Assay Detail
Binding
CHEMBL3102347
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Displacement of [3H]-dopamine from rat striatum DAT after 5 mins
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Flexible and biomimetic analogs of triple uptake inhibitor 4-((((3S,6S)-6-benzhydryltetrahydro-2H-pyran-3-yl)amino)methyl)phenol: Synthesis, biological characterization, and development of a pharmacophore model.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 6.70 | 7.95 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3099494 | — | — | 1 | 7.95 |
| CHEMBL3099495 | — | — | 1 | 7.49 |
| CHEMBL3099493 | — | — | 1 | 7.42 |
| CHEMBL211077 | — | — | 1 | 7.38 |
| CHEMBL3099502 | — | — | 1 | 7.34 |
| CHEMBL213627 | — | — | 1 | 7.21 |
| CHEMBL209808 | — | — | 1 | 7.07 |
| CHEMBL3099501 | — | — | 1 | 6.61 |
| CHEMBL3099487 | — | — | 1 | 6.58 |
| CHEMBL3099488 | — | — | 1 | 6.58 |
| CHEMBL3099492 | — | — | 1 | 6.34 |
| CHEMBL3099489 | — | — | 1 | 6.23 |
| CHEMBL3099490 | — | — | 1 | 6.19 |
| CHEMBL3099485 | — | — | 1 | 6.04 |
| CHEMBL3099486 | — | — | 1 | 6.03 |
| CHEMBL41 | FLUOXETINE | 4.0 | 1 | 5.96 |
| CHEMBL3099491 | — | — | 1 | 5.43 |
| CHEMBL14370 | REBOXETINE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3099494 | — | Ki | = | 11.2 | nM | 7.95 |
| CHEMBL3099495 | — | Ki | = | 32.5 | nM | 7.49 |
| CHEMBL3099493 | — | Ki | = | 38.4 | nM | 7.42 |
| CHEMBL211077 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL3099502 | — | Ki | = | 45.7 | nM | 7.34 |
| CHEMBL213627 | — | Ki | = | 62.4 | nM | 7.21 |
| CHEMBL209808 | — | Ki | = | 85.2 | nM | 7.07 |
| CHEMBL3099501 | — | Ki | = | 245.0 | nM | 6.61 |
| CHEMBL3099487 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL3099488 | — | Ki | = | 266.0 | nM | 6.58 |
| CHEMBL3099492 | — | Ki | = | 454.0 | nM | 6.34 |
| CHEMBL3099489 | — | Ki | = | 586.0 | nM | 6.23 |
| CHEMBL3099490 | — | Ki | = | 642.0 | nM | 6.19 |
| CHEMBL3099485 | — | Ki | = | 920.0 | nM | 6.04 |
| CHEMBL3099486 | — | Ki | = | 943.0 | nM | 6.03 |
| CHEMBL41 | FLUOXETINE | Ki | = | 1092.0 | nM | 5.96 |
| CHEMBL3099491 | — | Ki | = | 3690.0 | nM | 5.43 |
| CHEMBL14370 | REBOXETINE | Ki | > | 10000.0 | nM | - |