Assay Detail
Binding
CHEMBL872668
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Binding affinity for norepinephrine transporter in rat brain using [3H]-nisoxatine as radioligand
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Structure-activity relationships at monoamine transporters and muscarinic receptors for N-substituted-3alpha-(3'-chloro-, 4'-chloro-, and 4',4''-dichloro-substituted-diphenyl)methoxytropanes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 5.51 | 6.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3084870 | — | — | 1 | 6.35 |
| CHEMBL559215 | — | — | 1 | 6.29 |
| CHEMBL539821 | — | — | 1 | 6.00 |
| CHEMBL543231 | — | — | 1 | 5.91 |
| CHEMBL310310 | — | — | 1 | 5.83 |
| CHEMBL542275 | — | — | 1 | 5.83 |
| CHEMBL3084621 | — | — | 1 | 5.74 |
| CHEMBL3084608 | — | — | 1 | 5.63 |
| CHEMBL3084884 | — | — | 1 | 5.53 |
| CHEMBL545574 | — | — | 1 | 5.38 |
| CHEMBL545342 | — | — | 1 | 5.33 |
| CHEMBL3084607 | — | — | 1 | 5.30 |
| CHEMBL539829 | — | — | 1 | 5.22 |
| CHEMBL542521 | — | — | 1 | 5.19 |
| CHEMBL541612 | — | — | 1 | 5.12 |
| CHEMBL3084609 | — | — | 1 | 4.99 |
| CHEMBL544177 | — | — | 1 | 4.89 |
| CHEMBL3084623 | — | — | 1 | 4.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3084870 | — | Ki | = | 451.0 | nM | 6.35 |
| CHEMBL559215 | — | Ki | = | 508.0 | nM | 6.29 |
| CHEMBL539821 | — | Ki | = | 1010.0 | nM | 6.00 |
| CHEMBL543231 | — | Ki | = | 1230.0 | nM | 5.91 |
| CHEMBL310310 | — | Ki | = | 1470.0 | nM | 5.83 |
| CHEMBL542275 | — | Ki | = | 1470.0 | nM | 5.83 |
| CHEMBL3084621 | — | Ki | = | 1810.0 | nM | 5.74 |
| CHEMBL3084608 | — | Ki | = | 2320.0 | nM | 5.63 |
| CHEMBL3084884 | — | Ki | = | 2980.0 | nM | 5.53 |
| CHEMBL545574 | — | Ki | = | 4140.0 | nM | 5.38 |
| CHEMBL545342 | — | Ki | = | 4720.0 | nM | 5.33 |
| CHEMBL3084607 | — | Ki | = | 4950.0 | nM | 5.30 |
| CHEMBL539829 | — | Ki | = | 6040.0 | nM | 5.22 |
| CHEMBL542521 | — | Ki | = | 6460.0 | nM | 5.19 |
| CHEMBL541612 | — | Ki | = | 7660.0 | nM | 5.12 |
| CHEMBL3084609 | — | Ki | = | 10300.0 | nM | 4.99 |
| CHEMBL544177 | — | Ki | = | 12990.0 | nM | 4.89 |
| CHEMBL3084623 | — | Ki | = | 19800.0 | nM | 4.70 |