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Assay Detail

CHEMBL3367639

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

Binding
Inhibition of AChE (unknown origin) using ACh chloride as substrate preincubated for 15 mins before substrate addition by Ellman method
9
Total Activities
9
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 and characterization of novel 1,2-oxazine-based small molecules that targets acetylcholinesterase.
Sukhorukov AY, Nirvanappa AC, Swamy J, Ioffe SL, Nanjunda Swamy S, Basappa, Rangappa KS.
Bioorg Med Chem Lett (2014) 24 : 3618 -3621
PubMed 24909082 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 4.81 5.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL278020 NEOSTIGMINE 4.0 1 5.62
CHEMBL3310703 1 5.60
CHEMBL3360758 1 5.20
CHEMBL3310705 1 4.92
CHEMBL3310704 1 4.84
CHEMBL3360757 1 4.45
CHEMBL3310706 1 4.33
CHEMBL3310697 1 4.18
CHEMBL3310699 1 4.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL278020 NEOSTIGMINE IC50 = 2400.0 nM 5.62
CHEMBL3310703 IC50 = 2500.0 nM 5.60
CHEMBL3360758 IC50 = 6300.0 nM 5.20
CHEMBL3310705 IC50 = 12000.0 nM 4.92
CHEMBL3310704 IC50 = 14350.0 nM 4.84
CHEMBL3360757 IC50 = 35120.0 nM 4.45
CHEMBL3310706 IC50 = 46760.0 nM 4.33
CHEMBL3310697 IC50 = 65320.0 nM 4.18
CHEMBL3310699 IC50 = 75350.0 nM 4.12