Assay Detail
Binding
CHEMBL806863
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Inhibition of [3H]- citalopram binding to serotonin transporter of Cynomolgus monkey caudate-putamen
12
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | monkey |
| Tissue | Caudate-putamen |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium-dependent serotonin transporter (CHEMBL228) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
A technetium-99m SPECT imaging agent which targets the dopamine transporter in primate brain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 6.35 | 7.71 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL300183 | — | — | 1 | 7.71 |
| CHEMBL55097 | — | — | 1 | 7.30 |
| CHEMBL119561 | O-1186 | — | 4 | 7.17 |
| CHEMBL54628 | — | — | 1 | 6.88 |
| CHEMBL118075 | O-863 | — | 1 | 6.58 |
| CHEMBL53200 | — | — | 1 | 6.26 |
| CHEMBL299890 | — | — | 1 | 5.97 |
| CHEMBL55174 | — | — | 1 | 5.30 |
| CHEMBL55730 | [N-[2-[(3'-N'-PROPYL-3''ALPHA-(BIS(4-FLUORORPHENYL)METHOXY)TROPANE-2''BETA-CARBOXYLIC ACID METHYL ESTER)(2-MERCAPTOETHYL)AMINO]ACETYL]-2-AMINOETHANETHIOLATO]RHENIUM(V) OXIDE (DIASTEREOMERIC MIX) | — | 1 | 4.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL300183 | — | IC50 | = | 19.7 | nM | 7.71 |
| CHEMBL55097 | — | IC50 | = | 49.9 | nM | 7.30 |
| CHEMBL119561 | O-1186 | IC50 | = | 66.9 | nM | 7.17 |
| CHEMBL119561 | O-1186 | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL54628 | — | IC50 | = | 133.0 | nM | 6.88 |
| CHEMBL118075 | O-863 | IC50 | = | 264.0 | nM | 6.58 |
| CHEMBL119561 | O-1186 | IC50 | = | 299.0 | nM | 6.52 |
| CHEMBL53200 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL299890 | — | IC50 | = | 1073.0 | nM | 5.97 |
| CHEMBL55174 | — | IC50 | = | 4970.0 | nM | 5.30 |
| CHEMBL119561 | O-1186 | IC50 | = | 5020.0 | nM | 5.30 |
| CHEMBL55730 | [N-[2-[(3'-N'-PROPYL-3''ALPHA-(BIS(4-FLUORORPHENYL)METHOXY)TROPANE-2''BETA-CARBOXYLIC ACID METHYL ESTER)(2-MERCAPTOETHYL)AMINO]ACETYL]-2-AMINOETHANETHIOLATO]RHENIUM(V) OXIDE (DIASTEREOMERIC MIX) | IC50 | = | 55200.0 | nM | 4.26 |