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Assay Detail

CHEMBL4220758

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

Binding
Inhibition of AChE (unknown origin)
4
Total Activities
4
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

In silico studies, synthesis and pharmacological evaluation to explore multi-targeted approach for imidazole analogues as potential cholinesterase inhibitors with neuroprotective role for Alzheimer's disease.
Gurjar AS, Darekar MN, Yeong KY, Ooi L.
Bioorg Med Chem (2018) 26 : 1511 -1522
PubMed 29429576 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.78 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL709 ALFUZOSIN 4.0 1 7.75
CHEMBL1201217 DYCLONINE 4.0 1 6.74
CHEMBL94 PHYSOSTIGMINE 3.0 1 6.66
CHEMBL623 NEFAZODONE 4.0 1 5.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL709 ALFUZOSIN IC50 = 18.0 nM 7.75
CHEMBL1201217 DYCLONINE IC50 = 181.0 nM 6.74
CHEMBL94 PHYSOSTIGMINE IC50 = 220.0 nM 6.66
CHEMBL623 NEFAZODONE IC50 = 1037.0 nM 5.98