Assay Detail
Binding
CHEMBL4711022
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]citalopram from SERT in Sprague-Dawley rat midbrain membranes incubated for 60 mins by microbeta scintillation counting method
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Midbrain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent serotonin transporter (CHEMBL313) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Structure-activity relationships for a series of (Bis(4-fluorophenyl)methyl)sulfinylethyl-aminopiperidines and -piperidine amines at the dopamine transporter: Bioisosteric replacement of the piperazine improves metabolic stability.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 43 | 5.77 | 7.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4798638 | — | — | 1 | 7.17 |
| CHEMBL4795634 | — | — | 1 | 7.01 |
| CHEMBL4750607 | — | — | 1 | 6.89 |
| CHEMBL4748901 | — | — | 1 | 6.84 |
| CHEMBL4788854 | — | — | 1 | 6.57 |
| CHEMBL4794406 | — | — | 1 | 6.56 |
| CHEMBL4744824 | — | — | 1 | 6.55 |
| CHEMBL4791063 | — | — | 1 | 6.53 |
| CHEMBL4747413 | — | — | 1 | 6.48 |
| CHEMBL4795981 | — | — | 1 | 6.46 |
| CHEMBL4785770 | — | — | 1 | 6.45 |
| CHEMBL4750660 | — | — | 1 | 6.43 |
| CHEMBL4750997 | — | — | 1 | 6.40 |
| CHEMBL4788794 | — | — | 1 | 6.39 |
| CHEMBL4741279 | — | — | 1 | 6.31 |
| CHEMBL4758774 | — | — | 1 | 6.22 |
| CHEMBL4762414 | — | — | 1 | 6.16 |
| CHEMBL4742033 | — | — | 1 | 6.03 |
| CHEMBL4783618 | — | — | 1 | 6.02 |
| CHEMBL4765081 | — | — | 1 | 6.00 |
| CHEMBL4742866 | — | — | 1 | 6.00 |
| CHEMBL4784393 | — | — | 1 | 6.00 |
| CHEMBL4784884 | — | — | 1 | 5.98 |
| CHEMBL4781767 | — | — | 1 | 5.80 |
| CHEMBL4744739 | — | — | 1 | 5.79 |
| CHEMBL4746636 | — | — | 1 | 5.76 |
| CHEMBL4758124 | — | — | 1 | 5.61 |
| CHEMBL4782055 | — | — | 1 | 5.34 |
| CHEMBL4777080 | — | — | 1 | 5.33 |
| CHEMBL3916231 | — | — | 1 | 5.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4798638 | — | Ki | = | 66.8 | nM | 7.17 |
| CHEMBL4795634 | — | Ki | = | 97.0 | nM | 7.01 |
| CHEMBL4750607 | — | Ki | = | 129.0 | nM | 6.89 |
| CHEMBL4748901 | — | Ki | = | 144.0 | nM | 6.84 |
| CHEMBL4788854 | — | Ki | = | 268.0 | nM | 6.57 |
| CHEMBL4794406 | — | Ki | = | 278.0 | nM | 6.56 |
| CHEMBL4744824 | — | Ki | = | 283.0 | nM | 6.55 |
| CHEMBL4791063 | — | Ki | = | 296.0 | nM | 6.53 |
| CHEMBL4747413 | — | Ki | = | 331.0 | nM | 6.48 |
| CHEMBL4795981 | — | Ki | = | 351.0 | nM | 6.46 |
| CHEMBL4785770 | — | Ki | = | 358.0 | nM | 6.45 |
| CHEMBL4750660 | — | Ki | = | 373.0 | nM | 6.43 |
| CHEMBL4750997 | — | Ki | = | 397.0 | nM | 6.40 |
| CHEMBL4788794 | — | Ki | = | 409.0 | nM | 6.39 |
| CHEMBL4741279 | — | Ki | = | 489.0 | nM | 6.31 |
| CHEMBL4758774 | — | Ki | = | 599.0 | nM | 6.22 |
| CHEMBL4762414 | — | Ki | = | 695.0 | nM | 6.16 |
| CHEMBL4742033 | — | Ki | = | 944.0 | nM | 6.03 |
| CHEMBL4783618 | — | Ki | = | 947.0 | nM | 6.02 |
| CHEMBL4784393 | — | Ki | = | 992.0 | nM | 6.00 |
| CHEMBL4765081 | — | Ki | = | 1010.0 | nM | 6.00 |
| CHEMBL4742866 | — | Ki | = | 1010.0 | nM | 6.00 |
| CHEMBL4784884 | — | Ki | = | 1050.0 | nM | 5.98 |
| CHEMBL4781767 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL4744739 | — | Ki | = | 1630.0 | nM | 5.79 |
| CHEMBL4746636 | — | Ki | = | 1730.0 | nM | 5.76 |
| CHEMBL4758124 | — | Ki | = | 2440.0 | nM | 5.61 |
| CHEMBL4782055 | — | Ki | = | 4610.0 | nM | 5.34 |
| CHEMBL4777080 | — | Ki | = | 4640.0 | nM | 5.33 |
| CHEMBL3916231 | — | Ki | = | 6800.0 | nM | 5.17 |
| CHEMBL4764168 | — | Ki | = | 6990.0 | nM | 5.16 |
| CHEMBL4757505 | — | Ki | = | 7780.0 | nM | 5.11 |
| CHEMBL3918282 | — | Ki | = | 12700.0 | nM | 4.90 |
| CHEMBL4747068 | — | Ki | = | 14200.0 | nM | 4.85 |
| CHEMBL4636778 | — | Ki | = | 14800.0 | nM | 4.83 |
| CHEMBL4744200 | — | Ki | = | 15000.0 | nM | 4.82 |
| CHEMBL4789139 | — | Ki | = | 16300.0 | nM | 4.79 |
| CHEMBL4756427 | — | Ki | = | 32000.0 | nM | 4.50 |
| CHEMBL1373 | MODAFINIL | Ki | = | 31300.0 | nM | 4.50 |
| CHEMBL4785024 | — | Ki | = | 38900.0 | nM | 4.41 |
| CHEMBL1672359 | — | Ki | = | 48700.0 | nM | 4.31 |
| CHEMBL3931765 | — | Ki | = | 97800.0 | nM | 4.01 |
| CHEMBL4762706 | — | Ki | = | 251000.0 | nM | - |