Assay Detail
Binding
CHEMBL679568
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Affinity for GABA-A receptor alpha by inhibiting binding of [3H]muscimol to rat brain synaptosomes
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Synaptosomes |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Novel class of potent 4-arylalkyl substituted 3-isoxazolol GABA(A) antagonists: synthesis, pharmacology, and molecular modeling.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 5.83 | 7.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL538260 | — | — | 1 | 7.31 |
| CHEMBL544544 | — | — | 1 | 7.17 |
| CHEMBL303580 | GABAZINE BROMIDE | — | 1 | 7.16 |
| CHEMBL544302 | — | — | 1 | 7.00 |
| CHEMBL553552 | — | — | 1 | 6.44 |
| CHEMBL544301 | — | — | 1 | 6.40 |
| CHEMBL544776 | — | — | 1 | 6.31 |
| CHEMBL545008 | — | — | 1 | 6.16 |
| CHEMBL555181 | — | — | 1 | 6.02 |
| CHEMBL540042 | — | — | 1 | 5.96 |
| CHEMBL545238 | — | — | 1 | 5.77 |
| CHEMBL555167 | — | — | 1 | 5.75 |
| CHEMBL542896 | — | — | 1 | 5.42 |
| CHEMBL543603 | — | — | 1 | 5.35 |
| CHEMBL552688 | — | — | 1 | 5.31 |
| CHEMBL541566 | — | — | 1 | 5.30 |
| CHEMBL543125 | — | — | 1 | 5.23 |
| CHEMBL543365 | — | — | 1 | 5.20 |
| CHEMBL542665 | — | — | 1 | 5.18 |
| CHEMBL541065 | — | — | 1 | 5.11 |
| CHEMBL311761 | — | — | 1 | 5.04 |
| CHEMBL553129 | — | — | 1 | 5.00 |
| CHEMBL543840 | — | — | 1 | 4.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL538260 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL544544 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL303580 | GABAZINE BROMIDE | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL544302 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL553552 | — | Ki | = | 360.0 | nM | 6.44 |
| CHEMBL544301 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL544776 | — | Ki | = | 490.0 | nM | 6.31 |
| CHEMBL545008 | — | Ki | = | 700.0 | nM | 6.16 |
| CHEMBL555181 | — | Ki | = | 960.0 | nM | 6.02 |
| CHEMBL540042 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL545238 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL555167 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL542896 | — | Ki | = | 3800.0 | nM | 5.42 |
| CHEMBL543603 | — | Ki | = | 4500.0 | nM | 5.35 |
| CHEMBL552688 | — | Ki | = | 4900.0 | nM | 5.31 |
| CHEMBL541566 | — | Ki | = | 5000.0 | nM | 5.30 |
| CHEMBL543125 | — | Ki | = | 5900.0 | nM | 5.23 |
| CHEMBL543365 | — | Ki | = | 6300.0 | nM | 5.20 |
| CHEMBL542665 | — | Ki | = | 6600.0 | nM | 5.18 |
| CHEMBL541065 | — | Ki | = | 7700.0 | nM | 5.11 |
| CHEMBL311761 | — | Ki | = | 9100.0 | nM | 5.04 |
| CHEMBL553129 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL543840 | — | Ki | = | 37000.0 | nM | 4.43 |