Assay Detail
Binding
CHEMBL672118
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Tested for the ability to displace [125I]- RTI-55 binding in rat striatal membrane against dopamine transporter
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Striatum |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis of iodinated 3beta-aryltropanes with selective binding to either the dopamine or serotonin transporters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 7.94 | 10.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL168455 | — | — | 1 | 10.11 |
| CHEMBL169117 | — | — | 1 | 10.07 |
| CHEMBL355650 | — | — | 1 | 9.42 |
| CHEMBL355734 | — | — | 1 | 8.97 |
| CHEMBL352698 | — | — | 1 | 8.77 |
| CHEMBL354725 | — | — | 1 | 8.66 |
| CHEMBL169320 | — | — | 1 | 7.88 |
| CHEMBL171565 | — | — | 1 | 7.70 |
| CHEMBL2112943 | — | — | 1 | 7.33 |
| CHEMBL352913 | — | — | 1 | 7.29 |
| CHEMBL168305 | — | — | 1 | 7.25 |
| CHEMBL355259 | — | — | 1 | 7.18 |
| CHEMBL423275 | — | — | 1 | 6.40 |
| CHEMBL169361 | — | — | 1 | 6.12 |
| CHEMBL355733 | — | — | 1 | 5.95 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL168455 | — | IC50 | = | 0.077 | nM | 10.11 |
| CHEMBL169117 | — | IC50 | = | 0.085 | nM | 10.07 |
| CHEMBL355650 | — | IC50 | = | 0.38 | nM | 9.42 |
| CHEMBL355734 | — | IC50 | = | 1.08 | nM | 8.97 |
| CHEMBL352698 | — | IC50 | = | 1.69 | nM | 8.77 |
| CHEMBL354725 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL169320 | — | IC50 | = | 13.3 | nM | 7.88 |
| CHEMBL171565 | — | IC50 | = | 19.8 | nM | 7.70 |
| CHEMBL2112943 | — | IC50 | = | 47.2 | nM | 7.33 |
| CHEMBL352913 | — | IC50 | = | 51.3 | nM | 7.29 |
| CHEMBL168305 | — | IC50 | = | 56.5 | nM | 7.25 |
| CHEMBL355259 | — | IC50 | = | 66.5 | nM | 7.18 |
| CHEMBL423275 | — | IC50 | = | 401.0 | nM | 6.40 |
| CHEMBL169361 | — | IC50 | = | 753.0 | nM | 6.12 |
| CHEMBL355733 | — | IC50 | = | 1120.0 | nM | 5.95 |