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Assay Detail

CHEMBL654402

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

Binding
Ex vivo inhibition of human plasma Butyrylcholinesterase.
21
Total Activities
21
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

Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines.
Yu QS, Zhu X, Holloway HW, Whittaker NF, Brossi A, Greig NH.
J Med Chem (2002) 45 : 3684 -3691
PubMed 12166941 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 6.49 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL433041 EPTASTIGMINE 2.0 1 8.30
CHEMBL123248 ESERIDINE 2.0 1 7.92
CHEMBL338975 PHYSOSTIGMINE SALICYLATE -1.0 1 7.80
CHEMBL333580 1 7.60
CHEMBL636 RIVASTIGMINE 4.0 1 7.43
CHEMBL95 TACRINE 4.0 1 7.33
CHEMBL332760 1 7.30
CHEMBL121810 GANSTIGMINE 2.0 1 6.51
CHEMBL538852 1 6.18
CHEMBL123831 1 6.09
CHEMBL123249 1 5.81
CHEMBL124054 1 5.80
CHEMBL538109 1 5.77
CHEMBL120279 1 5.71
CHEMBL122834 1 5.54
CHEMBL502 DONEPEZIL 4.0 1 5.38
CHEMBL557400 1 5.28
CHEMBL659 GALANTAMINE 4.0 1 5.14
CHEMBL556186 1 -
CHEMBL395280 HUPERZINE A 2.0 1 -
CHEMBL538853 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL433041 EPTASTIGMINE IC50 = 5.0 nM 8.30
CHEMBL123248 ESERIDINE IC50 = 12.0 nM 7.92
CHEMBL338975 PHYSOSTIGMINE SALICYLATE IC50 = 16.0 nM 7.80
CHEMBL333580 IC50 = 25.0 nM 7.60
CHEMBL636 RIVASTIGMINE IC50 = 37.0 nM 7.43
CHEMBL95 TACRINE IC50 = 47.0 nM 7.33
CHEMBL332760 IC50 = 50.0 nM 7.30
CHEMBL121810 GANSTIGMINE IC50 = 310.0 nM 6.51
CHEMBL538852 IC50 = 660.0 nM 6.18
CHEMBL123831 IC50 = 815.0 nM 6.09
CHEMBL123249 IC50 = 1560.0 nM 5.81
CHEMBL124054 IC50 = 1570.0 nM 5.80
CHEMBL538109 IC50 = 1700.0 nM 5.77
CHEMBL120279 IC50 = 1950.0 nM 5.71
CHEMBL122834 IC50 = 2900.0 nM 5.54
CHEMBL502 DONEPEZIL IC50 = 4150.0 nM 5.38
CHEMBL557400 IC50 = 5200.0 nM 5.28
CHEMBL659 GALANTAMINE IC50 = 7300.0 nM 5.14
CHEMBL556186 IC50 > 10000.0 nM -
CHEMBL395280 HUPERZINE A IC50 > 10000.0 nM -
CHEMBL538853 IC50 > 10000.0 nM -