Assay Detail
Binding
CHEMBL2405422
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Inhibition of GABA uptake at murine GAT-2 expressed in HEK293 cells
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis of N-substituted acyclic β-amino acids and their investigation as GABA uptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 4.71 | 5.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2403781 | — | — | 1 | 5.47 |
| CHEMBL75035 | — | — | 1 | 5.29 |
| CHEMBL77575 | (R)-NIPECOTIC ACID | — | 1 | 4.71 |
| CHEMBL297569 | BETA-ALANINE | — | 1 | 4.66 |
| CHEMBL277498 | NIPECOTIC ACID | — | 1 | 4.64 |
| CHEMBL2403791 | — | — | 1 | 4.39 |
| CHEMBL1995111 | — | — | 1 | 4.33 |
| CHEMBL2403793 | — | — | 1 | 4.20 |
| CHEMBL2403789 | — | — | 1 | - |
| CHEMBL38686 | — | — | 1 | - |
| CHEMBL77484 | (S)-NIPECOTIC ACID | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2403781 | — | IC50 | = | 3388.44 | nM | 5.47 |
| CHEMBL75035 | — | IC50 | = | 5128.61 | nM | 5.29 |
| CHEMBL77575 | (R)-NIPECOTIC ACID | IC50 | = | 19498.45 | nM | 4.71 |
| CHEMBL297569 | BETA-ALANINE | IC50 | = | 21877.62 | nM | 4.66 |
| CHEMBL277498 | NIPECOTIC ACID | IC50 | = | 22908.68 | nM | 4.64 |
| CHEMBL2403791 | — | IC50 | = | 40738.03 | nM | 4.39 |
| CHEMBL1995111 | — | IC50 | = | 46773.51 | nM | 4.33 |
| CHEMBL2403793 | — | IC50 | = | 63095.73 | nM | 4.20 |
| CHEMBL2403789 | — | IC50 | = | 213796.21 | nM | - |
| CHEMBL38686 | — | IC50 | = | 194984.46 | nM | - |
| CHEMBL77484 | (S)-NIPECOTIC ACID | IC50 | = | 194984.46 | nM | - |