Assay Detail
Binding
CHEMBL864182
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Inhibition of [3H]GABA binding in GABAA receptor in rat brain synaptic membranes
5
Total Activities
5
Compounds Tested
1
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 |
|---|---|---|---|
| IC50 | 5 | 6.06 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | 1.0 | 1 | 7.89 |
| CHEMBL211176 | — | — | 1 | 5.70 |
| CHEMBL211542 | — | — | 1 | 4.60 |
| CHEMBL211350 | — | — | 1 | - |
| CHEMBL312443 | GABOXADOL | 3.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL211176 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL211542 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL211350 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL312443 | GABOXADOL | IC50 | - | — | - |