Assay Detail
Binding
CHEMBL4027495
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Inhibition of [3H]WIN5428 uptake at human DAT Y56F mutant expressed in African green monkey COS7 cells after 90 mins
11
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
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 | 6.37 | 7.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4062435 | — | — | 1 | 7.20 |
| CHEMBL322385 | — | — | 1 | 6.85 |
| CHEMBL4074774 | — | — | 2 | 6.74 |
| CHEMBL4090416 | — | — | 1 | 6.70 |
| CHEMBL328415 | — | — | 1 | 6.62 |
| CHEMBL429015 | — | — | 1 | 6.51 |
| CHEMBL371932 | — | — | 1 | 6.45 |
| CHEMBL4085107 | — | — | 1 | 5.97 |
| CHEMBL4063478 | — | — | 1 | 5.81 |
| CHEMBL199103 | — | — | 1 | 5.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4062435 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL322385 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL4074774 | — | Ki | = | 183.0 | nM | 6.74 |
| CHEMBL4090416 | — | Ki | = | 202.0 | nM | 6.70 |
| CHEMBL328415 | — | Ki | = | 242.0 | nM | 6.62 |
| CHEMBL429015 | — | Ki | = | 307.0 | nM | 6.51 |
| CHEMBL371932 | — | Ki | = | 355.0 | nM | 6.45 |
| CHEMBL4085107 | — | Ki | = | 1080.0 | nM | 5.97 |
| CHEMBL4063478 | — | Ki | = | 1560.0 | nM | 5.81 |
| CHEMBL199103 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL4074774 | — | Ki | = | 3490.0 | nM | 5.46 |