Assay Detail
Binding
CHEMBL804588
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Inhibition of [125I]RTI-55 binding to human serotonin transporter expressed in human embryonic kidney cells
13
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | kidney |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent serotonin transporter (CHEMBL228) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis, radiosynthesis, and biological evaluation of carbon-11 and iodine-123 labeled 2beta-carbomethoxy-3beta-[4'-((Z)-2-haloethenyl)phenyl]tropanes: candidate radioligands for in vivo imaging of the serotonin transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 9.27 | 10.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL428706 | — | — | 3 | 10.40 |
| CHEMBL14531 | — | — | 1 | 10.40 |
| CHEMBL14305 | — | — | 1 | 10.10 |
| CHEMBL14257 | — | — | 1 | 10.10 |
| CHEMBL275212 | — | — | 1 | 9.96 |
| CHEMBL14613 | — | — | 1 | 9.44 |
| CHEMBL14924 | — | — | 1 | 8.87 |
| CHEMBL549 | CITALOPRAM | 4.0 | 1 | 8.80 |
| CHEMBL311347 | — | — | 1 | 8.38 |
| CHEMBL14370 | REBOXETINE | 4.0 | 1 | 6.89 |
| CHEMBL14144 | — | — | 1 | 6.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL428706 | — | Ki | = | 0.04 | nM | 10.40 |
| CHEMBL428706 | — | Ki | = | 0.04 | nM | 10.40 |
| CHEMBL14531 | — | Ki | = | 0.04 | nM | 10.40 |
| CHEMBL428706 | — | Ki | = | 0.05 | nM | 10.30 |
| CHEMBL14305 | — | Ki | = | 0.08 | nM | 10.10 |
| CHEMBL14257 | — | Ki | = | 0.08 | nM | 10.10 |
| CHEMBL275212 | — | Ki | = | 0.11 | nM | 9.96 |
| CHEMBL14613 | — | Ki | = | 0.36 | nM | 9.44 |
| CHEMBL14924 | — | Ki | = | 1.35 | nM | 8.87 |
| CHEMBL549 | CITALOPRAM | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL311347 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL14370 | REBOXETINE | Ki | = | 129.0 | nM | 6.89 |
| CHEMBL14144 | — | Ki | = | 390.0 | nM | 6.41 |