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Assay Detail

CHEMBL4273249

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

Binding
Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect cells using p-tyramine as substrate pretreated for 15 mins followed by substrate addition by horse-radish peroxidase/amplex red-based fluorescence method
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Amine oxidase [flavin-containing] B (CHEMBL2039)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Neurogenic and neuroprotective donepezil-flavonoid hybrids with sigma-1 affinity and inhibition of key enzymes in Alzheimer's disease.
Estrada Valencia M, Herrera-Arozamena C, de Andrés L, Pérez C, Morales-García JA, Pérez-Castillo A, Ramos E, Romero A, Viña D, Yáñez M, Laurini E, Pricl S, Rodríguez-Franco MI.
Eur J Med Chem (2018) 156 : 534 -553
PubMed 30025348 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 4.57 5.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4287970 1 5.28
CHEMBL92401 IPRONIAZID 2.0 1 5.12
CHEMBL4285912 1 4.87
CHEMBL4280725 1 4.42
CHEMBL4291296 1 4.29
CHEMBL4282527 1 4.25
CHEMBL4294609 1 4.22
CHEMBL4290401 1 4.14
CHEMBL4295144 1 -
CHEMBL4286799 1 -
CHEMBL4283450 1 -
CHEMBL4285779 1 -
CHEMBL4277548 1 -
CHEMBL4292477 1 -
CHEMBL4277332 1 -
CHEMBL4291372 1 -
CHEMBL4283079 1 -
CHEMBL4294783 1 -
CHEMBL4287548 1 -
CHEMBL4293801 1 -
CHEMBL93 ZILEUTON 4.0 1 -
CHEMBL52 NORDIHYDROGUAIARETIC ACID 1 -
CHEMBL972 SELEGILINE 4.0 1 -
CHEMBL86304 MOCLOBEMIDE 4.0 1 -
CHEMBL4284165 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4287970 IC50 = 5200.0 nM 5.28
CHEMBL92401 IPRONIAZID IC50 = 7500.0 nM 5.12
CHEMBL4285912 IC50 = 13600.0 nM 4.87
CHEMBL4280725 IC50 = 37900.0 nM 4.42
CHEMBL4291296 IC50 = 51200.0 nM 4.29
CHEMBL4282527 IC50 = 56400.0 nM 4.25
CHEMBL4294609 IC50 = 59900.0 nM 4.22
CHEMBL4290401 IC50 = 71600.0 nM 4.14
CHEMBL4295144 IC50 - -
CHEMBL4286799 IC50 - -
CHEMBL4283450 IC50 > 100000.0 nM -
CHEMBL4285779 IC50 > 100000.0 nM -
CHEMBL4277548 IC50 > 100000.0 nM -
CHEMBL4292477 IC50 > 100000.0 nM -
CHEMBL4277332 IC50 - -
CHEMBL4291372 IC50 > 100000.0 nM -
CHEMBL4283079 IC50 - -
CHEMBL4294783 IC50 > 100000.0 nM -
CHEMBL4287548 IC50 > 100000.0 nM -
CHEMBL4293801 IC50 > 100000.0 nM -
CHEMBL93 ZILEUTON IC50 - -
CHEMBL52 NORDIHYDROGUAIARETIC ACID IC50 - -
CHEMBL972 SELEGILINE IC50 = 17.0 nM -
CHEMBL86304 MOCLOBEMIDE IC50 > 1000000.0 nM -
CHEMBL4284165 IC50 > 100000.0 nM -