Assay Detail
Functional
CHEMBL783619
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Ability to inhibit high-affinity uptake of [3H]DA into striatal nerve endings (synaptosomes)
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
Publication
Effects of two-carbon bridge region methoxylation of benztropine: discovery of novel chiral ligands for the dopamine transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 6.50 | 6.98 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL424565 | — | — | 1 | 6.98 |
| CHEMBL355286 | — | — | 1 | 6.78 |
| CHEMBL168814 | — | — | 1 | 6.75 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.68 |
| CHEMBL1201203 | BENZTROPINE | 4.0 | 1 | 6.39 |
| CHEMBL168371 | — | — | 1 | 6.29 |
| CHEMBL355258 | — | — | 1 | 5.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL424565 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL355286 | — | IC50 | = | 165.0 | nM | 6.78 |
| CHEMBL168814 | — | IC50 | = | 179.0 | nM | 6.75 |
| CHEMBL370805 | COCAINE | IC50 | = | 208.0 | nM | 6.68 |
| CHEMBL1201203 | BENZTROPINE | IC50 | = | 403.0 | nM | 6.39 |
| CHEMBL168371 | — | IC50 | = | 519.0 | nM | 6.29 |
| CHEMBL355258 | — | IC50 | = | 2280.0 | nM | 5.64 |