Assay Detail
Binding
CHEMBL890737
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Displacement of [3H]WIN-35428 from DAT in Sprague-Dawley rat brain
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis, monoamine transporter binding, properties, and functional monoamine uptake activity of 3beta-[4-methylphenyl and 4-chlorophenyl]-2 beta-[5-(substituted phenyl)thiazol-2-yl]tropanes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 7.64 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL226984 | — | — | 1 | 8.40 |
| CHEMBL388760 | — | — | 1 | 8.30 |
| CHEMBL227179 | — | — | 1 | 8.24 |
| CHEMBL390743 | — | — | 1 | 8.22 |
| CHEMBL436132 | — | — | 1 | 8.00 |
| CHEMBL229699 | — | — | 1 | 7.92 |
| CHEMBL227233 | — | — | 1 | 7.85 |
| CHEMBL226933 | — | — | 1 | 7.82 |
| CHEMBL227231 | — | — | 1 | 7.75 |
| CHEMBL227180 | — | — | 1 | 7.70 |
| CHEMBL227232 | — | — | 1 | 7.70 |
| CHEMBL229381 | — | — | 1 | 7.66 |
| CHEMBL390742 | TROPARIL | — | 1 | 7.64 |
| CHEMBL229436 | — | — | 1 | 7.39 |
| CHEMBL388832 | — | — | 1 | 7.19 |
| CHEMBL2113279 | — | — | 1 | 7.08 |
| CHEMBL376113 | — | — | 1 | 6.99 |
| CHEMBL388759 | — | — | 1 | 6.97 |
| CHEMBL388612 | — | — | 1 | 6.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL226984 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL388760 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL227179 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL390743 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL436132 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL229699 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL227233 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL226933 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL227231 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL227180 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL227232 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL229381 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL390742 | TROPARIL | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL229436 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL388832 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL2113279 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL376113 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL388759 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL388612 | — | IC50 | = | 440.0 | nM | 6.36 |