Assay Detail

CHEMBL2319650

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Binding

Inhibition of acetylcholinesterase (unknown origin)

ChEMBL ↗

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Target

Acetylcholinesterase (CHEMBL220) ↗

Open DB target context

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Acetylcholinesterase (CHEMBL220) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Acetylcholinesterase

CHEMBL220

Anchored from Assay target.

Protein identity Acetylcholinesterase

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

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

Design, synthesis and biological evaluation of coumarin alkylamines as potent and selective dual binding site inhibitors of acetylcholinesterase.

Catto M, Pisani L, Leonetti F, Nicolotti O, Pesce P, Stefanachi A, Cellamare S, Carotti A.
Bioorg Med Chem (2013) 21 : 146 -152
PubMed 23199476 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	4	7.10	8.70

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL502	DONEPEZIL	4.0	1	8.70
CHEMBL95	TACRINE	4.0	1	7.00
CHEMBL659	GALANTAMINE	4.0	1	6.52
CHEMBL636	RIVASTIGMINE	4.0	1	6.16

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL502	DONEPEZIL	IC50	=	2.0	nM	8.70
CHEMBL95	TACRINE	IC50	=	100.0	nM	7.00
CHEMBL659	GALANTAMINE	IC50	=	300.0	nM	6.52
CHEMBL636	RIVASTIGMINE	IC50	=	700.0	nM	6.16