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Assay Detail

CHEMBL1837219

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Binding
Inhibition of human AChE by Ellman's assay
25
Total Activities
25
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

Development of 2-substituted-N-(naphth-1-ylmethyl) and N-benzhydrylpyrimidin-4-amines as dual cholinesterase and Aβ-aggregation inhibitors: Synthesis and biological evaluation.
Mohamed T, Yeung JC, Rao PP.
Bioorg Med Chem Lett (2011) 21 : 5881 -5887
PubMed 21873056 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 4.96 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1678 DONEPEZIL HYDROCHLORIDE 4.0 1 7.50
CHEMBL95 TACRINE 4.0 1 7.11
CHEMBL1555 GALANTAMINE HYDROBROMIDE 4.0 1 5.50
CHEMBL1834063 1 5.10
CHEMBL1834067 1 5.01
CHEMBL1834074 1 5.00
CHEMBL1834068 1 4.93
CHEMBL1834064 1 4.86
CHEMBL1834069 1 4.86
CHEMBL1834073 1 4.84
CHEMBL1834060 1 4.80
CHEMBL1834061 1 4.78
CHEMBL1834066 1 4.76
CHEMBL1084213 1 4.76
CHEMBL1834062 1 4.72
CHEMBL1834071 1 4.69
CHEMBL1834078 1 4.67
CHEMBL1766151 1 4.59
CHEMBL1834075 1 4.54
CHEMBL1834077 1 4.50
CHEMBL1834070 1 4.49
CHEMBL1834079 1 4.41
CHEMBL1834072 1 4.37
CHEMBL1834065 1 4.29
CHEMBL1834076 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1678 DONEPEZIL HYDROCHLORIDE IC50 = 32.0 nM 7.50
CHEMBL95 TACRINE IC50 = 77.0 nM 7.11
CHEMBL1555 GALANTAMINE HYDROBROMIDE IC50 = 3200.0 nM 5.50
CHEMBL1834063 IC50 = 8000.0 nM 5.10
CHEMBL1834067 IC50 = 9800.0 nM 5.01
CHEMBL1834074 IC50 = 10000.0 nM 5.00
CHEMBL1834068 IC50 = 11700.0 nM 4.93
CHEMBL1834064 IC50 = 13800.0 nM 4.86
CHEMBL1834069 IC50 = 13700.0 nM 4.86
CHEMBL1834073 IC50 = 14600.0 nM 4.84
CHEMBL1834060 IC50 = 15800.0 nM 4.80
CHEMBL1834061 IC50 = 16700.0 nM 4.78
CHEMBL1834066 IC50 = 17500.0 nM 4.76
CHEMBL1084213 IC50 = 17500.0 nM 4.76
CHEMBL1834062 IC50 = 19000.0 nM 4.72
CHEMBL1834071 IC50 = 20300.0 nM 4.69
CHEMBL1834078 IC50 = 21600.0 nM 4.67
CHEMBL1766151 IC50 = 25800.0 nM 4.59
CHEMBL1834075 IC50 = 29000.0 nM 4.54
CHEMBL1834077 IC50 = 31300.0 nM 4.50
CHEMBL1834070 IC50 = 32200.0 nM 4.49
CHEMBL1834079 IC50 = 39200.0 nM 4.41
CHEMBL1834072 IC50 = 42500.0 nM 4.37
CHEMBL1834065 IC50 = 50800.0 nM 4.29
CHEMBL1834076 IC50 > 100000.0 nM -