Assay Detail
Binding
CHEMBL872597
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition the uptake of tritiated serotonin (5-HT) by the serotonin transporter SERT in rat synaptosomes
83
Total Activities
75
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
Pyrroloisoquinoline antidepressants. 2. In-depth exploration of structure-activity relationships.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 83 | 7.40 | 9.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL34990 | — | — | 3 | 9.41 |
| CHEMBL809 | SERTRALINE | 4.0 | 1 | 9.07 |
| CHEMBL286312 | — | — | 1 | 9.00 |
| CHEMBL1743782 | — | — | 1 | 8.82 |
| CHEMBL1743794 | — | — | 1 | 8.77 |
| CHEMBL287474 | — | — | 1 | 8.74 |
| CHEMBL35013 | — | — | 1 | 8.54 |
| CHEMBL284981 | — | — | 1 | 8.49 |
| CHEMBL1743785 | — | — | 1 | 8.49 |
| CHEMBL1743798 | — | — | 1 | 8.36 |
| CHEMBL32726 | — | — | 1 | 8.35 |
| CHEMBL1743786 | — | — | 1 | 8.32 |
| CHEMBL33364 | — | — | 1 | 8.31 |
| CHEMBL1743812 | — | — | 1 | 8.28 |
| CHEMBL1743803 | — | — | 3 | 8.26 |
| CHEMBL1743791 | — | — | 1 | 8.26 |
| CHEMBL431299 | — | — | 1 | 8.14 |
| CHEMBL1743790 | — | — | 1 | 8.14 |
| CHEMBL35441 | — | — | 1 | 8.10 |
| CHEMBL34891 | — | — | 1 | 8.09 |
| CHEMBL287859 | — | — | 1 | 8.07 |
| CHEMBL286849 | — | — | 3 | 8.04 |
| CHEMBL287257 | DICLOFENSINE | 2.0 | 1 | 7.99 |
| CHEMBL35184 | — | — | 3 | 7.91 |
| CHEMBL35166 | — | — | 1 | 7.91 |
| CHEMBL416777 | — | — | 1 | 7.90 |
| CHEMBL1743765 | — | — | 1 | 7.81 |
| CHEMBL1743775 | — | — | 1 | 7.78 |
| CHEMBL1743795 | — | — | 1 | 7.74 |
| CHEMBL1743820 | — | — | 1 | 7.74 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL34990 | — | Ki | = | 0.39 | nM | 9.41 |
| CHEMBL34990 | — | Ki | = | 0.62 | nM | 9.21 |
| CHEMBL809 | SERTRALINE | Ki | = | 0.85 | nM | 9.07 |
| CHEMBL286312 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL1743782 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL1743794 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL287474 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL35013 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL284981 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL1743785 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL1743798 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL32726 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL1743786 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL33364 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL1743812 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL1743803 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL1743791 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL431299 | — | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL1743790 | — | Ki | = | 7.3 | nM | 8.14 |
| CHEMBL35441 | — | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL34891 | — | Ki | = | 8.1 | nM | 8.09 |
| CHEMBL287859 | — | Ki | = | 8.5 | nM | 8.07 |
| CHEMBL1743803 | — | Ki | = | 8.5 | nM | 8.07 |
| CHEMBL286849 | — | Ki | = | 9.1 | nM | 8.04 |
| CHEMBL287257 | DICLOFENSINE | Ki | = | 10.3 | nM | 7.99 |
| CHEMBL35166 | — | Ki | = | 12.3 | nM | 7.91 |
| CHEMBL35184 | — | Ki | = | 12.4 | nM | 7.91 |
| CHEMBL416777 | — | Ki | = | 12.7 | nM | 7.90 |
| CHEMBL1743765 | — | Ki | = | 15.6 | nM | 7.81 |
| CHEMBL1743775 | — | Ki | = | 16.6 | nM | 7.78 |
| CHEMBL1743795 | — | Ki | = | 18.3 | nM | 7.74 |
| CHEMBL1743820 | — | Ki | = | 18.1 | nM | 7.74 |
| CHEMBL418038 | — | Ki | = | 19.1 | nM | 7.72 |
| CHEMBL286849 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL431898 | — | Ki | = | 23.1 | nM | 7.64 |
| CHEMBL35184 | — | Ki | = | 23.5 | nM | 7.63 |
| CHEMBL1743793 | — | Ki | = | 24.6 | nM | 7.61 |
| CHEMBL1743772 | — | Ki | = | 29.2 | nM | 7.54 |
| CHEMBL1743824 | — | Ki | = | 32.1 | nM | 7.49 |
| CHEMBL1743819 | — | Ki | = | 33.1 | nM | 7.48 |
| CHEMBL1743767 | — | Ki | = | 37.9 | nM | 7.42 |
| CHEMBL11 | IMIPRAMINE | Ki | = | 41.8 | nM | 7.38 |
| CHEMBL1743810 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL1743823 | — | Ki | = | 43.3 | nM | 7.36 |
| CHEMBL1743773 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL35071 | — | Ki | = | 45.7 | nM | 7.34 |
| CHEMBL285403 | — | Ki | = | 55.6 | nM | 7.25 |
| CHEMBL34990 | — | Ki | = | 58.4 | nM | 7.23 |
| CHEMBL32797 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL32209 | — | Ki | = | 72.0 | nM | 7.14 |