Assay Detail
Binding
CHEMBL838676
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Inhibitory constant against reuptake of [3H]NE at norepinephrine transporter of rat parietal-occipital cortex
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Discovery of novel conformationally constrained tropane-based biaryl and arylacetylene ligands as potent and selective norepinephrine transporter inhibitors and potential antidepressants.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 7.43 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2113083 | — | — | 1 | 9.10 |
| CHEMBL2113081 | — | — | 1 | 8.89 |
| CHEMBL195404 | — | — | 1 | 8.30 |
| CHEMBL195181 | — | — | 1 | 8.28 |
| CHEMBL195146 | — | — | 1 | 8.23 |
| CHEMBL371349 | — | — | 1 | 8.19 |
| CHEMBL72 | DESIPRAMINE | 4.0 | 1 | 8.13 |
| CHEMBL195138 | — | — | 1 | 8.06 |
| CHEMBL195475 | — | — | 1 | 8.03 |
| CHEMBL371344 | — | — | 1 | 7.28 |
| CHEMBL371816 | — | — | 1 | 7.28 |
| CHEMBL363189 | — | — | 1 | 7.21 |
| CHEMBL371679 | — | — | 1 | 6.98 |
| CHEMBL194439 | — | — | 1 | 6.96 |
| CHEMBL334027 | — | — | 1 | 6.56 |
| CHEMBL191985 | — | — | 1 | 6.41 |
| CHEMBL365519 | — | — | 1 | 5.80 |
| CHEMBL195709 | — | — | 1 | 5.76 |
| CHEMBL193806 | — | — | 1 | 5.68 |
| CHEMBL194024 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2113083 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL2113081 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL195404 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL195181 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL195146 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL371349 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL72 | DESIPRAMINE | Ki | = | 7.36 | nM | 8.13 |
| CHEMBL195138 | — | Ki | = | 8.8 | nM | 8.06 |
| CHEMBL195475 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL371344 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL371816 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL363189 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL371679 | — | Ki | = | 104.0 | nM | 6.98 |
| CHEMBL194439 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL334027 | — | Ki | = | 273.0 | nM | 6.56 |
| CHEMBL191985 | — | Ki | = | 393.0 | nM | 6.41 |
| CHEMBL365519 | — | Ki | = | 1570.0 | nM | 5.80 |
| CHEMBL195709 | — | Ki | = | 1720.0 | nM | 5.76 |
| CHEMBL193806 | — | Ki | = | 2110.0 | nM | 5.68 |
| CHEMBL194024 | — | Ki | > | 10000.0 | nM | - |