Assay Detail
Binding
CHEMBL680657
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In vitro inhibition of [3H]muscimol to rat brain synaptic membranes
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Membrane |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
A novel class of potent 3-isoxazolol GABA(A) antagonists: design, synthesis, and pharmacology.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 5.83 | 7.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL144718 | — | — | 1 | 7.31 |
| CHEMBL32503 | GABAZINE | — | 1 | 7.13 |
| CHEMBL143979 | — | — | 1 | 6.31 |
| CHEMBL144364 | — | — | 1 | 5.42 |
| CHEMBL359417 | — | — | 1 | 5.23 |
| CHEMBL143993 | — | — | 1 | 5.20 |
| CHEMBL311761 | — | — | 1 | 5.04 |
| CHEMBL144416 | — | — | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL144718 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL32503 | GABAZINE | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL143979 | — | Ki | = | 490.0 | nM | 6.31 |
| CHEMBL144364 | — | Ki | = | 3800.0 | nM | 5.42 |
| CHEMBL359417 | — | Ki | = | 5900.0 | nM | 5.23 |
| CHEMBL143993 | — | Ki | = | 6300.0 | nM | 5.20 |
| CHEMBL311761 | — | Ki | = | 9100.0 | nM | 5.04 |
| CHEMBL144416 | — | Ki | = | 10000.0 | nM | 5.00 |