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Assay Detail

CHEMBL5133661

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

Binding
Inhibition of human AChE 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

Acetylcholine receptor subunit epsilon (CHEMBL2484)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of novel 2-aminoalkyl-6-(2-hydroxyphenyl)pyridazin-3(2H)-one derivatives as balanced multifunctional agents against Alzheimer's disease.
Shi Y, Zhang H, Song Q, Yu G, Liu Z, Zhong F, Tan Z, Liu X, Deng Y.
Eur J Med Chem (2022) 230 : 114098 -114098
PubMed 35026532 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.27 8.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5179810 1 8.64
CHEMBL5204683 1 7.92
CHEMBL502 DONEPEZIL 4.0 1 7.49
CHEMBL5181578 1 7.49
CHEMBL5176418 1 7.44
CHEMBL5173121 1 7.36
CHEMBL5207035 1 7.24
CHEMBL5190924 1 7.15
CHEMBL5188135 1 7.08
CHEMBL5200573 1 7.06
CHEMBL5179648 1 7.04
CHEMBL5196896 1 6.39
CHEMBL5206933 1 6.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5179810 IC50 = 2.291 nM 8.64
CHEMBL5204683 IC50 = 12.02 nM 7.92
CHEMBL502 DONEPEZIL IC50 = 32.36 nM 7.49
CHEMBL5181578 IC50 = 32.36 nM 7.49
CHEMBL5176418 IC50 = 36.31 nM 7.44
CHEMBL5173121 IC50 = 43.65 nM 7.36
CHEMBL5207035 IC50 = 57.54 nM 7.24
CHEMBL5190924 IC50 = 70.79 nM 7.15
CHEMBL5188135 IC50 = 83.18 nM 7.08
CHEMBL5200573 IC50 = 87.1 nM 7.06
CHEMBL5179648 IC50 = 91.2 nM 7.04
CHEMBL5196896 IC50 = 407.38 nM 6.39
CHEMBL5206933 IC50 = 676.08 nM 6.17