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Assay Detail

CHEMBL4258539

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

Binding
Inhibition of equine serum BuChE using S-butyrylthiocholine iodide as substrate pretreated for 10 mins followed by substrate addition and measured after 10 mins by Ellman's method
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Equus caballus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cholinesterase (CHEMBL5763)
Type SINGLE PROTEIN
Organism Equus caballus

Publication

Design, synthesis and evaluation of indole derivatives as multifunctional agents against Alzheimer's disease.
Denya I, Malan SF, Enogieru AB, Omoruyi SI, Ekpo OE, Kapp E, Zindo FT, Joubert J.
Medchemcomm (2018) 9 : 357 -370
PubMed 30108930 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.49 5.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL255231 LADOSTIGIL 2.0 1 5.70
CHEMBL4290661 1 5.64
CHEMBL4280184 1 5.55
CHEMBL4278916 1 5.52
CHEMBL4280019 1 5.50
CHEMBL4284601 1 5.46
CHEMBL4288413 1 5.40
CHEMBL4294875 1 5.34
CHEMBL4286834 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL255231 LADOSTIGIL IC50 = 1980.0 nM 5.70
CHEMBL4290661 IC50 = 2290.0 nM 5.64
CHEMBL4280184 IC50 = 2820.0 nM 5.55
CHEMBL4278916 IC50 = 3010.0 nM 5.52
CHEMBL4280019 IC50 = 3180.0 nM 5.50
CHEMBL4284601 IC50 = 3480.0 nM 5.46
CHEMBL4288413 IC50 = 3960.0 nM 5.40
CHEMBL4294875 IC50 = 4550.0 nM 5.34
CHEMBL4286834 IC50 = 5010.0 nM 5.30