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Assay Detail

CHEMBL5142597

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

Binding
Inhibition of horse serum BChE using acetylthiocholine iodide or butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition by Ellman's method
42
Total Activities
42
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

<i>N</i>-Benzyl Benzamide Derivatives as Selective Sub-Nanomolar Butyrylcholinesterase Inhibitors for Possible Treatment in Advanced Alzheimer's Disease.
Du C, Wang L, Guan Q, Yang H, Chen T, Liu Y, Li Q, Lyu W, Lu X, Chen Y, Liu Y, Liu H, Feng F, Liu W, Liu Z, Li W, Chen Y, Sun H.
J Med Chem (2022) 65 : 11365 -11387
PubMed 35969197 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 42 8.23 10.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5201089 1 10.68
CHEMBL5181960 1 10.06
CHEMBL5185039 1 9.89
CHEMBL5184944 1 9.85
CHEMBL5195228 1 9.82
CHEMBL5184728 1 9.80
CHEMBL5173939 1 9.54
CHEMBL5200785 1 9.47
CHEMBL5199323 1 9.42
CHEMBL5197490 1 9.38
CHEMBL5208367 1 9.35
CHEMBL5201163 1 9.32
CHEMBL5191236 1 9.26
CHEMBL5188290 1 9.26
CHEMBL5201951 1 9.10
CHEMBL5183552 1 9.09
CHEMBL5195383 1 9.02
CHEMBL5198895 1 8.99
CHEMBL5190491 1 8.92
CHEMBL5185696 1 8.90
CHEMBL5208374 1 8.87
CHEMBL5174951 1 8.87
CHEMBL5186949 1 8.82
CHEMBL5169365 1 8.62
CHEMBL5182498 1 8.45
CHEMBL5190745 1 8.34
CHEMBL5174262 1 8.30
CHEMBL5198770 1 8.18
CHEMBL5171447 1 8.10
CHEMBL5172504 1 7.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5201089 IC50 = 0.021 nM 10.68
CHEMBL5181960 IC50 = 0.087 nM 10.06
CHEMBL5185039 IC50 = 0.13 nM 9.89
CHEMBL5184944 IC50 = 0.14 nM 9.85
CHEMBL5195228 IC50 = 0.15 nM 9.82
CHEMBL5184728 IC50 = 0.16 nM 9.80
CHEMBL5173939 IC50 = 0.29 nM 9.54
CHEMBL5200785 IC50 = 0.34 nM 9.47
CHEMBL5199323 IC50 = 0.38 nM 9.42
CHEMBL5197490 IC50 = 0.42 nM 9.38
CHEMBL5208367 IC50 = 0.45 nM 9.35
CHEMBL5201163 IC50 = 0.48 nM 9.32
CHEMBL5191236 IC50 = 0.55 nM 9.26
CHEMBL5188290 IC50 = 0.55 nM 9.26
CHEMBL5201951 IC50 = 0.79 nM 9.10
CHEMBL5183552 IC50 = 0.82 nM 9.09
CHEMBL5195383 IC50 = 0.96 nM 9.02
CHEMBL5198895 IC50 = 1.02 nM 8.99
CHEMBL5190491 IC50 = 1.19 nM 8.92
CHEMBL5185696 IC50 = 1.27 nM 8.90
CHEMBL5174951 IC50 = 1.35 nM 8.87
CHEMBL5208374 IC50 = 1.35 nM 8.87
CHEMBL5186949 IC50 = 1.51 nM 8.82
CHEMBL5169365 IC50 = 2.42 nM 8.62
CHEMBL5182498 IC50 = 3.53 nM 8.45
CHEMBL5190745 IC50 = 4.55 nM 8.34
CHEMBL5174262 IC50 = 4.99 nM 8.30
CHEMBL5198770 IC50 = 6.54 nM 8.18
CHEMBL5171447 IC50 = 7.9 nM 8.10
CHEMBL5172504 IC50 = 14.37 nM 7.84
CHEMBL95 TACRINE IC50 = 15.22 nM 7.82
CHEMBL5195425 IC50 = 77.33 nM 7.11
CHEMBL5186019 IC50 = 120.0 nM 6.92
CHEMBL5178120 IC50 = 157.9 nM 6.80
CHEMBL5201295 IC50 = 186.7 nM 6.73
CHEMBL5188959 IC50 = 349.6 nM 6.46
CHEMBL5185423 IC50 = 480.0 nM 6.32
CHEMBL5179673 IC50 = 1910.0 nM 5.72
CHEMBL5196163 IC50 = 5950.0 nM 5.22
CHEMBL5178677 IC50 = 12920.0 nM 4.89
CHEMBL5185740 IC50 = 54970.0 nM 4.26
CHEMBL5200557 IC50 = 97270.0 nM 4.01