Assay Detail
Binding
CHEMBL838825
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Inhibitory constant against reuptake of [3H]5-HT at serotonin transporter of rat midbrain cortex
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Midbrain |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent serotonin transporter (CHEMBL313) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Discovery of novel conformationally constrained tropane-based biaryl and arylacetylene ligands as potent and selective norepinephrine transporter inhibitors and potential antidepressants.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 6.70 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2113081 | — | — | 1 | 8.92 |
| CHEMBL371679 | — | — | 1 | 7.77 |
| CHEMBL195181 | — | — | 1 | 7.50 |
| CHEMBL195146 | — | — | 1 | 7.50 |
| CHEMBL194439 | — | — | 1 | 7.16 |
| CHEMBL194329 | — | — | 1 | 7.07 |
| CHEMBL195404 | — | — | 1 | 6.86 |
| CHEMBL365519 | — | — | 1 | 6.85 |
| CHEMBL72 | DESIPRAMINE | 4.0 | 1 | 6.79 |
| CHEMBL194024 | — | — | 1 | 6.68 |
| CHEMBL195709 | — | — | 1 | 6.67 |
| CHEMBL2113083 | — | — | 1 | 6.53 |
| CHEMBL193806 | — | — | 1 | 6.50 |
| CHEMBL195475 | — | — | 1 | 6.46 |
| CHEMBL191985 | — | — | 1 | 6.33 |
| CHEMBL371344 | — | — | 1 | 6.04 |
| CHEMBL363189 | — | — | 1 | 5.97 |
| CHEMBL195138 | — | — | 1 | 5.93 |
| CHEMBL371349 | — | — | 1 | 5.87 |
| CHEMBL371816 | — | — | 1 | 5.86 |
| CHEMBL334027 | — | — | 1 | 5.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2113081 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL371679 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL195181 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL195146 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL194439 | — | Ki | = | 69.0 | nM | 7.16 |
| CHEMBL194329 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL195404 | — | Ki | = | 138.0 | nM | 6.86 |
| CHEMBL365519 | — | Ki | = | 142.0 | nM | 6.85 |
| CHEMBL72 | DESIPRAMINE | Ki | = | 163.0 | nM | 6.79 |
| CHEMBL194024 | — | Ki | = | 207.0 | nM | 6.68 |
| CHEMBL195709 | — | Ki | = | 215.0 | nM | 6.67 |
| CHEMBL2113083 | — | Ki | = | 295.0 | nM | 6.53 |
| CHEMBL193806 | — | Ki | = | 317.0 | nM | 6.50 |
| CHEMBL195475 | — | Ki | = | 346.0 | nM | 6.46 |
| CHEMBL191985 | — | Ki | = | 466.0 | nM | 6.33 |
| CHEMBL371344 | — | Ki | = | 914.0 | nM | 6.04 |
| CHEMBL363189 | — | Ki | = | 1080.0 | nM | 5.97 |
| CHEMBL195138 | — | Ki | = | 1170.0 | nM | 5.93 |
| CHEMBL371349 | — | Ki | = | 1340.0 | nM | 5.87 |
| CHEMBL371816 | — | Ki | = | 1390.0 | nM | 5.86 |
| CHEMBL334027 | — | Ki | = | 3320.0 | nM | 5.48 |