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Assay Detail

CHEMBL982933

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

Binding
Inhibition of human serum BChE by Ellman's method
6
Total Activities
6
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

Inhibition of acetylcholinesterase, beta-amyloid aggregation, and NMDA receptors in Alzheimer's disease: a promising direction for the multi-target-directed ligands gold rush.
Rosini M, Simoni E, Bartolini M, Cavalli A, Ceccarini L, Pascu N, McClymont DW, Tarozzi A, Bolognesi ML, Minarini A, Tumiatti V, Andrisano V, Mellor IR, Melchiorre C.
J Med Chem (2008) 51 : 4381 -4384
PubMed 18605718 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.62 7.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL95 TACRINE 4.0 1 7.34
CHEMBL474268 1 6.86
CHEMBL473866 1 6.72
CHEMBL478667 1 6.68
CHEMBL478666 CARBACRINE 1 6.53
CHEMBL191758 1 5.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL95 TACRINE IC50 = 45.8 nM 7.34
CHEMBL474268 IC50 = 137.0 nM 6.86
CHEMBL473866 IC50 = 189.0 nM 6.72
CHEMBL478667 IC50 = 211.0 nM 6.68
CHEMBL478666 CARBACRINE IC50 = 296.0 nM 6.53
CHEMBL191758 IC50 = 2580.0 nM 5.59