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Assay Detail

CHEMBL3292817

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

Binding
Inhibition of MAO-B in rat liver homogenate using [14C]-phenylethylamine as substrate preincubated for 30 mins followed by substrate addition measured after 4 mins by liquid scintillation counting analysis
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Liver
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Amine oxidase [flavin-containing] B (CHEMBL2993)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Donepezil + propargylamine + 8-hydroxyquinoline hybrids as new multifunctional metal-chelators, ChE and MAO inhibitors for the potential treatment of Alzheimer's disease.
Wang L, Esteban G, Ojima M, Bautista-Aguilera OM, Inokuchi T, Moraleda I, Iriepa I, Samadi A, Youdim MB, Romero A, Soriano E, Herrero R, Fernández Fernández AP, Ricardo-Martínez-Murillo, Marco-Contelles J, Unzeta M.
Eur J Med Chem (2014) 80 : 543 -561
PubMed 24813882 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.17 8.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL972 SELEGILINE 4.0 1 8.17
CHEMBL3291021 1 5.82
CHEMBL8706 CLORGILINE 2.0 1 5.10
CHEMBL3291019 1 4.99
CHEMBL3291017 1 4.91
CHEMBL502 DONEPEZIL 4.0 1 4.82
CHEMBL3291016 1 4.71
CHEMBL3291020 1 4.46
CHEMBL3291015 1 4.40
CHEMBL3291018 1 4.30
CHEMBL3291014 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL972 SELEGILINE IC50 = 6.7 nM 8.17
CHEMBL3291021 IC50 = 1500.0 nM 5.82
CHEMBL8706 CLORGILINE IC50 = 8000.0 nM 5.10
CHEMBL3291019 IC50 = 10200.0 nM 4.99
CHEMBL3291017 IC50 = 12400.0 nM 4.91
CHEMBL502 DONEPEZIL IC50 = 15000.0 nM 4.82
CHEMBL3291016 IC50 = 19400.0 nM 4.71
CHEMBL3291020 IC50 = 34500.0 nM 4.46
CHEMBL3291015 IC50 = 39500.0 nM 4.40
CHEMBL3291018 IC50 = 50100.0 nM 4.30
CHEMBL3291014 IC50 >= 100000.0 nM -