Assay Detail
Binding
CHEMBL681951
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Binding affinity in vivo for gamma-aminobutyric-acid A receptor measured by its ability to displace [3H]-GABA agonist from rat brain preparations after iv injection.
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 | 23 | 6.39 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL273481 | MUSCIMOL | 1.0 | 1 | 8.70 |
| CHEMBL540583 | — | — | 1 | 7.77 |
| CHEMBL133628 | — | — | 1 | 7.72 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | 1.0 | 1 | 7.60 |
| CHEMBL1161036 | — | — | 1 | 7.37 |
| CHEMBL545066 | — | — | 1 | 7.30 |
| CHEMBL554239 | — | — | 1 | 7.12 |
| CHEMBL544140 | — | — | 1 | 6.92 |
| CHEMBL32503 | GABAZINE | — | 1 | 6.85 |
| CHEMBL555843 | — | — | 1 | 6.82 |
| CHEMBL544360 | — | — | 1 | 6.80 |
| CHEMBL131516 | — | — | 1 | 6.55 |
| CHEMBL536549 | — | — | 1 | 6.00 |
| CHEMBL539556 | — | — | 1 | 5.92 |
| CHEMBL133180 | — | — | 1 | 5.92 |
| CHEMBL132060 | — | — | 1 | 5.80 |
| CHEMBL552953 | — | — | 1 | 5.75 |
| CHEMBL132561 | — | — | 1 | 5.64 |
| CHEMBL334805 | — | — | 1 | 5.62 |
| CHEMBL543901 | — | — | 1 | 5.18 |
| CHEMBL131910 | — | — | 1 | 4.97 |
| CHEMBL417990 | BICUCULLINE | — | 1 | 4.36 |
| CHEMBL133047 | — | — | 1 | 4.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL273481 | MUSCIMOL | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL540583 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL133628 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL1161036 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL545066 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL554239 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL544140 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL32503 | GABAZINE | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL555843 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL544360 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL131516 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL536549 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL539556 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL133180 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL132060 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL552953 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL132561 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL334805 | — | IC50 | = | 2370.0 | nM | 5.62 |
| CHEMBL543901 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL131910 | — | IC50 | = | 10600.0 | nM | 4.97 |
| CHEMBL417990 | BICUCULLINE | IC50 | = | 44000.0 | nM | 4.36 |
| CHEMBL133047 | — | IC50 | = | 56000.0 | nM | 4.25 |