Assay Detail
Binding
CHEMBL2388198
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Inhibition of mouse GAT3 expressed in HEK cells assessed as inhibition of [3H]-GABA uptake after 25 mins by liquid scintillation counting analysis
11
Total Activities
11
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 evaluation of N-substituted nipecotic acid derivatives with an unsymmetrical bis-aromatic residue attached to a vinyl ether spacer as potential GABA uptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 4.60 | 4.94 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | 1.0 | 1 | 4.94 |
| CHEMBL2387671 | — | — | 1 | 4.71 |
| CHEMBL277498 | NIPECOTIC ACID | — | 1 | 4.71 |
| CHEMBL2387675 | — | — | 1 | 4.70 |
| CHEMBL2387677 | — | — | 1 | 4.55 |
| CHEMBL2387669 | — | — | 1 | 4.46 |
| CHEMBL2387666 | — | — | 1 | 4.43 |
| CHEMBL2387673 | — | — | 1 | 4.30 |
| CHEMBL2387662 | — | — | 1 | - |
| CHEMBL2387658 | — | — | 1 | - |
| CHEMBL2387678 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | IC50 | = | 11481.54 | nM | 4.94 |
| CHEMBL2387671 | — | IC50 | = | 19498.45 | nM | 4.71 |
| CHEMBL277498 | NIPECOTIC ACID | IC50 | = | 19498.45 | nM | 4.71 |
| CHEMBL2387675 | — | IC50 | = | 19952.62 | nM | 4.70 |
| CHEMBL2387677 | — | IC50 | = | 28183.83 | nM | 4.55 |
| CHEMBL2387669 | — | IC50 | = | 34673.69 | nM | 4.46 |
| CHEMBL2387666 | — | IC50 | = | 37153.52 | nM | 4.43 |
| CHEMBL2387673 | — | IC50 | = | 50118.72 | nM | 4.30 |
| CHEMBL2387662 | — | IC50 | = | 338844.16 | nM | - |
| CHEMBL2387658 | — | IC50 | = | 371535.23 | nM | - |
| CHEMBL2387678 | — | IC50 | = | 194984.46 | nM | - |