Assay Detail
Binding
CHEMBL652368
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Concentration to inhibit [3H]flunitrazepam binding to rat cerebral cortical membrane
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Synthesis of novel 2-phenyl-2H-pyrazolo[4,3-c]isoquinolin-3-ols: topological comparisons with analogues of 2-phenyl-2,5-dihydropyrazolo[4,3-c]quinolin-3(3H)-ones at benzodiazepine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 9.02 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL19732 | CGS-8216 | — | 1 | 9.40 |
| CHEMBL20042 | CGS-9896 | — | 1 | 9.22 |
| CHEMBL3144739 | — | — | 1 | 9.05 |
| CHEMBL301605 | — | — | 1 | 8.40 |
| CHEMBL3144807 | — | — | 1 | - |
| CHEMBL122688 | — | — | 1 | - |
| CHEMBL3144779 | — | — | 1 | - |
| CHEMBL440335 | — | — | 1 | - |
| CHEMBL3144681 | — | — | 1 | - |
| CHEMBL3142992 | — | — | 1 | - |
| CHEMBL122567 | — | — | 1 | - |
| CHEMBL123427 | — | — | 1 | - |
| CHEMBL3144671 | — | — | 1 | - |
| CHEMBL421429 | — | — | 1 | - |
| CHEMBL122288 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL19732 | CGS-8216 | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL20042 | CGS-9896 | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3144739 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL301605 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3144807 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL122688 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL3144779 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL440335 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL3144681 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL3142992 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL122567 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL123427 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL3144671 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL421429 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL122288 | — | IC50 | > | 2000.0 | nM | - |