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Assay Detail

CHEMBL832431

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

Binding
Inhibition of isolated human BuChE
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 Expert

Target

Cholinesterase (CHEMBL1914)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Cholinesterase inhibitors: xanthostigmine derivatives blocking the acetylcholinesterase-induced beta-amyloid aggregation.
Belluti F, Rampa A, Piazzi L, Bisi A, Gobbi S, Bartolini M, Andrisano V, Cavalli A, Recanatini M, Valenti P.
J Med Chem (2005) 48 : 4444 -4456
PubMed 15974596 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 4.29 4.78

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL189957 1 4.78
CHEMBL94 PHYSOSTIGMINE 3.0 1 4.64
CHEMBL364545 1 4.40
CHEMBL190060 1 4.35
CHEMBL340427 XANTHOSTIGMINE 1 4.32
CHEMBL370961 1 4.24
CHEMBL191386 1 4.15
CHEMBL365678 1 4.13
CHEMBL191461 1 4.09
CHEMBL365136 1 4.07
CHEMBL372710 1 4.02
CHEMBL191416 1 -
CHEMBL190528 1 -
CHEMBL191314 1 -
CHEMBL364678 1 -
CHEMBL363588 1 -
CHEMBL371798 1 -
CHEMBL189797 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL189957 IC50 = 16500.0 nM 4.78
CHEMBL94 PHYSOSTIGMINE IC50 = 23000.0 nM 4.64
CHEMBL364545 IC50 = 40200.0 nM 4.40
CHEMBL190060 IC50 = 44300.0 nM 4.35
CHEMBL340427 XANTHOSTIGMINE IC50 = 48000.0 nM 4.32
CHEMBL370961 IC50 = 57900.0 nM 4.24
CHEMBL191386 IC50 = 70300.0 nM 4.15
CHEMBL365678 IC50 = 74800.0 nM 4.13
CHEMBL191461 IC50 = 81300.0 nM 4.09
CHEMBL365136 IC50 = 84400.0 nM 4.07
CHEMBL372710 IC50 = 94600.0 nM 4.02
CHEMBL191416 IC50 = 155000.0 nM -
CHEMBL190528 IC50 = 136000.0 nM -
CHEMBL191314 IC50 = 761000.0 nM -
CHEMBL364678 IC50 = 130000.0 nM -
CHEMBL363588 IC50 = 153000.0 nM -
CHEMBL371798 IC50 = 4650000.0 nM -
CHEMBL189797 IC50 = 11400000.0 nM -