Assay Detail
Functional
CHEMBL785010
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Inhibition of high affinity neuronal GABA uptake by synaptosomes of rat brain membrane
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Synaptosomes |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Expert |
Publication
Hydroxy- and amino-substituted piperidinecarboxylic acids as gamma-aminobutyric acid agonists and uptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 5.29 | 5.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | 1.0 | 1 | 5.70 |
| CHEMBL277498 | NIPECOTIC ACID | — | 1 | 5.22 |
| CHEMBL277372 | — | — | 1 | 4.96 |
| CHEMBL429974 | — | — | 1 | - |
| CHEMBL280511 | — | — | 1 | - |
| CHEMBL16132 | — | — | 1 | - |
| CHEMBL15851 | — | — | 1 | - |
| CHEMBL279998 | ISONIPECOTIC ACID | — | 1 | - |
| CHEMBL16226 | — | — | 1 | - |
| CHEMBL16357 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL277498 | NIPECOTIC ACID | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL277372 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL429974 | — | IC50 | = | 240000.0 | nM | - |
| CHEMBL280511 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL16132 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL15851 | — | IC50 | = | 173000.0 | nM | - |
| CHEMBL279998 | ISONIPECOTIC ACID | IC50 | > | 300000.0 | nM | - |
| CHEMBL16226 | — | IC50 | = | 203000.0 | nM | - |
| CHEMBL16357 | — | IC50 | > | 300000.0 | nM | - |