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Assay Detail

CHEMBL932016

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Binding
Inhibition of AChE by Ellman's assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Acetylcholinesterase (CHEMBL220)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological evaluation of NO-donor-tacrine hybrids as hepatoprotective anti-Alzheimer drug candidates.
Fang L, Appenroth D, Decker M, Kiehntopf M, Roegler C, Deufel T, Fleck C, Peng S, Zhang Y, Lehmann J.
J Med Chem (2008) 51 : 713 -716
PubMed 18232655 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 7.59 8.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL407320 1 8.25
CHEMBL261384 1 8.20
CHEMBL270491 1 8.19
CHEMBL272229 1 8.00
CHEMBL277984 1 7.96
CHEMBL260308 1 7.74
CHEMBL271385 1 7.67
CHEMBL273078 1 7.65
CHEMBL269865 1 7.55
CHEMBL273051 1 7.45
CHEMBL95 TACRINE 4.0 1 7.35
CHEMBL272230 1 7.34
CHEMBL260964 1 7.29
CHEMBL270349 1 7.16
CHEMBL269863 1 7.03
CHEMBL271746 1 6.65

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL407320 IC50 = 5.6 nM 8.25
CHEMBL261384 IC50 = 6.3 nM 8.20
CHEMBL270491 IC50 = 6.4 nM 8.19
CHEMBL272229 IC50 = 10.0 nM 8.00
CHEMBL277984 IC50 = 11.1 nM 7.96
CHEMBL260308 IC50 = 18.1 nM 7.74
CHEMBL271385 IC50 = 21.6 nM 7.67
CHEMBL273078 IC50 = 22.6 nM 7.65
CHEMBL269865 IC50 = 28.2 nM 7.55
CHEMBL273051 IC50 = 35.5 nM 7.45
CHEMBL95 TACRINE IC50 = 45.1 nM 7.35
CHEMBL272230 IC50 = 45.7 nM 7.34
CHEMBL260964 IC50 = 50.7 nM 7.29
CHEMBL270349 IC50 = 69.5 nM 7.16
CHEMBL269863 IC50 = 93.0 nM 7.03
CHEMBL271746 IC50 = 226.0 nM 6.65