Assay Detail
Binding
CHEMBL946205
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Inhibition of norepinephrine uptake at NET in rat brain synaptosome
39
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Studies on the structure-activity relationship of bicifadine analogs as monoamine transporter inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 39 | 6.52 | 8.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL180101 | ESREBOXETINE | 3.0 | 1 | 8.51 |
| CHEMBL448893 | — | — | 1 | 7.54 |
| CHEMBL451785 | — | — | 1 | 7.47 |
| CHEMBL452045 | — | — | 1 | 7.44 |
| CHEMBL509158 | — | — | 1 | 7.32 |
| CHEMBL592374 | AMITIFADINE | 2.0 | 2 | 7.29 |
| CHEMBL448714 | — | — | 1 | 7.28 |
| CHEMBL444992 | — | — | 1 | 7.17 |
| CHEMBL508171 | — | — | 1 | 7.11 |
| CHEMBL508156 | — | — | 1 | 7.04 |
| CHEMBL488473 | — | — | 1 | 6.92 |
| CHEMBL444247 | — | — | 1 | 6.89 |
| CHEMBL500739 | — | — | 1 | 6.89 |
| CHEMBL449514 | — | — | 1 | 6.82 |
| CHEMBL519552 | — | — | 1 | 6.82 |
| CHEMBL506040 | — | — | 1 | 6.72 |
| CHEMBL453327 | — | — | 1 | 6.66 |
| CHEMBL505382 | — | — | 1 | 6.52 |
| CHEMBL453576 | — | — | 1 | 6.50 |
| CHEMBL503805 | — | — | 1 | 6.47 |
| CHEMBL503383 | — | — | 1 | 6.46 |
| CHEMBL505313 | — | — | 1 | 6.44 |
| CHEMBL488638 | — | — | 1 | 6.37 |
| CHEMBL453328 | — | — | 1 | 6.33 |
| CHEMBL521058 | — | — | 1 | 6.30 |
| CHEMBL451504 | — | — | 1 | 6.25 |
| CHEMBL509214 | — | — | 1 | 6.23 |
| CHEMBL503444 | — | — | 1 | 5.85 |
| CHEMBL486255 | — | — | 1 | 5.80 |
| CHEMBL519717 | — | — | 1 | 5.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL180101 | ESREBOXETINE | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL448893 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL451785 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL452045 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL509158 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL592374 | AMITIFADINE | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL448714 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL444992 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL508171 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL592374 | AMITIFADINE | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL508156 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL488473 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL444247 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL500739 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL449514 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL519552 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL506040 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL453327 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL505382 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL453576 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL503805 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL503383 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL505313 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL488638 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL453328 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL521058 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL451504 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL509214 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL503444 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL486255 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL519717 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL452543 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL505742 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL449825 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL449052 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL454285 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL508896 | — | IC50 | = | 6800.0 | nM | 5.17 |
| CHEMBL488639 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL505812 | — | IC50 | > | 10000.0 | nM | - |