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Assay Detail

CHEMBL3595654

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

Binding
Inhibition of human recombinant BChE using butyrylthiocholine iodide as substrate after 5 mins by Ellman's method
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cholinesterase (CHEMBL1914)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-based development of nitroxoline derivatives as potential multifunctional anti-Alzheimer agents.
Knez D, Brus B, Coquelle N, Sosič I, Šink R, Brazzolotto X, Mravljak J, Colletier JP, Gobec S.
Bioorg Med Chem (2015) 23 : 4442 -4452
PubMed 26116179 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.99 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL95 TACRINE 4.0 1 7.92
CHEMBL3338391 1 7.68
CHEMBL3593658 1 6.67
CHEMBL3593652 1 5.67

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL95 TACRINE IC50 = 12.0 nM 7.92
CHEMBL3338391 IC50 = 21.0 nM 7.68
CHEMBL3593658 IC50 = 215.0 nM 6.67
CHEMBL3593652 IC50 = 2140.0 nM 5.67