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Assay Detail

CHEMBL1815009

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Binding
Inhibition of human MAO-B assessed as inhibition of p-tyramine oxidation to p-hydroxyphenyl-acetaldehyde after 15 mins by fluorimetric method
15
Total Activities
15
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

Chromone, a privileged scaffold for the development of monoamine oxidase inhibitors.
Gaspar A, Silva T, Yáñez M, Vina D, Orallo F, Ortuso F, Uriarte E, Alcaro S, Borges F.
J Med Chem (2011) 54 : 5165 -5173
PubMed 21696156 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 5.98 7.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1814068 1 7.20
CHEMBL1814064 1 7.19
CHEMBL1814065 1 7.12
CHEMBL1814070 1 6.96
CHEMBL1814066 1 6.80
CHEMBL1643120 1 6.40
CHEMBL1814072 1 6.03
CHEMBL1814069 1 5.97
CHEMBL1814067 1 5.63
CHEMBL1814057 1 5.58
CHEMBL92401 IPRONIAZID 2.0 1 5.12
CHEMBL1814071 1 4.93
CHEMBL1814073 1 4.42
CHEMBL1814055 1 4.38
CHEMBL972 SELEGILINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1814068 IC50 = 63.0 nM 7.20
CHEMBL1814064 IC50 = 64.0 nM 7.19
CHEMBL1814065 IC50 = 76.0 nM 7.12
CHEMBL1814070 IC50 = 110.0 nM 6.96
CHEMBL1814066 IC50 = 160.0 nM 6.80
CHEMBL1643120 IC50 = 400.0 nM 6.40
CHEMBL1814072 IC50 = 930.0 nM 6.03
CHEMBL1814069 IC50 = 1080.0 nM 5.97
CHEMBL1814067 IC50 = 2330.0 nM 5.63
CHEMBL1814057 IC50 = 2660.0 nM 5.58
CHEMBL92401 IPRONIAZID IC50 = 7540.0 nM 5.12
CHEMBL1814071 IC50 = 11780.0 nM 4.93
CHEMBL1814073 IC50 = 37690.0 nM 4.42
CHEMBL1814055 IC50 = 41900.0 nM 4.38
CHEMBL972 SELEGILINE IC50 = 17.0 nM -