Assay Detail
Binding
CHEMBL746903
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Ability to inhibit high affinity reuptake of [3H]-NE (Norepinephrine transporter) into nerve ending synaptosomes prepared from brain regions
47
Total Activities
47
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
Further studies on conformationally constrained tricyclic tropane analogues and their uptake inhibition at monoamine transporter sites: synthesis of (Z)-9-(substituted arylmethylene)-7-azatricyclo[4.3.1.0(3,7)]decanes as a novel class of serotonin transporter inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 47 | 6.02 | 7.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL58414 | — | — | 1 | 7.28 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.97 |
| CHEMBL60540 | — | — | 1 | 6.84 |
| CHEMBL58485 | — | — | 1 | 6.80 |
| CHEMBL41 | FLUOXETINE | 4.0 | 1 | 6.78 |
| CHEMBL300818 | — | — | 1 | 6.75 |
| CHEMBL57260 | — | — | 1 | 6.73 |
| CHEMBL292129 | — | — | 1 | 6.70 |
| CHEMBL292394 | — | — | 1 | 6.68 |
| CHEMBL291321 | — | — | 1 | 6.67 |
| CHEMBL300146 | — | — | 1 | 6.64 |
| CHEMBL294429 | — | — | 1 | 6.57 |
| CHEMBL301275 | — | — | 1 | 6.49 |
| CHEMBL58280 | — | — | 1 | 6.41 |
| CHEMBL293574 | — | — | 1 | 6.40 |
| CHEMBL57934 | — | — | 1 | 6.38 |
| CHEMBL57596 | — | — | 1 | 6.34 |
| CHEMBL293524 | — | — | 1 | 6.29 |
| CHEMBL58308 | — | — | 1 | 6.23 |
| CHEMBL417960 | — | — | 1 | 6.20 |
| CHEMBL58307 | — | — | 1 | 6.19 |
| CHEMBL56495 | — | — | 1 | 6.18 |
| CHEMBL58253 | — | — | 1 | 6.17 |
| CHEMBL298815 | — | — | 1 | 6.00 |
| CHEMBL58318 | — | — | 1 | 5.96 |
| CHEMBL57320 | — | — | 1 | 5.93 |
| CHEMBL299901 | — | — | 1 | 5.92 |
| CHEMBL418494 | — | — | 1 | 5.74 |
| CHEMBL291494 | — | — | 1 | 5.70 |
| CHEMBL59545 | — | — | 1 | 5.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL58414 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL370805 | COCAINE | Ki | = | 108.0 | nM | 6.97 |
| CHEMBL60540 | — | Ki | = | 146.0 | nM | 6.84 |
| CHEMBL58485 | — | Ki | = | 157.0 | nM | 6.80 |
| CHEMBL41 | FLUOXETINE | Ki | = | 167.0 | nM | 6.78 |
| CHEMBL300818 | — | Ki | = | 178.0 | nM | 6.75 |
| CHEMBL57260 | — | Ki | = | 187.0 | nM | 6.73 |
| CHEMBL292129 | — | Ki | = | 198.0 | nM | 6.70 |
| CHEMBL292394 | — | Ki | = | 208.0 | nM | 6.68 |
| CHEMBL291321 | — | Ki | = | 213.0 | nM | 6.67 |
| CHEMBL300146 | — | Ki | = | 231.0 | nM | 6.64 |
| CHEMBL294429 | — | Ki | = | 272.0 | nM | 6.57 |
| CHEMBL301275 | — | Ki | = | 325.0 | nM | 6.49 |
| CHEMBL58280 | — | Ki | = | 394.0 | nM | 6.41 |
| CHEMBL293574 | — | Ki | = | 396.0 | nM | 6.40 |
| CHEMBL57934 | — | Ki | = | 417.0 | nM | 6.38 |
| CHEMBL57596 | — | Ki | = | 459.0 | nM | 6.34 |
| CHEMBL293524 | — | Ki | = | 508.0 | nM | 6.29 |
| CHEMBL58308 | — | Ki | = | 584.0 | nM | 6.23 |
| CHEMBL417960 | — | Ki | = | 638.0 | nM | 6.20 |
| CHEMBL58307 | — | Ki | = | 651.0 | nM | 6.19 |
| CHEMBL56495 | — | Ki | = | 659.0 | nM | 6.18 |
| CHEMBL58253 | — | Ki | = | 672.0 | nM | 6.17 |
| CHEMBL298815 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL58318 | — | Ki | = | 1110.0 | nM | 5.96 |
| CHEMBL57320 | — | Ki | = | 1180.0 | nM | 5.93 |
| CHEMBL299901 | — | Ki | = | 1210.0 | nM | 5.92 |
| CHEMBL418494 | — | Ki | = | 1830.0 | nM | 5.74 |
| CHEMBL291494 | — | Ki | = | 2020.0 | nM | 5.70 |
| CHEMBL59545 | — | Ki | = | 2410.0 | nM | 5.62 |
| CHEMBL60915 | — | Ki | = | 2510.0 | nM | 5.60 |
| CHEMBL59047 | — | Ki | = | 2790.0 | nM | 5.55 |
| CHEMBL57281 | — | Ki | = | 3070.0 | nM | 5.51 |
| CHEMBL294259 | — | Ki | = | 3220.0 | nM | 5.49 |
| CHEMBL301020 | — | Ki | = | 3840.0 | nM | 5.42 |
| CHEMBL300787 | — | Ki | = | 4100.0 | nM | 5.39 |
| CHEMBL300155 | — | Ki | = | 4470.0 | nM | 5.35 |
| CHEMBL58942 | — | Ki | = | 5370.0 | nM | 5.27 |
| CHEMBL58392 | — | Ki | = | 5950.0 | nM | 5.22 |
| CHEMBL292469 | — | Ki | = | 6580.0 | nM | 5.18 |
| CHEMBL58195 | — | Ki | = | 8190.0 | nM | 5.09 |
| CHEMBL299019 | — | Ki | = | 8590.0 | nM | 5.07 |
| CHEMBL58960 | — | Ki | = | 13000.0 | nM | 4.89 |
| CHEMBL293540 | — | Ki | = | 33400.0 | nM | 4.48 |
| CHEMBL294376 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL265808 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL58858 | — | Ki | > | 10000.0 | nM | - |