Assay Detail
Binding
CHEMBL2433695
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]Nisoxetine from human recombinant NET over-expressed in dog MDCK cells
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MDCK |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent noradrenaline transporter (CHEMBL222) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and biological evaluation of novel 3,4-diaryl lactam derivatives as triple reuptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.03 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL72 | DESIPRAMINE | 4.0 | 1 | 8.82 |
| CHEMBL415 | CLOMIPRAMINE | 4.0 | 1 | 7.19 |
| CHEMBL2430692 | — | — | 1 | 6.42 |
| CHEMBL2430699 | — | — | 1 | 6.32 |
| CHEMBL2430688 | — | — | 1 | 6.29 |
| CHEMBL2430695 | — | — | 1 | 6.06 |
| CHEMBL2430684 | — | — | 1 | 6.00 |
| CHEMBL2430700 | — | — | 1 | 5.93 |
| CHEMBL2430701 | — | — | 1 | 5.86 |
| CHEMBL2430682 | — | — | 1 | 5.78 |
| CHEMBL2430685 | — | — | 1 | 5.72 |
| CHEMBL2430680 | — | — | 1 | 5.69 |
| CHEMBL2430687 | — | — | 1 | 5.60 |
| CHEMBL2430686 | — | — | 1 | 5.56 |
| CHEMBL2430689 | — | — | 1 | 5.45 |
| CHEMBL2430693 | — | — | 1 | 5.42 |
| CHEMBL2430681 | — | — | 1 | 5.29 |
| CHEMBL2430683 | — | — | 1 | 5.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL72 | DESIPRAMINE | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL415 | CLOMIPRAMINE | IC50 | = | 64.6 | nM | 7.19 |
| CHEMBL2430692 | — | IC50 | = | 384.2 | nM | 6.42 |
| CHEMBL2430699 | — | IC50 | = | 482.9 | nM | 6.32 |
| CHEMBL2430688 | — | IC50 | = | 509.5 | nM | 6.29 |
| CHEMBL2430695 | — | IC50 | = | 865.7 | nM | 6.06 |
| CHEMBL2430684 | — | IC50 | = | 990.3 | nM | 6.00 |
| CHEMBL2430700 | — | IC50 | = | 1187.0 | nM | 5.93 |
| CHEMBL2430701 | — | IC50 | = | 1376.0 | nM | 5.86 |
| CHEMBL2430682 | — | IC50 | = | 1662.0 | nM | 5.78 |
| CHEMBL2430685 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL2430680 | — | IC50 | = | 2033.0 | nM | 5.69 |
| CHEMBL2430687 | — | IC50 | = | 2521.0 | nM | 5.60 |
| CHEMBL2430686 | — | IC50 | = | 2745.0 | nM | 5.56 |
| CHEMBL2430689 | — | IC50 | = | 3570.0 | nM | 5.45 |
| CHEMBL2430693 | — | IC50 | = | 3825.0 | nM | 5.42 |
| CHEMBL2430681 | — | IC50 | = | 5176.0 | nM | 5.29 |
| CHEMBL2430683 | — | IC50 | = | 7619.0 | nM | 5.12 |