Assay Detail
Binding
CHEMBL809055
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Inhibitory activity against rat GABA transporter-2 (rGAT2)
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium- and chloride-dependent GABA transporter 2 (CHEMBL4889) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Design, synthesis and evaluation of substituted triarylnipecotic acid derivatives as GABA uptake inhibitors: identification of a ligand with moderate affinity and selectivity for the cloned human GABA transporter GAT-3.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 4.43 | 5.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | 1.0 | 1 | 5.30 |
| CHEMBL77575 | (R)-NIPECOTIC ACID | — | 1 | 4.72 |
| CHEMBL75035 | — | — | 1 | 4.68 |
| CHEMBL309357 | — | — | 1 | 4.52 |
| CHEMBL432737 | — | — | 1 | 4.47 |
| CHEMBL269439 | — | — | 1 | 4.41 |
| CHEMBL277498 | NIPECOTIC ACID | — | 1 | 4.41 |
| CHEMBL310236 | — | — | 1 | 4.35 |
| CHEMBL72499 | — | — | 1 | 4.31 |
| CHEMBL75800 | — | — | 1 | 4.29 |
| CHEMBL76768 | GUVACINE | — | 1 | 4.24 |
| CHEMBL78166 | — | — | 1 | 4.21 |
| CHEMBL307361 | — | — | 1 | 4.08 |
| CHEMBL308528 | — | — | 1 | 4.07 |
| CHEMBL77166 | — | — | 1 | - |
| CHEMBL77287 | — | — | 1 | - |
| CHEMBL77423 | — | — | 1 | - |
| CHEMBL308391 | — | — | 1 | - |
| CHEMBL74138 | — | — | 1 | - |
| CHEMBL77111 | — | — | 1 | - |
| CHEMBL405620 | — | — | 1 | - |
| CHEMBL1027 | TIAGABINE | 4.0 | 1 | - |
| CHEMBL77626 | — | — | 1 | - |
| CHEMBL77484 | (S)-NIPECOTIC ACID | — | 1 | - |
| CHEMBL419823 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL77575 | (R)-NIPECOTIC ACID | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL75035 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL309357 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL432737 | — | IC50 | = | 34000.0 | nM | 4.47 |
| CHEMBL269439 | — | IC50 | = | 39000.0 | nM | 4.41 |
| CHEMBL277498 | NIPECOTIC ACID | IC50 | = | 39000.0 | nM | 4.41 |
| CHEMBL310236 | — | IC50 | = | 45000.0 | nM | 4.35 |
| CHEMBL72499 | — | IC50 | = | 49000.0 | nM | 4.31 |
| CHEMBL75800 | — | IC50 | = | 51000.0 | nM | 4.29 |
| CHEMBL76768 | GUVACINE | IC50 | = | 58000.0 | nM | 4.24 |
| CHEMBL78166 | — | IC50 | = | 62000.0 | nM | 4.21 |
| CHEMBL307361 | — | IC50 | = | 84000.0 | nM | 4.08 |
| CHEMBL308528 | — | IC50 | = | 85000.0 | nM | 4.07 |
| CHEMBL77166 | — | IC50 | = | 177000.0 | nM | - |
| CHEMBL77287 | — | IC50 | = | 1280000.0 | nM | - |
| CHEMBL77423 | — | IC50 | = | 3670000.0 | nM | - |
| CHEMBL308391 | — | IC50 | = | 103000.0 | nM | - |
| CHEMBL74138 | — | IC50 | = | 417000.0 | nM | - |
| CHEMBL77111 | — | IC50 | = | 137000.0 | nM | - |
| CHEMBL405620 | — | IC50 | = | 2800000.0 | nM | - |
| CHEMBL1027 | TIAGABINE | IC50 | = | 1410000.0 | nM | - |
| CHEMBL77626 | — | IC50 | = | 550000.0 | nM | - |
| CHEMBL77484 | (S)-NIPECOTIC ACID | IC50 | = | 763000.0 | nM | - |
| CHEMBL419823 | — | IC50 | = | 240000.0 | nM | - |