Assay Detail
Binding
CHEMBL932888
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Inhibition of human NET
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent noradrenaline transporter (CHEMBL222) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Studies on the SAR and pharmacophore of milnacipran derivatives as monoamine transporter inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 42 | 6.48 | 8.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL260440 | — | — | 1 | 8.36 |
| CHEMBL641 | ATOMOXETINE | 4.0 | 1 | 8.29 |
| CHEMBL256667 | — | — | 1 | 8.08 |
| CHEMBL1175 | DULOXETINE | 4.0 | 1 | 8.05 |
| CHEMBL410622 | — | — | 1 | 7.92 |
| CHEMBL260439 | — | — | 1 | 7.85 |
| CHEMBL415098 | — | — | 1 | 7.68 |
| CHEMBL404364 | — | — | 1 | 7.39 |
| CHEMBL404474 | — | — | 1 | 7.20 |
| CHEMBL259209 | MILNACIPRAN | 4.0 | 1 | 7.11 |
| CHEMBL272285 | — | — | 1 | 6.89 |
| CHEMBL406156 | — | — | 1 | 6.82 |
| CHEMBL256020 | — | — | 1 | 6.77 |
| CHEMBL402999 | — | — | 1 | 6.75 |
| CHEMBL256646 | — | — | 1 | 6.70 |
| CHEMBL256039 | — | — | 1 | 6.44 |
| CHEMBL256408 | — | — | 1 | 6.35 |
| CHEMBL272790 | — | — | 1 | 6.24 |
| CHEMBL1169524 | — | — | 1 | 6.16 |
| CHEMBL272744 | — | — | 1 | 6.07 |
| CHEMBL256021 | — | — | 1 | 6.02 |
| CHEMBL269799 | — | — | 1 | 5.85 |
| CHEMBL256019 | — | — | 1 | 5.64 |
| CHEMBL270569 | — | — | 1 | 5.58 |
| CHEMBL256397 | — | — | 1 | 5.55 |
| CHEMBL272286 | — | — | 1 | 5.54 |
| CHEMBL256447 | — | — | 1 | 5.43 |
| CHEMBL404345 | — | — | 1 | 5.31 |
| CHEMBL272531 | — | — | 1 | 5.21 |
| CHEMBL402365 | — | — | 1 | 5.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL260440 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL641 | ATOMOXETINE | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL256667 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL1175 | DULOXETINE | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL410622 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL260439 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL415098 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL404364 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL404474 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL259209 | MILNACIPRAN | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL272285 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL406156 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL256020 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL402999 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL256646 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL256039 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL256408 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL272790 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL1169524 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL272744 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL256021 | — | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL269799 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL256019 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL270569 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL256397 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL272286 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL256447 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL404345 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL272531 | — | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL402365 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL272530 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL401621 | — | IC50 | = | 8100.0 | nM | 5.09 |
| CHEMBL404475 | — | IC50 | = | 8400.0 | nM | 5.08 |
| CHEMBL256841 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL272986 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL272074 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL270240 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL257047 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL257048 | N,N-DIMETHYL MILNACIPRAN | IC50 | > | 10000.0 | nM | - |
| CHEMBL255839 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL450623 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL269798 | — | IC50 | > | 10000.0 | nM | - |