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Assay Detail

CHEMBL4003322

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

Binding
Uncompetitive inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition measured every 1 min for 30 mins by Cornish-Bowden plot method
22
Total Activities
22
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

Amino derivatives of platanic acid act as selective and potent inhibitors of butyrylcholinesterase.
Heller L, Kahnt M, Loesche A, Grabandt P, Schwarz S, Brandt W, Csuk R.
Eur J Med Chem (2017) 126 : 652 -668
PubMed 27936444 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 4.90 6.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4071069 1 6.68
CHEMBL4063629 1 5.39
CHEMBL4085251 1 5.34
CHEMBL4100709 1 5.17
CHEMBL4090532 1 5.01
CHEMBL4082718 1 4.96
CHEMBL4075135 1 4.85
CHEMBL4063777 1 4.79
CHEMBL4091899 1 4.77
CHEMBL4062429 1 4.47
CHEMBL80460 PLATANIC ACID 1 4.43
CHEMBL4089507 1 4.34
CHEMBL4084140 1 4.32
CHEMBL4072365 1 4.12
CHEMBL4104205 1 -
CHEMBL4086293 1 -
CHEMBL4066524 1 -
CHEMBL4061347 1 -
CHEMBL4081627 1 -
CHEMBL4101798 1 -
CHEMBL4093124 1 -
CHEMBL4062563 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4071069 Ki = 210.0 nM 6.68
CHEMBL4063629 Ki = 4060.0 nM 5.39
CHEMBL4085251 Ki = 4590.0 nM 5.34
CHEMBL4100709 Ki = 6830.0 nM 5.17
CHEMBL4090532 Ki = 9710.0 nM 5.01
CHEMBL4082718 Ki = 10910.0 nM 4.96
CHEMBL4075135 Ki = 13990.0 nM 4.85
CHEMBL4063777 Ki = 16390.0 nM 4.79
CHEMBL4091899 Ki = 17000.0 nM 4.77
CHEMBL4062429 Ki = 34180.0 nM 4.47
CHEMBL80460 PLATANIC ACID Ki = 36860.0 nM 4.43
CHEMBL4089507 Ki = 45570.0 nM 4.34
CHEMBL4084140 Ki = 47810.0 nM 4.32
CHEMBL4072365 Ki = 76600.0 nM 4.12
CHEMBL4104205 Ki > 80000.0 nM -
CHEMBL4086293 Ki - -
CHEMBL4066524 Ki - -
CHEMBL4061347 Ki - -
CHEMBL4081627 Ki = 103680.0 nM -
CHEMBL4101798 Ki - -
CHEMBL4093124 Ki > 90000.0 nM -
CHEMBL4062563 Ki > 120000.0 nM -