Assay Detail
Functional
CHEMBL784482
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibition of [3H]GABA uptake in rat synaptosomes
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Tissue | Brain |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
The synthesis of novel GABA uptake inhibitors. 1. Elucidation of the structure-activity studies leading to the choice of (R)-1-[4,4-bis(3-methyl-2-thienyl)-3-butenyl]-3-piperidinecarboxylic acid (tiagabine) as an anticonvulsant drug candidate.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 6.60 | 7.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL542112 | — | — | 1 | 7.22 |
| CHEMBL1695 | TIAGABINE HYDROCHLORIDE | 4.0 | 1 | 7.17 |
| CHEMBL541287 | — | — | 1 | 7.11 |
| CHEMBL540792 | — | — | 1 | 7.09 |
| CHEMBL540529 | — | — | 1 | 7.06 |
| CHEMBL544729 | — | — | 1 | 6.95 |
| CHEMBL542615 | — | — | 1 | 6.95 |
| CHEMBL538239 | — | — | 1 | 6.89 |
| CHEMBL543081 | — | — | 1 | 6.89 |
| CHEMBL543550 | — | — | 1 | 6.86 |
| CHEMBL556829 | — | — | 1 | 6.66 |
| CHEMBL542110 | — | — | 1 | 6.61 |
| CHEMBL555999 | — | — | 1 | 6.59 |
| CHEMBL554197 | — | — | 1 | 6.58 |
| CHEMBL542114 | — | — | 1 | 6.58 |
| CHEMBL544259 | — | — | 1 | 6.54 |
| CHEMBL545426 | — | — | 1 | 6.52 |
| CHEMBL554208 | — | — | 1 | 6.50 |
| CHEMBL543557 | — | — | 1 | 6.48 |
| CHEMBL556054 | — | — | 1 | 6.47 |
| CHEMBL540276 | — | — | 1 | 6.42 |
| CHEMBL553494 | — | — | 1 | 6.41 |
| CHEMBL538998 | — | — | 1 | 6.16 |
| CHEMBL555997 | — | — | 1 | 6.07 |
| CHEMBL542610 | — | — | 1 | 5.86 |
| CHEMBL554627 | — | — | 1 | 5.73 |
| CHEMBL544963 | — | — | 1 | 5.72 |
| CHEMBL543556 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL542112 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL1695 | TIAGABINE HYDROCHLORIDE | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL541287 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL540792 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL540529 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL544729 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL542615 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL538239 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL543081 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL543550 | — | IC50 | = | 138.0 | nM | 6.86 |
| CHEMBL556829 | — | IC50 | = | 218.0 | nM | 6.66 |
| CHEMBL542110 | — | IC50 | = | 247.0 | nM | 6.61 |
| CHEMBL555999 | — | IC50 | = | 256.0 | nM | 6.59 |
| CHEMBL554197 | — | IC50 | = | 265.0 | nM | 6.58 |
| CHEMBL542114 | — | IC50 | = | 264.0 | nM | 6.58 |
| CHEMBL544259 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL545426 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL554208 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL543557 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL556054 | — | IC50 | = | 341.0 | nM | 6.47 |
| CHEMBL540276 | — | IC50 | = | 383.0 | nM | 6.42 |
| CHEMBL553494 | — | IC50 | = | 388.0 | nM | 6.41 |
| CHEMBL538998 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL555997 | — | IC50 | = | 848.0 | nM | 6.07 |
| CHEMBL542610 | — | IC50 | = | 1370.0 | nM | 5.86 |
| CHEMBL554627 | — | IC50 | = | 1864.0 | nM | 5.73 |
| CHEMBL544963 | — | IC50 | = | 1920.0 | nM | 5.72 |
| CHEMBL543556 | — | IC50 | > | 3000.0 | nM | - |