Assay Detail
Binding
CHEMBL749356
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Affinity for the displacement of [3H]paroxetine binding to norepinephrine transporter (NET) in rat frontal cortex membranes
17
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Frontal cortex |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Synthesis of 2beta-acyl-3beta-(substituted naphthyl)-8-azabicyclo[3.2.1]octanes and their binding affinities at dopamine and serotonin transport sites.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 6.97 | 8.69 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL36720 | — | — | 1 | 8.69 |
| CHEMBL418190 | — | — | 2 | 8.54 |
| CHEMBL22930 | — | — | 1 | 8.31 |
| CHEMBL34243 | — | — | 1 | 7.56 |
| CHEMBL39589 | — | — | 1 | 7.42 |
| CHEMBL278572 | — | — | 1 | 7.31 |
| CHEMBL23142 | — | — | 1 | 7.19 |
| CHEMBL39340 | — | — | 1 | 6.79 |
| CHEMBL23672 | — | — | 1 | 6.78 |
| CHEMBL289849 | — | — | 1 | 6.30 |
| CHEMBL290412 | — | — | 1 | 6.11 |
| CHEMBL39764 | — | — | 1 | 5.63 |
| CHEMBL287940 | — | — | 1 | 5.47 |
| CHEMBL285039 | — | — | 1 | 5.32 |
| CHEMBL278122 | — | — | 1 | - |
| CHEMBL290662 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL36720 | — | Ki | = | 2.05 | nM | 8.69 |
| CHEMBL418190 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL22930 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL34243 | — | Ki | = | 27.7 | nM | 7.56 |
| CHEMBL39589 | — | Ki | = | 37.6 | nM | 7.42 |
| CHEMBL278572 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL23142 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL418190 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL39340 | — | Ki | = | 163.0 | nM | 6.79 |
| CHEMBL23672 | — | Ki | = | 165.0 | nM | 6.78 |
| CHEMBL289849 | — | Ki | = | 498.0 | nM | 6.30 |
| CHEMBL290412 | — | Ki | = | 781.0 | nM | 6.11 |
| CHEMBL39764 | — | Ki | = | 2334.0 | nM | 5.63 |
| CHEMBL287940 | — | Ki | = | 3362.0 | nM | 5.47 |
| CHEMBL285039 | — | Ki | = | 4769.0 | nM | 5.32 |
| CHEMBL290662 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL278122 | — | Ki | > | 10000.0 | nM | - |