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Assay Detail

CHEMBL5626975

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

Binding
Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated with enzyme for 10 mins followed by substrate addition and measured every 1 min for 20 mins by spectrophotometric analysis
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Electrophorus electricus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Acetylcholinesterase (CHEMBL4078)
Type SINGLE PROTEIN
Organism Electrophorus electricus

Publication

Discovery of triazole-bridged aryl adamantane analogs as an intriguing class of multifunctional agents for treatment of Alzheimer's disease.
Gutti G, Leifeld J, Kakarla R, Bajad NG, Ganeshpurkar A, Kumar A, Krishnamurthy S, Klein-Schmidt C, Tapken D, Hollmann M, Singh SK.
Eur J Med Chem (2023) 259 : 115670 -115670
PubMed 37515920 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.27 7.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL502 DONEPEZIL 4.0 1 7.51
CHEMBL5631356 1 7.07
CHEMBL5633239 1 6.87
CHEMBL5632891 1 6.71
CHEMBL5632465 1 6.47
CHEMBL5631365 1 6.44
CHEMBL5629932 1 6.26
CHEMBL5633087 1 6.22
CHEMBL5633141 1 6.10
CHEMBL5632160 1 5.91
CHEMBL5631752 1 5.85
CHEMBL5632181 1 5.82
CHEMBL5632076 1 5.79
CHEMBL5632219 1 5.74
CHEMBL5631427 1 5.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL502 DONEPEZIL IC50 = 31.0 nM 7.51
CHEMBL5631356 IC50 = 86.0 nM 7.07
CHEMBL5633239 IC50 = 135.0 nM 6.87
CHEMBL5632891 IC50 = 194.0 nM 6.71
CHEMBL5632465 IC50 = 340.0 nM 6.47
CHEMBL5631365 IC50 = 360.0 nM 6.44
CHEMBL5629932 IC50 = 550.0 nM 6.26
CHEMBL5633087 IC50 = 607.0 nM 6.22
CHEMBL5633141 IC50 = 799.0 nM 6.10
CHEMBL5632160 IC50 = 1219.0 nM 5.91
CHEMBL5631752 IC50 = 1415.0 nM 5.85
CHEMBL5632181 IC50 = 1518.0 nM 5.82
CHEMBL5632076 IC50 = 1608.0 nM 5.79
CHEMBL5632219 IC50 = 1824.0 nM 5.74
CHEMBL5631427 IC50 = 4637.0 nM 5.33