Assay Detail
Binding
CHEMBL4125142
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Inhibition of [2H10]NO 711 binding to mouse GAT1 expressed in HEK293 cell membranes after 40 mins by LC-ESI-MS-MS analysis
16
Total Activities
16
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 novel N-substituted nipecotic acid derivatives with an alkyne spacer as GABA uptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 5.20 | 7.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4126090 | — | — | 1 | 7.04 |
| CHEMBL4128306 | — | — | 1 | 5.96 |
| CHEMBL4125831 | — | — | 1 | 5.72 |
| CHEMBL4128157 | — | — | 1 | 5.72 |
| CHEMBL4129538 | — | — | 1 | 5.67 |
| CHEMBL4129397 | — | — | 1 | 5.56 |
| CHEMBL4129672 | — | — | 1 | 5.36 |
| CHEMBL4128299 | — | — | 1 | 5.31 |
| CHEMBL4127205 | — | — | 1 | 5.28 |
| CHEMBL4127325 | — | — | 1 | 4.84 |
| CHEMBL4127466 | — | — | 1 | 4.83 |
| CHEMBL75035 | — | — | 1 | 4.56 |
| CHEMBL4125948 | — | — | 1 | 4.43 |
| CHEMBL4128707 | — | — | 1 | 4.42 |
| CHEMBL2403781 | — | — | 1 | 4.33 |
| CHEMBL4126231 | — | — | 1 | 4.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4126090 | — | Ki | = | 91.2 | nM | 7.04 |
| CHEMBL4128306 | — | Ki | = | 1096.48 | nM | 5.96 |
| CHEMBL4125831 | — | Ki | = | 1905.46 | nM | 5.72 |
| CHEMBL4128157 | — | Ki | = | 1905.46 | nM | 5.72 |
| CHEMBL4129538 | — | Ki | = | 2137.96 | nM | 5.67 |
| CHEMBL4129397 | — | Ki | = | 2754.23 | nM | 5.56 |
| CHEMBL4129672 | — | Ki | = | 4365.16 | nM | 5.36 |
| CHEMBL4128299 | — | Ki | = | 4897.79 | nM | 5.31 |
| CHEMBL4127205 | — | Ki | = | 5248.07 | nM | 5.28 |
| CHEMBL4127325 | — | Ki | = | 14454.4 | nM | 4.84 |
| CHEMBL4127466 | — | Ki | = | 14791.08 | nM | 4.83 |
| CHEMBL75035 | — | Ki | = | 27542.29 | nM | 4.56 |
| CHEMBL4125948 | — | Ki | = | 37153.52 | nM | 4.43 |
| CHEMBL4128707 | — | Ki | = | 38018.94 | nM | 4.42 |
| CHEMBL2403781 | — | Ki | = | 46773.51 | nM | 4.33 |
| CHEMBL4126231 | — | Ki | = | 77624.71 | nM | 4.11 |