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Assay Detail

CHEMBL2050778

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of [3H]noradrenaline uptake at human NET expressed in CHO cells after 10 mins by scintillation counting
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sodium-dependent noradrenaline transporter (CHEMBL222)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and antidepressant activity of arylalkanol-piperidine derivatives as triple reuptake inhibitors.
Zheng YY, Guo L, Zhen XC, Li JQ.
Eur J Med Chem (2012) 54 : 123 -136
PubMed 22608762 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.52 7.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1818442 AMITIFADINE HYDROCHLORIDE 2.0 1 7.15
CHEMBL2047574 1 6.75
CHEMBL2047573 1 6.58
CHEMBL2047561 1 6.49
CHEMBL2047570 1 6.42
CHEMBL2047571 1 6.38
CHEMBL2047580 1 6.28
CHEMBL2047572 1 6.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1818442 AMITIFADINE HYDROCHLORIDE IC50 = 71.0 nM 7.15
CHEMBL2047574 IC50 = 178.0 nM 6.75
CHEMBL2047573 IC50 = 265.0 nM 6.58
CHEMBL2047561 IC50 = 327.0 nM 6.49
CHEMBL2047570 IC50 = 385.0 nM 6.42
CHEMBL2047571 IC50 = 420.0 nM 6.38
CHEMBL2047580 IC50 = 531.0 nM 6.28
CHEMBL2047572 IC50 = 800.0 nM 6.10