Assay Detail
Binding
CHEMBL1120740
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]nisoxetine from human NET expressed in MDCK-Net6 cells
30
Total Activities
30
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MDCK-Net6 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent noradrenaline transporter (CHEMBL222) ↗| 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 | 29 | 7.80 | 8.96 |
| Ki | 1 | 8.68 | 8.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1085831 | — | — | 1 | 8.96 |
| CHEMBL1083429 | — | — | 1 | 8.70 |
| CHEMBL1083392 | — | — | 1 | 8.70 |
| CHEMBL1083083 | — | — | 1 | 8.70 |
| CHEMBL1084042 | — | — | 1 | 8.70 |
| CHEMBL1083409 | — | — | 1 | 8.70 |
| CHEMBL1083118 | — | — | 1 | 8.70 |
| CHEMBL72 | DESIPRAMINE | 4.0 | 1 | 8.68 |
| CHEMBL1085338 | — | — | 1 | 8.57 |
| CHEMBL1083410 | — | — | 1 | 8.40 |
| CHEMBL1085339 | — | — | 1 | 8.30 |
| CHEMBL1082458 | — | — | 1 | 8.22 |
| CHEMBL1083428 | — | — | 1 | 8.22 |
| CHEMBL1086035 | — | — | 1 | 8.10 |
| CHEMBL1083408 | — | — | 1 | 8.05 |
| CHEMBL1085323 | — | — | 1 | 7.72 |
| CHEMBL1084312 | — | — | 1 | 7.72 |
| CHEMBL1085066 | — | — | 1 | 7.66 |
| CHEMBL1084313 | — | — | 1 | 7.47 |
| CHEMBL1082611 | — | — | 1 | 7.44 |
| CHEMBL1082459 | — | — | 1 | 7.32 |
| CHEMBL1084829 | — | — | 1 | 7.29 |
| CHEMBL1085233 | — | — | 1 | 7.24 |
| CHEMBL1085322 | — | — | 1 | 7.10 |
| CHEMBL1085830 | — | — | 1 | 7.03 |
| CHEMBL1084311 | — | — | 1 | 6.96 |
| CHEMBL1082292 | — | — | 1 | 6.81 |
| CHEMBL1084828 | — | — | 1 | 6.61 |
| CHEMBL1083430 | — | — | 1 | 6.56 |
| CHEMBL1083741 | — | — | 1 | 6.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1085831 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL1083429 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1083392 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1083083 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1084042 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1083409 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1083118 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL72 | DESIPRAMINE | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL1085338 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL1083410 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1085339 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1082458 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1083428 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1086035 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL1083408 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1085323 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1084312 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1085066 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL1084313 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL1082611 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL1082459 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL1084829 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL1085233 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL1085322 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL1085830 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL1084311 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL1082292 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL1084828 | — | IC50 | = | 244.0 | nM | 6.61 |
| CHEMBL1083430 | — | IC50 | = | 277.0 | nM | 6.56 |
| CHEMBL1083741 | — | IC50 | = | 441.0 | nM | 6.36 |