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Assay Detail

CHEMBL1065424

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

Binding
Inhibition of Torpedo california AChE by Ellman's method
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Torpedo californica
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Acetylcholinesterase (CHEMBL4780)
Type SINGLE PROTEIN
Organism Torpedo californica

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 8.78 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL606348 1 10.70
CHEMBL594870 1 10.61
CHEMBL596236 1 10.39
CHEMBL593933 1 10.35
CHEMBL606372 1 9.92
CHEMBL605303 1 9.07
CHEMBL594187 1 8.79
CHEMBL595114 1 8.74
CHEMBL604478 1 8.17
CHEMBL395280 HUPERZINE A 2.0 1 7.94
CHEMBL606538 1 7.86
CHEMBL596457 1 7.74
CHEMBL338975 PHYSOSTIGMINE SALICYLATE -1.0 1 7.67
CHEMBL595115 1 7.63
CHEMBL594186 1 6.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL606348 IC50 = 0.02 nM 10.70
CHEMBL594870 IC50 = 0.0246 nM 10.61
CHEMBL596236 IC50 = 0.0412 nM 10.39
CHEMBL593933 IC50 = 0.0446 nM 10.35
CHEMBL606372 IC50 = 0.121 nM 9.92
CHEMBL605303 IC50 = 0.842 nM 9.07
CHEMBL594187 IC50 = 1.63 nM 8.79
CHEMBL595114 IC50 = 1.81 nM 8.74
CHEMBL604478 IC50 = 6.7 nM 8.17
CHEMBL395280 HUPERZINE A IC50 = 11.4 nM 7.94
CHEMBL606538 IC50 = 13.9 nM 7.86
CHEMBL596457 IC50 = 18.2 nM 7.74
CHEMBL338975 PHYSOSTIGMINE SALICYLATE IC50 = 21.3 nM 7.67
CHEMBL595115 IC50 = 23.3 nM 7.63
CHEMBL594186 IC50 = 796.0 nM 6.10