Assay Detail
Binding
CHEMBL941523
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Inhibition of [3H]GABA uptake at mouse GAT4 expressed in HEK cells
18
Total Activities
18
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 and biological evaluation of aminomethylphenol derivatives as inhibitors of the murine GABA transporters mGAT1-mGAT4.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 4.77 | 5.81 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL75035 | — | — | 1 | 5.81 |
| CHEMBL516192 | — | — | 1 | 5.11 |
| CHEMBL473037 | — | — | 1 | 5.06 |
| CHEMBL470499 | — | — | 1 | 4.84 |
| CHEMBL473312 | — | — | 1 | 4.83 |
| CHEMBL77575 | (R)-NIPECOTIC ACID | — | 1 | 4.79 |
| CHEMBL473113 | — | — | 1 | 4.79 |
| CHEMBL277498 | NIPECOTIC ACID | — | 1 | 4.70 |
| CHEMBL472718 | — | — | 1 | 4.68 |
| CHEMBL515546 | — | — | 1 | 4.64 |
| CHEMBL473311 | — | — | 1 | 4.60 |
| CHEMBL473117 | — | — | 1 | 4.60 |
| CHEMBL76768 | GUVACINE | — | 1 | 4.59 |
| CHEMBL473118 | — | — | 1 | 4.30 |
| CHEMBL473310 | — | — | 1 | 4.20 |
| CHEMBL473104 | — | — | 1 | - |
| CHEMBL38686 | — | — | 1 | - |
| CHEMBL77484 | (S)-NIPECOTIC ACID | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL75035 | — | IC50 | = | 1548.82 | nM | 5.81 |
| CHEMBL516192 | — | IC50 | = | 7762.47 | nM | 5.11 |
| CHEMBL473037 | — | IC50 | = | 8709.64 | nM | 5.06 |
| CHEMBL470499 | — | IC50 | = | 14454.4 | nM | 4.84 |
| CHEMBL473312 | — | IC50 | = | 14791.08 | nM | 4.83 |
| CHEMBL77575 | (R)-NIPECOTIC ACID | IC50 | = | 16218.1 | nM | 4.79 |
| CHEMBL473113 | — | IC50 | = | 16218.1 | nM | 4.79 |
| CHEMBL277498 | NIPECOTIC ACID | IC50 | = | 19952.62 | nM | 4.70 |
| CHEMBL472718 | — | IC50 | = | 20892.96 | nM | 4.68 |
| CHEMBL515546 | — | IC50 | = | 22908.68 | nM | 4.64 |
| CHEMBL473311 | — | IC50 | = | 25118.86 | nM | 4.60 |
| CHEMBL473117 | — | IC50 | = | 25118.86 | nM | 4.60 |
| CHEMBL76768 | GUVACINE | IC50 | = | 25703.96 | nM | 4.59 |
| CHEMBL473118 | — | IC50 | = | 50118.72 | nM | 4.30 |
| CHEMBL473310 | — | IC50 | = | 63095.73 | nM | 4.20 |
| CHEMBL473104 | — | IC50 | = | 851138.04 | nM | - |
| CHEMBL38686 | — | IC50 | = | 275422.87 | nM | - |
| CHEMBL77484 | (S)-NIPECOTIC ACID | IC50 | = | 309029.54 | nM | - |