Assay Detail
Binding
CHEMBL673607
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Ability to inhibit high affinity reuptake of [3H]DA from dopamine transporter into nerve endings synaptosomes
48
Total Activities
48
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
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 | 48 | 5.49 | 6.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.37 |
| CHEMBL58414 | — | — | 1 | 6.32 |
| CHEMBL300818 | — | — | 1 | 6.30 |
| CHEMBL60540 | — | — | 1 | 6.19 |
| CHEMBL58253 | — | — | 1 | 6.19 |
| CHEMBL58485 | — | — | 1 | 6.13 |
| CHEMBL291321 | — | — | 1 | 6.12 |
| CHEMBL292394 | — | — | 1 | 6.07 |
| CHEMBL299901 | — | — | 1 | 6.07 |
| CHEMBL301275 | — | — | 1 | 5.89 |
| CHEMBL58960 | — | — | 1 | 5.79 |
| CHEMBL417960 | — | — | 1 | 5.73 |
| CHEMBL298815 | — | — | 1 | 5.72 |
| CHEMBL59047 | — | — | 1 | 5.68 |
| CHEMBL57260 | — | — | 1 | 5.50 |
| CHEMBL294429 | — | — | 1 | 5.50 |
| CHEMBL300155 | — | — | 1 | 5.48 |
| CHEMBL57934 | — | — | 1 | 5.42 |
| CHEMBL292469 | — | — | 1 | 5.39 |
| CHEMBL59545 | — | — | 1 | 5.35 |
| CHEMBL41 | FLUOXETINE | 4.0 | 1 | 5.34 |
| CHEMBL57596 | — | — | 1 | 5.27 |
| CHEMBL294259 | — | — | 1 | 5.26 |
| CHEMBL300787 | — | — | 1 | 5.25 |
| CHEMBL57320 | — | — | 1 | 5.22 |
| CHEMBL293524 | — | — | 1 | 5.18 |
| CHEMBL58308 | — | — | 1 | 5.18 |
| CHEMBL291494 | — | — | 1 | 5.17 |
| CHEMBL58307 | — | — | 1 | 5.17 |
| CHEMBL58280 | — | — | 1 | 5.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL370805 | COCAINE | Ki | = | 423.0 | nM | 6.37 |
| CHEMBL58414 | — | Ki | = | 481.0 | nM | 6.32 |
| CHEMBL300818 | — | Ki | = | 495.0 | nM | 6.30 |
| CHEMBL60540 | — | Ki | = | 649.0 | nM | 6.19 |
| CHEMBL58253 | — | Ki | = | 652.0 | nM | 6.19 |
| CHEMBL58485 | — | Ki | = | 735.0 | nM | 6.13 |
| CHEMBL291321 | — | Ki | = | 764.0 | nM | 6.12 |
| CHEMBL292394 | — | Ki | = | 853.0 | nM | 6.07 |
| CHEMBL299901 | — | Ki | = | 850.0 | nM | 6.07 |
| CHEMBL301275 | — | Ki | = | 1290.0 | nM | 5.89 |
| CHEMBL58960 | — | Ki | = | 1640.0 | nM | 5.79 |
| CHEMBL417960 | — | Ki | = | 1870.0 | nM | 5.73 |
| CHEMBL298815 | — | Ki | = | 1920.0 | nM | 5.72 |
| CHEMBL59047 | — | Ki | = | 2110.0 | nM | 5.68 |
| CHEMBL294429 | — | Ki | = | 3140.0 | nM | 5.50 |
| CHEMBL57260 | — | Ki | = | 3130.0 | nM | 5.50 |
| CHEMBL300155 | — | Ki | = | 3300.0 | nM | 5.48 |
| CHEMBL57934 | — | Ki | = | 3780.0 | nM | 5.42 |
| CHEMBL292469 | — | Ki | = | 4040.0 | nM | 5.39 |
| CHEMBL59545 | — | Ki | = | 4440.0 | nM | 5.35 |
| CHEMBL41 | FLUOXETINE | Ki | = | 4580.0 | nM | 5.34 |
| CHEMBL57596 | — | Ki | = | 5420.0 | nM | 5.27 |
| CHEMBL294259 | — | Ki | = | 5530.0 | nM | 5.26 |
| CHEMBL300787 | — | Ki | = | 5600.0 | nM | 5.25 |
| CHEMBL57320 | — | Ki | = | 5980.0 | nM | 5.22 |
| CHEMBL58308 | — | Ki | = | 6620.0 | nM | 5.18 |
| CHEMBL293524 | — | Ki | = | 6640.0 | nM | 5.18 |
| CHEMBL291494 | — | Ki | = | 6680.0 | nM | 5.17 |
| CHEMBL58307 | — | Ki | = | 6840.0 | nM | 5.17 |
| CHEMBL58280 | — | Ki | = | 7440.0 | nM | 5.13 |
| CHEMBL300146 | — | Ki | = | 7780.0 | nM | 5.11 |
| CHEMBL293574 | — | Ki | = | 8620.0 | nM | 5.06 |
| CHEMBL58942 | — | Ki | = | 9720.0 | nM | 5.01 |
| CHEMBL61046 | — | Ki | = | 9920.0 | nM | 5.00 |
| CHEMBL60915 | — | Ki | = | 13700.0 | nM | 4.86 |
| CHEMBL57281 | — | Ki | = | 14100.0 | nM | 4.85 |
| CHEMBL299019 | — | Ki | = | 17700.0 | nM | 4.75 |
| CHEMBL293540 | — | Ki | = | 38900.0 | nM | 4.41 |
| CHEMBL58195 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL294376 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL418494 | — | Ki | = | - | nM | - |
| CHEMBL58858 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL58392 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL301020 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL265808 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL292129 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL56495 | — | Ki | = | - | nM | - |
| CHEMBL58318 | — | Ki | = | - | nM | - |