Assay Detail
Binding
CHEMBL3860689
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Inhibition of [3H]choline uptake at human choline transporter expressed in HEK293 cells preincubated for 15 mins followed by [3H]choline addition measured after 10 to 15 mins by scintillation proximity assay
7
Total Activities
7
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
Optimization of the choline transporter (CHT) inhibitor ML352: Development of VU6001221, an improved in vivo tool compound.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 6.24 | 7.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3304438 | — | — | 1 | 7.14 |
| CHEMBL3933906 | — | — | 1 | 6.57 |
| CHEMBL3899143 | — | — | 1 | 6.33 |
| CHEMBL3959257 | — | — | 1 | 6.19 |
| CHEMBL3923550 | — | — | 1 | 5.74 |
| CHEMBL3970338 | — | — | 1 | 5.47 |
| CHEMBL3905894 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3304438 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL3933906 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL3899143 | — | IC50 | = | 467.0 | nM | 6.33 |
| CHEMBL3959257 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL3923550 | — | IC50 | = | 1840.0 | nM | 5.74 |
| CHEMBL3970338 | — | IC50 | = | 3350.0 | nM | 5.47 |
| CHEMBL3905894 | — | IC50 | > | 10000.0 | nM | - |