Assay Detail
Binding
CHEMBL650280
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Displacing potential to [3H]diazepam binding to benzodiazepine receptor in Wistar rat cerebral cortex
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cerebral cortex |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Thienylpyrazoloquinolines with high affinity to benzodiazepine receptors: continuous shift from inverse agonist to agonist properties depending on the size of the alkyl substituent.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 9.06 | 9.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL19732 | CGS-8216 | — | 1 | 9.66 |
| CHEMBL3144734 | — | — | 1 | 9.49 |
| CHEMBL3144724 | — | — | 1 | 9.49 |
| CHEMBL3144590 | — | — | 1 | 9.39 |
| CHEMBL3144725 | — | — | 1 | 9.39 |
| CHEMBL3144726 | — | — | 1 | 9.32 |
| CHEMBL3144594 | — | — | 1 | 9.22 |
| CHEMBL3144727 | — | — | 1 | 9.14 |
| CHEMBL20042 | CGS-9896 | — | 1 | 9.08 |
| CHEMBL3144588 | — | — | 1 | 9.07 |
| CHEMBL3144589 | — | — | 1 | 9.02 |
| CHEMBL3144598 | — | — | 1 | 9.00 |
| CHEMBL3144596 | — | — | 1 | 8.99 |
| CHEMBL3144597 | — | — | 1 | 8.99 |
| CHEMBL3144591 | — | — | 1 | 8.98 |
| CHEMBL11709 | — | — | 1 | 8.94 |
| CHEMBL3144595 | — | — | 1 | 8.83 |
| CHEMBL3144592 | — | — | 1 | 8.73 |
| CHEMBL3144731 | — | — | 1 | 8.69 |
| CHEMBL3144593 | — | — | 1 | 8.64 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 8.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL19732 | CGS-8216 | Ki | = | 0.22 | nM | 9.66 |
| CHEMBL3144734 | — | Ki | = | 0.32 | nM | 9.49 |
| CHEMBL3144724 | — | Ki | = | 0.32 | nM | 9.49 |
| CHEMBL3144590 | — | Ki | = | 0.41 | nM | 9.39 |
| CHEMBL3144725 | — | Ki | = | 0.41 | nM | 9.39 |
| CHEMBL3144726 | — | Ki | = | 0.48 | nM | 9.32 |
| CHEMBL3144594 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL3144727 | — | Ki | = | 0.73 | nM | 9.14 |
| CHEMBL20042 | CGS-9896 | Ki | = | 0.83 | nM | 9.08 |
| CHEMBL3144588 | — | Ki | = | 0.86 | nM | 9.07 |
| CHEMBL3144589 | — | Ki | = | 0.95 | nM | 9.02 |
| CHEMBL3144598 | — | Ki | = | 1.01 | nM | 9.00 |
| CHEMBL3144596 | — | Ki | = | 1.02 | nM | 8.99 |
| CHEMBL3144597 | — | Ki | = | 1.02 | nM | 8.99 |
| CHEMBL3144591 | — | Ki | = | 1.04 | nM | 8.98 |
| CHEMBL11709 | — | Ki | = | 1.14 | nM | 8.94 |
| CHEMBL3144595 | — | Ki | = | 1.48 | nM | 8.83 |
| CHEMBL3144592 | — | Ki | = | 1.86 | nM | 8.73 |
| CHEMBL3144731 | — | Ki | = | 2.04 | nM | 8.69 |
| CHEMBL3144593 | — | Ki | = | 2.27 | nM | 8.64 |
| CHEMBL12 | DIAZEPAM | Ki | = | 5.02 | nM | 8.30 |