Assay Detail
Binding
CHEMBL809443
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In vitro binding affinity towards serotonin transporter using [3H]citalopram as radioligand in rat cerebral cortex membranes
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cerebral cortex |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium-dependent serotonin transporter (CHEMBL313) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
SAR development of a selective 5-HT1D antagonist/serotonin reuptake inhibitor lead using rapid parallel synthesis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 27 | 8.85 | 9.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL83617 | — | — | 1 | 9.96 |
| CHEMBL1159649 | — | — | 1 | 9.70 |
| CHEMBL84305 | — | — | 1 | 9.55 |
| CHEMBL82488 | — | — | 1 | 9.54 |
| CHEMBL82523 | — | — | 1 | 9.52 |
| CHEMBL1169435 | — | — | 1 | 9.52 |
| CHEMBL309872 | — | — | 1 | 9.42 |
| CHEMBL441259 | — | — | 1 | 9.30 |
| CHEMBL442974 | — | — | 1 | 9.27 |
| CHEMBL83112 | — | — | 1 | 9.12 |
| CHEMBL311787 | — | — | 1 | 9.11 |
| CHEMBL311323 | — | — | 1 | 9.01 |
| CHEMBL81703 | — | — | 1 | 9.00 |
| CHEMBL313452 | — | — | 1 | 9.00 |
| CHEMBL79561 | — | — | 1 | 8.80 |
| CHEMBL2112307 | — | — | 1 | 8.72 |
| CHEMBL79674 | — | — | 1 | 8.70 |
| CHEMBL79725 | — | — | 1 | 8.68 |
| CHEMBL311694 | — | — | 1 | 8.68 |
| CHEMBL310082 | — | — | 1 | 8.66 |
| CHEMBL81191 | — | — | 1 | 8.49 |
| CHEMBL84171 | — | — | 1 | 8.46 |
| CHEMBL79853 | — | — | 1 | 8.10 |
| CHEMBL83732 | — | — | 1 | 7.89 |
| CHEMBL79693 | — | — | 1 | 7.82 |
| CHEMBL310744 | — | — | 1 | 7.72 |
| CHEMBL444843 | — | — | 1 | 7.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL83617 | — | Ki | = | 0.11 | nM | 9.96 |
| CHEMBL1159649 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL84305 | — | Ki | = | 0.28 | nM | 9.55 |
| CHEMBL82488 | — | Ki | = | 0.29 | nM | 9.54 |
| CHEMBL82523 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL1169435 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL309872 | — | Ki | = | 0.38 | nM | 9.42 |
| CHEMBL441259 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL442974 | — | Ki | = | 0.54 | nM | 9.27 |
| CHEMBL83112 | — | Ki | = | 0.76 | nM | 9.12 |
| CHEMBL311787 | — | Ki | = | 0.78 | nM | 9.11 |
| CHEMBL311323 | — | Ki | = | 0.98 | nM | 9.01 |
| CHEMBL81703 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL313452 | — | Ki | = | 0.99 | nM | 9.00 |
| CHEMBL79561 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL2112307 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL79674 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL79725 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL311694 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL310082 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL81191 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL84171 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL79853 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL83732 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL79693 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL310744 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL444843 | — | Ki | = | 53.0 | nM | 7.28 |