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Assay Detail

CHEMBL755915

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

Binding
Compound was tested for the inhibition of norepinephrine [3H]NE reuptake into rat cortical membranes
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Norepinephrine transporter (CHEMBL304)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Discovery of substituted 3,4-diphenyl-thiazoles as a novel class of monoamine transporter inhibitors through 3-D pharmacophore search using a new pharmacophore model derived from mazindol.
Enyedy IJ, Wang J, Zaman WA, Johnson KM, Wang S.
Bioorg Med Chem Lett (2002) 12 : 1775 -1778
PubMed 12067559 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 6.72 7.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL296907 1 7.58
CHEMBL49736 1 7.44
CHEMBL301094 1 7.07
CHEMBL48892 1 7.00
CHEMBL120901 1 6.97
CHEMBL52392 1 6.85
CHEMBL297102 1 6.85
CHEMBL51993 1 6.10
CHEMBL50901 1 4.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL296907 Ki = 26.0 nM 7.58
CHEMBL49736 Ki = 36.0 nM 7.44
CHEMBL301094 Ki = 86.0 nM 7.07
CHEMBL48892 Ki = 99.0 nM 7.00
CHEMBL120901 Ki = 108.0 nM 6.97
CHEMBL52392 Ki = 141.0 nM 6.85
CHEMBL297102 Ki = 140.0 nM 6.85
CHEMBL51993 Ki = 801.0 nM 6.10
CHEMBL50901 Ki = 22100.0 nM 4.66