Assay Detail
Binding
CHEMBL888163
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Inhibition of [3H]GABA uptake at mouse GAT1 expressed in D8 cells
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | D8 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Sodium- and chloride-dependent GABA transporter 1 (CHEMBL5445) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
Synthesis and biological evaluation of (R)-N-(diarylmethylthio/sulfinyl)ethyl/propyl-piperidine-3-carboxylic acid hydrochlorides as novel GABA uptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 5.60 | 7.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1695 | TIAGABINE HYDROCHLORIDE | 4.0 | 1 | 7.10 |
| CHEMBL538839 | — | — | 1 | 6.04 |
| CHEMBL558578 | — | — | 1 | 5.93 |
| CHEMBL538596 | — | — | 1 | 4.94 |
| CHEMBL536532 | — | — | 1 | 4.80 |
| CHEMBL541139 | — | — | 1 | 4.77 |
| CHEMBL537448 | — | — | 1 | - |
| CHEMBL536762 | — | — | 1 | - |
| CHEMBL536534 | — | — | 1 | - |
| CHEMBL536533 | — | — | 1 | - |
| CHEMBL537671 | — | — | 1 | - |
| CHEMBL537449 | — | — | 1 | - |
| CHEMBL539347 | — | — | 1 | - |
| CHEMBL77575 | (R)-NIPECOTIC ACID | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1695 | TIAGABINE HYDROCHLORIDE | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL538839 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL558578 | — | IC50 | = | 1180.0 | nM | 5.93 |
| CHEMBL538596 | — | IC50 | = | 11600.0 | nM | 4.94 |
| CHEMBL536532 | — | IC50 | = | 15800.0 | nM | 4.80 |
| CHEMBL541139 | — | IC50 | = | 16900.0 | nM | 4.77 |
| CHEMBL537448 | — | IC50 | = | 1600000.0 | nM | - |
| CHEMBL536762 | — | IC50 | = | 105000.0 | nM | - |
| CHEMBL536534 | — | IC50 | = | 589000.0 | nM | - |
| CHEMBL536533 | — | IC50 | = | 120000.0 | nM | - |
| CHEMBL537671 | — | IC50 | = | 2130000.0 | nM | - |
| CHEMBL537449 | — | IC50 | = | 4800000.0 | nM | - |
| CHEMBL539347 | — | IC50 | = | 240000.0 | nM | - |
| CHEMBL77575 | (R)-NIPECOTIC ACID | IC50 | = | 456000.0 | nM | - |