Assay Detail
Binding
CHEMBL671632
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory concentration required to inhibit dopamine transporter DAT was determined by using [3H]WIN-35428 radioligand
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous 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 behavioral pharmacology of a series of 3beta-(substituted phenyl)-2beta-(3'-substituted isoxazol-5-yl)tropanes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 8.47 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL103227 | — | — | 1 | 9.30 |
| CHEMBL316528 | — | — | 1 | 9.23 |
| CHEMBL103523 | — | — | 1 | 9.11 |
| CHEMBL103228 | — | — | 1 | 9.03 |
| CHEMBL321780 | — | — | 1 | 8.92 |
| CHEMBL298580 | — | — | 1 | 8.89 |
| CHEMBL317905 | — | — | 1 | 8.86 |
| CHEMBL320627 | — | — | 1 | 8.80 |
| CHEMBL316585 | — | — | 1 | 8.80 |
| CHEMBL317904 | — | — | 1 | 8.79 |
| CHEMBL329517 | — | — | 1 | 8.73 |
| CHEMBL14144 | — | — | 1 | 8.70 |
| CHEMBL322856 | — | — | 1 | 8.41 |
| CHEMBL322385 | — | — | 1 | 8.39 |
| CHEMBL322400 | — | — | 1 | 8.35 |
| CHEMBL103223 | — | — | 1 | 8.19 |
| CHEMBL321806 | — | — | 1 | 8.19 |
| CHEMBL102279 | — | — | 1 | 8.19 |
| CHEMBL100652 | — | — | 1 | 8.14 |
| CHEMBL328415 | — | — | 1 | 8.06 |
| CHEMBL103867 | — | — | 1 | 7.89 |
| CHEMBL1790051 | — | — | 1 | 7.64 |
| CHEMBL317909 | — | — | 1 | 7.58 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 7.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL103227 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL316528 | — | IC50 | = | 0.59 | nM | 9.23 |
| CHEMBL103523 | — | IC50 | = | 0.77 | nM | 9.11 |
| CHEMBL103228 | — | IC50 | = | 0.93 | nM | 9.03 |
| CHEMBL321780 | — | IC50 | = | 1.19 | nM | 8.92 |
| CHEMBL298580 | — | IC50 | = | 1.28 | nM | 8.89 |
| CHEMBL317905 | — | IC50 | = | 1.37 | nM | 8.86 |
| CHEMBL320627 | — | IC50 | = | 1.57 | nM | 8.80 |
| CHEMBL316585 | — | IC50 | = | 1.58 | nM | 8.80 |
| CHEMBL317904 | — | IC50 | = | 1.62 | nM | 8.79 |
| CHEMBL329517 | — | IC50 | = | 1.86 | nM | 8.73 |
| CHEMBL14144 | — | IC50 | = | 1.98 | nM | 8.70 |
| CHEMBL322856 | — | IC50 | = | 3.93 | nM | 8.41 |
| CHEMBL322385 | — | IC50 | = | 4.09 | nM | 8.39 |
| CHEMBL322400 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL103223 | — | IC50 | = | 6.42 | nM | 8.19 |
| CHEMBL321806 | — | IC50 | = | 6.45 | nM | 8.19 |
| CHEMBL102279 | — | IC50 | = | 6.45 | nM | 8.19 |
| CHEMBL100652 | — | IC50 | = | 7.31 | nM | 8.14 |
| CHEMBL328415 | — | IC50 | = | 8.74 | nM | 8.06 |
| CHEMBL103867 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1790051 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL317909 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL370805 | COCAINE | IC50 | = | 89.1 | nM | 7.05 |