Assay Detail
Binding
CHEMBL3363499
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Inhibition of human BGT1 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium- and chloride-dependent betaine transporter (CHEMBL3715) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Conformationally Restricted GABA with Bicyclo[3.1.0]hexane Backbone as the First Highly Selective BGT-1 Inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 5.23 | 6.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3326391 | — | — | 1 | 6.23 |
| CHEMBL1446457 | — | — | 1 | 5.29 |
| CHEMBL3040189 | — | — | 1 | 5.26 |
| CHEMBL75035 | — | — | 1 | 4.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3326391 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL1446457 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL3040189 | — | IC50 | = | 5480.0 | nM | 5.26 |
| CHEMBL75035 | — | IC50 | = | 71700.0 | nM | 4.14 |