Assay Detail
Binding
CHEMBL5114469
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Inhibition of GAT-mediated [3H]-GABA uptake in rat forebrain synaptosomes preincubated for 8 mins followed by [3H]-GABA addition measured after 8 mins by scintillation counting method
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Forebrain |
| Subcellular | Synaptosomes |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Nipecotic acid as potential lead molecule for the development of GABA uptake inhibitors; structural insights and design strategies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 7.15 | 7.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5170782 | — | — | 1 | 7.21 |
| CHEMBL1695 | TIAGABINE HYDROCHLORIDE | 4.0 | 1 | 7.17 |
| CHEMBL5204409 | — | — | 1 | 7.11 |
| CHEMBL5177063 | — | — | 1 | 7.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5170782 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL1695 | TIAGABINE HYDROCHLORIDE | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL5204409 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL5177063 | — | IC50 | = | 80.0 | nM | 7.10 |