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Assay Detail

CHEMBL654403

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

Binding
In vitro inhibition of Butyrylcholinesterase 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

Cholinesterase (CHEMBL1914)
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 5.75 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL95 TACRINE 4.0 1 8.22
CHEMBL95020 1 5.66
CHEMBL328468 1 5.41
CHEMBL329231 1 5.40
CHEMBL94546 1 5.35
CHEMBL329012 ICOPEZIL MALEATE 2.0 1 5.14
CHEMBL94217 1 5.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL95 TACRINE IC50 = 6.0 nM 8.22
CHEMBL95020 IC50 = 2200.0 nM 5.66
CHEMBL328468 IC50 = 3900.0 nM 5.41
CHEMBL329231 IC50 = 4000.0 nM 5.40
CHEMBL94546 IC50 = 4500.0 nM 5.35
CHEMBL329012 ICOPEZIL MALEATE IC50 = 7200.0 nM 5.14
CHEMBL94217 IC50 = 9000.0 nM 5.05