Assay Detail
Binding
CHEMBL840038
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Displacement of [3H]nisoxetine from norepinephrine transporter of rat cerebral cortex
13
Total Activities
13
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 | Expert |
Publication
Synthesis and monoamine transporter affinity of new 2beta-carbomethoxy-3beta-[4-(substituted thiophenyl)]phenyltropanes: discovery of a selective SERT antagonist with picomolar potency.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 6.62 | 8.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL14391 | — | — | 1 | 8.55 |
| CHEMBL179498 | — | — | 1 | 7.41 |
| CHEMBL181557 | — | — | 1 | 7.12 |
| CHEMBL181609 | — | — | 1 | 6.80 |
| CHEMBL435287 | — | — | 1 | 6.72 |
| CHEMBL369098 | — | — | 1 | 6.51 |
| CHEMBL180918 | — | — | 1 | 6.49 |
| CHEMBL178773 | — | — | 1 | 5.94 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 5.48 |
| CHEMBL549 | CITALOPRAM | 4.0 | 1 | 5.21 |
| CHEMBL433560 | — | — | 1 | - |
| CHEMBL181613 | — | — | 1 | - |
| CHEMBL180618 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL14391 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL179498 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL181557 | — | Ki | = | 75.3 | nM | 7.12 |
| CHEMBL181609 | — | Ki | = | 158.0 | nM | 6.80 |
| CHEMBL435287 | — | Ki | = | 189.0 | nM | 6.72 |
| CHEMBL369098 | — | Ki | = | 311.0 | nM | 6.51 |
| CHEMBL180918 | — | Ki | = | 324.0 | nM | 6.49 |
| CHEMBL178773 | — | Ki | = | 1137.0 | nM | 5.94 |
| CHEMBL370805 | COCAINE | Ki | = | 3320.0 | nM | 5.48 |
| CHEMBL549 | CITALOPRAM | Ki | = | 6190.0 | nM | 5.21 |
| CHEMBL433560 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL181613 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL180618 | — | Ki | > | 10000.0 | nM | - |