Assay Detail
Binding
CHEMBL3404113
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human CHT Leu530Ala and Val531Ala mutant expressed in HEK293 cells assessed as remaining transporter activity in presence of 100 nM [3H]choline by [3H]choline uptake assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and structure-activity relationships of a series of 4-methoxy-3-(piperidin-4-yl)oxy benzamides as novel inhibitors of the presynaptic choline transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 5.68 | 6.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1872483 | — | — | 1 | 6.62 |
| CHEMBL3304438 | — | — | 1 | 6.57 |
| CHEMBL3303792 | — | — | 1 | 6.12 |
| CHEMBL3303292 | — | — | 1 | 5.90 |
| CHEMBL3182315 | — | — | 1 | 5.80 |
| CHEMBL3183447 | — | — | 1 | 5.67 |
| CHEMBL3187862 | — | — | 1 | 5.46 |
| CHEMBL3188567 | — | — | 1 | 5.38 |
| CHEMBL3187348 | — | — | 1 | 5.31 |
| CHEMBL3303803 | — | — | 1 | 5.21 |
| CHEMBL3186365 | — | — | 1 | 5.09 |
| CHEMBL3183383 | — | — | 1 | 5.03 |
| CHEMBL3183609 | — | — | 1 | - |
| CHEMBL3401758 | — | — | 1 | - |
| CHEMBL3301712 | — | — | 1 | - |
| CHEMBL3301821 | — | — | 1 | - |
| CHEMBL3187345 | — | — | 1 | - |
| CHEMBL3188740 | — | — | 1 | - |
| CHEMBL3304288 | — | — | 1 | - |
| CHEMBL3184436 | — | — | 1 | - |
| CHEMBL1878664 | — | — | 1 | - |
| CHEMBL3184012 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1872483 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL3304438 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL3303792 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL3303292 | — | IC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL3182315 | — | IC50 | = | 1580.0 | nM | 5.80 |
| CHEMBL3183447 | — | IC50 | = | 2130.0 | nM | 5.67 |
| CHEMBL3187862 | — | IC50 | = | 3480.0 | nM | 5.46 |
| CHEMBL3188567 | — | IC50 | = | 4120.0 | nM | 5.38 |
| CHEMBL3187348 | — | IC50 | = | 4930.0 | nM | 5.31 |
| CHEMBL3303803 | — | IC50 | = | 6120.0 | nM | 5.21 |
| CHEMBL3186365 | — | IC50 | = | 8090.0 | nM | 5.09 |
| CHEMBL3183383 | — | IC50 | = | 9270.0 | nM | 5.03 |
| CHEMBL3183609 | — | IC50 | - | — | - | |
| CHEMBL3401758 | — | IC50 | - | — | - | |
| CHEMBL3301712 | — | IC50 | - | — | - | |
| CHEMBL3301821 | — | IC50 | - | — | - | |
| CHEMBL3187345 | — | IC50 | - | — | - | |
| CHEMBL3188740 | — | IC50 | - | — | - | |
| CHEMBL3304288 | — | IC50 | - | — | - | |
| CHEMBL3184436 | — | IC50 | - | — | - | |
| CHEMBL1878664 | — | IC50 | - | — | - | |
| CHEMBL3184012 | — | IC50 | - | — | - |