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Assay Detail

CHEMBL3603059

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

Binding
Inhibition of human recombinant AChE using acetylthiocholine iodide as substrate preincubated with enzyme for 20 mins prior to substrate addition by Ellman's method
6
Total Activities
6
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

Acetylcholinesterase (CHEMBL220)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis, biological profiling and mechanistic studies of 4-aminoquinoline-based heterodimeric compounds with dual trypanocidal-antiplasmodial activity.
Sola I, Castellà S, Viayna E, Galdeano C, Taylor MC, Gbedema SY, Pérez B, Clos MV, Jones DC, Fairlamb AH, Wright CW, Kelly JM, Muñoz-Torrero D.
Bioorg Med Chem (2015) 23 : 5156 -5167
PubMed 25678015 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 8.44 8.83

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3600555 1 8.83
CHEMBL3600551 1 8.72
CHEMBL3600552 1 8.46
CHEMBL3600556 1 8.44
CHEMBL3600553 1 8.19
CHEMBL3600554 1 8.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3600555 IC50 = 1.48 nM 8.83
CHEMBL3600551 IC50 = 1.92 nM 8.72
CHEMBL3600552 IC50 = 3.46 nM 8.46
CHEMBL3600556 IC50 = 3.66 nM 8.44
CHEMBL3600553 IC50 = 6.46 nM 8.19
CHEMBL3600554 IC50 = 10.1 nM 8.00