Assay Detail
Binding
CHEMBL805175
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of high affinity re-uptake of [3H]5-HT (serotonin) into nerve ending 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 serotonin transporter (CHEMBL313) ↗| 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 | 7.67 | 10.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL58858 | — | — | 1 | 10.22 |
| CHEMBL294259 | — | — | 1 | 10.00 |
| CHEMBL58195 | — | — | 1 | 10.00 |
| CHEMBL417960 | — | — | 1 | 8.80 |
| CHEMBL294429 | — | — | 1 | 8.74 |
| CHEMBL294376 | — | — | 1 | 8.70 |
| CHEMBL58307 | — | — | 1 | 8.66 |
| CHEMBL57596 | — | — | 1 | 8.64 |
| CHEMBL57281 | — | — | 1 | 8.51 |
| CHEMBL301020 | — | — | 1 | 8.49 |
| CHEMBL300155 | — | — | 1 | 8.40 |
| CHEMBL58253 | — | — | 1 | 8.36 |
| CHEMBL292129 | — | — | 1 | 8.19 |
| CHEMBL41 | FLUOXETINE | 4.0 | 1 | 8.14 |
| CHEMBL265808 | — | — | 1 | 8.07 |
| CHEMBL58392 | — | — | 1 | 8.03 |
| CHEMBL56495 | — | — | 1 | 8.00 |
| CHEMBL58318 | — | — | 1 | 7.99 |
| CHEMBL300818 | — | — | 1 | 7.96 |
| CHEMBL292469 | — | — | 1 | 7.96 |
| CHEMBL418494 | — | — | 1 | 7.90 |
| CHEMBL60540 | — | — | 1 | 7.82 |
| CHEMBL298815 | — | — | 1 | 7.70 |
| CHEMBL58485 | — | — | 1 | 7.68 |
| CHEMBL291321 | — | — | 1 | 7.66 |
| CHEMBL291494 | — | — | 1 | 7.54 |
| CHEMBL57934 | — | — | 1 | 7.53 |
| CHEMBL293574 | — | — | 1 | 7.51 |
| CHEMBL292394 | — | — | 1 | 7.46 |
| CHEMBL59545 | — | — | 1 | 7.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL58858 | — | Ki | = | 0.06 | nM | 10.22 |
| CHEMBL294259 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL58195 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL417960 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL294429 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL294376 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL58307 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL57596 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL57281 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL301020 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL300155 | — | Ki | = | 3.95 | nM | 8.40 |
| CHEMBL58253 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL292129 | — | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL41 | FLUOXETINE | Ki | = | 7.3 | nM | 8.14 |
| CHEMBL265808 | — | Ki | = | 8.5 | nM | 8.07 |
| CHEMBL58392 | — | Ki | = | 9.3 | nM | 8.03 |
| CHEMBL56495 | — | Ki | = | 10.1 | nM | 8.00 |
| CHEMBL58318 | — | Ki | = | 10.2 | nM | 7.99 |
| CHEMBL300818 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL292469 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL418494 | — | Ki | = | 12.6 | nM | 7.90 |
| CHEMBL60540 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL298815 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL58485 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL291321 | — | Ki | = | 21.9 | nM | 7.66 |
| CHEMBL291494 | — | Ki | = | 28.9 | nM | 7.54 |
| CHEMBL57934 | — | Ki | = | 29.8 | nM | 7.53 |
| CHEMBL293574 | — | Ki | = | 30.7 | nM | 7.51 |
| CHEMBL292394 | — | Ki | = | 34.3 | nM | 7.46 |
| CHEMBL59545 | — | Ki | = | 48.3 | nM | 7.32 |
| CHEMBL299019 | — | Ki | = | 48.7 | nM | 7.31 |
| CHEMBL300146 | — | Ki | = | 53.6 | nM | 7.27 |
| CHEMBL57260 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL293524 | — | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL301275 | — | Ki | = | 85.7 | nM | 7.07 |
| CHEMBL57320 | — | Ki | = | 92.9 | nM | 7.03 |
| CHEMBL58280 | — | Ki | = | 101.0 | nM | 7.00 |
| CHEMBL58942 | — | Ki | = | 121.0 | nM | 6.92 |
| CHEMBL370805 | COCAINE | Ki | = | 155.0 | nM | 6.81 |
| CHEMBL58960 | — | Ki | = | 233.0 | nM | 6.63 |
| CHEMBL59047 | — | Ki | = | 245.0 | nM | 6.61 |
| CHEMBL58308 | — | Ki | = | 335.0 | nM | 6.47 |
| CHEMBL299901 | — | Ki | = | 354.0 | nM | 6.45 |
| CHEMBL300787 | — | Ki | = | 437.0 | nM | 6.36 |
| CHEMBL61046 | — | Ki | = | 860.0 | nM | 6.07 |
| CHEMBL293540 | — | Ki | = | 993.0 | nM | 6.00 |
| CHEMBL58414 | — | Ki | = | 1140.0 | nM | 5.94 |
| CHEMBL60915 | — | Ki | = | 1170.0 | nM | 5.93 |