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Assay Detail

CHEMBL4427587

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

Binding
Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured after 5 mins by Ellmans method
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Electrophorus electricus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Acetylcholinesterase (CHEMBL4078)
Type SINGLE PROTEIN
Organism Electrophorus electricus

Publication

Cholinesterase inhibitory activity of chlorophenoxy derivatives-Histamine H3 receptor ligands.
Łażewska D, Jończyk J, Bajda M, Szałaj N, Więckowska A, Panek D, Moore C, Kuder K, Malawska B, Kieć-Kononowicz K.
Bioorg Med Chem Lett (2016) 26 : 4140 -4145
PubMed 27445168 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 5.54 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL502 DONEPEZIL 4.0 1 8.00
CHEMBL95 TACRINE 4.0 1 7.62
CHEMBL3747910 1 5.71
CHEMBL3747906 1 5.62
CHEMBL3747909 1 5.56
CHEMBL3747904 1 5.42
CHEMBL3747907 1 5.41
CHEMBL3747902 1 5.41
CHEMBL3747908 1 5.35
CHEMBL3747900 1 5.32
CHEMBL3747905 1 5.31
CHEMBL3747898 1 5.27
CHEMBL3747903 1 5.27
CHEMBL3747896 1 5.21
CHEMBL3747897 1 5.14
CHEMBL4452966 1 5.10
CHEMBL3747901 1 5.09
CHEMBL3747895 1 4.73
CHEMBL3747892 1 4.63
CHEMBL3747894 1 -
CHEMBL3747893 1 -
CHEMBL3747899 1 -
CHEMBL3747891 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL502 DONEPEZIL IC50 = 10.0 nM 8.00
CHEMBL95 TACRINE IC50 = 24.0 nM 7.62
CHEMBL3747910 IC50 = 1930.0 nM 5.71
CHEMBL3747906 IC50 = 2420.0 nM 5.62
CHEMBL3747909 IC50 = 2740.0 nM 5.56
CHEMBL3747904 IC50 = 3800.0 nM 5.42
CHEMBL3747907 IC50 = 3940.0 nM 5.41
CHEMBL3747902 IC50 = 3880.0 nM 5.41
CHEMBL3747908 IC50 = 4510.0 nM 5.35
CHEMBL3747900 IC50 = 4800.0 nM 5.32
CHEMBL3747905 IC50 = 4900.0 nM 5.31
CHEMBL3747898 IC50 = 5400.0 nM 5.27
CHEMBL3747903 IC50 = 5330.0 nM 5.27
CHEMBL3747896 IC50 = 6220.0 nM 5.21
CHEMBL3747897 IC50 = 7310.0 nM 5.14
CHEMBL4452966 IC50 = 7910.0 nM 5.10
CHEMBL3747901 IC50 = 8110.0 nM 5.09
CHEMBL3747895 IC50 = 18570.0 nM 4.73
CHEMBL3747892 IC50 = 23610.0 nM 4.63
CHEMBL3747894 IC50 > 10000.0 nM -
CHEMBL3747893 IC50 > 10000.0 nM -
CHEMBL3747899 IC50 > 10000.0 nM -
CHEMBL3747891 IC50 > 10000.0 nM -