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Assay Detail

CHEMBL5362932

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

Binding
Inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition by DTNB based Ellman's method
13
Total Activities
13
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

Synthesis and anti-Alzheimer potential of novel α-amino phosphonate derivatives and probing their molecular interaction mechanism with acetylcholinesterase.
Yelamanda Rao K, Jeelan Basha S, Monika K, Sreelakshmi M, Sivakumar I, Mallikarjuna G, Yadav RM, Kumar S, Subramanyam R, Damu AG.
Eur J Med Chem (2023) 253 : 115288 -115288
PubMed 37031527 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.54 6.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL659 GALANTAMINE 4.0 1 6.23
CHEMBL5433354 1 5.94
CHEMBL5421943 1 5.75
CHEMBL5402496 1 5.59
CHEMBL5429003 1 5.58
CHEMBL5407606 1 5.53
CHEMBL5407691 1 5.52
CHEMBL5424712 1 5.47
CHEMBL5426913 1 5.36
CHEMBL5424767 1 5.31
CHEMBL5433166 1 5.27
CHEMBL5412970 1 5.25
CHEMBL5420040 1 5.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL659 GALANTAMINE IC50 = 594.0 nM 6.23
CHEMBL5433354 IC50 = 1157.0 nM 5.94
CHEMBL5421943 IC50 = 1782.0 nM 5.75
CHEMBL5402496 IC50 = 2554.0 nM 5.59
CHEMBL5429003 IC50 = 2653.0 nM 5.58
CHEMBL5407606 IC50 = 2943.0 nM 5.53
CHEMBL5407691 IC50 = 3016.0 nM 5.52
CHEMBL5424712 IC50 = 3365.0 nM 5.47
CHEMBL5426913 IC50 = 4344.0 nM 5.36
CHEMBL5424767 IC50 = 4927.0 nM 5.31
CHEMBL5433166 IC50 = 5353.0 nM 5.27
CHEMBL5412970 IC50 = 5623.0 nM 5.25
CHEMBL5420040 IC50 = 6052.0 nM 5.22