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Assay Detail

CHEMBL1837220

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Binding
Inhibition of equine BuChE by Ellman's method
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Equus caballus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cholinesterase (CHEMBL5763)
Type SINGLE PROTEIN
Organism Equus caballus

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 4.99 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL95 TACRINE 4.0 1 7.68
CHEMBL1766151 1 5.66
CHEMBL1084213 1 5.58
CHEMBL1678 DONEPEZIL HYDROCHLORIDE 4.0 1 5.44
CHEMBL1834063 1 5.41
CHEMBL1834074 1 5.12
CHEMBL1834060 1 5.12
CHEMBL1834061 1 5.04
CHEMBL1834071 1 5.01
CHEMBL1555 GALANTAMINE HYDROBROMIDE 4.0 1 4.90
CHEMBL1834073 1 4.76
CHEMBL1834067 1 4.75
CHEMBL1834062 1 4.74
CHEMBL1834069 1 4.62
CHEMBL1834066 1 4.59
CHEMBL1834068 1 4.58
CHEMBL1834079 1 4.55
CHEMBL1834064 1 4.48
CHEMBL1834070 1 4.47
CHEMBL1834078 1 4.22
CHEMBL1834072 1 4.06
CHEMBL1834077 1 -
CHEMBL1834076 1 -
CHEMBL1834075 1 -
CHEMBL1834065 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL95 TACRINE IC50 = 21.0 nM 7.68
CHEMBL1766151 IC50 = 2200.0 nM 5.66
CHEMBL1084213 IC50 = 2600.0 nM 5.58
CHEMBL1678 DONEPEZIL HYDROCHLORIDE IC50 = 3600.0 nM 5.44
CHEMBL1834063 IC50 = 3900.0 nM 5.41
CHEMBL1834074 IC50 = 7600.0 nM 5.12
CHEMBL1834060 IC50 = 7600.0 nM 5.12
CHEMBL1834061 IC50 = 9100.0 nM 5.04
CHEMBL1834071 IC50 = 9700.0 nM 5.01
CHEMBL1555 GALANTAMINE HYDROBROMIDE IC50 = 12600.0 nM 4.90
CHEMBL1834073 IC50 = 17500.0 nM 4.76
CHEMBL1834067 IC50 = 17900.0 nM 4.75
CHEMBL1834062 IC50 = 18100.0 nM 4.74
CHEMBL1834069 IC50 = 23800.0 nM 4.62
CHEMBL1834066 IC50 = 25400.0 nM 4.59
CHEMBL1834068 IC50 = 26500.0 nM 4.58
CHEMBL1834079 IC50 = 28400.0 nM 4.55
CHEMBL1834064 IC50 = 32900.0 nM 4.48
CHEMBL1834070 IC50 = 33800.0 nM 4.47
CHEMBL1834078 IC50 = 59500.0 nM 4.22
CHEMBL1834072 IC50 = 87000.0 nM 4.06
CHEMBL1834077 IC50 > 100000.0 nM -
CHEMBL1834076 IC50 > 100000.0 nM -
CHEMBL1834075 IC50 > 100000.0 nM -
CHEMBL1834065 IC50 > 100000.0 nM -