Assay Detail
Binding
CHEMBL941522
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Inhibition of [3H]GABA uptake at mouse GAT3 expressed in HEK cells
20
Total Activities
19
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 | 20 | 4.95 | 5.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL473037 | — | — | 1 | 5.57 |
| CHEMBL75035 | — | — | 1 | 5.29 |
| CHEMBL473311 | — | — | 1 | 5.25 |
| CHEMBL473312 | — | — | 1 | 5.11 |
| CHEMBL472718 | — | — | 1 | 5.10 |
| CHEMBL473113 | — | — | 1 | 5.08 |
| CHEMBL470499 | — | — | 1 | 5.05 |
| CHEMBL516192 | — | — | 1 | 5.02 |
| CHEMBL472577 | — | — | 2 | 4.99 |
| CHEMBL515546 | — | — | 1 | 4.92 |
| CHEMBL473310 | — | — | 1 | 4.73 |
| CHEMBL77575 | (R)-NIPECOTIC ACID | — | 1 | 4.71 |
| CHEMBL277498 | NIPECOTIC ACID | — | 1 | 4.64 |
| CHEMBL473117 | — | — | 1 | 4.61 |
| CHEMBL76768 | GUVACINE | — | 1 | 4.59 |
| CHEMBL473118 | — | — | 1 | 4.42 |
| CHEMBL38686 | — | — | 1 | - |
| CHEMBL473104 | — | — | 1 | - |
| CHEMBL77484 | (S)-NIPECOTIC ACID | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL473037 | — | IC50 | = | 2691.53 | nM | 5.57 |
| CHEMBL75035 | — | IC50 | = | 5128.61 | nM | 5.29 |
| CHEMBL473311 | — | IC50 | = | 5623.41 | nM | 5.25 |
| CHEMBL473312 | — | IC50 | = | 7762.47 | nM | 5.11 |
| CHEMBL472718 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL473113 | — | IC50 | = | 8317.64 | nM | 5.08 |
| CHEMBL470499 | — | IC50 | = | 8912.51 | nM | 5.05 |
| CHEMBL516192 | — | IC50 | = | 9549.93 | nM | 5.02 |
| CHEMBL472577 | — | IC50 | = | 10232.93 | nM | 4.99 |
| CHEMBL472577 | — | IC50 | = | 10200.0 | nM | 4.99 |
| CHEMBL515546 | — | IC50 | = | 12022.64 | nM | 4.92 |
| CHEMBL473310 | — | IC50 | = | 18620.87 | nM | 4.73 |
| CHEMBL77575 | (R)-NIPECOTIC ACID | IC50 | = | 19498.45 | nM | 4.71 |
| CHEMBL277498 | NIPECOTIC ACID | IC50 | = | 22908.68 | nM | 4.64 |
| CHEMBL473117 | — | IC50 | = | 24547.09 | nM | 4.61 |
| CHEMBL76768 | GUVACINE | IC50 | = | 25703.96 | nM | 4.59 |
| CHEMBL473118 | — | IC50 | = | 38018.94 | nM | 4.42 |
| CHEMBL473104 | — | IC50 | = | 239883.29 | nM | - |
| CHEMBL38686 | — | IC50 | = | 194984.46 | nM | - |
| CHEMBL77484 | (S)-NIPECOTIC ACID | IC50 | = | 194984.46 | nM | - |