Assay Detail
Binding
CHEMBL2050196
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Displacement of [125I]IPT from DAT overexpressed in LLC-PK1 cell membrane by competitive binding assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | LLC-PK1 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent dopamine transporter (CHEMBL238) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and evaluation of novel tropane derivatives as potential PET imaging agents for the dopamine transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 7.79 | 8.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL543876 | — | — | 1 | 8.62 |
| CHEMBL2048520 | — | — | 1 | 8.58 |
| CHEMBL2048519 | — | — | 1 | 8.42 |
| CHEMBL2048521 | — | — | 1 | 8.33 |
| CHEMBL2048524 | — | — | 1 | 7.74 |
| CHEMBL2048525 | — | — | 1 | 7.57 |
| CHEMBL2048523 | — | — | 1 | 6.87 |
| CHEMBL2048522 | — | — | 1 | 6.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL543876 | — | Ki | = | 2.42 | nM | 8.62 |
| CHEMBL2048520 | — | Ki | = | 2.64 | nM | 8.58 |
| CHEMBL2048519 | — | Ki | = | 3.79 | nM | 8.42 |
| CHEMBL2048521 | — | Ki | = | 4.63 | nM | 8.33 |
| CHEMBL2048524 | — | Ki | = | 18.3 | nM | 7.74 |
| CHEMBL2048525 | — | Ki | = | 26.9 | nM | 7.57 |
| CHEMBL2048523 | — | Ki | = | 135.0 | nM | 6.87 |
| CHEMBL2048522 | — | Ki | = | 699.0 | nM | 6.16 |