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Assay Detail

CHEMBL644837

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

Binding
In vitro inhibition of Acetylcholinesterase from human erythrocytes
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Acetylcholinesterase (CHEMBL220)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

5,7-dihydro-3-[2-[1-(phenylmethyl)-4-piperidinyl]ethyl]-6H- pyrrolo[3,2-f]-1,2-benzisoxazol-6-one: a potent and centrally-selective inhibitor of acetylcholinesterase with an improved margin of safety.
Villalobos A, Butler TW, Chapin DS, Chen YL, DeMattos SB, Ives JL, Jones SB, Liston DR, Nagel AA, Nason DM.
J Med Chem (1995) 38 : 2802 -2808
PubMed 7636841 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 8.69 9.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL329012 ICOPEZIL MALEATE 2.0 1 9.48
CHEMBL94546 1 9.32
CHEMBL329231 1 9.24
CHEMBL328468 1 9.02
CHEMBL94217 1 8.55
CHEMBL95020 1 8.44
CHEMBL95 TACRINE 4.0 1 6.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL329012 ICOPEZIL MALEATE IC50 = 0.33 nM 9.48
CHEMBL94546 IC50 = 0.48 nM 9.32
CHEMBL329231 IC50 = 0.57 nM 9.24
CHEMBL328468 IC50 = 0.95 nM 9.02
CHEMBL94217 IC50 = 2.8 nM 8.55
CHEMBL95020 IC50 = 3.6 nM 8.44
CHEMBL95 TACRINE IC50 = 170.0 nM 6.77