Assay Detail
Binding
CHEMBL2417030
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human GAT1 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis
5
Total Activities
5
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 GABA transporter 1 (CHEMBL1903) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Cyclopropane-based conformational restriction of GABA by a stereochemical diversity-oriented strategy: identification of an efficient lead for potent inhibitors of GABA transports.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 6.27 | 7.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1695 | TIAGABINE HYDROCHLORIDE | 4.0 | 1 | 7.31 |
| CHEMBL77575 | (R)-NIPECOTIC ACID | — | 1 | 5.23 |
| CHEMBL77484 | (S)-NIPECOTIC ACID | — | 1 | - |
| CHEMBL75035 | — | — | 1 | - |
| CHEMBL2415009 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1695 | TIAGABINE HYDROCHLORIDE | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL77575 | (R)-NIPECOTIC ACID | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL77484 | (S)-NIPECOTIC ACID | IC50 | = | 116000.0 | nM | - |
| CHEMBL75035 | — | IC50 | = | 170000.0 | nM | - |
| CHEMBL2415009 | — | IC50 | > | 100000.0 | nM | - |