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Assay Detail

CHEMBL4424916

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

Binding
Inhibition of recombinant human AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition and measured for 5 mins by Ellman's method
13
Total Activities
13
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

Highly potent and selective aryl-1,2,3-triazolyl benzylpiperidine inhibitors toward butyrylcholinesterase in Alzheimer's disease.
de Andrade P, Mantoani SP, Gonçalves Nunes PS, Magadán CR, Pérez C, Xavier DJ, Hojo ETS, Campillo NE, Martínez A, Carvalho I.
Bioorg Med Chem (2019) 27 : 931 -943
PubMed 30765302 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.71 8.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL502 DONEPEZIL 4.0 1 8.24
CHEMBL4534345 1 5.41
CHEMBL4440392 1 5.38
CHEMBL4574766 1 5.31
CHEMBL4438642 1 5.31
CHEMBL4557745 1 5.16
CHEMBL4446441 1 5.13
CHEMBL4445099 1 -
CHEMBL4464964 1 -
CHEMBL4467345 1 -
CHEMBL4520568 1 -
CHEMBL4437391 1 -
CHEMBL4448634 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL502 DONEPEZIL IC50 = 5.7 nM 8.24
CHEMBL4534345 IC50 = 3940.0 nM 5.41
CHEMBL4440392 IC50 = 4220.0 nM 5.38
CHEMBL4574766 IC50 = 4900.0 nM 5.31
CHEMBL4438642 IC50 = 4920.0 nM 5.31
CHEMBL4557745 IC50 = 6900.0 nM 5.16
CHEMBL4446441 IC50 = 7330.0 nM 5.13
CHEMBL4445099 IC50 > 10000.0 nM -
CHEMBL4464964 IC50 > 10000.0 nM -
CHEMBL4467345 IC50 > 10000.0 nM -
CHEMBL4520568 IC50 > 10000.0 nM -
CHEMBL4437391 IC50 > 10000.0 nM -
CHEMBL4448634 IC50 > 10000.0 nM -