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Assay Detail

CHEMBL985545

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

Binding
Inhibition of [3H]NA uptake at human NET expressed in HEK293 cells
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Derivatives of (3S)-N-(biphenyl-2-ylmethyl)pyrrolidin-3-amine as selective noradrenaline reuptake inhibitors: Reducing P-gp mediated efflux by modulation of H-bond acceptor capacity.
Fish PV, Barta NS, Gray DL, Ryckmans T, Stobie A, Wakenhut F, Whitlock GA.
Bioorg Med Chem Lett (2008) 18 : 4355 -4359
PubMed 18621528 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.95 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL245880 1 8.30
CHEMBL245687 1 7.92
CHEMBL476954 1 7.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL245880 IC50 = 5.0 nM 8.30
CHEMBL245687 IC50 = 12.0 nM 7.92
CHEMBL476954 IC50 = 23.0 nM 7.64