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Assay Detail

CHEMBL872842

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

Binding
Affinity at norepinephrine transporter (NET) in rat striatum, using [3H]- nisoxatine as radioligand
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Striatum
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Norepinephrine transporter (CHEMBL304)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Structure-activity relationship studies of 4-[2-(diphenylmethoxy)ethyl]-1-benzylpiperidine derivatives and their N-analogues: evaluation of O-and N-analogues and their binding to monoamine transporters.
Dutta AK, Fei XS, Beardsley PM, Newman JL, Reith ME.
J Med Chem (2001) 44 : 937 -948
PubMed 11300876 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.00 6.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL35239 1 6.47
CHEMBL281594 VANOXERINE 3.0 1 6.30
CHEMBL424005 1 6.16
CHEMBL433733 1 6.04
CHEMBL110530 1 6.03
CHEMBL369406 1 5.99
CHEMBL39262 1 5.96
CHEMBL159128 1 5.58
CHEMBL370805 COCAINE 4.0 1 5.45

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL35239 IC50 = 342.0 nM 6.47
CHEMBL281594 VANOXERINE IC50 = 496.0 nM 6.30
CHEMBL424005 IC50 = 691.0 nM 6.16
CHEMBL433733 IC50 = 921.0 nM 6.04
CHEMBL110530 IC50 = 945.0 nM 6.03
CHEMBL369406 IC50 = 1027.0 nM 5.99
CHEMBL39262 IC50 = 1110.0 nM 5.96
CHEMBL159128 IC50 = 2620.0 nM 5.58
CHEMBL370805 COCAINE IC50 = 3530.0 nM 5.45