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Assay Detail

CHEMBL3875277

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

Binding
Inhibition of human recombinant AChE preincubated for 5 mins followed by acetylthiocholine iodide substrate addition measured after 5 mins by Ellman's method
8
Total Activities
8
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

Acetylcholinesterase (CHEMBL220)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel multi-target-directed ligands for Alzheimer's disease: Combining cholinesterase inhibitors and 5-HT6 receptor antagonists. Design, synthesis and biological evaluation.
Więckowska A, Kołaczkowski M, Bucki A, Godyń J, Marcinkowska M, Więckowski K, Zaręba P, Siwek A, Kazek G, Głuch-Lutwin M, Mierzejewski P, Bienkowski P, Sienkiewicz-Jarosz H, Knez D, Wichur T, Gobec S, Malawska B.
Eur J Med Chem (2016) 124 : 63 -81
PubMed 27560283 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.90 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3883432 1 8.89
CHEMBL502 DONEPEZIL 4.0 1 8.22
CHEMBL3884690 1 8.21
CHEMBL3884618 1 8.01
CHEMBL3885186 1 7.89
CHEMBL3884858 1 7.74
CHEMBL3884988 1 7.36
CHEMBL95 TACRINE 4.0 1 6.88

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3883432 IC50 = 1.3 nM 8.89
CHEMBL502 DONEPEZIL IC50 = 6.0 nM 8.22
CHEMBL3884690 IC50 = 6.2 nM 8.21
CHEMBL3884618 IC50 = 9.7 nM 8.01
CHEMBL3885186 IC50 = 12.9 nM 7.89
CHEMBL3884858 IC50 = 18.2 nM 7.74
CHEMBL3884988 IC50 = 43.6 nM 7.36
CHEMBL95 TACRINE IC50 = 131.0 nM 6.88