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Assay Detail

CHEMBL4197756

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

Binding
Inhibition of human MAO-B expressed in baculovirus infected insect cell membranes using kynuramine as substrate preincubated for 30 mins followed by substrate addition measured after 15 to 20 mins by discontinuous fluorimetric method
5
Total Activities
5
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

Novel indanone derivatives as MAO B/H3R dual-targeting ligands for treatment of Parkinson's disease.
Affini A, Hagenow S, Zivkovic A, Marco-Contelles J, Stark H.
Eur J Med Chem (2018) 148 : 487 -497
PubMed 29477889 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.11 8.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL972 SELEGILINE 4.0 1 8.41
CHEMBL396778 SAFINAMIDE 4.0 1 7.68
CHEMBL4217355 1 6.63
CHEMBL4205653 1 6.58
CHEMBL4218833 1 6.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL972 SELEGILINE IC50 = 3.9 nM 8.41
CHEMBL396778 SAFINAMIDE IC50 = 21.0 nM 7.68
CHEMBL4217355 IC50 = 232.0 nM 6.63
CHEMBL4205653 IC50 = 262.0 nM 6.58
CHEMBL4218833 IC50 = 541.0 nM 6.27