Assay Detail
Functional
CHEMBL825142
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Inhibition of [3H]dopamine uptake into rat striatal synaptosomes
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Synaptosomes |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and pharmacology of 6-substituted benztropines: discovery of novel dopamine uptake inhibitors possessing low binding affinity to the dopamine transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 6.81 | 8.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL425008 | — | — | 1 | 8.09 |
| CHEMBL425907 | — | — | 1 | 7.91 |
| CHEMBL192317 | — | — | 1 | 7.41 |
| CHEMBL365397 | — | — | 1 | 7.10 |
| CHEMBL541630 | — | — | 1 | 6.98 |
| CHEMBL534927 | — | — | 1 | 6.86 |
| CHEMBL191722 | — | — | 1 | 6.83 |
| CHEMBL365353 | — | — | 1 | 6.79 |
| CHEMBL2113366 | — | — | 1 | 6.78 |
| CHEMBL558788 | — | — | 1 | 6.75 |
| CHEMBL192672 | — | — | 1 | 6.71 |
| CHEMBL192040 | — | — | 1 | 6.70 |
| CHEMBL2113360 | — | — | 1 | 6.62 |
| CHEMBL189989 | — | — | 1 | 6.46 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.45 |
| CHEMBL1201203 | BENZTROPINE | 4.0 | 1 | 6.39 |
| CHEMBL361277 | — | — | 1 | 6.31 |
| CHEMBL2113359 | — | — | 1 | 6.29 |
| CHEMBL363814 | — | — | 1 | 5.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL425008 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL425907 | — | IC50 | = | 12.4 | nM | 7.91 |
| CHEMBL192317 | — | IC50 | = | 39.1 | nM | 7.41 |
| CHEMBL365397 | — | IC50 | = | 79.7 | nM | 7.10 |
| CHEMBL541630 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL534927 | — | IC50 | = | 138.8 | nM | 6.86 |
| CHEMBL191722 | — | IC50 | = | 149.4 | nM | 6.83 |
| CHEMBL365353 | — | IC50 | = | 162.3 | nM | 6.79 |
| CHEMBL2113366 | — | IC50 | = | 165.0 | nM | 6.78 |
| CHEMBL558788 | — | IC50 | = | 179.0 | nM | 6.75 |
| CHEMBL192672 | — | IC50 | = | 193.7 | nM | 6.71 |
| CHEMBL192040 | — | IC50 | = | 199.0 | nM | 6.70 |
| CHEMBL2113360 | — | IC50 | = | 239.7 | nM | 6.62 |
| CHEMBL189989 | — | IC50 | = | 347.0 | nM | 6.46 |
| CHEMBL370805 | COCAINE | IC50 | = | 353.1 | nM | 6.45 |
| CHEMBL1201203 | BENZTROPINE | IC50 | = | 403.0 | nM | 6.39 |
| CHEMBL361277 | — | IC50 | = | 490.9 | nM | 6.31 |
| CHEMBL2113359 | — | IC50 | = | 519.0 | nM | 6.29 |
| CHEMBL363814 | — | IC50 | = | 1083.7 | nM | 5.96 |