Assay Detail
Binding
CHEMBL803030
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]paroxetine binding to 5-hydroxytryptamine (5-HT) transporter
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent serotonin transporter (CHEMBL313) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Secondary amine analogues of 3 beta-(4'-substituted phenyl)tropane-2 beta-carboxylic acid esters and N-norcocaine exhibit enhanced affinity for serotonin and norepinephrine transporters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 7.39 | 9.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2112889 | — | — | 1 | 9.44 |
| CHEMBL2112877 | — | — | 1 | 8.45 |
| CHEMBL300226 | — | — | 1 | 8.38 |
| CHEMBL429772 | — | — | 1 | 8.38 |
| CHEMBL2112860 | — | — | 1 | 8.09 |
| CHEMBL50157 | — | — | 1 | 7.55 |
| CHEMBL610897 | — | — | 1 | 7.35 |
| CHEMBL610894 | — | — | 1 | 7.17 |
| CHEMBL21112 | — | — | 1 | 7.16 |
| CHEMBL21256 | — | — | 1 | 6.90 |
| CHEMBL279657 | — | — | 1 | 6.81 |
| CHEMBL2079586 | — | — | 1 | 6.12 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 5.98 |
| CHEMBL1790051 | — | — | 1 | 5.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2112889 | — | IC50 | = | 0.36 | nM | 9.44 |
| CHEMBL2112877 | — | IC50 | = | 3.59 | nM | 8.45 |
| CHEMBL300226 | — | IC50 | = | 4.21 | nM | 8.38 |
| CHEMBL429772 | — | IC50 | = | 4.13 | nM | 8.38 |
| CHEMBL2112860 | — | IC50 | = | 8.13 | nM | 8.09 |
| CHEMBL50157 | — | IC50 | = | 28.4 | nM | 7.55 |
| CHEMBL610897 | — | IC50 | = | 44.5 | nM | 7.35 |
| CHEMBL610894 | — | IC50 | = | 66.8 | nM | 7.17 |
| CHEMBL21112 | — | IC50 | = | 68.6 | nM | 7.16 |
| CHEMBL21256 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL279657 | — | IC50 | = | 156.0 | nM | 6.81 |
| CHEMBL2079586 | — | IC50 | = | 759.0 | nM | 6.12 |
| CHEMBL370805 | COCAINE | IC50 | = | 1045.0 | nM | 5.98 |
| CHEMBL1790051 | — | IC50 | = | 1999.0 | nM | 5.70 |