Assay Detail
Binding
CHEMBL832789
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Inhibition of [3H]citalopram binding to serotonin transporter of rat cerebral cortex
22
Total Activities
22
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
Further structurally constrained analogues of cis-(6-benzhydrylpiperidin-3-yl)benzylamine with elucidation of bioactive conformation: discovery of 1,4-diazabicyclo[3.3.1]nonane derivatives and evaluation of their biological properties for the monoamine transporters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 5.65 | 6.88 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL543876 | — | — | 1 | 6.88 |
| CHEMBL39262 | — | — | 1 | 6.86 |
| CHEMBL189082 | — | — | 1 | 6.36 |
| CHEMBL189095 | — | — | 1 | 6.17 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.13 |
| CHEMBL188363 | — | — | 1 | 5.98 |
| CHEMBL40607 | — | — | 1 | 5.88 |
| CHEMBL186918 | — | — | 1 | 5.72 |
| CHEMBL188953 | — | — | 1 | 5.63 |
| CHEMBL361268 | — | — | 1 | 5.63 |
| CHEMBL436084 | — | — | 1 | 5.59 |
| CHEMBL185803 | — | — | 1 | 5.46 |
| CHEMBL187429 | — | — | 1 | 5.38 |
| CHEMBL280518 | — | — | 1 | 5.23 |
| CHEMBL2096807 | — | — | 1 | 5.18 |
| CHEMBL364561 | — | — | 1 | 5.08 |
| CHEMBL408192 | — | — | 1 | 5.06 |
| CHEMBL189084 | — | — | 1 | 5.05 |
| CHEMBL189805 | — | — | 1 | 4.91 |
| CHEMBL187142 | — | — | 1 | 4.72 |
| CHEMBL189713 | — | — | 1 | - |
| CHEMBL362707 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL543876 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL39262 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL189082 | — | IC50 | = | 434.0 | nM | 6.36 |
| CHEMBL189095 | — | IC50 | = | 672.0 | nM | 6.17 |
| CHEMBL370805 | COCAINE | IC50 | = | 737.0 | nM | 6.13 |
| CHEMBL188363 | — | IC50 | = | 1040.0 | nM | 5.98 |
| CHEMBL40607 | — | IC50 | = | 1330.0 | nM | 5.88 |
| CHEMBL186918 | — | IC50 | = | 1890.0 | nM | 5.72 |
| CHEMBL188953 | — | IC50 | = | 2360.0 | nM | 5.63 |
| CHEMBL361268 | — | IC50 | = | 2340.0 | nM | 5.63 |
| CHEMBL436084 | — | IC50 | = | 2550.0 | nM | 5.59 |
| CHEMBL185803 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL187429 | — | IC50 | = | 4130.0 | nM | 5.38 |
| CHEMBL280518 | — | IC50 | = | 5830.0 | nM | 5.23 |
| CHEMBL2096807 | — | IC50 | = | 6630.0 | nM | 5.18 |
| CHEMBL364561 | — | IC50 | = | 8320.0 | nM | 5.08 |
| CHEMBL408192 | — | IC50 | = | 8650.0 | nM | 5.06 |
| CHEMBL189084 | — | IC50 | = | 8860.0 | nM | 5.05 |
| CHEMBL189805 | — | IC50 | = | 12200.0 | nM | 4.91 |
| CHEMBL187142 | — | IC50 | = | 18900.0 | nM | 4.72 |
| CHEMBL189713 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL362707 | — | IC50 | = | 157000.0 | nM | - |