Assay Detail
Binding
CHEMBL4027504
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Inhibition of [3H]DA uptake at wild type human DAT expressed in African green monkey COS7 cells after 5 mins by beta scintillation counting method
11
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent dopamine transporter (CHEMBL238) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure-Activity Relationship Studies on a Series of 3α-[Bis(4-fluorophenyl)methoxy]tropanes and 3α-[Bis(4-fluorophenyl)methylamino]tropanes As Novel Atypical Dopamine Transporter (DAT) Inhibitors for the Treatment of Cocaine Use Disorders.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 6.91 | 8.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL328415 | — | — | 1 | 8.01 |
| CHEMBL322385 | — | — | 1 | 7.80 |
| CHEMBL4090416 | — | — | 1 | 7.40 |
| CHEMBL4062435 | — | — | 1 | 7.33 |
| CHEMBL371932 | — | — | 1 | 7.21 |
| CHEMBL429015 | — | — | 1 | 6.88 |
| CHEMBL11493 | — | — | 1 | 6.79 |
| CHEMBL4074774 | — | — | 2 | 6.67 |
| CHEMBL4085107 | — | — | 1 | 6.03 |
| CHEMBL4063478 | — | — | 1 | 5.98 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL328415 | — | Ki | = | 9.7 | nM | 8.01 |
| CHEMBL322385 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL4090416 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL4062435 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL371932 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL429015 | — | Ki | = | 133.0 | nM | 6.88 |
| CHEMBL11493 | — | Ki | = | 161.0 | nM | 6.79 |
| CHEMBL4074774 | — | Ki | = | 212.0 | nM | 6.67 |
| CHEMBL4085107 | — | Ki | = | 944.0 | nM | 6.03 |
| CHEMBL4063478 | — | Ki | = | 1050.0 | nM | 5.98 |
| CHEMBL4074774 | — | Ki | = | 1300.0 | nM | 5.89 |