Assay Detail
Binding
CHEMBL1816473
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Inhibition of norepinephrine reuptake at NET expressed in MDCK cells
40
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | MDCK |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent noradrenaline transporter (CHEMBL222) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and pharmacological characterization of bicyclic triple reuptake inhibitor 3-aryl octahydrocyclopenta[c]pyrrole analogues.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 40 | 6.40 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL295467 | NISOXETINE | 2.0 | 1 | 8.10 |
| CHEMBL1813476 | — | — | 1 | 7.85 |
| CHEMBL1813484 | — | — | 1 | 7.65 |
| CHEMBL1813478 | — | — | 2 | 7.62 |
| CHEMBL1813316 | — | — | 1 | 7.57 |
| CHEMBL1813317 | — | — | 1 | 7.42 |
| CHEMBL1813314 | — | — | 1 | 7.25 |
| CHEMBL1813477 | — | — | 1 | 7.22 |
| CHEMBL1813475 | — | — | 1 | 6.97 |
| CHEMBL1813471 | — | — | 2 | 6.95 |
| CHEMBL1813315 | — | — | 1 | 6.85 |
| CHEMBL1813485 | — | — | 1 | 6.72 |
| CHEMBL1813318 | — | — | 1 | 6.69 |
| CHEMBL1813472 | — | — | 1 | 6.69 |
| CHEMBL1813483 | — | — | 2 | 6.68 |
| CHEMBL1813474 | — | — | 1 | 6.68 |
| CHEMBL1813312 | — | — | 2 | 6.38 |
| CHEMBL1813470 | — | — | 1 | 6.27 |
| CHEMBL1813313 | — | — | 2 | 6.27 |
| CHEMBL1813307 | — | — | 1 | 6.25 |
| CHEMBL1813306 | — | — | 1 | 6.04 |
| CHEMBL1813473 | — | — | 2 | 5.67 |
| CHEMBL1813308 | — | — | 1 | 5.63 |
| CHEMBL1813309 | — | — | 1 | 5.61 |
| CHEMBL1813489 | — | — | 1 | 5.53 |
| CHEMBL1813487 | — | — | 1 | 5.42 |
| CHEMBL1813482 | — | — | 1 | 5.37 |
| CHEMBL1813486 | — | — | 1 | 5.35 |
| CHEMBL1813488 | — | — | 1 | 5.27 |
| CHEMBL1813311 | — | — | 1 | 5.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL295467 | NISOXETINE | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL1813476 | — | IC50 | = | 14.13 | nM | 7.85 |
| CHEMBL1813484 | — | IC50 | = | 22.39 | nM | 7.65 |
| CHEMBL1813478 | — | IC50 | = | 23.99 | nM | 7.62 |
| CHEMBL1813316 | — | IC50 | = | 26.92 | nM | 7.57 |
| CHEMBL1813317 | — | IC50 | = | 38.02 | nM | 7.42 |
| CHEMBL1813314 | — | IC50 | = | 56.23 | nM | 7.25 |
| CHEMBL1813477 | — | IC50 | = | 60.26 | nM | 7.22 |
| CHEMBL1813478 | — | IC50 | = | 95.5 | nM | 7.02 |
| CHEMBL1813475 | — | IC50 | = | 107.15 | nM | 6.97 |
| CHEMBL1813471 | — | IC50 | = | 112.2 | nM | 6.95 |
| CHEMBL1813315 | — | IC50 | = | 141.25 | nM | 6.85 |
| CHEMBL1813471 | — | IC50 | = | 177.83 | nM | 6.75 |
| CHEMBL1813485 | — | IC50 | = | 190.55 | nM | 6.72 |
| CHEMBL1813318 | — | IC50 | = | 204.17 | nM | 6.69 |
| CHEMBL1813472 | — | IC50 | = | 204.17 | nM | 6.69 |
| CHEMBL1813483 | — | IC50 | = | 208.93 | nM | 6.68 |
| CHEMBL1813474 | — | IC50 | = | 208.93 | nM | 6.68 |
| CHEMBL1813312 | — | IC50 | = | 416.87 | nM | 6.38 |
| CHEMBL1813483 | — | IC50 | = | 467.74 | nM | 6.33 |
| CHEMBL1813313 | — | IC50 | = | 537.03 | nM | 6.27 |
| CHEMBL1813470 | — | IC50 | = | 537.03 | nM | 6.27 |
| CHEMBL1813307 | — | IC50 | = | 562.34 | nM | 6.25 |
| CHEMBL1813313 | — | IC50 | = | 724.44 | nM | 6.14 |
| CHEMBL1813306 | — | IC50 | = | 912.01 | nM | 6.04 |
| CHEMBL1813473 | — | IC50 | = | 2137.96 | nM | 5.67 |
| CHEMBL1813308 | — | IC50 | = | 2344.23 | nM | 5.63 |
| CHEMBL1813309 | — | IC50 | = | 2454.71 | nM | 5.61 |
| CHEMBL1813489 | — | IC50 | = | 2951.21 | nM | 5.53 |
| CHEMBL1813487 | — | IC50 | = | 3801.89 | nM | 5.42 |
| CHEMBL1813482 | — | IC50 | = | 4265.8 | nM | 5.37 |
| CHEMBL1813486 | — | IC50 | = | 4466.84 | nM | 5.35 |
| CHEMBL1813488 | — | IC50 | = | 5370.32 | nM | 5.27 |
| CHEMBL1813311 | — | IC50 | = | 5888.44 | nM | 5.23 |
| CHEMBL1813473 | — | IC50 | = | 6025.6 | nM | 5.22 |
| CHEMBL1813479 | — | IC50 | = | 6456.54 | nM | 5.19 |
| CHEMBL1813310 | — | IC50 | = | 14125.38 | nM | 4.85 |
| CHEMBL1813480 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1813481 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1813312 | — | IC50 | > | 10000.0 | nM | - |