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Assay Detail

CHEMBL902667

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

Binding
Inhibition of human serum recombinant AChE by Ellman's method
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Acetylcholinesterase (CHEMBL220)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Multi-target-directed drug design strategy: from a dual binding site acetylcholinesterase inhibitor to a trifunctional compound against Alzheimer's disease.
Bolognesi ML, Cavalli A, Valgimigli L, Bartolini M, Rosini M, Andrisano V, Recanatini M, Melchiorre C.
J Med Chem (2007) 50 : 6446 -6449
PubMed 18047264 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 8.02 9.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL32823 1 9.09
CHEMBL238230 1 8.74
CHEMBL440983 1 8.18
CHEMBL235014 1 7.71
CHEMBL95 TACRINE 4.0 1 6.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL32823 IC50 = 0.81 nM 9.09
CHEMBL238230 IC50 = 1.83 nM 8.74
CHEMBL440983 IC50 = 6.65 nM 8.18
CHEMBL235014 IC50 = 19.7 nM 7.71
CHEMBL95 TACRINE IC50 = 424.0 nM 6.37