Assay Detail
Binding
CHEMBL806330
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In vitro inhibition of [3H]GABA uptake in rat synaptosomes
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium- and chloride-dependent GABA transporter 1 (CHEMBL4054) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis of novel GABA uptake inhibitors. 4. Bioisosteric transformation and successive optimization of known GABA uptake inhibitors leading to a series of potent anticonvulsant drug candidates.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 6.41 | 7.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL541093 | — | — | 1 | 7.32 |
| CHEMBL541053 | — | — | 1 | 7.26 |
| CHEMBL1695 | TIAGABINE HYDROCHLORIDE | 4.0 | 1 | 7.17 |
| CHEMBL545775 | — | — | 1 | 7.12 |
| CHEMBL543204 | — | — | 1 | 7.07 |
| CHEMBL543107 | — | — | 1 | 7.05 |
| CHEMBL539775 | — | — | 1 | 6.98 |
| CHEMBL538782 | — | — | 1 | 6.94 |
| CHEMBL542642 | — | — | 1 | 6.86 |
| CHEMBL543913 | — | — | 1 | 6.63 |
| CHEMBL542960 | — | — | 1 | 6.63 |
| CHEMBL542965 | — | — | 1 | 6.59 |
| CHEMBL545309 | — | — | 1 | 6.52 |
| CHEMBL543557 | — | — | 1 | 6.48 |
| CHEMBL544850 | — | — | 1 | 6.45 |
| CHEMBL542233 | — | — | 1 | 6.18 |
| CHEMBL544610 | — | — | 1 | 6.17 |
| CHEMBL553524 | — | — | 1 | 6.02 |
| CHEMBL540076 | — | — | 1 | 5.89 |
| CHEMBL542241 | — | — | 1 | 5.87 |
| CHEMBL542485 | — | — | 1 | 5.86 |
| CHEMBL542610 | — | — | 1 | 5.85 |
| CHEMBL555540 | — | — | 1 | 5.83 |
| CHEMBL544149 | — | — | 1 | 5.80 |
| CHEMBL555770 | — | — | 1 | 5.65 |
| CHEMBL541861 | — | — | 1 | 5.58 |
| CHEMBL541863 | — | — | 1 | 5.24 |
| CHEMBL543676 | — | — | 1 | - |
| CHEMBL543908 | — | — | 1 | - |
| CHEMBL557612 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL541093 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL541053 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL1695 | TIAGABINE HYDROCHLORIDE | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL545775 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL543204 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL543107 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL539775 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL538782 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL542642 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL543913 | — | IC50 | = | 232.0 | nM | 6.63 |
| CHEMBL542960 | — | IC50 | = | 236.0 | nM | 6.63 |
| CHEMBL542965 | — | IC50 | = | 258.0 | nM | 6.59 |
| CHEMBL545309 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL543557 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL544850 | — | IC50 | = | 358.0 | nM | 6.45 |
| CHEMBL542233 | — | IC50 | = | 659.0 | nM | 6.18 |
| CHEMBL544610 | — | IC50 | = | 675.0 | nM | 6.17 |
| CHEMBL553524 | — | IC50 | = | 955.0 | nM | 6.02 |
| CHEMBL540076 | — | IC50 | = | 1293.0 | nM | 5.89 |
| CHEMBL542241 | — | IC50 | = | 1359.0 | nM | 5.87 |
| CHEMBL542485 | — | IC50 | = | 1381.0 | nM | 5.86 |
| CHEMBL542610 | — | IC50 | = | 1407.0 | nM | 5.85 |
| CHEMBL555540 | — | IC50 | = | 1462.0 | nM | 5.83 |
| CHEMBL544149 | — | IC50 | = | 1585.0 | nM | 5.80 |
| CHEMBL555770 | — | IC50 | = | 2256.0 | nM | 5.65 |
| CHEMBL541861 | — | IC50 | = | 2608.0 | nM | 5.58 |
| CHEMBL541863 | — | IC50 | = | 5699.0 | nM | 5.24 |
| CHEMBL543676 | — | IC50 | > | 9000.0 | nM | - |
| CHEMBL543908 | — | IC50 | > | 9000.0 | nM | - |
| CHEMBL557612 | — | IC50 | > | 9000.0 | nM | - |
| CHEMBL538530 | — | IC50 | > | 3000.0 | nM | - |