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Assay Detail

CHEMBL1003710

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

Binding
Inhibition of human serum BChE by Ellman's method
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cholinesterase (CHEMBL1914)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Tacripyrines, the first tacrine-dihydropyridine hybrids, as multitarget-directed ligands for the treatment of Alzheimer's disease.
Marco-Contelles J, León R, de los Ríos C, Samadi A, Bartolini M, Andrisano V, Huertas O, Barril X, Luque FJ, Rodríguez-Franco MI, López B, López MG, García AG, Carreiras Mdo C, Villarroya M.
J Med Chem (2009) 52 : 2724 -2732
PubMed 19374444 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 5.55 7.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL95 TACRINE 4.0 1 7.44
CHEMBL219400 1 5.32
CHEMBL470715 1 4.96
CHEMBL219405 1 4.46
CHEMBL490359 1 -
CHEMBL491360 1 -
CHEMBL491359 1 -
CHEMBL491358 1 -
CHEMBL374184 1 -
CHEMBL218940 1 -
CHEMBL490338 1 -
CHEMBL219406 1 -
CHEMBL220294 1 -
CHEMBL491561 1 -
CHEMBL219172 1 -
CHEMBL218939 1 -
CHEMBL436302 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL95 TACRINE IC50 = 36.0 nM 7.44
CHEMBL219400 IC50 = 4800.0 nM 5.32
CHEMBL470715 IC50 = 11000.0 nM 4.96
CHEMBL219405 IC50 = 34400.0 nM 4.46
CHEMBL490359 IC50 > 100000.0 nM -
CHEMBL491360 IC50 > 100000.0 nM -
CHEMBL491359 IC50 > 100000.0 nM -
CHEMBL491358 IC50 > 100000.0 nM -
CHEMBL374184 IC50 > 100000.0 nM -
CHEMBL218940 IC50 > 100000.0 nM -
CHEMBL490338 IC50 > 100000.0 nM -
CHEMBL219406 IC50 > 100000.0 nM -
CHEMBL220294 IC50 > 100000.0 nM -
CHEMBL491561 IC50 > 100000.0 nM -
CHEMBL219172 IC50 > 100000.0 nM -
CHEMBL218939 IC50 > 100000.0 nM -
CHEMBL436302 IC50 > 100000.0 nM -