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Assay Detail

CHEMBL4339337

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

Binding
Inhibition of recombinant human AChE using acetylthiocholine iodide as substrate pre-incubated for 20 mins before substrate addition and measured for 180 secs by spectrophotometry based Ellman's method
19
Total Activities
19
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

Tackling neuroinflammation and cholinergic deficit in Alzheimer's disease: Multi-target inhibitors of cholinesterases, cyclooxygenase-2 and 15-lipoxygenase.
AlFadly ED, Elzahhar PA, Tramarin A, Elkazaz S, Shaltout H, Abu-Serie MM, Janockova J, Soukup O, Ghareeb DA, El-Yazbi AF, Rafeh RW, Bakkar NZ, Kobeissy F, Iriepa I, Moraleda I, Saudi MNS, Bartolini M, Belal ASF.
Eur J Med Chem (2019) 167 : 161 -186
PubMed 30771604 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 5.86 6.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4458648 1 6.66
CHEMBL4525409 1 6.53
CHEMBL95 TACRINE 4.0 1 6.38
CHEMBL4435178 1 6.24
CHEMBL4580216 1 6.21
CHEMBL4435058 1 6.11
CHEMBL4445026 1 6.05
CHEMBL4459154 1 6.02
CHEMBL4466829 1 5.98
CHEMBL4441059 1 5.98
CHEMBL4444030 1 5.96
CHEMBL4447258 1 5.84
CHEMBL4553902 1 5.64
CHEMBL4542112 1 5.56
CHEMBL4592037 1 5.43
CHEMBL4557164 1 5.39
CHEMBL4556651 1 5.24
CHEMBL4443988 1 5.15
CHEMBL4526428 1 4.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4458648 IC50 = 218.0 nM 6.66
CHEMBL4525409 IC50 = 293.0 nM 6.53
CHEMBL95 TACRINE IC50 = 412.0 nM 6.38
CHEMBL4435178 IC50 = 571.0 nM 6.24
CHEMBL4580216 IC50 = 610.0 nM 6.21
CHEMBL4435058 IC50 = 786.0 nM 6.11
CHEMBL4445026 IC50 = 900.0 nM 6.05
CHEMBL4459154 IC50 = 961.0 nM 6.02
CHEMBL4466829 IC50 = 1050.0 nM 5.98
CHEMBL4441059 IC50 = 1050.0 nM 5.98
CHEMBL4444030 IC50 = 1110.0 nM 5.96
CHEMBL4447258 IC50 = 1460.0 nM 5.84
CHEMBL4553902 IC50 = 2300.0 nM 5.64
CHEMBL4542112 IC50 = 2730.0 nM 5.56
CHEMBL4592037 IC50 = 3750.0 nM 5.43
CHEMBL4557164 IC50 = 4030.0 nM 5.39
CHEMBL4556651 IC50 = 5770.0 nM 5.24
CHEMBL4443988 IC50 = 7030.0 nM 5.15
CHEMBL4526428 IC50 = 12800.0 nM 4.89