Assay Detail
Binding
CHEMBL4371901
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Inhibition of mouse GAT4 expressed in HEK cells assessed as reduction in [3H]GABA uptake by measuring remaining [3H]GABA uptake levels preincubated for 25 mins followed by [3H]GABA addition and measured after 4 mins by microbeta liquid scintillation counting analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Generation and screening of pseudostatic hydrazone libraries derived from 5-substituted nipecotic acid derivatives at the GABA transporter mGAT4.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 5.13 | 5.65 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL75035 | — | — | 1 | 5.65 |
| CHEMBL4447559 | — | — | 1 | 5.27 |
| CHEMBL4548691 | — | — | 1 | 4.99 |
| CHEMBL4566905 | — | — | 1 | 4.61 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL75035 | — | IC50 | = | 2238.72 | nM | 5.65 |
| CHEMBL4447559 | — | IC50 | = | 5370.32 | nM | 5.27 |
| CHEMBL4548691 | — | IC50 | = | 10232.93 | nM | 4.99 |
| CHEMBL4566905 | — | IC50 | = | 24547.09 | nM | 4.61 |