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Assay Detail

CHEMBL3379809

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Binding
Inhibition of human BuChE pre-incubated for 5 mins before butylthiocholine substrate addition by Ellman's method
13
Total Activities
13
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

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
IC50 13 5.94 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL95 TACRINE 4.0 1 7.64
CHEMBL3322142 1 6.64
CHEMBL3322141 1 6.57
CHEMBL3322160 1 6.48
CHEMBL3322140 1 6.12
CHEMBL3322159 1 6.08
CHEMBL3322161 1 5.85
CHEMBL3322155 1 5.69
CHEMBL3322157 1 5.65
CHEMBL3322156 1 5.62
CHEMBL3322162 1 5.25
CHEMBL3322158 1 4.90
CHEMBL1256415 1 4.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL95 TACRINE IC50 = 23.0 nM 7.64
CHEMBL3322142 IC50 = 228.0 nM 6.64
CHEMBL3322141 IC50 = 267.0 nM 6.57
CHEMBL3322160 IC50 = 328.0 nM 6.48
CHEMBL3322140 IC50 = 765.0 nM 6.12
CHEMBL3322159 IC50 = 827.0 nM 6.08
CHEMBL3322161 IC50 = 1420.0 nM 5.85
CHEMBL3322155 IC50 = 2030.0 nM 5.69
CHEMBL3322157 IC50 = 2230.0 nM 5.65
CHEMBL3322156 IC50 = 2380.0 nM 5.62
CHEMBL3322162 IC50 = 5620.0 nM 5.25
CHEMBL3322158 IC50 = 12600.0 nM 4.90
CHEMBL1256415 IC50 = 21000.0 nM 4.68