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Assay Detail

CHEMBL5626978

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Binding
Inhibition of human AChE
6
Total Activities
6
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

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 6 6.68 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL502 DONEPEZIL 4.0 1 7.60
CHEMBL5631356 1 7.04
CHEMBL5633239 1 6.88
CHEMBL5633979 1 6.33
CHEMBL5629932 1 6.21
CHEMBL5633087 1 6.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL502 DONEPEZIL IC50 = 25.0 nM 7.60
CHEMBL5631356 IC50 = 92.0 nM 7.04
CHEMBL5633239 IC50 = 133.0 nM 6.88
CHEMBL5633979 IC50 = 470.0 nM 6.33
CHEMBL5629932 IC50 = 621.0 nM 6.21
CHEMBL5633087 IC50 = 927.0 nM 6.03