Assay Detail
Functional
CHEMBL828033
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Inhibition of rat brain Norepinephrine transporter as accumulation of [3H]NE
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Discovery of novel trisubstituted asymmetric derivatives of (2S,4R,5R)-2-benzhydryl-5-benzylaminotetrahydropyran-4-ol, exhibiting high affinity for serotonin and norepinephrine transporters in a stereospecific manner.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.70 | 8.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2113048 | — | — | 1 | 8.25 |
| CHEMBL2112061 | — | — | 1 | 7.88 |
| CHEMBL211484 | — | — | 1 | 7.75 |
| CHEMBL2112057 | — | — | 1 | 7.11 |
| CHEMBL2113053 | — | — | 1 | 6.97 |
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 6.94 |
| CHEMBL2113050 | — | — | 1 | 6.94 |
| CHEMBL2113049 | — | — | 1 | 6.47 |
| CHEMBL2113044 | — | — | 1 | 6.36 |
| CHEMBL2112056 | — | — | 1 | 6.35 |
| CHEMBL2113052 | — | — | 1 | 6.12 |
| CHEMBL2112058 | — | — | 1 | 6.11 |
| CHEMBL2113047 | — | — | 1 | 5.95 |
| CHEMBL2112059 | — | — | 1 | 5.74 |
| CHEMBL2112060 | — | — | 1 | 5.49 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2113048 | — | IC50 | = | 5.59 | nM | 8.25 |
| CHEMBL2112061 | — | IC50 | = | 13.3 | nM | 7.88 |
| CHEMBL211484 | — | IC50 | = | 17.7 | nM | 7.75 |
| CHEMBL2112057 | — | IC50 | = | 77.3 | nM | 7.11 |
| CHEMBL2113053 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL281594 | VANOXERINE | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL2113050 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL2113049 | — | IC50 | = | 336.0 | nM | 6.47 |
| CHEMBL2113044 | — | IC50 | = | 439.0 | nM | 6.36 |
| CHEMBL2112056 | — | IC50 | = | 445.0 | nM | 6.35 |
| CHEMBL2113052 | — | IC50 | = | 765.0 | nM | 6.12 |
| CHEMBL2112058 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL2113047 | — | IC50 | = | 1130.0 | nM | 5.95 |
| CHEMBL2112059 | — | IC50 | = | 1840.0 | nM | 5.74 |
| CHEMBL2112060 | — | IC50 | = | 3220.0 | nM | 5.49 |