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Assay Detail

CHEMBL3877902

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

Binding
Inhibition of human BChE pretreated for 20 mins followed by butyrylthiocholine iodide substrate addition measured for 5 mins by Ellman's method
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cholinesterase (CHEMBL1914)
Type SINGLE PROTEIN
Organism Homo sapiens

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 3 7.31 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3960040 1 8.74
CHEMBL3971112 1 7.89
CHEMBL3919289 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3960040 IC50 = 1.8 nM 8.74
CHEMBL3971112 IC50 = 13.0 nM 7.89
CHEMBL3919289 IC50 = 5000.0 nM 5.30