Assay Detail
Binding
CHEMBL680643
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Binding affinity against Gamma-aminobutyric acid A receptor in rat cerebral cortex
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Partial GABAA receptor agonists. Synthesis and in vitro pharmacology of a series of nonannulated analogs of 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 5.79 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | 1.0 | 1 | 7.75 |
| CHEMBL39071 | ISOGUVACINE | — | 1 | 7.66 |
| CHEMBL312443 | GABOXADOL | 3.0 | 1 | 7.04 |
| CHEMBL109209 | — | — | 1 | 5.89 |
| CHEMBL262445 | — | — | 1 | 5.40 |
| CHEMBL311761 | — | — | 1 | 5.03 |
| CHEMBL110210 | — | — | 1 | 4.58 |
| CHEMBL331588 | — | — | 1 | 4.50 |
| CHEMBL113450 | — | — | 1 | 4.28 |
| CHEMBL322544 | — | — | 1 | - |
| CHEMBL110858 | — | — | 1 | - |
| CHEMBL112853 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL39071 | ISOGUVACINE | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL312443 | GABOXADOL | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL109209 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL262445 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL311761 | — | IC50 | = | 9300.0 | nM | 5.03 |
| CHEMBL110210 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL331588 | — | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL113450 | — | IC50 | = | 52000.0 | nM | 4.28 |
| CHEMBL322544 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL110858 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL112853 | — | IC50 | > | 100000.0 | nM | - |