Assay Detail
Binding
CHEMBL948898
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Inhibition of [3H]dopamine uptake at human dopamine transporter expressed in HEK293 cells
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent dopamine transporter (CHEMBL238) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
1-(2-Phenoxyphenyl)methanamines: SAR for dual serotonin/noradrenaline reuptake inhibition, metabolic stability and hERG affinity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 6.01 | 7.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL403090 | — | — | 1 | 7.33 |
| CHEMBL257423 | — | — | 1 | 6.91 |
| CHEMBL438889 | — | — | 1 | 6.86 |
| CHEMBL272493 | — | — | 1 | 6.76 |
| CHEMBL257424 | — | — | 1 | 6.71 |
| CHEMBL402057 | — | — | 1 | 6.71 |
| CHEMBL258062 | — | — | 1 | 6.56 |
| CHEMBL258060 | — | — | 1 | 6.50 |
| CHEMBL404317 | — | — | 1 | 6.41 |
| CHEMBL256819 | — | — | 1 | 6.38 |
| CHEMBL403071 | — | — | 1 | 6.38 |
| CHEMBL256816 | — | — | 1 | 6.30 |
| CHEMBL247733 | — | — | 1 | 6.14 |
| CHEMBL404754 | — | — | 1 | 6.10 |
| CHEMBL258271 | — | — | 1 | 5.92 |
| CHEMBL256817 | — | — | 1 | 5.67 |
| CHEMBL402851 | — | — | 1 | 5.56 |
| CHEMBL401819 | — | — | 1 | 5.55 |
| CHEMBL258063 | — | — | 1 | 5.52 |
| CHEMBL404258 | — | — | 1 | 5.42 |
| CHEMBL255957 | — | — | 1 | 5.22 |
| CHEMBL256168 | — | — | 1 | 5.19 |
| CHEMBL257481 | — | — | 1 | 4.80 |
| CHEMBL256818 | — | — | 1 | 4.71 |
| CHEMBL401877 | — | — | 1 | 4.68 |
| CHEMBL403441 | — | — | 1 | - |
| CHEMBL256058 | — | — | 1 | - |
| CHEMBL402345 | — | — | 1 | - |
| CHEMBL407815 | — | — | 1 | - |
| CHEMBL401878 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL403090 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL257423 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL438889 | — | IC50 | = | 138.0 | nM | 6.86 |
| CHEMBL272493 | — | IC50 | = | 172.0 | nM | 6.76 |
| CHEMBL257424 | — | IC50 | = | 194.0 | nM | 6.71 |
| CHEMBL402057 | — | IC50 | = | 195.0 | nM | 6.71 |
| CHEMBL258062 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL258060 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL404317 | — | IC50 | = | 387.0 | nM | 6.41 |
| CHEMBL256819 | — | IC50 | = | 421.0 | nM | 6.38 |
| CHEMBL403071 | — | IC50 | = | 421.0 | nM | 6.38 |
| CHEMBL256816 | — | IC50 | = | 506.0 | nM | 6.30 |
| CHEMBL247733 | — | IC50 | = | 727.0 | nM | 6.14 |
| CHEMBL404754 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL258271 | — | IC50 | = | 1210.0 | nM | 5.92 |
| CHEMBL256817 | — | IC50 | = | 2130.0 | nM | 5.67 |
| CHEMBL402851 | — | IC50 | = | 2730.0 | nM | 5.56 |
| CHEMBL401819 | — | IC50 | = | 2820.0 | nM | 5.55 |
| CHEMBL258063 | — | IC50 | = | 3010.0 | nM | 5.52 |
| CHEMBL404258 | — | IC50 | = | 3780.0 | nM | 5.42 |
| CHEMBL255957 | — | IC50 | = | 5950.0 | nM | 5.22 |
| CHEMBL256168 | — | IC50 | = | 6510.0 | nM | 5.19 |
| CHEMBL257481 | — | IC50 | = | 15700.0 | nM | 4.80 |
| CHEMBL256818 | — | IC50 | = | 19600.0 | nM | 4.71 |
| CHEMBL401877 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL403441 | — | IC50 | > | 400.0 | nM | - |
| CHEMBL256058 | — | IC50 | - | — | - | |
| CHEMBL402345 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL407815 | — | IC50 | - | — | - | |
| CHEMBL401878 | — | IC50 | > | 40000.0 | nM | - |