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Assay Detail

CHEMBL4393365

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

Binding
Inhibition of AChE in erythrocytes (unknown origin) pre-incubated for 20 mins before acetylthiocholine substrate addition and measured over 30 mins by DTNB dye based spectrophotometry
9
Total Activities
8
Compounds Tested
2
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

Cu-mediated synthesis of differentially substituted diazepines as AChE inhibitors; validation through molecular docking and Lipinski's filter to develop novel anti-neurodegenerative drugs.
Sudhapriya N, Manikandan A, Kumar MR, Perumal PT.
Bioorg Med Chem Lett (2019) 29 : 1308 -1312
PubMed 30956014 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Inhibition 8 - -
IC50 1 6.60 6.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4519496 2 6.60
CHEMBL1200569 CAFFEINE CITRATE 4.0 1 -
CHEMBL4554996 1 -
CHEMBL4576139 1 -
CHEMBL4437448 1 -
CHEMBL4527412 1 -
CHEMBL4452323 1 -
CHEMBL4452426 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4519496 IC50 = 250.0 nM 6.60
CHEMBL1200569 CAFFEINE CITRATE Inhibition - % -
CHEMBL4554996 Inhibition - % -
CHEMBL4576139 Inhibition - % -
CHEMBL4437448 Inhibition - % -
CHEMBL4519496 Inhibition - % -
CHEMBL4527412 Inhibition - % -
CHEMBL4452323 Inhibition - % -
CHEMBL4452426 Inhibition - % -