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Assay Detail

CHEMBL3379812

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

Binding
Inhibition of human recombinant AChE assessed as dissociation constant for enzyme-inhibitor-substrate complex by Lineweaver-Burk plot
7
Total Activities
7
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

Synthesis and biological evaluation of novel tacrine derivatives and tacrine-coumarin hybrids as cholinesterase inhibitors.
Hamulakova S, Janovec L, Hrabinova M, Spilovska K, Korabecny J, Kristian P, Kuca K, Imrich J.
J Med Chem (2014) 57 : 7073 -7084
PubMed 25089370 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 5.95 7.63

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3322160 1 7.63
CHEMBL3322141 1 7.10
CHEMBL95 TACRINE 4.0 1 7.00
CHEMBL3322142 1 6.48
CHEMBL1256415 1 5.20
CHEMBL3322162 1 4.18
CHEMBL3322161 1 4.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3322160 Ki = 23.4 nM 7.63
CHEMBL3322141 Ki = 78.9 nM 7.10
CHEMBL95 TACRINE Ki = 101.0 nM 7.00
CHEMBL3322142 Ki = 328.0 nM 6.48
CHEMBL1256415 Ki = 6340.0 nM 5.20
CHEMBL3322162 Ki = 65300.0 nM 4.18
CHEMBL3322161 Ki = 92800.0 nM 4.03