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Assay Detail

CHEMBL4711036

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 preincubated for 30 mins followed by substrate addition and measured after 1 hr by fluorimetric analysis
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

A dual-acting 5-HT receptor inverse agonist/MAO-B inhibitor displays glioprotective and pro-cognitive properties.
Canale V,Grychowska K,Kurczab R,Ryng M,Keeri AR,Satała G,Olejarz-Maciej A,Koczurkiewicz P,Drop M,Blicharz K,Piska K,Pękala E,Janiszewska P,Krawczyk M,Walczak M,Chaumont-Dubel S,Bojarski AJ,Marin P,Popik P,Zajdel P
Eur J Med Chem (2020) 208 : 112765 -112765
PubMed 32949963 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 7.06 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL396778 SAFINAMIDE 4.0 1 8.15
CHEMBL887 RASAGILINE 4.0 1 7.81
CHEMBL4778708 1 7.52
CHEMBL4741978 1 6.81
CHEMBL4780498 1 6.79
CHEMBL4794139 1 6.57
CHEMBL4786924 1 6.49
CHEMBL4754407 1 6.34
CHEMBL4780446 1 -
CHEMBL4745652 1 -
CHEMBL4742220 1 -
CHEMBL4792096 1 -
CHEMBL4777701 1 -
CHEMBL4796358 1 -
CHEMBL4793457 1 -
CHEMBL4757296 1 -
CHEMBL4754024 1 -
CHEMBL4780366 1 -
CHEMBL4761469 1 -
CHEMBL4750021 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL396778 SAFINAMIDE IC50 = 7.0 nM 8.15
CHEMBL887 RASAGILINE IC50 = 15.4 nM 7.81
CHEMBL4778708 IC50 = 30.0 nM 7.52
CHEMBL4741978 IC50 = 154.0 nM 6.81
CHEMBL4780498 IC50 = 163.0 nM 6.79
CHEMBL4794139 IC50 = 270.0 nM 6.57
CHEMBL4786924 IC50 = 323.0 nM 6.49
CHEMBL4754407 IC50 = 460.0 nM 6.34
CHEMBL4780446 IC50 > 1000.0 nM -
CHEMBL4745652 IC50 > 1000.0 nM -
CHEMBL4742220 IC50 > 1000.0 nM -
CHEMBL4792096 IC50 > 1000.0 nM -
CHEMBL4777701 IC50 > 1000.0 nM -
CHEMBL4796358 IC50 > 1000.0 nM -
CHEMBL4793457 IC50 > 1000.0 nM -
CHEMBL4757296 IC50 > 1000.0 nM -
CHEMBL4754024 IC50 > 1000.0 nM -
CHEMBL4780366 IC50 > 1000.0 nM -
CHEMBL4761469 IC50 > 1000.0 nM -
CHEMBL4750021 IC50 > 1000.0 nM -