Assay Detail
Binding
CHEMBL827185
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]paroxetine from serotonin transporter of rat cerebral cortex
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent serotonin transporter (CHEMBL313) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and monoamine transporter affinity of new 2beta-carbomethoxy-3beta-[4-(substituted thiophenyl)]phenyltropanes: discovery of a selective SERT antagonist with picomolar potency.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 8.63 | 10.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL435287 | — | — | 1 | 10.77 |
| CHEMBL181557 | — | — | 1 | 9.96 |
| CHEMBL181609 | — | — | 1 | 9.82 |
| CHEMBL179498 | — | — | 1 | 9.64 |
| CHEMBL180918 | — | — | 1 | 9.42 |
| CHEMBL14391 | — | — | 1 | 9.34 |
| CHEMBL369098 | — | — | 1 | 9.19 |
| CHEMBL549 | CITALOPRAM | 4.0 | 1 | 8.80 |
| CHEMBL433560 | — | — | 1 | 8.40 |
| CHEMBL178773 | — | — | 1 | 8.34 |
| CHEMBL181613 | — | — | 1 | 7.19 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 5.98 |
| CHEMBL180618 | — | — | 1 | 5.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL435287 | — | Ki | = | 0.017 | nM | 10.77 |
| CHEMBL181557 | — | Ki | = | 0.11 | nM | 9.96 |
| CHEMBL181609 | — | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL179498 | — | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL180918 | — | Ki | = | 0.38 | nM | 9.42 |
| CHEMBL14391 | — | Ki | = | 0.46 | nM | 9.34 |
| CHEMBL369098 | — | Ki | = | 0.64 | nM | 9.19 |
| CHEMBL549 | CITALOPRAM | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL433560 | — | Ki | = | 4.02 | nM | 8.40 |
| CHEMBL178773 | — | Ki | = | 4.56 | nM | 8.34 |
| CHEMBL181613 | — | Ki | = | 64.7 | nM | 7.19 |
| CHEMBL370805 | COCAINE | Ki | = | 1050.0 | nM | 5.98 |
| CHEMBL180618 | — | Ki | = | 5000.0 | nM | 5.30 |