Assay Detail
Binding
CHEMBL671786
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Inhibition of [3H]WIN-35428 binding to dopamine (DA) transporter
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Secondary amine analogues of 3 beta-(4'-substituted phenyl)tropane-2 beta-carboxylic acid esters and N-norcocaine exhibit enhanced affinity for serotonin and norepinephrine transporters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 8.16 | 9.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL610894 | — | — | 1 | 9.37 |
| CHEMBL429772 | — | — | 1 | 9.21 |
| CHEMBL2112889 | — | — | 1 | 9.16 |
| CHEMBL2112877 | — | — | 1 | 8.97 |
| CHEMBL610897 | — | — | 1 | 8.95 |
| CHEMBL300226 | — | — | 1 | 8.90 |
| CHEMBL21112 | — | — | 1 | 8.36 |
| CHEMBL2079586 | — | — | 1 | 7.80 |
| CHEMBL1790051 | — | — | 1 | 7.64 |
| CHEMBL279657 | — | — | 1 | 7.51 |
| CHEMBL2112860 | — | — | 1 | 7.30 |
| CHEMBL50157 | — | — | 1 | 7.26 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 7.05 |
| CHEMBL21256 | — | — | 1 | 6.69 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL610894 | — | IC50 | = | 0.43 | nM | 9.37 |
| CHEMBL429772 | — | IC50 | = | 0.62 | nM | 9.21 |
| CHEMBL2112889 | — | IC50 | = | 0.69 | nM | 9.16 |
| CHEMBL2112877 | — | IC50 | = | 1.06 | nM | 8.97 |
| CHEMBL610897 | — | IC50 | = | 1.12 | nM | 8.95 |
| CHEMBL300226 | — | IC50 | = | 1.26 | nM | 8.90 |
| CHEMBL21112 | — | IC50 | = | 4.39 | nM | 8.36 |
| CHEMBL2079586 | — | IC50 | = | 15.7 | nM | 7.80 |
| CHEMBL1790051 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL279657 | — | IC50 | = | 30.8 | nM | 7.51 |
| CHEMBL2112860 | — | IC50 | = | 49.9 | nM | 7.30 |
| CHEMBL50157 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL370805 | COCAINE | IC50 | = | 89.1 | nM | 7.05 |
| CHEMBL21256 | — | IC50 | = | 206.0 | nM | 6.69 |