Assay Detail
Binding
CHEMBL806333
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory activity against human GABA transporter-1 (hGAT1)
28
Total Activities
28
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 1 (CHEMBL1903) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 28 | 5.18 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1027 | TIAGABINE | 4.0 | 1 | 7.16 |
| CHEMBL77626 | — | — | 1 | 6.89 |
| CHEMBL77287 | — | — | 1 | 6.58 |
| CHEMBL76966 | — | — | 1 | 5.85 |
| CHEMBL76868 | — | — | 1 | 5.52 |
| CHEMBL74854 | — | — | 1 | 5.30 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | 1.0 | 1 | 5.30 |
| CHEMBL77575 | (R)-NIPECOTIC ACID | — | 1 | 5.23 |
| CHEMBL77111 | — | — | 1 | 5.16 |
| CHEMBL277498 | NIPECOTIC ACID | — | 1 | 5.10 |
| CHEMBL74138 | — | — | 1 | 5.00 |
| CHEMBL76768 | GUVACINE | — | 1 | 4.85 |
| CHEMBL72499 | — | — | 1 | 4.72 |
| CHEMBL309357 | — | — | 1 | 4.58 |
| CHEMBL308528 | — | — | 1 | 4.37 |
| CHEMBL78166 | — | — | 1 | 4.37 |
| CHEMBL77423 | — | — | 1 | 4.24 |
| CHEMBL77166 | — | — | 1 | 4.14 |
| CHEMBL307361 | — | — | 1 | 4.11 |
| CHEMBL310236 | — | — | 1 | - |
| CHEMBL308391 | — | — | 1 | - |
| CHEMBL419823 | — | — | 1 | - |
| CHEMBL405620 | — | — | 1 | - |
| CHEMBL75035 | — | — | 1 | - |
| CHEMBL269439 | — | — | 1 | - |
| CHEMBL432737 | — | — | 1 | - |
| CHEMBL77484 | (S)-NIPECOTIC ACID | — | 1 | - |
| CHEMBL75800 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1027 | TIAGABINE | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL77626 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL77287 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL76966 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL76868 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL74854 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL77575 | (R)-NIPECOTIC ACID | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL77111 | — | IC50 | = | 6900.0 | nM | 5.16 |
| CHEMBL277498 | NIPECOTIC ACID | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL74138 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL76768 | GUVACINE | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL72499 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL309357 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL308528 | — | IC50 | = | 43000.0 | nM | 4.37 |
| CHEMBL78166 | — | IC50 | = | 43000.0 | nM | 4.37 |
| CHEMBL77423 | — | IC50 | = | 58000.0 | nM | 4.24 |
| CHEMBL77166 | — | IC50 | = | 73000.0 | nM | 4.14 |
| CHEMBL307361 | — | IC50 | = | 78000.0 | nM | 4.11 |
| CHEMBL310236 | — | IC50 | = | 142000.0 | nM | - |
| CHEMBL308391 | — | IC50 | = | 121000.0 | nM | - |
| CHEMBL419823 | — | IC50 | = | 439000.0 | nM | - |
| CHEMBL405620 | — | IC50 | = | 268000.0 | nM | - |
| CHEMBL75035 | — | IC50 | = | 388000.0 | nM | - |
| CHEMBL269439 | — | IC50 | = | 122000.0 | nM | - |
| CHEMBL432737 | — | IC50 | = | 233000.0 | nM | - |
| CHEMBL77484 | (S)-NIPECOTIC ACID | IC50 | = | 116000.0 | nM | - |
| CHEMBL75800 | — | IC50 | = | 133000.0 | nM | - |