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Assay Detail

CHEMBL1775597

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

Binding
Inhibition of human BChE using butyrylthiocholine iodide as substrate by Ellman's method
18
Total Activities
18
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

Benzophenone-based derivatives: a novel series of potent and selective dual inhibitors of acetylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation.
Belluti F, Bartolini M, Bottegoni G, Bisi A, Cavalli A, Andrisano V, Rampa A.
Eur J Med Chem (2011) 46 : 1682 -1693
PubMed 21397996 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 4.70 5.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL502 DONEPEZIL 4.0 1 5.13
CHEMBL1773489 1 5.01
CHEMBL1773487 1 4.98
CHEMBL1773483 1 4.96
CHEMBL345124 PROPIDIUM 1 4.88
CHEMBL1773484 1 4.68
CHEMBL1773488 1 4.66
CHEMBL1773490 1 4.64
CHEMBL1773491 1 4.62
CHEMBL1773486 1 4.47
CHEMBL1773482 1 4.46
CHEMBL1773485 1 4.41
CHEMBL1773481 1 4.17
CHEMBL1773480 1 -
CHEMBL1773492 1 -
CHEMBL514966 1 -
CHEMBL1773479 1 -
CHEMBL1773478 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL502 DONEPEZIL IC50 = 7400.0 nM 5.13
CHEMBL1773489 IC50 = 9700.0 nM 5.01
CHEMBL1773487 IC50 = 10400.0 nM 4.98
CHEMBL1773483 IC50 = 11000.0 nM 4.96
CHEMBL345124 PROPIDIUM IC50 = 13200.0 nM 4.88
CHEMBL1773484 IC50 = 21000.0 nM 4.68
CHEMBL1773488 IC50 = 21900.0 nM 4.66
CHEMBL1773490 IC50 = 23000.0 nM 4.64
CHEMBL1773491 IC50 = 24200.0 nM 4.62
CHEMBL1773486 IC50 = 34000.0 nM 4.47
CHEMBL1773482 IC50 = 35000.0 nM 4.46
CHEMBL1773485 IC50 = 39000.0 nM 4.41
CHEMBL1773481 IC50 = 68000.0 nM 4.17
CHEMBL1773480 IC50 = 179000.0 nM -
CHEMBL1773492 IC50 = 209000.0 nM -
CHEMBL514966 IC50 > 10000.0 nM -
CHEMBL1773479 IC50 = 145000.0 nM -
CHEMBL1773478 IC50 = 144000.0 nM -