Assay Detail
Binding
CHEMBL681237
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Binding affinity against the BZD site of the Gamma-aminobutyric acid A receptor in rat cerebral cortex using radioligand ([3H]flunitrazepam) assay in the absence of Gamma-aminobutyric acid
27
Total Activities
27
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
Potential anxiolytic agents. 2. Improvement of oral efficacy for the pyrido[1,2-a]benzimidazole (PBI) class of GABA-A receptor modulators
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 6.71 | 8.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2052026 | — | — | 1 | 8.04 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 7.55 |
| CHEMBL325075 | — | — | 1 | 7.54 |
| CHEMBL324701 | — | — | 1 | 7.43 |
| CHEMBL111883 | — | — | 1 | 7.34 |
| CHEMBL113879 | — | — | 1 | 7.30 |
| CHEMBL326762 | — | — | 1 | 7.29 |
| CHEMBL325661 | — | — | 1 | 7.28 |
| CHEMBL321631 | — | — | 1 | 7.27 |
| CHEMBL113812 | — | — | 1 | 7.23 |
| CHEMBL115947 | — | — | 1 | 7.19 |
| CHEMBL115325 | — | — | 1 | 7.17 |
| CHEMBL324454 | — | — | 1 | 7.10 |
| CHEMBL111978 | — | — | 1 | 6.92 |
| CHEMBL327014 | — | — | 1 | 6.82 |
| CHEMBL326123 | — | — | 1 | 6.80 |
| CHEMBL326324 | — | — | 1 | 6.66 |
| CHEMBL112298 | — | — | 1 | 6.58 |
| CHEMBL421893 | — | — | 1 | 6.57 |
| CHEMBL114581 | — | — | 1 | 6.44 |
| CHEMBL420121 | — | — | 1 | 6.32 |
| CHEMBL432805 | — | — | 1 | 5.40 |
| CHEMBL114567 | — | — | 1 | 5.20 |
| CHEMBL323875 | — | — | 1 | 5.15 |
| CHEMBL423877 | — | — | 1 | 5.00 |
| CHEMBL114973 | — | — | 1 | 4.89 |
| CHEMBL112489 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2052026 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL12 | DIAZEPAM | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL325075 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL324701 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL111883 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL113879 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL326762 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL325661 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL321631 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL113812 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL115947 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL115325 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL324454 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL111978 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL327014 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL326123 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL326324 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL112298 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL421893 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL114581 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL420121 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL432805 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL114567 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL323875 | — | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL423877 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL114973 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL112489 | — | IC50 | > | 10000.0 | nM | - |