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Assay Detail

CHEMBL3877892

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

Binding
Inhibition of electric eel AChE pretreated for 20 mins followed by acetylthiocholine iodide substrate addition measured for 5 mins 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

New azepino[4,3-b]indole derivatives as nanomolar selective inhibitors of human butyrylcholinesterase showing protective effects against NMDA-induced neurotoxicity.
de Candia M, Zaetta G, Denora N, Tricarico D, Majellaro M, Cellamare S, Altomare CD.
Eur J Med Chem (2017) 125 : 288 -298
PubMed 27688184 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 4.79 6.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL659 GALANTAMINE 4.0 1 6.25
CHEMBL3962358 1 5.00
CHEMBL3935090 1 4.99
CHEMBL3971112 1 4.70
CHEMBL3892498 1 4.35
CHEMBL3900327 1 4.22
CHEMBL3910836 1 4.00
CHEMBL3971444 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL659 GALANTAMINE IC50 = 560.0 nM 6.25
CHEMBL3962358 IC50 = 10000.0 nM 5.00
CHEMBL3935090 IC50 = 10300.0 nM 4.99
CHEMBL3971112 IC50 = 20000.0 nM 4.70
CHEMBL3892498 IC50 = 44800.0 nM 4.35
CHEMBL3900327 IC50 = 60000.0 nM 4.22
CHEMBL3910836 IC50 = 100000.0 nM 4.00
CHEMBL3971444 IC50 = 110000.0 nM -