Assay Detail
Binding
CHEMBL672587
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50% Inhibition against dopamine transporter (DAT) in rat striatal tissue by displacing [3H]WIN-35428 radioligand
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Striatum |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and transporter binding properties of 3beta-[4'-(phenylalkyl, -phenylalkenyl, and -phenylalkynyl)phenyl]tropane-2beta-carboxylic acid methyl esters: evidence of a remote phenyl binding domain on the dopamine transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 7.89 | 9.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2310867 | — | — | 1 | 9.29 |
| CHEMBL2310874 | — | — | 1 | 8.96 |
| CHEMBL3350431 | — | — | 1 | 8.92 |
| CHEMBL2310868 | — | — | 1 | 8.91 |
| CHEMBL2373962 | — | — | 1 | 8.77 |
| CHEMBL2310871 | — | — | 1 | 8.74 |
| CHEMBL2310869 | — | — | 1 | 8.62 |
| CHEMBL2310883 | — | — | 1 | 8.51 |
| CHEMBL2310872 | — | — | 1 | 8.43 |
| CHEMBL2310877 | — | — | 1 | 8.29 |
| CHEMBL84680 | — | — | 1 | 8.29 |
| CHEMBL2310884 | — | — | 1 | 8.28 |
| CHEMBL2310873 | — | — | 1 | 8.20 |
| CHEMBL2310882 | — | — | 1 | 7.93 |
| CHEMBL2310876 | — | — | 1 | 7.81 |
| CHEMBL2310881 | — | — | 1 | 7.80 |
| CHEMBL1790051 | — | — | 1 | 7.64 |
| CHEMBL50157 | — | — | 1 | 7.26 |
| CHEMBL2310870 | — | — | 1 | 7.24 |
| CHEMBL2310866 | — | — | 1 | 7.16 |
| CHEMBL2310865 | — | — | 1 | 6.64 |
| CHEMBL2310875 | — | — | 1 | 6.52 |
| CHEMBL2310878 | — | — | 1 | 6.46 |
| CHEMBL2310879 | — | — | 1 | 6.32 |
| CHEMBL2310880 | — | — | 1 | 6.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2310867 | — | IC50 | = | 0.51 | nM | 9.29 |
| CHEMBL2310874 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3350431 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL2310868 | — | IC50 | = | 1.24 | nM | 8.91 |
| CHEMBL2373962 | — | IC50 | = | 1.71 | nM | 8.77 |
| CHEMBL2310871 | — | IC50 | = | 1.82 | nM | 8.74 |
| CHEMBL2310869 | — | IC50 | = | 2.37 | nM | 8.62 |
| CHEMBL2310883 | — | IC50 | = | 3.09 | nM | 8.51 |
| CHEMBL2310872 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL2310877 | — | IC50 | = | 5.14 | nM | 8.29 |
| CHEMBL84680 | — | IC50 | = | 5.17 | nM | 8.29 |
| CHEMBL2310884 | — | IC50 | = | 5.29 | nM | 8.28 |
| CHEMBL2310873 | — | IC50 | = | 6.28 | nM | 8.20 |
| CHEMBL2310882 | — | IC50 | = | 11.7 | nM | 7.93 |
| CHEMBL2310876 | — | IC50 | = | 15.6 | nM | 7.81 |
| CHEMBL2310881 | — | IC50 | = | 15.8 | nM | 7.80 |
| CHEMBL1790051 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL50157 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL2310870 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL2310866 | — | IC50 | = | 68.5 | nM | 7.16 |
| CHEMBL2310865 | — | IC50 | = | 228.0 | nM | 6.64 |
| CHEMBL2310875 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL2310878 | — | IC50 | = | 351.0 | nM | 6.46 |
| CHEMBL2310879 | — | IC50 | = | 474.0 | nM | 6.32 |
| CHEMBL2310880 | — | IC50 | = | 526.0 | nM | 6.28 |