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Assay Detail

CHEMBL4822912

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

Binding
Inhibition of recombinant human AChE using acetylthiocholine as substrate by DTNB-reagent based Ellman's method
9
Total Activities
9
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

Huprine Y - Tryptophan heterodimers with potential implication to Alzheimer's disease treatment.
Mezeiova E, Hrabinova M, Hepnarova V, Jun D, Janockova J, Muckova L, Prchal L, Kristofikova Z, Kucera T, Gorecki L, Chalupova K, Kunes J, Hroudova J, Soukup O, Korabecny J.
Bioorg Med Chem Lett (2021) 43 : 128100 -128100
PubMed 33984470 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.25 8.79

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL536047 1 8.79
CHEMBL4556281 1 8.20
CHEMBL4856400 1 7.93
CHEMBL4878434 1 7.92
CHEMBL292314 1 7.70
CHEMBL4874244 1 7.64
CHEMBL95 TACRINE 4.0 1 6.50
CHEMBL4850590 1 5.58
CHEMBL1256415 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL536047 IC50 = 1.64 nM 8.79
CHEMBL4556281 IC50 = 6.31 nM 8.20
CHEMBL4856400 IC50 = 11.7 nM 7.93
CHEMBL4878434 IC50 = 12.1 nM 7.92
CHEMBL292314 IC50 = 20.0 nM 7.70
CHEMBL4874244 IC50 = 22.7 nM 7.64
CHEMBL95 TACRINE IC50 = 320.0 nM 6.50
CHEMBL4850590 IC50 = 2630.0 nM 5.58
CHEMBL1256415 IC50 = 10000.0 nM 5.00