Assay Detail
Binding
CHEMBL864181
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]muscimol from GABAA receptor in rat brain synaptic membranes
5
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Hydroxy-1,2,5-oxadiazolyl moiety as bioisoster of the carboxy function. Synthesis, ionization constants, and pharmacological characterization of gamma-aminobutyric acid (GABA) related compounds.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 4 | 5.89 | 7.31 |
| IC50 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | 1.0 | 1 | 7.31 |
| CHEMBL312443 | GABOXADOL | 3.0 | 1 | 6.80 |
| CHEMBL211176 | — | — | 1 | 4.89 |
| CHEMBL211542 | — | — | 1 | 4.57 |
| CHEMBL211350 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL312443 | GABOXADOL | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL211176 | — | Ki | = | 13000.0 | nM | 4.89 |
| CHEMBL211542 | — | Ki | = | 27000.0 | nM | 4.57 |
| CHEMBL211350 | — | IC50 | > | 100000.0 | nM | - |