Assay Detail
Binding
CHEMBL940676
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Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK cells
20
Total Activities
20
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 |
Target
Sodium- and chloride-dependent GABA transporter 1 (CHEMBL5445) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
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 | 4.82 | 6.88 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1027 | TIAGABINE | 4.0 | 1 | 6.88 |
| CHEMBL473104 | — | — | 1 | 6.83 |
| CHEMBL38686 | — | — | 1 | 6.16 |
| CHEMBL77575 | (R)-NIPECOTIC ACID | — | 1 | 5.07 |
| CHEMBL473037 | — | — | 1 | 4.91 |
| CHEMBL277498 | NIPECOTIC ACID | — | 1 | 4.88 |
| CHEMBL76768 | GUVACINE | — | 1 | 4.87 |
| CHEMBL515546 | — | — | 1 | 4.73 |
| CHEMBL473311 | — | — | 1 | 4.68 |
| CHEMBL470499 | — | — | 1 | 4.59 |
| CHEMBL473113 | — | — | 1 | 4.57 |
| CHEMBL472718 | — | — | 1 | 4.54 |
| CHEMBL473312 | — | — | 1 | 4.48 |
| CHEMBL516192 | — | — | 1 | 4.36 |
| CHEMBL473117 | — | — | 1 | 4.28 |
| CHEMBL473310 | — | — | 1 | 4.23 |
| CHEMBL77484 | (S)-NIPECOTIC ACID | — | 1 | 4.13 |
| CHEMBL472577 | — | — | 1 | 4.07 |
| CHEMBL75035 | — | — | 1 | 4.07 |
| CHEMBL473118 | — | — | 1 | 4.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1027 | TIAGABINE | IC50 | = | 131.83 | nM | 6.88 |
| CHEMBL473104 | — | IC50 | = | 147.91 | nM | 6.83 |
| CHEMBL38686 | — | IC50 | = | 691.83 | nM | 6.16 |
| CHEMBL77575 | (R)-NIPECOTIC ACID | IC50 | = | 8511.38 | nM | 5.07 |
| CHEMBL473037 | — | IC50 | = | 12302.69 | nM | 4.91 |
| CHEMBL277498 | NIPECOTIC ACID | IC50 | = | 13182.57 | nM | 4.88 |
| CHEMBL76768 | GUVACINE | IC50 | = | 13489.63 | nM | 4.87 |
| CHEMBL515546 | — | IC50 | = | 18620.87 | nM | 4.73 |
| CHEMBL473311 | — | IC50 | = | 20892.96 | nM | 4.68 |
| CHEMBL470499 | — | IC50 | = | 25703.96 | nM | 4.59 |
| CHEMBL473113 | — | IC50 | = | 26915.35 | nM | 4.57 |
| CHEMBL472718 | — | IC50 | = | 28840.32 | nM | 4.54 |
| CHEMBL473312 | — | IC50 | = | 33113.11 | nM | 4.48 |
| CHEMBL516192 | — | IC50 | = | 43651.58 | nM | 4.36 |
| CHEMBL473117 | — | IC50 | = | 52480.75 | nM | 4.28 |
| CHEMBL473310 | — | IC50 | = | 58884.37 | nM | 4.23 |
| CHEMBL77484 | (S)-NIPECOTIC ACID | IC50 | = | 74131.02 | nM | 4.13 |
| CHEMBL472577 | — | IC50 | = | 85113.8 | nM | 4.07 |
| CHEMBL75035 | — | IC50 | = | 85113.8 | nM | 4.07 |
| CHEMBL473118 | — | IC50 | = | 87096.36 | nM | 4.06 |