Assay Detail
Binding
CHEMBL680647
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Binding affinity against benzodiazepine site of gamma-aminobutyric-acid A receptor of rat cerebral cortex by using [3H]flunitrazepam in the presence of GABA 1 mM.
26
Total Activities
26
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
Potential anxiolytic agents. Pyrido[1,2-a]benzimidazoles: a new structural class of ligands for the benzodiazepine binding site on GABA-A receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 7.69 | 9.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL413744 | — | — | 1 | 9.96 |
| CHEMBL59764 | — | — | 1 | 9.59 |
| CHEMBL64169 | — | — | 1 | 8.85 |
| CHEMBL64768 | — | — | 1 | 8.85 |
| CHEMBL292583 | — | — | 1 | 8.77 |
| CHEMBL303784 | — | — | 1 | 8.68 |
| CHEMBL304464 | — | — | 1 | 8.57 |
| CHEMBL294727 | — | — | 1 | 8.28 |
| CHEMBL2052026 | — | — | 1 | 8.23 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 7.89 |
| CHEMBL64225 | — | — | 1 | 7.85 |
| CHEMBL63832 | — | — | 1 | 7.80 |
| CHEMBL60668 | — | — | 1 | 7.80 |
| CHEMBL292675 | — | — | 1 | 7.75 |
| CHEMBL292651 | — | — | 1 | 7.60 |
| CHEMBL292595 | — | — | 1 | 7.58 |
| CHEMBL304012 | — | — | 1 | 7.14 |
| CHEMBL64106 | — | — | 1 | 7.02 |
| CHEMBL64637 | — | — | 1 | 6.82 |
| CHEMBL60127 | — | — | 1 | 6.77 |
| CHEMBL432298 | — | — | 1 | 6.58 |
| CHEMBL416318 | — | — | 1 | 6.50 |
| CHEMBL302420 | — | — | 1 | 6.08 |
| CHEMBL58181 | — | — | 1 | 6.03 |
| CHEMBL58120 | — | — | 1 | 5.22 |
| CHEMBL60466 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL413744 | — | IC50 | = | 0.11 | nM | 9.96 |
| CHEMBL59764 | — | IC50 | = | 0.26 | nM | 9.59 |
| CHEMBL64169 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL64768 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL292583 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL303784 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL304464 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL294727 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL2052026 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL12 | DIAZEPAM | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL64225 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL63832 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL60668 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL292675 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL292651 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL292595 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL304012 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL64106 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL64637 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL60127 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL432298 | — | IC50 | = | 265.0 | nM | 6.58 |
| CHEMBL416318 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL302420 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL58181 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL58120 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL60466 | — | IC50 | > | 10000.0 | nM | - |