Assay Detail
Binding
CHEMBL828956
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Displacement of [3H]muscimol from rat brain gamma-aminobutyric-acid GABA-A receptor
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Potent 4-aryl- or 4-arylalkyl-substituted 3-isoxazolol GABA(A) antagonists: synthesis, pharmacology, and molecular modeling.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 7.02 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL191991 | — | — | 1 | 8.00 |
| CHEMBL190925 | — | — | 1 | 7.80 |
| CHEMBL371854 | — | — | 1 | 7.72 |
| CHEMBL193370 | — | — | 1 | 7.68 |
| CHEMBL192050 | — | — | 1 | 7.55 |
| CHEMBL371775 | — | — | 1 | 7.55 |
| CHEMBL382320 | — | — | 1 | 7.44 |
| CHEMBL366160 | — | — | 1 | 7.35 |
| CHEMBL144718 | — | — | 1 | 7.31 |
| CHEMBL303580 | GABAZINE BROMIDE | — | 1 | 7.13 |
| CHEMBL365174 | — | — | 1 | 7.10 |
| CHEMBL191771 | — | — | 1 | 7.00 |
| CHEMBL191704 | — | — | 1 | 6.96 |
| CHEMBL195164 | — | — | 1 | 6.66 |
| CHEMBL194544 | — | — | 1 | 6.60 |
| CHEMBL370714 | — | — | 1 | 6.09 |
| CHEMBL144364 | — | — | 1 | 5.42 |
| CHEMBL311761 | — | — | 1 | 5.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL191991 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL190925 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL371854 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL193370 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL192050 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL371775 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL382320 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL366160 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL144718 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL303580 | GABAZINE BROMIDE | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL365174 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL191771 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL191704 | — | Ki | = | 109.0 | nM | 6.96 |
| CHEMBL195164 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL194544 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL370714 | — | Ki | = | 820.0 | nM | 6.09 |
| CHEMBL144364 | — | Ki | = | 3800.0 | nM | 5.42 |
| CHEMBL311761 | — | Ki | = | 9100.0 | nM | 5.04 |