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Assay Detail

CHEMBL4273242

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

Binding
Inhibition of human serum BuChE using butyrylthiocholine as substrate pretreated for 5 mins followed by substrate addition and measured for 5 mins by Ellman's method
30
Total Activities
30
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

Neurogenic and neuroprotective donepezil-flavonoid hybrids with sigma-1 affinity and inhibition of key enzymes in Alzheimer's disease.
Estrada Valencia M, Herrera-Arozamena C, de Andrés L, Pérez C, Morales-García JA, Pérez-Castillo A, Ramos E, Romero A, Viña D, Yáñez M, Laurini E, Pricl S, Rodríguez-Franco MI.
Eur J Med Chem (2018) 156 : 534 -553
PubMed 30025348 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 5.20 5.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL502 DONEPEZIL 4.0 1 5.60
CHEMBL4292477 1 5.37
CHEMBL4286799 1 5.29
CHEMBL4291372 1 5.24
CHEMBL4284591 1 5.20
CHEMBL4283450 1 5.19
CHEMBL4289318 1 5.06
CHEMBL4277548 1 5.03
CHEMBL4294609 1 5.00
CHEMBL4285779 1 5.00
CHEMBL4294701 1 -
CHEMBL4285912 1 -
CHEMBL4287548 1 -
CHEMBL4290401 1 -
CHEMBL4282527 1 -
CHEMBL4277332 1 -
CHEMBL4287970 1 -
CHEMBL4280725 1 -
CHEMBL4284165 1 -
CHEMBL4294783 1 -
CHEMBL4293801 1 -
CHEMBL4284495 1 -
CHEMBL4295144 1 -
CHEMBL4287889 1 -
CHEMBL4285601 1 -
CHEMBL4286731 1 -
CHEMBL4292446 1 -
CHEMBL4283079 1 -
CHEMBL4290940 1 -
CHEMBL4291296 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL502 DONEPEZIL IC50 = 2500.0 nM 5.60
CHEMBL4292477 IC50 = 4300.0 nM 5.37
CHEMBL4286799 IC50 = 5090.0 nM 5.29
CHEMBL4291372 IC50 = 5800.0 nM 5.24
CHEMBL4284591 IC50 = 6300.0 nM 5.20
CHEMBL4283450 IC50 = 6500.0 nM 5.19
CHEMBL4289318 IC50 = 8790.0 nM 5.06
CHEMBL4277548 IC50 = 9300.0 nM 5.03
CHEMBL4294609 IC50 = 9880.0 nM 5.00
CHEMBL4285779 IC50 = 9900.0 nM 5.00
CHEMBL4294701 IC50 > 10000.0 nM -
CHEMBL4285912 IC50 > 10000.0 nM -
CHEMBL4287548 IC50 > 10000.0 nM -
CHEMBL4290401 IC50 > 10000.0 nM -
CHEMBL4282527 IC50 > 10000.0 nM -
CHEMBL4277332 IC50 > 10000.0 nM -
CHEMBL4287970 IC50 > 10000.0 nM -
CHEMBL4280725 IC50 > 10000.0 nM -
CHEMBL4284165 IC50 > 10000.0 nM -
CHEMBL4294783 IC50 > 10000.0 nM -
CHEMBL4293801 IC50 > 10000.0 nM -
CHEMBL4284495 IC50 > 10000.0 nM -
CHEMBL4295144 IC50 > 10000.0 nM -
CHEMBL4287889 IC50 > 10000.0 nM -
CHEMBL4285601 IC50 > 10000.0 nM -
CHEMBL4286731 IC50 > 10000.0 nM -
CHEMBL4292446 IC50 > 10000.0 nM -
CHEMBL4283079 IC50 > 10000.0 nM -
CHEMBL4290940 IC50 > 10000.0 nM -
CHEMBL4291296 IC50 > 10000.0 nM -