Assay Detail
Binding
CHEMBL879550
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Inhibition of [3H]WIN-35428 binding to dopamine transporter using of Cynomolgus monkey caudate-putamen
14
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Macaca fascicularis |
| Tissue | Caudate-putamen |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL5032) ↗| Type | SINGLE PROTEIN |
| Organism | Macaca fascicularis |
Publication
A technetium-99m SPECT imaging agent which targets the dopamine transporter in primate brain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 7.33 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54628 | — | — | 1 | 8.85 |
| CHEMBL55097 | — | — | 1 | 8.47 |
| CHEMBL119561 | O-1186 | — | 4 | 8.39 |
| CHEMBL300183 | — | — | 1 | 7.66 |
| CHEMBL118075 | O-863 | — | 1 | 7.43 |
| CHEMBL299890 | — | — | 1 | 7.23 |
| CHEMBL53200 | — | — | 1 | 7.00 |
| CHEMBL55174 | — | — | 1 | 6.65 |
| 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) | — | 3 | 6.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54628 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL55097 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL119561 | O-1186 | IC50 | = | 4.04 | nM | 8.39 |
| CHEMBL119561 | O-1186 | IC50 | = | 5.99 | nM | 8.22 |
| CHEMBL119561 | O-1186 | IC50 | = | 7.38 | nM | 8.13 |
| CHEMBL300183 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL118075 | O-863 | IC50 | = | 37.2 | nM | 7.43 |
| CHEMBL299890 | — | IC50 | = | 58.9 | nM | 7.23 |
| CHEMBL53200 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL55174 | — | IC50 | = | 223.0 | nM | 6.65 |
| 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 | = | 343.0 | nM | 6.46 |
| 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 | = | 482.0 | nM | 6.32 |
| 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 | = | 616.0 | nM | 6.21 |
| CHEMBL119561 | O-1186 | IC50 | = | 2960.0 | nM | 5.53 |