Assay Detail
Functional
CHEMBL782605
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Inhibition of GABA uptake from rat diencephalon-midbrain,
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
Publication
Orally active and potent inhibitors of gamma-aminobutyric acid uptake.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 5.73 | 6.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL77626 | — | — | 1 | 6.96 |
| CHEMBL38686 | — | — | 1 | 6.70 |
| CHEMBL103623 | — | — | 1 | 6.70 |
| CHEMBL351355 | — | — | 1 | 5.81 |
| CHEMBL77575 | (R)-NIPECOTIC ACID | — | 1 | 5.77 |
| CHEMBL160709 | — | — | 1 | 5.72 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | 1.0 | 1 | 5.58 |
| CHEMBL277498 | NIPECOTIC ACID | — | 1 | 5.41 |
| CHEMBL348084 | — | — | 1 | 5.34 |
| CHEMBL76768 | GUVACINE | — | 1 | 5.31 |
| CHEMBL346013 | — | — | 1 | 5.09 |
| CHEMBL158564 | — | — | 1 | 4.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL77626 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL38686 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL103623 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL351355 | — | IC50 | = | 1540.0 | nM | 5.81 |
| CHEMBL77575 | (R)-NIPECOTIC ACID | IC50 | = | 1690.0 | nM | 5.77 |
| CHEMBL160709 | — | IC50 | = | 1910.0 | nM | 5.72 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL277498 | NIPECOTIC ACID | IC50 | = | 3940.0 | nM | 5.41 |
| CHEMBL348084 | — | IC50 | = | 4560.0 | nM | 5.34 |
| CHEMBL76768 | GUVACINE | IC50 | = | 4920.0 | nM | 5.31 |
| CHEMBL346013 | — | IC50 | = | 8130.0 | nM | 5.09 |
| CHEMBL158564 | — | IC50 | = | 43000.0 | nM | 4.37 |