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Assay Detail

CHEMBL864025

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

Binding
Inhibition of AchE from bovine erythrocytes
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Acetylcholinesterase (CHEMBL4768)
Type SINGLE PROTEIN
Organism Bos taurus

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 15 8.25 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL381499 1 9.70
CHEMBL199670 1 9.00
CHEMBL199585 1 8.70
CHEMBL383663 1 8.70
CHEMBL382260 1 8.64
CHEMBL199538 1 8.46
CHEMBL199861 1 8.40
CHEMBL372202 1 8.30
CHEMBL199454 1 8.05
CHEMBL199748 1 7.92
CHEMBL200008 1 7.60
CHEMBL370807 1 7.46
CHEMBL95 TACRINE 4.0 1 7.40
CHEMBL202661 1 7.19
CHEMBL45 MELATONIN 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL381499 IC50 = 0.2 nM 9.70
CHEMBL199670 IC50 = 1.0 nM 9.00
CHEMBL199585 IC50 = 2.0 nM 8.70
CHEMBL383663 IC50 = 2.0 nM 8.70
CHEMBL382260 IC50 = 2.3 nM 8.64
CHEMBL199538 IC50 = 3.5 nM 8.46
CHEMBL199861 IC50 = 4.0 nM 8.40
CHEMBL372202 IC50 = 5.0 nM 8.30
CHEMBL199454 IC50 = 9.0 nM 8.05
CHEMBL199748 IC50 = 12.0 nM 7.92
CHEMBL200008 IC50 = 25.0 nM 7.60
CHEMBL370807 IC50 = 35.0 nM 7.46
CHEMBL95 TACRINE IC50 = 40.0 nM 7.40
CHEMBL202661 IC50 = 65.0 nM 7.19
CHEMBL45 MELATONIN IC50 > 100.0 nM -