Assay Detail
Functional
CHEMBL806813
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GABA uptake into crude synaptosomes prepared from adult rat brain
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 1 — Organism |
| Curated By | Expert |
Publication
Selective inhibitors of glial GABA uptake: synthesis, absolute stereochemistry, and pharmacology of the enantiomers of 3-hydroxy-4-amino-4,5,6,7-tetrahydro-1,2-benzisoxazole (exo-THPO) and analogues.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 4.57 | 5.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL77575 | (R)-NIPECOTIC ACID | — | 1 | 5.30 |
| CHEMBL76768 | GUVACINE | — | 1 | 4.92 |
| CHEMBL346444 | — | — | 1 | 4.41 |
| CHEMBL149914 | — | — | 1 | 4.20 |
| CHEMBL357762 | — | — | 1 | 4.01 |
| CHEMBL151070 | — | — | 1 | - |
| CHEMBL150865 | — | — | 1 | - |
| CHEMBL149415 | — | — | 1 | - |
| CHEMBL150489 | — | — | 1 | - |
| CHEMBL150830 | — | — | 1 | - |
| CHEMBL151721 | — | — | 1 | - |
| CHEMBL150142 | — | — | 1 | - |
| CHEMBL150916 | — | — | 1 | - |
| CHEMBL151722 | — | — | 1 | - |
| CHEMBL149417 | — | — | 1 | - |
| CHEMBL346880 | — | — | 1 | - |
| CHEMBL150265 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL77575 | (R)-NIPECOTIC ACID | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL76768 | GUVACINE | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL346444 | — | IC50 | = | 39000.0 | nM | 4.41 |
| CHEMBL149914 | — | IC50 | = | 63000.0 | nM | 4.20 |
| CHEMBL357762 | — | IC50 | = | 98000.0 | nM | 4.01 |
| CHEMBL151070 | — | IC50 | = | 105000.0 | nM | - |
| CHEMBL150865 | — | IC50 | = | 181000.0 | nM | - |
| CHEMBL149415 | — | IC50 | = | 291000.0 | nM | - |
| CHEMBL150489 | — | IC50 | = | 242000.0 | nM | - |
| CHEMBL150830 | — | IC50 | = | 162000.0 | nM | - |
| CHEMBL151721 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL150142 | — | IC50 | = | 201000.0 | nM | - |
| CHEMBL150916 | — | IC50 | = | 125000.0 | nM | - |
| CHEMBL151722 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL149417 | — | IC50 | = | 173000.0 | nM | - |
| CHEMBL346880 | — | IC50 | = | 290000.0 | nM | - |
| CHEMBL150265 | — | IC50 | = | 118000.0 | nM | - |