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Assay Detail

CHEMBL1068909

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

Binding
Inhibition of [3H]noradrenalin reuptake at human NET expressed in LLCPK cells by scintillation proximity assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

1-(Aryl)-6-[alkoxyalkyl]-3-azabicyclo[3.1.0]hexanes and 6-(aryl)-6-[alkoxyalkyl]-3-azabicyclo[3.1.0]hexanes: a new series of potent and selective triple reuptake inhibitors.
Micheli F, Cavanni P, Arban R, Benedetti R, Bertani B, Bettati M, Bettelini L, Bonanomi G, Braggio S, Checchia A, Davalli S, Di Fabio R, Fazzolari E, Fontana S, Marchioro C, Minick D, Negri M, Oliosi B, Read KD, Sartori I, Tedesco G, Tarsi L, Terreni S, Visentini F, Zocchi A, Zonzini L.
J Med Chem (2010) 53 : 2534 -2551
PubMed 20170186 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 9.60 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL608151 1 9.80
CHEMBL597000 1 9.60
CHEMBL2021580 1 9.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL608151 IC50 = 0.1585 nM 9.80
CHEMBL597000 IC50 = 0.2512 nM 9.60
CHEMBL2021580 IC50 = 0.3981 nM 9.40