Assay Detail
Binding
CHEMBL977015
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Displacement of [125I]RTI55 from DAT
33
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Sodium-dependent dopamine transporter (CHEMBL238) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design and synthesis of 2- and 3-substituted-3-phenylpropyl analogs of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine and 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine: role of amino, fluoro, hydroxyl, methoxyl, methyl, methylene, and oxo substituents on affinity for the dopamine and serotonin transporters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 33 | 7.70 | 9.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL27646 | — | — | 1 | 9.12 |
| CHEMBL28149 | — | — | 1 | 8.64 |
| CHEMBL468211 | — | — | 1 | 8.57 |
| CHEMBL26477 | — | — | 1 | 8.52 |
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 8.43 |
| CHEMBL26320 | — | — | 1 | 8.43 |
| CHEMBL512636 | — | — | 1 | 8.40 |
| CHEMBL26478 | — | — | 1 | 8.36 |
| CHEMBL511950 | — | — | 1 | 8.19 |
| CHEMBL469165 | — | — | 1 | 8.15 |
| CHEMBL26649 | — | — | 1 | 8.10 |
| CHEMBL466750 | — | — | 1 | 8.00 |
| CHEMBL27490 | — | — | 1 | 7.92 |
| CHEMBL511718 | — | — | 2 | 7.77 |
| CHEMBL467585 | — | — | 1 | 7.75 |
| CHEMBL466936 | — | — | 1 | 7.70 |
| CHEMBL468212 | — | — | 1 | 7.66 |
| CHEMBL282380 | — | — | 1 | 7.60 |
| CHEMBL468573 | — | — | 1 | 7.57 |
| CHEMBL513858 | — | — | 1 | 7.54 |
| CHEMBL467757 | — | — | 1 | 7.52 |
| CHEMBL466145 | — | — | 1 | 7.41 |
| CHEMBL283662 | — | — | 1 | 7.32 |
| CHEMBL468207 | — | — | 1 | 7.27 |
| CHEMBL468376 | — | — | 1 | 7.24 |
| CHEMBL466538 | — | — | 1 | 7.00 |
| CHEMBL513859 | — | — | 1 | 6.96 |
| CHEMBL468208 | — | — | 1 | 6.85 |
| CHEMBL512280 | — | — | 1 | 6.82 |
| CHEMBL27907 | — | — | 1 | 6.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL27646 | — | Ki | = | 0.75 | nM | 9.12 |
| CHEMBL28149 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL468211 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL26477 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL281594 | VANOXERINE | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL26320 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL512636 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL26478 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL511950 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL469165 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL26649 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL466750 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL27490 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL511718 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL511718 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL467585 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL466936 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL468212 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL282380 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL468573 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL513858 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL467757 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL466145 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL283662 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL468207 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL468376 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL466538 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL513859 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL468208 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL512280 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL27907 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL466733 | — | Ki | = | 410.0 | nM | 6.39 |
| CHEMBL511756 | — | Ki | = | 450.0 | nM | 6.35 |