Assay Detail
Binding
CHEMBL5336802
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of mouse GAT2 transfected in HEK293 cells assessed as reduction in [3H]-GABA uptake preincubated for 25 mins followed by [3H]-GABA addition and measured after 10 mins by liquid scintillation counting analysis
30
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of novel multifunctional ligands targeting GABA transporters, butyrylcholinesterase, β-secretase, and amyloid β aggregation as potential treatment of Alzheimer's disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 4.89 | 5.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5411369 | — | — | 2 | 5.52 |
| CHEMBL5423337 | — | — | 1 | 5.18 |
| CHEMBL5409309 | — | — | 1 | 5.11 |
| CHEMBL5416293 | — | — | 1 | 5.08 |
| CHEMBL5409538 | — | — | 1 | 5.02 |
| CHEMBL5403788 | — | — | 2 | 5.01 |
| CHEMBL5411905 | — | — | 1 | 4.99 |
| CHEMBL5423441 | — | — | 1 | 4.96 |
| CHEMBL5407267 | — | — | 1 | 4.94 |
| CHEMBL5423316 | — | — | 1 | 4.91 |
| CHEMBL5419107 | — | — | 1 | 4.89 |
| CHEMBL5412199 | — | — | 1 | 4.89 |
| CHEMBL5394533 | — | — | 2 | 4.87 |
| CHEMBL5423098 | — | — | 1 | 4.86 |
| CHEMBL5405236 | — | — | 1 | 4.85 |
| CHEMBL5424877 | — | — | 2 | 4.82 |
| CHEMBL5440565 | — | — | 1 | 4.80 |
| CHEMBL5435638 | — | — | 1 | 4.79 |
| CHEMBL5398245 | — | — | 1 | 4.72 |
| CHEMBL5438498 | — | — | 1 | 4.70 |
| CHEMBL5425025 | — | — | 1 | 4.70 |
| CHEMBL5414446 | — | — | 1 | 4.69 |
| CHEMBL5397274 | — | — | 1 | 4.65 |
| CHEMBL5413754 | — | — | 1 | 4.61 |
| CHEMBL5416743 | — | — | 1 | 4.57 |
| CHEMBL5397616 | — | — | 1 | 4.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5411369 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL5411369 | — | IC50 | = | 3090.3 | nM | 5.51 |
| CHEMBL5423337 | — | IC50 | = | 6606.93 | nM | 5.18 |
| CHEMBL5409309 | — | IC50 | = | 7762.47 | nM | 5.11 |
| CHEMBL5416293 | — | IC50 | = | 8317.64 | nM | 5.08 |
| CHEMBL5409538 | — | IC50 | = | 9549.93 | nM | 5.02 |
| CHEMBL5403788 | — | IC50 | = | 9772.37 | nM | 5.01 |
| CHEMBL5411905 | — | IC50 | = | 10232.93 | nM | 4.99 |
| CHEMBL5423441 | — | IC50 | = | 10964.78 | nM | 4.96 |
| CHEMBL5407267 | — | IC50 | = | 11481.54 | nM | 4.94 |
| CHEMBL5403788 | — | IC50 | = | 11748.98 | nM | 4.93 |
| CHEMBL5423316 | — | IC50 | = | 12302.69 | nM | 4.91 |
| CHEMBL5412199 | — | IC50 | = | 12882.5 | nM | 4.89 |
| CHEMBL5419107 | — | IC50 | = | 12882.5 | nM | 4.89 |
| CHEMBL5394533 | — | IC50 | = | 13489.63 | nM | 4.87 |
| CHEMBL5423098 | — | IC50 | = | 13803.84 | nM | 4.86 |
| CHEMBL5405236 | — | IC50 | = | 14125.38 | nM | 4.85 |
| CHEMBL5424877 | — | IC50 | = | 15135.61 | nM | 4.82 |
| CHEMBL5394533 | — | IC50 | = | 15488.17 | nM | 4.81 |
| CHEMBL5440565 | — | IC50 | = | 15848.93 | nM | 4.80 |
| CHEMBL5435638 | — | IC50 | = | 16218.1 | nM | 4.79 |
| CHEMBL5424877 | — | IC50 | = | 18197.01 | nM | 4.74 |
| CHEMBL5398245 | — | IC50 | = | 19054.61 | nM | 4.72 |
| CHEMBL5438498 | — | IC50 | = | 19952.62 | nM | 4.70 |
| CHEMBL5425025 | — | IC50 | = | 19952.62 | nM | 4.70 |
| CHEMBL5414446 | — | IC50 | = | 20417.38 | nM | 4.69 |
| CHEMBL5397274 | — | IC50 | = | 22387.21 | nM | 4.65 |
| CHEMBL5413754 | — | IC50 | = | 24547.09 | nM | 4.61 |
| CHEMBL5416743 | — | IC50 | = | 26915.35 | nM | 4.57 |
| CHEMBL5397616 | — | IC50 | = | 31622.78 | nM | 4.50 |