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Assay Detail

CHEMBL5729883

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.
123
Total Activities
41
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Amine oxidase [flavin-containing] A (CHEMBL1951)
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 4.33 4.33
kon 41 - -
k_off 41 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3660740 3 4.33
CHEMBL3660747 3 -
CHEMBL3918259 3 -
CHEMBL3660719 3 -
CHEMBL3660718 3 -
CHEMBL3660717 3 -
CHEMBL3660716 3 -
CHEMBL3935026 3 -
CHEMBL3660714 3 -
CHEMBL3660713 3 -
CHEMBL3660722 3 -
CHEMBL3660752 3 -
CHEMBL3660751 3 -
CHEMBL5856466 3 -
CHEMBL3660749 3 -
CHEMBL3660748 3 -
CHEMBL3660746 3 -
CHEMBL3660745 3 -
CHEMBL3660744 3 -
CHEMBL3660732 3 -
CHEMBL3660742 3 -
CHEMBL3660741 3 -
CHEMBL3660739 3 -
CHEMBL3660738 3 -
CHEMBL3915386 3 -
CHEMBL3660736 3 -
CHEMBL3660735 3 -
CHEMBL3660734 3 -
CHEMBL3660733 3 -
CHEMBL3660743 3 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3660740 IC50 = 46947.0 nM 4.33
CHEMBL3660751 IC50 = 110381.0 nM -
CHEMBL3660741 IC50 > 130000.0 nM -
CHEMBL3660741 kon = - -
CHEMBL3660741 k_off = - s-1 -
CHEMBL3660742 IC50 > 130000.0 nM -
CHEMBL3660742 kon = - -
CHEMBL3660747 k_off = - s-1 -
CHEMBL3660752 k_off = - s-1 -
CHEMBL3660752 kon = - -
CHEMBL3660752 IC50 > 130000.0 nM -
CHEMBL3660751 k_off = - s-1 -
CHEMBL3660751 kon = - -
CHEMBL3660740 k_off = - s-1 -
CHEMBL5856466 k_off = - s-1 -
CHEMBL5856466 kon = - -
CHEMBL5856466 IC50 > 130000.0 nM -
CHEMBL3660749 k_off = - s-1 -
CHEMBL3660749 kon = - -
CHEMBL3660749 IC50 > 130000.0 nM -
CHEMBL3660748 k_off = - s-1 -
CHEMBL3660748 kon = - -
CHEMBL3660748 IC50 > 130000.0 nM -
CHEMBL3660744 k_off = - s-1 -
CHEMBL3660744 kon = - -
CHEMBL3660744 IC50 > 130000.0 nM -
CHEMBL3660736 IC50 > 130000.0 nM -
CHEMBL3660742 k_off = - s-1 -
CHEMBL3660732 k_off = - s-1 -
CHEMBL3660733 IC50 > 86479.0 nM -
CHEMBL3660733 kon = - -
CHEMBL3660733 k_off = - s-1 -
CHEMBL3660734 IC50 > 130000.0 nM -
CHEMBL3660734 kon = - -
CHEMBL3660734 k_off = - s-1 -
CHEMBL3660735 IC50 > 130000.0 nM -
CHEMBL3660735 kon = - -
CHEMBL3660735 k_off = - s-1 -
CHEMBL3660740 kon = - -
CHEMBL3660736 kon = - -
CHEMBL3660736 k_off = - s-1 -
CHEMBL3915386 IC50 > 130000.0 nM -
CHEMBL3915386 kon = - -
CHEMBL3915386 k_off = - s-1 -
CHEMBL3660738 IC50 > 130000.0 nM -
CHEMBL3660738 kon = - -
CHEMBL3660738 k_off = - s-1 -
CHEMBL3660739 IC50 > 130000.0 nM -
CHEMBL3660739 kon = - -
CHEMBL3660739 k_off = - s-1 -