Assay Detail
Binding
CHEMBL2417028
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human GAT3 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 3 (CHEMBL5208) ↗| 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 | 4.87 | 5.95 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL75035 | — | — | 1 | 5.95 |
| CHEMBL2415009 | — | — | 1 | 4.86 |
| CHEMBL297569 | BETA-ALANINE | — | 1 | 4.38 |
| CHEMBL77575 | (R)-NIPECOTIC ACID | — | 1 | 4.29 |
| CHEMBL77484 | (S)-NIPECOTIC ACID | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL75035 | — | IC50 | = | 1120.0 | nM | 5.95 |
| CHEMBL2415009 | — | IC50 | = | 13900.0 | nM | 4.86 |
| CHEMBL297569 | BETA-ALANINE | IC50 | = | 41200.0 | nM | 4.38 |
| CHEMBL77575 | (R)-NIPECOTIC ACID | IC50 | = | 51000.0 | nM | 4.29 |
| CHEMBL77484 | (S)-NIPECOTIC ACID | IC50 | = | 2320000.0 | nM | - |