Assay Detail
Binding
CHEMBL4009966
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Activity at SERT in rat synaptosomes assessed as release of [3H]HT after 5 mins by liquid scintillation counting method
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent serotonin transporter (CHEMBL313) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
The 2014 Philip S. Portoghese Medicinal Chemistry Lectureship: The "Phenylalkylaminome" with a Focus on Selected Drugs of Abuse.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 13 | 6.82 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3330645 | — | — | 1 | 7.70 |
| CHEMBL4104749 | — | — | 1 | 7.39 |
| CHEMBL3330646 | — | — | 1 | 7.17 |
| CHEMBL43048 | MIDOMAFETAMINE | 3.0 | 1 | 7.14 |
| CHEMBL195390 | — | — | 1 | 7.13 |
| CHEMBL1788307 | — | — | 1 | 7.00 |
| CHEMBL87493 | FENFLURAMINE | 4.0 | 1 | 6.97 |
| CHEMBL4086874 | — | — | 1 | 6.87 |
| CHEMBL6731 | TENAMFETAMINE | 2.0 | 1 | 6.80 |
| CHEMBL1927025 | — | — | 1 | 6.51 |
| CHEMBL382757 | — | — | 1 | 6.47 |
| CHEMBL612 | DEXTROAMPHETAMINE | 4.0 | 1 | 5.75 |
| CHEMBL4084187 | — | — | 1 | 5.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3330645 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4104749 | — | EC50 | = | 41.0 | nM | 7.39 |
| CHEMBL3330646 | — | EC50 | = | 68.0 | nM | 7.17 |
| CHEMBL43048 | MIDOMAFETAMINE | EC50 | = | 72.0 | nM | 7.14 |
| CHEMBL195390 | — | EC50 | = | 74.0 | nM | 7.13 |
| CHEMBL1788307 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL87493 | FENFLURAMINE | EC50 | = | 108.0 | nM | 6.97 |
| CHEMBL4086874 | — | EC50 | = | 134.0 | nM | 6.87 |
| CHEMBL6731 | TENAMFETAMINE | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL1927025 | — | EC50 | = | 310.0 | nM | 6.51 |
| CHEMBL382757 | — | EC50 | = | 340.0 | nM | 6.47 |
| CHEMBL612 | DEXTROAMPHETAMINE | EC50 | = | 1765.0 | nM | 5.75 |
| CHEMBL4084187 | — | EC50 | = | 1772.0 | nM | 5.75 |