Assay Detail
Binding
CHEMBL866382
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Displacement of [3H]muscimol from GABAA alpha-1-beta-3-gamma-2S in rat brain membrane
19
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
GABA A receptor alpha-5/beta-3/gamma-2 (CHEMBL2111374) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Potent 4-arylalkyl-substituted 3-isothiazolol GABA(A) competitive/noncompetitive antagonists: synthesis and pharmacology.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 7.00 | 8.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL442789 | — | — | 2 | 8.75 |
| CHEMBL204017 | — | — | 2 | 8.28 |
| CHEMBL202028 | — | — | 2 | 8.02 |
| CHEMBL144718 | — | — | 1 | 7.31 |
| CHEMBL377925 | — | — | 1 | 7.17 |
| CHEMBL32503 | GABAZINE | — | 1 | 7.13 |
| CHEMBL203718 | — | — | 2 | 6.48 |
| CHEMBL204189 | — | — | 2 | 6.41 |
| CHEMBL382791 | — | — | 2 | 6.36 |
| CHEMBL109209 | — | — | 2 | 5.73 |
| CHEMBL204110 | — | — | 2 | 5.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL442789 | — | Ki | = | 1.778 | nM | 8.75 |
| CHEMBL442789 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL204017 | — | Ki | = | 5.248 | nM | 8.28 |
| CHEMBL204017 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL202028 | — | Ki | = | 9.6 | nM | 8.02 |
| CHEMBL202028 | — | Ki | = | 9.55 | nM | 8.02 |
| CHEMBL144718 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL377925 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL32503 | GABAZINE | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL203718 | — | Ki | = | 331.0 | nM | 6.48 |
| CHEMBL203718 | — | Ki | = | 331.13 | nM | 6.48 |
| CHEMBL204189 | — | Ki | = | 389.05 | nM | 6.41 |
| CHEMBL204189 | — | Ki | = | 388.0 | nM | 6.41 |
| CHEMBL382791 | — | Ki | = | 440.0 | nM | 6.36 |
| CHEMBL382791 | — | Ki | = | 446.68 | nM | 6.35 |
| CHEMBL109209 | — | Ki | = | 1862.09 | nM | 5.73 |
| CHEMBL109209 | — | Ki | = | 1870.0 | nM | 5.73 |
| CHEMBL204110 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL204110 | — | Ki | = | 2187.76 | nM | 5.66 |