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Assay Detail

CHEMBL3707988

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

Binding
MAO-A and MAO-B Assays: MAO assays included luminogenic MAO substrate, reaction buffers, Luciferin Detection and the reconstitution buffer with esterase. Standard MAO reaction mixtures included microsome contained MAO-A (2 ug) or MAO-B (10 ug), 160 uM substrate for MAO-A or 16 uM substrate for MAO-B, MAO-A buffer (100 mM Hepes buffer, pH 7.5, 5% glycerol) or MAO-B buffer (100 mM Hepes, pH 7.5, 5% glycerol, 10% dimethyl sulfoxide) in a final volume of 30 ul. After 20 minutes of pre-incubation of the enzyme with compounds, the reaction was initiated by adding enzyme substrate and the reaction was allowed to proceed for 60 minutes. Reconstituted Luciferin Detection Reagent (30 ul) was then added is added to simultaneously stop the MAO reaction and convert the methyl ester derivative to luciferin and produce light. The amount of light produced is directly proportional to the activity of MAO.
41
Total Activities
41
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

ALDH-2 inhibitors in the treatment of addiction
(2014)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 41 6.44 6.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3935026 1 6.44
CHEMBL3660748 1 -
CHEMBL3660736 1 -
CHEMBL3660752 1 -
CHEMBL3660726 1 -
CHEMBL3918259 1 -
CHEMBL3660731 1 -
CHEMBL3660733 1 -
CHEMBL3660747 1 -
CHEMBL3660728 1 -
CHEMBL3660742 1 -
CHEMBL3660730 1 -
CHEMBL3660734 1 -
CHEMBL3660745 1 -
CHEMBL3660749 1 -
CHEMBL3915386 1 -
CHEMBL3660719 1 -
CHEMBL3660722 1 -
CHEMBL3660735 1 -
CHEMBL3660732 1 -
CHEMBL3660724 1 -
CHEMBL3660713 1 -
CHEMBL3660743 1 -
CHEMBL3660721 1 -
CHEMBL3660714 1 -
CHEMBL3660739 1 -
CHEMBL3660740 1 -
CHEMBL3660712 1 -
CHEMBL3660718 1 -
CHEMBL3660717 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3935026 IC50 = 365.0 nM 6.44
CHEMBL3660744 IC50 > 130000.0 nM -
CHEMBL3660728 IC50 > 130000.0 nM -
CHEMBL3660747 IC50 > 130000.0 nM -
CHEMBL3660733 IC50 > 130000.0 nM -
CHEMBL3660731 IC50 > 130000.0 nM -
CHEMBL3918259 IC50 > 130000.0 nM -
CHEMBL3660726 IC50 > 130000.0 nM -
CHEMBL3660752 IC50 > 130000.0 nM -
CHEMBL3660736 IC50 > 130000.0 nM -
CHEMBL3660725 IC50 > 130000.0 nM -
CHEMBL3660730 IC50 > 130000.0 nM -
CHEMBL3660727 IC50 > 130000.0 nM -
CHEMBL3660723 IC50 > 130000.0 nM -
CHEMBL3660751 IC50 > 130000.0 nM -
CHEMBL3660738 IC50 > 130000.0 nM -
CHEMBL3660729 IC50 > 130000.0 nM -
CHEMBL3660716 IC50 > 130000.0 nM -
CHEMBL3660741 IC50 > 130000.0 nM -
CHEMBL3660746 IC50 > 130000.0 nM -
CHEMBL5856466 IC50 > 130000.0 nM -
CHEMBL3660724 IC50 > 130000.0 nM -
CHEMBL3660717 IC50 > 130000.0 nM -
CHEMBL3660718 IC50 > 130000.0 nM -
CHEMBL3660712 IC50 > 13000.0 nM -
CHEMBL3660740 IC50 > 130000.0 nM -
CHEMBL3660739 IC50 > 130000.0 nM -
CHEMBL3660714 IC50 > 91000.0 nM -
CHEMBL3660721 IC50 = 114002.0 nM -
CHEMBL3660743 IC50 > 130000.0 nM -
CHEMBL3660713 IC50 > 13000.0 nM -
CHEMBL3660742 IC50 > 130000.0 nM -
CHEMBL3660732 IC50 > 130000.0 nM -
CHEMBL3660735 IC50 > 130000.0 nM -
CHEMBL3660722 IC50 > 130000.0 nM -
CHEMBL3660719 IC50 > 130000.0 nM -
CHEMBL3660748 IC50 > 130000.0 nM -
CHEMBL3915386 IC50 > 130000.0 nM -
CHEMBL3660749 IC50 > 130000.0 nM -
CHEMBL3660745 IC50 > 130000.0 nM -
CHEMBL3660734 IC50 > 94402.0 nM -