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Assay Detail

CHEMBL864026

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

Binding
Inhibition of human AChE
9
Total Activities
9
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

Acetylcholinesterase (CHEMBL220)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel tacrine-melatonin hybrids as dual-acting drugs for Alzheimer disease, with improved acetylcholinesterase inhibitory and antioxidant properties.
Rodríguez-Franco MI, Fernández-Bachiller MI, Pérez C, Hernández-Ledesma B, Bartolomé B.
J Med Chem (2006) 49 : 459 -462
PubMed 16420031 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 9.11 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL372202 1 10.40
CHEMBL381499 1 10.00
CHEMBL370807 1 9.35
CHEMBL199670 1 9.30
CHEMBL382260 1 9.19
CHEMBL202661 1 9.06
CHEMBL95 TACRINE 4.0 1 6.46
CHEMBL45 MELATONIN 4.0 1 -
CHEMBL199585 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL372202 IC50 = 0.04 nM 10.40
CHEMBL381499 IC50 = 0.1 nM 10.00
CHEMBL370807 IC50 = 0.45 nM 9.35
CHEMBL199670 IC50 = 0.5 nM 9.30
CHEMBL382260 IC50 = 0.65 nM 9.19
CHEMBL202661 IC50 = 0.87 nM 9.06
CHEMBL95 TACRINE IC50 = 350.0 nM 6.46
CHEMBL45 MELATONIN IC50 - -
CHEMBL199585 IC50 = 0.008 nM -