Assay Detail
Binding
CHEMBL3385967
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human DAT expressed in HEK293 cells at incubated for 15 mins by neurotransmitter reuptake assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent dopamine transporter (CHEMBL238) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Exploration of 3-Aminoazetidines as Triple Reuptake Inhibitors by Bioisosteric Modification of 3-α-Oxyazetidine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 6.24 | 6.93 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3331502 | — | — | 1 | 6.93 |
| CHEMBL3331498 | — | — | 1 | 6.82 |
| CHEMBL3331500 | — | — | 1 | 6.73 |
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 6.72 |
| CHEMBL3331484 | — | — | 1 | 6.58 |
| CHEMBL3331501 | — | — | 1 | 6.49 |
| CHEMBL3331503 | — | — | 1 | 6.48 |
| CHEMBL3331507 | — | — | 1 | 6.41 |
| CHEMBL3331505 | — | — | 1 | 6.39 |
| CHEMBL3331506 | — | — | 1 | 6.38 |
| CHEMBL3331508 | — | — | 1 | 6.36 |
| CHEMBL3331468 | — | — | 1 | 6.30 |
| CHEMBL3331486 | — | — | 1 | 6.27 |
| CHEMBL3331504 | — | — | 1 | 6.27 |
| CHEMBL3331485 | — | — | 1 | 6.17 |
| CHEMBL3331469 | — | — | 1 | 6.17 |
| CHEMBL3331479 | — | — | 1 | 6.16 |
| CHEMBL1175 | DULOXETINE | 4.0 | 1 | 6.01 |
| CHEMBL295467 | NISOXETINE | 2.0 | 1 | 5.94 |
| CHEMBL1201066 | VENLAFAXINE HYDROCHLORIDE | 4.0 | 1 | 4.80 |
| CHEMBL41 | FLUOXETINE | 4.0 | 1 | 4.74 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3331502 | — | IC50 | = | 118.0 | nM | 6.93 |
| CHEMBL3331498 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3331500 | — | IC50 | = | 187.0 | nM | 6.73 |
| CHEMBL281594 | VANOXERINE | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3331484 | — | IC50 | = | 265.0 | nM | 6.58 |
| CHEMBL3331501 | — | IC50 | = | 327.0 | nM | 6.49 |
| CHEMBL3331503 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL3331507 | — | IC50 | = | 394.0 | nM | 6.41 |
| CHEMBL3331505 | — | IC50 | = | 406.0 | nM | 6.39 |
| CHEMBL3331506 | — | IC50 | = | 415.0 | nM | 6.38 |
| CHEMBL3331508 | — | IC50 | = | 441.0 | nM | 6.36 |
| CHEMBL3331468 | — | IC50 | = | 498.0 | nM | 6.30 |
| CHEMBL3331486 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL3331504 | — | IC50 | = | 533.0 | nM | 6.27 |
| CHEMBL3331485 | — | IC50 | = | 684.0 | nM | 6.17 |
| CHEMBL3331469 | — | IC50 | = | 678.0 | nM | 6.17 |
| CHEMBL3331479 | — | IC50 | = | 696.0 | nM | 6.16 |
| CHEMBL1175 | DULOXETINE | IC50 | = | 977.0 | nM | 6.01 |
| CHEMBL295467 | NISOXETINE | IC50 | = | 1150.0 | nM | 5.94 |
| CHEMBL1201066 | VENLAFAXINE HYDROCHLORIDE | IC50 | = | 15700.0 | nM | 4.80 |
| CHEMBL41 | FLUOXETINE | IC50 | = | 18400.0 | nM | 4.74 |