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Assay Detail

CHEMBL654884

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

Binding
Ability to inhibit butyrylcholinesterase (BChE), freshly prepared from human plasma
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Plasma
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Cholinesterase (CHEMBL1914)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis of novel phenserine-based-selective inhibitors of butyrylcholinesterase for Alzheimer's disease.
Yu Q, Holloway HW, Utsuki T, Brossi A, Greig NH.
J Med Chem (1999) 42 : 1855 -1861
PubMed 10346939 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.75 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54470 1 9.00
CHEMBL54577 1 8.22
CHEMBL54420 1 8.08
CHEMBL417915 1 7.30
CHEMBL294208 1 7.11
CHEMBL293720 1 7.07
CHEMBL300808 1 6.88
CHEMBL54864 1 6.40
CHEMBL54014 1 6.22
CHEMBL292695 1 6.19
CHEMBL55315 1 5.84
CHEMBL54727 1 5.81
CHEMBL54956 1 5.75
CHEMBL300143 1 5.71
CHEMBL53623 1 5.67

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54470 IC50 = 1.0 nM 9.00
CHEMBL54577 IC50 = 6.0 nM 8.22
CHEMBL54420 IC50 = 8.3 nM 8.08
CHEMBL417915 IC50 = 50.0 nM 7.30
CHEMBL294208 IC50 = 78.0 nM 7.11
CHEMBL293720 IC50 = 85.0 nM 7.07
CHEMBL300808 IC50 = 132.0 nM 6.88
CHEMBL54864 IC50 = 396.0 nM 6.40
CHEMBL54014 IC50 = 600.0 nM 6.22
CHEMBL292695 IC50 = 641.0 nM 6.19
CHEMBL55315 IC50 = 1430.0 nM 5.84
CHEMBL54727 IC50 = 1560.0 nM 5.81
CHEMBL54956 IC50 = 1790.0 nM 5.75
CHEMBL300143 IC50 = 1950.0 nM 5.71
CHEMBL53623 IC50 = 2165.0 nM 5.67