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Assay Detail

CHEMBL797692

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

Functional
Inhibition of neuronal uptake of Noradrenaline in rat brain homogenate
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Tissue Brain
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Norepinephrine transporter (CHEMBL304)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Novel tacrine analogues for potential use against Alzheimer's disease: potent and selective acetylcholinesterase inhibitors and 5-HT uptake inhibitors.
McKenna MT, Proctor GR, Young LC, Harvey AL.
J Med Chem (1997) 40 : 3516 -3523
PubMed 9357518 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.52 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL117826 1 6.70
CHEMBL118752 1 6.22
CHEMBL118968 1 6.10
CHEMBL118033 1 5.85
CHEMBL72 DESIPRAMINE 4.0 1 5.77
CHEMBL332454 1 5.75
CHEMBL60167 1 5.64
CHEMBL325203 1 5.60
CHEMBL115697 1 5.52
CHEMBL119634 1 5.44
CHEMBL431844 1 5.21
CHEMBL330883 1 5.16
CHEMBL95 TACRINE 4.0 1 5.10
CHEMBL89012 1 4.92
CHEMBL119528 1 4.92
CHEMBL333011 1 4.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL117826 IC50 = 200.0 nM 6.70
CHEMBL118752 IC50 = 600.0 nM 6.22
CHEMBL118968 IC50 = 800.0 nM 6.10
CHEMBL118033 IC50 = 1400.0 nM 5.85
CHEMBL72 DESIPRAMINE IC50 = 1700.0 nM 5.77
CHEMBL332454 IC50 = 1800.0 nM 5.75
CHEMBL60167 IC50 = 2300.0 nM 5.64
CHEMBL325203 IC50 = 2500.0 nM 5.60
CHEMBL115697 IC50 = 3000.0 nM 5.52
CHEMBL119634 IC50 = 3600.0 nM 5.44
CHEMBL431844 IC50 = 6100.0 nM 5.21
CHEMBL330883 IC50 = 6900.0 nM 5.16
CHEMBL95 TACRINE IC50 = 7900.0 nM 5.10
CHEMBL89012 IC50 = 12100.0 nM 4.92
CHEMBL119528 IC50 = 12000.0 nM 4.92
CHEMBL333011 IC50 = 41040.0 nM 4.39