Assay Detail
Binding
CHEMBL3102345
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Displacement of [3H]-dopamine from rat cerebral cortex NET after 7 mins
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
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 | 7.16 | 9.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL14370 | REBOXETINE | 4.0 | 1 | 9.16 |
| CHEMBL3099493 | — | — | 1 | 8.38 |
| CHEMBL3099494 | — | — | 1 | 8.21 |
| CHEMBL3099495 | — | — | 1 | 8.08 |
| CHEMBL213627 | — | — | 1 | 7.90 |
| CHEMBL209808 | — | — | 1 | 7.59 |
| CHEMBL211077 | — | — | 1 | 7.52 |
| CHEMBL3099502 | — | — | 1 | 7.42 |
| CHEMBL41 | FLUOXETINE | 4.0 | 1 | 6.80 |
| CHEMBL3099487 | — | — | 1 | 6.78 |
| CHEMBL3099501 | — | — | 1 | 6.74 |
| CHEMBL3099489 | — | — | 1 | 6.71 |
| CHEMBL3099488 | — | — | 1 | 6.70 |
| CHEMBL3099485 | — | — | 1 | 6.62 |
| CHEMBL3099490 | — | — | 1 | 6.37 |
| CHEMBL3099492 | — | — | 1 | 6.13 |
| CHEMBL3099491 | — | — | 1 | 6.01 |
| CHEMBL3099486 | — | — | 1 | 5.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL14370 | REBOXETINE | Ki | = | 0.69 | nM | 9.16 |
| CHEMBL3099493 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL3099494 | — | Ki | = | 6.1 | nM | 8.21 |
| CHEMBL3099495 | — | Ki | = | 8.4 | nM | 8.08 |
| CHEMBL213627 | — | Ki | = | 12.6 | nM | 7.90 |
| CHEMBL209808 | — | Ki | = | 25.5 | nM | 7.59 |
| CHEMBL211077 | — | Ki | = | 30.5 | nM | 7.52 |
| CHEMBL3099502 | — | Ki | = | 37.7 | nM | 7.42 |
| CHEMBL41 | FLUOXETINE | Ki | = | 158.0 | nM | 6.80 |
| CHEMBL3099487 | — | Ki | = | 165.0 | nM | 6.78 |
| CHEMBL3099501 | — | Ki | = | 181.0 | nM | 6.74 |
| CHEMBL3099489 | — | Ki | = | 196.0 | nM | 6.71 |
| CHEMBL3099488 | — | Ki | = | 198.0 | nM | 6.70 |
| CHEMBL3099485 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL3099490 | — | Ki | = | 427.0 | nM | 6.37 |
| CHEMBL3099492 | — | Ki | = | 739.0 | nM | 6.13 |
| CHEMBL3099491 | — | Ki | = | 975.0 | nM | 6.01 |
| CHEMBL3099486 | — | Ki | = | 1511.0 | nM | 5.82 |