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Assay Detail

CHEMBL4193552

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

Binding
Competitive inhibition of electric eel AChE assessed as inhibition constant for enzyme inhibitor complex preincubated for 20 mins followed by acetylthiocholine iodide substrate addition and measured for 30 mins at 1 min intervals by Ellman's method
8
Total Activities
8
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

Piperlongumine B and analogs are promising and selective inhibitors for acetylcholinesterase.
Wiemann J, Karasch J, Loesche A, Heller L, Brandt W, Csuk R.
Eur J Med Chem (2017) 139 : 222 -231
PubMed 28802122 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 5.46 6.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1555 GALANTAMINE HYDROBROMIDE 4.0 1 6.43
CHEMBL4207493 1 5.69
CHEMBL4214790 1 5.50
CHEMBL4211036 1 5.47
CHEMBL4210163 1 5.29
CHEMBL4212392 1 5.17
CHEMBL4204224 1 5.13
CHEMBL4207906 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1555 GALANTAMINE HYDROBROMIDE Ki = 370.0 nM 6.43
CHEMBL4207493 Ki = 2040.0 nM 5.69
CHEMBL4214790 Ki = 3160.0 nM 5.50
CHEMBL4211036 Ki = 3410.0 nM 5.47
CHEMBL4210163 Ki = 5090.0 nM 5.29
CHEMBL4212392 Ki = 6830.0 nM 5.17
CHEMBL4204224 Ki = 7450.0 nM 5.13
CHEMBL4207906 Ki = 9990.0 nM 5.00