Assay Detail
Binding
CHEMBL3379358
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Displacement of [125I]-RTI-55 from recombinant DAT (unknown origin) expressed in HEK cells by saturation binding analysis
14
Total Activities
14
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
Design and synthesis of 4-heteroaryl 1,2,3,4-tetrahydroisoquinolines as triple reuptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 7.35 | 8.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3323181 | — | — | 1 | 8.51 |
| CHEMBL3323095 | — | — | 1 | 8.29 |
| CHEMBL3323184 | — | — | 1 | 8.24 |
| CHEMBL3323102 | — | — | 1 | 7.92 |
| CHEMBL3323104 | — | — | 1 | 7.64 |
| CHEMBL3323108 | — | — | 1 | 7.36 |
| CHEMBL3323106 | — | — | 1 | 7.28 |
| CHEMBL3323176 | — | — | 1 | 7.18 |
| CHEMBL3323107 | — | — | 1 | 7.11 |
| CHEMBL3323177 | — | — | 1 | 6.96 |
| CHEMBL3323100 | — | — | 1 | 6.96 |
| CHEMBL3323182 | — | — | 1 | 6.85 |
| CHEMBL3323105 | — | — | 1 | 6.57 |
| CHEMBL3323109 | — | — | 1 | 6.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3323181 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL3323095 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL3323184 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL3323102 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3323104 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3323108 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL3323106 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL3323176 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL3323107 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL3323177 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3323100 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3323182 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3323105 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL3323109 | — | IC50 | = | 890.0 | nM | 6.05 |