
| CHEMBL3144834 | — | — | 1 | 9.12 |
| CHEMBL3144613 | — | — | 1 | 9.11 |
| CHEMBL20042 | CGS-9896 | — | 1 | 9.08 |
| CHEMBL3144750 | — | — | 1 | 9.08 |
| CHEMBL3144751 | — | — | 1 | 9.04 |
| CHEMBL3144724 | — | — | 1 | 9.02 |
| CHEMBL3144627 | — | — | 1 | 8.99 |
| CHEMBL3144625 | — | — | 1 | 8.98 |
| CHEMBL3144749 | — | — | 1 | 8.83 |
| CHEMBL3144734 | — | — | 1 | 8.63 |
| CHEMBL3144624 | — | — | 1 | 8.61 |
| CHEMBL3144619 | — | — | 1 | 8.33 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 8.30 |
| CHEMBL3144623 | — | — | 1 | 8.16 |
| CHEMBL3144621 | — | — | 1 | 8.01 |
| CHEMBL3144851 | — | — | 1 | 7.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL19732 | CGS-8216 | Ki | = | 0.22 | nM | 9.66 |
| CHEMBL3144626 | — | Ki | = | 0.32 | nM | 9.49 |
| CHEMBL3144843 | — | Ki | = | 0.32 | nM | 9.49 |
| CHEMBL3144616 | — | Ki | = | 0.37 | nM | 9.43 |
| CHEMBL3144847 | — | Ki | = | 0.38 | nM | 9.42 |
| CHEMBL3144612 | — | Ki | = | 0.41 | nM | 9.39 |
| CHEMBL3144747 | — | Ki | = | 0.41 | nM | 9.39 |
| CHEMBL3144614 | — | Ki | = | 0.48 | nM | 9.32 |
| CHEMBL3144622 | — | Ki | = | 0.63 | nM | 9.20 |
| CHEMBL3144833 | — | Ki | = | 0.64 | nM | 9.19 |
| CHEMBL3144618 | — | Ki | = | 0.65 | nM | 9.19 |
| CHEMBL3144755 | — | Ki | = | 0.73 | nM | 9.14 |
| CHEMBL3144746 | — | Ki | = | 0.73 | nM | 9.14 |
| CHEMBL3144740 | — | Ki | = | 0.73 | nM | 9.14 |
| CHEMBL3144834 | — | Ki | = | 0.75 | nM | 9.12 |
| CHEMBL3144613 | — | Ki | = | 0.78 | nM | 9.11 |
| CHEMBL20042 | CGS-9896 | Ki | = | 0.83 | nM | 9.08 |
| CHEMBL3144750 | — | Ki | = | 0.83 | nM | 9.08 |
| CHEMBL3144751 | — | Ki | = | 0.92 | nM | 9.04 |
| CHEMBL3144724 | — | Ki | = | 0.96 | nM | 9.02 |
| CHEMBL3144627 | — | Ki | = | 1.02 | nM | 8.99 |
| CHEMBL3144625 | — | Ki | = | 1.05 | nM | 8.98 |
| CHEMBL3144749 | — | Ki | = | 1.48 | nM | 8.83 |
| CHEMBL3144734 | — | Ki | = | 2.34 | nM | 8.63 |
| CHEMBL3144624 | — | Ki | = | 2.48 | nM | 8.61 |
| CHEMBL3144619 | — | Ki | = | 4.69 | nM | 8.33 |
| CHEMBL12 | DIAZEPAM | Ki | = | 5.02 | nM | 8.30 |
| CHEMBL3144623 | — | Ki | = | 6.86 | nM | 8.16 |
| CHEMBL3144621 | — | Ki | = | 9.84 | nM | 8.01 |
| CHEMBL3144851 | — | Ki | = | 17.8 | nM | 7.75 |
| CHEMBL3144741 | — | Ki | = | 21.6 | nM | 7.67 |
| CHEMBL3144802 | — | Ki | = | 27.2 | nM | 7.57 |
| CHEMBL3144763 | — | Ki | = | 142.0 | nM | 6.85 |
| CHEMBL47625 | — | Ki | = | 215.0 | nM | 6.67 |
| CHEMBL430765 | — | Ki | = | 436.0 | nM | 6.36 |
| CHEMBL412652 | — | Ki | = | 1023.0 | nM | 5.99 |