Assay Detail
Binding
CHEMBL681303
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Inhibition of [3H]GABA binding to Gamma-aminobutyric acid receptor of rat brain synaptosomal membranes
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Membrane |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
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 | 5.81 | 7.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | 1.0 | 1 | 7.48 |
| CHEMBL279998 | ISONIPECOTIC ACID | — | 1 | 6.48 |
| CHEMBL16132 | — | — | 1 | 4.92 |
| CHEMBL16357 | — | — | 1 | 4.37 |
| CHEMBL429974 | — | — | 1 | - |
| CHEMBL280511 | — | — | 1 | - |
| CHEMBL15851 | — | — | 1 | - |
| CHEMBL277498 | NIPECOTIC ACID | — | 1 | - |
| CHEMBL277372 | — | — | 1 | - |
| CHEMBL16226 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL279998 | ISONIPECOTIC ACID | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL16132 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL16357 | — | IC50 | = | 43000.0 | nM | 4.37 |
| CHEMBL429974 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL280511 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL15851 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL277498 | NIPECOTIC ACID | IC50 | > | 100000.0 | nM | - |
| CHEMBL277372 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL16226 | — | IC50 | > | 100000.0 | nM | - |