Assay Detail
Binding
CHEMBL853393
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Inhibition of NET-mediated [3H]NE uptake in rat cerebral cortex
15
Total Activities
15
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
Further structural exploration of trisubstituted asymmetric pyran derivatives (2S,4R,5R)-2-benzhydryl-5-benzylamino-tetrahydropyran-4-ol and their corresponding disubstituted (3S,6S) pyran derivatives: a proposed pharmacophore model for high-affinity interaction with the dopamine, serotonin, and norepinephrine transporters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 7.74 | 8.67 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL209808 | — | — | 1 | 8.67 |
| CHEMBL377129 | — | — | 1 | 8.31 |
| CHEMBL211077 | — | — | 1 | 8.29 |
| CHEMBL209603 | — | — | 1 | 8.18 |
| CHEMBL211994 | — | — | 1 | 7.98 |
| CHEMBL213627 | — | — | 1 | 7.90 |
| CHEMBL379716 | — | — | 1 | 7.88 |
| CHEMBL378437 | — | — | 1 | 7.81 |
| CHEMBL211484 | — | — | 1 | 7.80 |
| CHEMBL209843 | — | — | 1 | 7.59 |
| CHEMBL209809 | — | — | 1 | 7.39 |
| CHEMBL211302 | — | — | 1 | 7.26 |
| CHEMBL209651 | — | — | 1 | 7.09 |
| CHEMBL379706 | — | — | 1 | 7.03 |
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 6.99 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL209808 | — | Ki | = | 2.13 | nM | 8.67 |
| CHEMBL377129 | — | Ki | = | 4.92 | nM | 8.31 |
| CHEMBL211077 | — | Ki | = | 5.09 | nM | 8.29 |
| CHEMBL209603 | — | Ki | = | 6.56 | nM | 8.18 |
| CHEMBL211994 | — | Ki | = | 10.4 | nM | 7.98 |
| CHEMBL213627 | — | Ki | = | 12.6 | nM | 7.90 |
| CHEMBL379716 | — | Ki | = | 13.2 | nM | 7.88 |
| CHEMBL378437 | — | Ki | = | 15.6 | nM | 7.81 |
| CHEMBL211484 | — | Ki | = | 15.8 | nM | 7.80 |
| CHEMBL209843 | — | Ki | = | 25.6 | nM | 7.59 |
| CHEMBL209809 | — | Ki | = | 40.9 | nM | 7.39 |
| CHEMBL211302 | — | Ki | = | 54.3 | nM | 7.26 |
| CHEMBL209651 | — | Ki | = | 81.6 | nM | 7.09 |
| CHEMBL379706 | — | Ki | = | 94.4 | nM | 7.03 |
| CHEMBL281594 | VANOXERINE | Ki | = | 102.0 | nM | 6.99 |