Assay Detail
Binding
CHEMBL681132
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro affinity for GABA binding sites on purified synaptic membranes from rat brain.
6
Total Activities
6
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
4,5,6,7-Tetrahydroisothiazolo[5,4-c]pyridin-3-ol and related analogues of THIP. Synthesis and biological activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 5.62 | 7.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | 1.0 | 1 | 7.48 |
| CHEMBL312443 | GABOXADOL | 3.0 | 1 | 6.89 |
| CHEMBL309689 | — | — | 1 | 4.82 |
| CHEMBL170753 | — | — | 1 | 4.51 |
| CHEMBL170539 | — | — | 1 | 4.38 |
| CHEMBL171241 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL312443 | GABOXADOL | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL309689 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL170753 | — | IC50 | = | 31000.0 | nM | 4.51 |
| CHEMBL170539 | — | IC50 | = | 42000.0 | nM | 4.38 |
| CHEMBL171241 | — | IC50 | > | 100000.0 | nM | - |