Assay Detail
Functional
CHEMBL681950
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Affinity for gamma-aminobutyric-acid A receptor measured by its ability to displace [3H]gabazine antagonist from rat brain preparations.
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Tissue | Brain |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Gamma-aminobutyric acid receptor subunit alpha-1 (CHEMBL3139) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
Condensation of muscimol or thiomuscimol with aminopyridazines yields GABA-A antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 6.59 | 7.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL132060 | — | — | 1 | 7.06 |
| CHEMBL552953 | — | — | 1 | 6.62 |
| CHEMBL132561 | — | — | 1 | 6.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL132060 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL552953 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL132561 | — | IC50 | = | 800.0 | nM | 6.10 |