Assay Detail
Binding
CHEMBL1166716
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Inhibition of GAT1-mediated [3H]GABA uptake in bovine brain stem
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Bos taurus |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Azetidine derivatives as novel gamma-aminobutyric acid uptake inhibitors: synthesis, biological evaluation, and structure-activity relationship.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 5.51 | 6.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1027 | TIAGABINE | 4.0 | 1 | 6.80 |
| CHEMBL603863 | — | — | 1 | 6.46 |
| CHEMBL594213 | — | — | 1 | 6.40 |
| CHEMBL38686 | — | — | 1 | 5.93 |
| CHEMBL77575 | (R)-NIPECOTIC ACID | — | 1 | 5.67 |
| CHEMBL277498 | NIPECOTIC ACID | — | 1 | 5.32 |
| CHEMBL77484 | (S)-NIPECOTIC ACID | — | 1 | 4.49 |
| CHEMBL1164498 | — | — | 1 | 4.42 |
| CHEMBL75035 | — | — | 1 | 4.08 |
| CHEMBL1163348 | — | — | 1 | - |
| CHEMBL1164855 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1027 | TIAGABINE | IC50 | = | 159.0 | nM | 6.80 |
| CHEMBL603863 | — | IC50 | = | 343.0 | nM | 6.46 |
| CHEMBL594213 | — | IC50 | = | 396.0 | nM | 6.40 |
| CHEMBL38686 | — | IC50 | = | 1180.0 | nM | 5.93 |
| CHEMBL77575 | (R)-NIPECOTIC ACID | IC50 | = | 2150.0 | nM | 5.67 |
| CHEMBL277498 | NIPECOTIC ACID | IC50 | = | 4770.0 | nM | 5.32 |
| CHEMBL77484 | (S)-NIPECOTIC ACID | IC50 | = | 32600.0 | nM | 4.49 |
| CHEMBL1164498 | — | IC50 | = | 37800.0 | nM | 4.42 |
| CHEMBL75035 | — | IC50 | = | 83300.0 | nM | 4.08 |
| CHEMBL1163348 | — | IC50 | = | 214000.0 | nM | - |
| CHEMBL1164855 | — | IC50 | = | 482000.0 | nM | - |