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Assay Detail

CHEMBL5162941

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

Binding
Inhibition of AChE in mouse cerebral cortex using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition and measured for 180 secs by Ellman's spectrophotometric method
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Tissue Cerebral cortex
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Acetylcholinesterase (CHEMBL3198)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Novel inhibitors of AChE and Aβ aggregation with neuroprotective properties as lead compounds for the treatment of Alzheimer's disease.
Liu Y, Uras G, Onuwaje I, Li W, Yao H, Xu S, Li X, Li X, Phillips J, Allen S, Gong Q, Zhang H, Zhu Z, Liu J, Xu J.
Eur J Med Chem (2022) 235 : 114305 -114305
PubMed 35339839 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 7.65 8.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5180947 1 8.62
CHEMBL5198028 1 8.42
CHEMBL5204649 1 8.39
CHEMBL5202413 1 8.36
CHEMBL5190674 1 8.36
CHEMBL5200196 1 8.33
CHEMBL5173612 1 8.30
CHEMBL5188181 1 8.29
CHEMBL502 DONEPEZIL 4.0 1 8.27
CHEMBL5206971 1 8.26
CHEMBL5204001 1 8.15
CHEMBL5199752 1 8.07
CHEMBL5187084 1 7.96
CHEMBL5186127 1 7.95
CHEMBL5201084 1 7.95
CHEMBL5174806 1 7.94
CHEMBL5182685 1 7.94
CHEMBL5179256 1 7.92
CHEMBL5205085 1 7.89
CHEMBL5174088 1 7.83
CHEMBL5209880 1 7.17
CHEMBL5169530 1 6.89
CHEMBL5190328 1 6.50
CHEMBL5208030 1 6.47
CHEMBL5197334 1 5.74
CHEMBL5193449 1 5.52
CHEMBL5173396 1 5.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5180947 IC50 = 2.4 nM 8.62
CHEMBL5198028 IC50 = 3.8 nM 8.42
CHEMBL5204649 IC50 = 4.1 nM 8.39
CHEMBL5202413 IC50 = 4.4 nM 8.36
CHEMBL5190674 IC50 = 4.4 nM 8.36
CHEMBL5200196 IC50 = 4.7 nM 8.33
CHEMBL5173612 IC50 = 5.0 nM 8.30
CHEMBL5188181 IC50 = 5.1 nM 8.29
CHEMBL502 DONEPEZIL IC50 = 5.4 nM 8.27
CHEMBL5206971 IC50 = 5.5 nM 8.26
CHEMBL5204001 IC50 = 7.1 nM 8.15
CHEMBL5199752 IC50 = 8.5 nM 8.07
CHEMBL5187084 IC50 = 11.1 nM 7.96
CHEMBL5186127 IC50 = 11.3 nM 7.95
CHEMBL5201084 IC50 = 11.3 nM 7.95
CHEMBL5174806 IC50 = 11.5 nM 7.94
CHEMBL5182685 IC50 = 11.5 nM 7.94
CHEMBL5179256 IC50 = 12.1 nM 7.92
CHEMBL5205085 IC50 = 12.9 nM 7.89
CHEMBL5174088 IC50 = 14.7 nM 7.83
CHEMBL5209880 IC50 = 67.6 nM 7.17
CHEMBL5169530 IC50 = 128.0 nM 6.89
CHEMBL5190328 IC50 = 317.0 nM 6.50
CHEMBL5208030 IC50 = 340.0 nM 6.47
CHEMBL5197334 IC50 = 1820.0 nM 5.74
CHEMBL5193449 IC50 = 3007.0 nM 5.52
CHEMBL5173396 IC50 = 8437.0 nM 5.07