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Assay Detail

CHEMBL1065425

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

Binding
Inhibition of human AChE by Ellman's method
15
Total Activities
15
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

Rational design and synthesis of highly potent anti-acetylcholinesterase activity huperzine A derivatives.
Yan J, Sun L, Wu G, Yi P, Yang F, Zhou L, Zhang X, Li Z, Yang X, Luo H, Qiu M.
Bioorg Med Chem (2009) 17 : 6937 -6941
PubMed 19726199 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 7.47 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL604478 1 7.80
CHEMBL395280 HUPERZINE A 2.0 1 7.68
CHEMBL596236 1 7.66
CHEMBL595114 1 7.62
CHEMBL605303 1 7.60
CHEMBL594187 1 7.60
CHEMBL606348 1 7.54
CHEMBL595115 1 7.51
CHEMBL594870 1 7.51
CHEMBL606538 1 7.51
CHEMBL606372 1 7.40
CHEMBL596457 1 7.39
CHEMBL594186 1 7.29
CHEMBL593933 1 7.08
CHEMBL95 TACRINE 4.0 1 6.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL604478 IC50 = 16.0 nM 7.80
CHEMBL395280 HUPERZINE A IC50 = 21.0 nM 7.68
CHEMBL596236 IC50 = 22.0 nM 7.66
CHEMBL595114 IC50 = 24.0 nM 7.62
CHEMBL605303 IC50 = 25.0 nM 7.60
CHEMBL594187 IC50 = 25.0 nM 7.60
CHEMBL606348 IC50 = 29.0 nM 7.54
CHEMBL595115 IC50 = 31.0 nM 7.51
CHEMBL594870 IC50 = 31.0 nM 7.51
CHEMBL606538 IC50 = 31.0 nM 7.51
CHEMBL606372 IC50 = 40.0 nM 7.40
CHEMBL596457 IC50 = 41.0 nM 7.39
CHEMBL594186 IC50 = 51.0 nM 7.29
CHEMBL593933 IC50 = 84.0 nM 7.08
CHEMBL95 TACRINE IC50 = 128.0 nM 6.89