Assay Detail
Binding
CHEMBL680646
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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 absence of GABA.
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 | 7.50 | 9.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL413744 | — | — | 1 | 9.64 |
| CHEMBL59764 | — | — | 1 | 9.38 |
| CHEMBL64169 | — | — | 1 | 8.77 |
| CHEMBL64768 | — | — | 1 | 8.68 |
| CHEMBL292583 | — | — | 1 | 8.55 |
| CHEMBL303784 | — | — | 1 | 8.24 |
| CHEMBL2052026 | — | — | 1 | 8.04 |
| CHEMBL304464 | — | — | 1 | 7.92 |
| CHEMBL294727 | — | — | 1 | 7.92 |
| CHEMBL292675 | — | — | 1 | 7.80 |
| CHEMBL64225 | — | — | 1 | 7.62 |
| CHEMBL60668 | — | — | 1 | 7.58 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 7.55 |
| CHEMBL292595 | — | — | 1 | 7.54 |
| CHEMBL292651 | — | — | 1 | 7.52 |
| CHEMBL63832 | — | — | 1 | 7.39 |
| CHEMBL64106 | — | — | 1 | 6.92 |
| CHEMBL304012 | — | — | 1 | 6.85 |
| CHEMBL64637 | — | — | 1 | 6.70 |
| CHEMBL60127 | — | — | 1 | 6.50 |
| CHEMBL416318 | — | — | 1 | 6.44 |
| CHEMBL432298 | — | — | 1 | 6.21 |
| CHEMBL302420 | — | — | 1 | 6.17 |
| CHEMBL58181 | — | — | 1 | 6.00 |
| CHEMBL58120 | — | — | 1 | 5.62 |
| CHEMBL60466 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL413744 | — | IC50 | = | 0.23 | nM | 9.64 |
| CHEMBL59764 | — | IC50 | = | 0.42 | nM | 9.38 |
| CHEMBL64169 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL64768 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL292583 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL303784 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL2052026 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL304464 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL294727 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL292675 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL64225 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL60668 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL12 | DIAZEPAM | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL292595 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL292651 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL63832 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL64106 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL304012 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL64637 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL60127 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL416318 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL432298 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL302420 | — | IC50 | = | 675.0 | nM | 6.17 |
| CHEMBL58181 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL58120 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL60466 | — | IC50 | > | 10000.0 | nM | - |