Assay Detail
Functional
CHEMBL681949
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.
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Bos taurus |
| Tissue | Brain |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL2093872) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Homo sapiens |
Publication
Condensation of muscimol or thiomuscimol with aminopyridazines yields GABA-A antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.24 | 9.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL540583 | — | — | 1 | 9.12 |
| CHEMBL1161036 | — | — | 1 | 8.52 |
| CHEMBL554239 | — | — | 1 | 8.22 |
| CHEMBL32503 | GABAZINE | — | 1 | 8.10 |
| CHEMBL544360 | — | — | 1 | 7.60 |
| CHEMBL555843 | — | — | 1 | 7.54 |
| CHEMBL539556 | — | — | 1 | 7.10 |
| CHEMBL273481 | MUSCIMOL | 1.0 | 1 | 6.87 |
| CHEMBL544140 | — | — | 1 | 6.72 |
| CHEMBL543901 | — | — | 1 | 6.00 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | 1.0 | 1 | 5.84 |
| CHEMBL417990 | BICUCULLINE | — | 1 | 5.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL540583 | — | IC50 | = | 0.76 | nM | 9.12 |
| CHEMBL1161036 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL554239 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL32503 | GABAZINE | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL544360 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL555843 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL539556 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL273481 | MUSCIMOL | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL544140 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL543901 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | IC50 | = | 1450.0 | nM | 5.84 |
| CHEMBL417990 | BICUCULLINE | IC50 | = | 6200.0 | nM | 5.21 |