Assay Detail
Binding
CHEMBL809434
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Ability to inhibit reuptake of serotonin ([3H]5-HT) at serotonin transporter of rat midbrian
26
Total Activities
26
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 serotonin transporter (CHEMBL313) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and pharmacological evaluation of (Z)-9-(heteroarylmethylene)-7-azatricyclo[4.3.1.0(3,7)]decanes: thiophene analogues as potent norepinephrine transporter inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 26 | 6.46 | 8.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL116369 | — | — | 1 | 8.17 |
| CHEMBL119477 | — | — | 1 | 7.54 |
| CHEMBL331425 | — | — | 1 | 7.44 |
| CHEMBL116431 | — | — | 1 | 7.32 |
| CHEMBL118261 | — | — | 1 | 7.28 |
| CHEMBL325404 | — | — | 1 | 7.15 |
| CHEMBL641 | ATOMOXETINE | 4.0 | 1 | 7.11 |
| CHEMBL331639 | — | — | 1 | 7.03 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.81 |
| CHEMBL72 | DESIPRAMINE | 4.0 | 1 | 6.79 |
| CHEMBL117047 | — | — | 1 | 6.75 |
| CHEMBL324031 | — | — | 1 | 6.57 |
| CHEMBL118530 | — | — | 1 | 6.46 |
| CHEMBL440332 | — | — | 1 | 6.32 |
| CHEMBL119137 | — | — | 1 | 6.28 |
| CHEMBL331321 | — | — | 1 | 6.26 |
| CHEMBL118853 | — | — | 1 | 6.18 |
| CHEMBL443281 | — | — | 1 | 6.09 |
| CHEMBL331565 | — | — | 1 | 5.69 |
| CHEMBL118725 | — | — | 1 | 5.50 |
| CHEMBL333912 | — | — | 1 | 5.50 |
| CHEMBL334027 | — | — | 1 | 5.48 |
| CHEMBL331780 | — | — | 1 | 5.34 |
| CHEMBL118500 | — | — | 1 | 5.29 |
| CHEMBL116374 | — | — | 1 | 5.15 |
| CHEMBL119706 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL116369 | — | Ki | = | 6.75 | nM | 8.17 |
| CHEMBL119477 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL331425 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL116431 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL118261 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL325404 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL641 | ATOMOXETINE | Ki | = | 77.0 | nM | 7.11 |
| CHEMBL331639 | — | Ki | = | 93.0 | nM | 7.03 |
| CHEMBL370805 | COCAINE | Ki | = | 155.0 | nM | 6.81 |
| CHEMBL72 | DESIPRAMINE | Ki | = | 163.0 | nM | 6.79 |
| CHEMBL117047 | — | Ki | = | 179.0 | nM | 6.75 |
| CHEMBL324031 | — | Ki | = | 269.0 | nM | 6.57 |
| CHEMBL118530 | — | Ki | = | 346.0 | nM | 6.46 |
| CHEMBL440332 | — | Ki | = | 477.0 | nM | 6.32 |
| CHEMBL119137 | — | Ki | = | 531.0 | nM | 6.28 |
| CHEMBL331321 | — | Ki | = | 544.0 | nM | 6.26 |
| CHEMBL118853 | — | Ki | = | 665.0 | nM | 6.18 |
| CHEMBL443281 | — | Ki | = | 810.0 | nM | 6.09 |
| CHEMBL331565 | — | Ki | = | 2050.0 | nM | 5.69 |
| CHEMBL118725 | — | Ki | = | 3150.0 | nM | 5.50 |
| CHEMBL333912 | — | Ki | = | 3140.0 | nM | 5.50 |
| CHEMBL334027 | — | Ki | = | 3320.0 | nM | 5.48 |
| CHEMBL331780 | — | Ki | = | 4580.0 | nM | 5.34 |
| CHEMBL118500 | — | Ki | = | 5140.0 | nM | 5.29 |
| CHEMBL116374 | — | Ki | = | 7140.0 | nM | 5.15 |
| CHEMBL119706 | — | Ki | > | 10000.0 | nM | - |