Assay Detail
Binding
CHEMBL1120738
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]WIN-35428 from human recombinant DAT expressed in CHO cells
19
Total Activities
19
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent dopamine transporter (CHEMBL238) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of novel selective norepinephrine reuptake inhibitors: 4-[3-aryl-2,2-dioxido-2,1,3-benzothiadiazol-1(3H)-yl]-1-(methylamino)butan-2-ols (WYE-103231).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 5.90 | 6.58 |
| Ki | 1 | 7.66 | 7.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL781 | MAZINDOL | 4.0 | 1 | 7.66 |
| CHEMBL1084828 | — | — | 1 | 6.58 |
| CHEMBL1085322 | — | — | 1 | 6.57 |
| CHEMBL1083430 | — | — | 1 | 6.54 |
| CHEMBL1084829 | — | — | 1 | 6.41 |
| CHEMBL1085338 | — | — | 1 | 6.29 |
| CHEMBL1084313 | — | — | 1 | 6.29 |
| CHEMBL1084311 | — | — | 1 | 6.00 |
| CHEMBL1083392 | — | — | 1 | 5.83 |
| CHEMBL1082292 | — | — | 1 | 5.73 |
| CHEMBL1083118 | — | — | 1 | 5.68 |
| CHEMBL1083409 | — | — | 1 | 5.67 |
| CHEMBL1085066 | — | — | 1 | 5.63 |
| CHEMBL1083410 | — | — | 1 | 5.62 |
| CHEMBL1085323 | — | — | 1 | 5.59 |
| CHEMBL1083429 | — | — | 1 | 5.58 |
| CHEMBL1084312 | — | — | 1 | 5.50 |
| CHEMBL1082458 | — | — | 1 | 5.44 |
| CHEMBL1083428 | — | — | 1 | 5.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL781 | MAZINDOL | Ki | = | 22.1 | nM | 7.66 |
| CHEMBL1084828 | — | IC50 | = | 262.0 | nM | 6.58 |
| CHEMBL1085322 | — | IC50 | = | 267.0 | nM | 6.57 |
| CHEMBL1083430 | — | IC50 | = | 291.0 | nM | 6.54 |
| CHEMBL1084829 | — | IC50 | = | 386.0 | nM | 6.41 |
| CHEMBL1085338 | — | IC50 | = | 512.0 | nM | 6.29 |
| CHEMBL1084313 | — | IC50 | = | 509.0 | nM | 6.29 |
| CHEMBL1084311 | — | IC50 | = | 998.0 | nM | 6.00 |
| CHEMBL1083392 | — | IC50 | = | 1475.0 | nM | 5.83 |
| CHEMBL1082292 | — | IC50 | = | 1872.0 | nM | 5.73 |
| CHEMBL1083118 | — | IC50 | = | 2086.0 | nM | 5.68 |
| CHEMBL1083409 | — | IC50 | = | 2113.0 | nM | 5.67 |
| CHEMBL1085066 | — | IC50 | = | 2326.0 | nM | 5.63 |
| CHEMBL1083410 | — | IC50 | = | 2409.0 | nM | 5.62 |
| CHEMBL1085323 | — | IC50 | = | 2570.0 | nM | 5.59 |
| CHEMBL1083429 | — | IC50 | = | 2618.0 | nM | 5.58 |
| CHEMBL1084312 | — | IC50 | = | 3185.0 | nM | 5.50 |
| CHEMBL1082458 | — | IC50 | = | 3617.0 | nM | 5.44 |
| CHEMBL1083428 | — | IC50 | = | 5500.0 | nM | 5.26 |