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Assay Detail

CHEMBL636825

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

Binding
Inhibition of acetylcholinesterase
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Acetylcholinesterase (CHEMBL3199)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and biological activity of putative mono-hydroxylated metabolites of velnacrine
Shutske GM, Bores GM, Bradshaw KC, Huger FP, Kapples KJ, Larsen RD, Rush DK, Tomer JD
Bioorg Med Chem Lett (1992) 2 : 865 -870
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.05 6.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL95 TACRINE 4.0 1 6.64
CHEMBL51934 VELNACRINE 2.0 1 5.89
CHEMBL166854 1 5.34
CHEMBL354304 1 5.27
CHEMBL354601 1 4.97
CHEMBL172733 1 4.83
CHEMBL349428 1 4.60
CHEMBL169407 1 4.56
CHEMBL168213 1 4.21
CHEMBL172102 1 4.19
CHEMBL355059 1 -
CHEMBL354617 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL95 TACRINE IC50 = 230.0 nM 6.64
CHEMBL51934 VELNACRINE IC50 = 1300.0 nM 5.89
CHEMBL166854 IC50 = 4600.0 nM 5.34
CHEMBL354304 IC50 = 5400.0 nM 5.27
CHEMBL354601 IC50 = 10600.0 nM 4.97
CHEMBL172733 IC50 = 14700.0 nM 4.83
CHEMBL349428 IC50 = 25100.0 nM 4.60
CHEMBL169407 IC50 = 27400.0 nM 4.56
CHEMBL168213 IC50 = 62100.0 nM 4.21
CHEMBL172102 IC50 = 64400.0 nM 4.19
CHEMBL355059 IC50 > 100000.0 nM -
CHEMBL354617 IC50 > 100000.0 nM -