Assay Detail
Binding
CHEMBL829502
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Inhibition of [3H]WIN-35428 binding to dopamine transporter of rat striatum
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Striatum |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Further structurally constrained analogues of cis-(6-benzhydrylpiperidin-3-yl)benzylamine with elucidation of bioactive conformation: discovery of 1,4-diazabicyclo[3.3.1]nonane derivatives and evaluation of their biological properties for the monoamine transporters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 6.77 | 7.97 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL543876 | — | — | 1 | 7.97 |
| CHEMBL189082 | — | — | 1 | 7.95 |
| CHEMBL39262 | — | — | 1 | 7.71 |
| CHEMBL408192 | — | — | 1 | 7.65 |
| CHEMBL40607 | — | — | 1 | 7.47 |
| CHEMBL188363 | — | — | 1 | 7.32 |
| CHEMBL280518 | — | — | 1 | 7.16 |
| CHEMBL189084 | — | — | 1 | 7.09 |
| CHEMBL185803 | — | — | 1 | 6.96 |
| CHEMBL361268 | — | — | 1 | 6.68 |
| CHEMBL189805 | — | — | 1 | 6.67 |
| CHEMBL188953 | — | — | 1 | 6.65 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.58 |
| CHEMBL189095 | — | — | 1 | 6.51 |
| CHEMBL2096807 | — | — | 1 | 6.48 |
| CHEMBL187429 | — | — | 1 | 6.43 |
| CHEMBL436084 | — | — | 1 | 6.25 |
| CHEMBL364561 | — | — | 1 | 6.24 |
| CHEMBL186918 | — | — | 1 | 6.02 |
| CHEMBL187142 | — | — | 1 | 5.91 |
| CHEMBL189713 | — | — | 1 | 5.85 |
| CHEMBL362707 | — | — | 1 | 5.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL543876 | — | IC50 | = | 10.6 | nM | 7.97 |
| CHEMBL189082 | — | IC50 | = | 11.2 | nM | 7.95 |
| CHEMBL39262 | — | IC50 | = | 19.7 | nM | 7.71 |
| CHEMBL408192 | — | IC50 | = | 22.5 | nM | 7.65 |
| CHEMBL40607 | — | IC50 | = | 33.8 | nM | 7.47 |
| CHEMBL188363 | — | IC50 | = | 47.5 | nM | 7.32 |
| CHEMBL280518 | — | IC50 | = | 68.9 | nM | 7.16 |
| CHEMBL189084 | — | IC50 | = | 81.2 | nM | 7.09 |
| CHEMBL185803 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL361268 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL189805 | — | IC50 | = | 215.0 | nM | 6.67 |
| CHEMBL188953 | — | IC50 | = | 225.0 | nM | 6.65 |
| CHEMBL370805 | COCAINE | IC50 | = | 266.0 | nM | 6.58 |
| CHEMBL189095 | — | IC50 | = | 308.0 | nM | 6.51 |
| CHEMBL2096807 | — | IC50 | = | 329.0 | nM | 6.48 |
| CHEMBL187429 | — | IC50 | = | 371.0 | nM | 6.43 |
| CHEMBL436084 | — | IC50 | = | 565.0 | nM | 6.25 |
| CHEMBL364561 | — | IC50 | = | 581.0 | nM | 6.24 |
| CHEMBL186918 | — | IC50 | = | 958.0 | nM | 6.02 |
| CHEMBL187142 | — | IC50 | = | 1240.0 | nM | 5.91 |
| CHEMBL189713 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL362707 | — | IC50 | = | 4710.0 | nM | 5.33 |