Assay Detail
Binding
CHEMBL4398027
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]muscimol from GABA(A) receptor in Sprague-Dawley rat cortical synaptic membranes by liquid scintillation counting
30
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Five-Membered N-Heterocyclic Scaffolds as Novel Amino Bioisosteres at γ-Aminobutyric Acid (GABA) Type A Receptors and GABA Transporters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 30 | 6.07 | 7.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4547372 | — | — | 2 | 7.23 |
| CHEMBL4458674 | — | — | 2 | 7.05 |
| CHEMBL79325 | — | — | 2 | 6.97 |
| CHEMBL1788265 | — | — | 2 | 6.69 |
| CHEMBL4442696 | — | — | 2 | 6.54 |
| CHEMBL4464494 | — | — | 4 | 6.49 |
| CHEMBL4554798 | — | — | 2 | 6.44 |
| CHEMBL4526098 | — | — | 2 | 6.37 |
| CHEMBL4455221 | — | — | 2 | 5.80 |
| CHEMBL4566832 | — | — | 2 | 5.66 |
| CHEMBL4586460 | — | — | 2 | 5.26 |
| CHEMBL349005 | — | — | 2 | 5.26 |
| CHEMBL4471977 | — | — | 2 | 4.96 |
| CHEMBL71460 | — | — | 2 | 4.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4547372 | — | Ki | = | 58.88 | nM | 7.23 |
| CHEMBL4547372 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL4458674 | — | Ki | = | 89.13 | nM | 7.05 |
| CHEMBL4458674 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL79325 | — | Ki | = | 107.15 | nM | 6.97 |
| CHEMBL79325 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL1788265 | — | Ki | = | 204.17 | nM | 6.69 |
| CHEMBL1788265 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL4442696 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL4442696 | — | Ki | = | 295.12 | nM | 6.53 |
| CHEMBL4464494 | — | Ki | = | 323.59 | nM | 6.49 |
| CHEMBL4464494 | — | Ki | = | 330.0 | nM | 6.48 |
| CHEMBL4554798 | — | Ki | = | 360.0 | nM | 6.44 |
| CHEMBL4554798 | — | Ki | = | 363.08 | nM | 6.44 |
| CHEMBL4526098 | — | Ki | = | 426.58 | nM | 6.37 |
| CHEMBL4526098 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL4464494 | — | Ki | = | 1230.27 | nM | 5.91 |
| CHEMBL4464494 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL4455221 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL4455221 | — | Ki | = | 1621.81 | nM | 5.79 |
| CHEMBL4566832 | — | Ki | = | 2187.76 | nM | 5.66 |
| CHEMBL4566832 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL349005 | — | Ki | = | 5495.41 | nM | 5.26 |
| CHEMBL4586460 | — | Ki | = | 5500.0 | nM | 5.26 |
| CHEMBL4586460 | — | Ki | = | 5495.41 | nM | 5.26 |
| CHEMBL349005 | — | Ki | = | 5600.0 | nM | 5.25 |
| CHEMBL4471977 | — | Ki | = | 10964.78 | nM | 4.96 |
| CHEMBL4471977 | — | Ki | = | 12000.0 | nM | 4.92 |
| CHEMBL71460 | — | Ki | = | 31622.78 | nM | 4.50 |
| CHEMBL71460 | — | Ki | = | 32000.0 | nM | 4.50 |