Assay Detail
Binding
CHEMBL747094
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Ability to inhibit reuptake of norepinephrine ([3H]NE) at norepinephrine transporter of rat parietal/occipital region
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Synthesis and pharmacological evaluation of (Z)-9-(heteroarylmethylene)-7-azatricyclo[4.3.1.0(3,7)]decanes: thiophene analogues as potent norepinephrine transporter inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 26 | 6.89 | 8.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL117047 | — | — | 1 | 8.31 |
| CHEMBL119477 | — | — | 1 | 8.30 |
| CHEMBL641 | ATOMOXETINE | 4.0 | 1 | 8.30 |
| CHEMBL72 | DESIPRAMINE | 4.0 | 1 | 8.13 |
| CHEMBL118261 | — | — | 1 | 8.01 |
| CHEMBL119137 | — | — | 1 | 7.99 |
| CHEMBL325404 | — | — | 1 | 7.87 |
| CHEMBL331425 | — | — | 1 | 7.70 |
| CHEMBL331565 | — | — | 1 | 7.58 |
| CHEMBL333912 | — | — | 1 | 7.48 |
| CHEMBL116369 | — | — | 1 | 7.43 |
| CHEMBL331639 | — | — | 1 | 7.24 |
| CHEMBL116431 | — | — | 1 | 7.01 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.97 |
| CHEMBL118725 | — | — | 1 | 6.94 |
| CHEMBL334027 | — | — | 1 | 6.56 |
| CHEMBL440332 | — | — | 1 | 6.51 |
| CHEMBL118853 | — | — | 1 | 6.44 |
| CHEMBL324031 | — | — | 1 | 6.21 |
| CHEMBL119706 | — | — | 1 | 6.07 |
| CHEMBL116374 | — | — | 1 | 5.71 |
| CHEMBL118530 | — | — | 1 | 5.67 |
| CHEMBL331321 | — | — | 1 | 5.65 |
| CHEMBL443281 | — | — | 1 | 5.19 |
| CHEMBL118500 | — | — | 1 | 5.03 |
| CHEMBL331780 | — | — | 1 | 4.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL117047 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL119477 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL641 | ATOMOXETINE | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL72 | DESIPRAMINE | Ki | = | 7.36 | nM | 8.13 |
| CHEMBL118261 | — | Ki | = | 9.7 | nM | 8.01 |
| CHEMBL119137 | — | Ki | = | 10.3 | nM | 7.99 |
| CHEMBL325404 | — | Ki | = | 13.5 | nM | 7.87 |
| CHEMBL331425 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL331565 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL333912 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL116369 | — | Ki | = | 36.8 | nM | 7.43 |
| CHEMBL331639 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL116431 | — | Ki | = | 98.0 | nM | 7.01 |
| CHEMBL370805 | COCAINE | Ki | = | 108.0 | nM | 6.97 |
| CHEMBL118725 | — | Ki | = | 115.0 | nM | 6.94 |
| CHEMBL334027 | — | Ki | = | 273.0 | nM | 6.56 |
| CHEMBL440332 | — | Ki | = | 308.0 | nM | 6.51 |
| CHEMBL118853 | — | Ki | = | 364.0 | nM | 6.44 |
| CHEMBL324031 | — | Ki | = | 624.0 | nM | 6.21 |
| CHEMBL119706 | — | Ki | = | 855.0 | nM | 6.07 |
| CHEMBL116374 | — | Ki | = | 1930.0 | nM | 5.71 |
| CHEMBL118530 | — | Ki | = | 2130.0 | nM | 5.67 |
| CHEMBL331321 | — | Ki | = | 2250.0 | nM | 5.65 |
| CHEMBL443281 | — | Ki | = | 6510.0 | nM | 5.19 |
| CHEMBL118500 | — | Ki | = | 9450.0 | nM | 5.03 |
| CHEMBL331780 | — | Ki | = | 12700.0 | nM | 4.90 |