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Assay Detail

CHEMBL655896

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

Binding
Inhibition of Butyrylcholinesterase (BChE) of human erythrocytes [-log IC50 (uM)]
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Cholinesterase (CHEMBL1914)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Acetylcholinesterase noncovalent inhibitors based on a polyamine backbone for potential use against Alzheimer's disease.
Melchiorre C, Andrisano V, Bolognesi ML, Budriesi R, Cavalli A, Cavrini V, Rosini M, Tumiatti V, Recanatini M.
J Med Chem (1998) 41 : 4186 -4189
PubMed 9784091 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.67 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL94 PHYSOSTIGMINE 3.0 1 7.64
CHEMBL95 TACRINE 4.0 1 6.44
CHEMBL27673 METHOCTRAMINE 1 6.01
CHEMBL302179 1 5.86
CHEMBL422977 1 5.43
CHEMBL132377 1 5.22
CHEMBL19060 BENEXTRAMINE 1 5.21
CHEMBL134382 1 5.06
CHEMBL134488 1 4.94
CHEMBL11805 CAPROCTAMINE 1 4.93
CHEMBL132133 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL94 PHYSOSTIGMINE IC50 = 22.91 nM 7.64
CHEMBL95 TACRINE IC50 = 363.08 nM 6.44
CHEMBL27673 METHOCTRAMINE IC50 = 977.24 nM 6.01
CHEMBL302179 IC50 = 1380.38 nM 5.86
CHEMBL422977 IC50 = 3715.35 nM 5.43
CHEMBL132377 IC50 = 6025.6 nM 5.22
CHEMBL19060 BENEXTRAMINE IC50 = 6165.95 nM 5.21
CHEMBL134382 IC50 = 8709.64 nM 5.06
CHEMBL134488 IC50 = 11481.54 nM 4.94
CHEMBL11805 CAPROCTAMINE IC50 = 11748.98 nM 4.93
CHEMBL132133 IC50 = 645654.23 nM -