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Assay Detail

CHEMBL3096737

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

Binding
Inhibition of Sprague-Dawley rat MAO-A using Kynuramine as substrate assessed as formation of 4-hydroxyquinoline preincubated for 5 mins prior to substrate addition measured for 5 mins by spectrophotometry
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Amine oxidase [flavin-containing] A (CHEMBL3358)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Fine molecular tuning at position 4 of 2H-chromen-2-one derivatives in the search of potent and selective monoamine oxidase B inhibitors.
Pisani L, Catto M, Nicolotti O, Grossi G, Di Braccio M, Soto-Otero R, Mendez-Alvarez E, Stefanachi A, Gadaleta D, Carotti A.
Eur J Med Chem (2013) 70 : 723 -739
PubMed 24231308 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 5.36 6.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3094011 1 6.55
CHEMBL575093 1 6.33
CHEMBL575931 1 6.30
CHEMBL572534 1 5.70
CHEMBL3094007 1 5.39
CHEMBL3094030 1 5.38
CHEMBL575934 1 5.28
CHEMBL239507 1 5.23
CHEMBL3094017 1 5.05
CHEMBL3094024 1 5.05
CHEMBL3094008 1 5.03
CHEMBL3094037 1 4.99
CHEMBL3093992 1 4.93
CHEMBL3094016 1 4.62
CHEMBL575738 1 4.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3094011 IC50 = 281.84 nM 6.55
CHEMBL575093 IC50 = 467.74 nM 6.33
CHEMBL575931 IC50 = 501.19 nM 6.30
CHEMBL572534 IC50 = 1995.26 nM 5.70
CHEMBL3094007 IC50 = 4073.8 nM 5.39
CHEMBL3094030 IC50 = 4168.69 nM 5.38
CHEMBL575934 IC50 = 5248.07 nM 5.28
CHEMBL239507 IC50 = 5888.44 nM 5.23
CHEMBL3094017 IC50 = 8912.51 nM 5.05
CHEMBL3094024 IC50 = 8912.51 nM 5.05
CHEMBL3094008 IC50 = 9332.54 nM 5.03
CHEMBL3094037 IC50 = 10232.93 nM 4.99
CHEMBL3093992 IC50 = 11748.98 nM 4.93
CHEMBL3094016 IC50 = 23988.33 nM 4.62
CHEMBL575738 IC50 = 25703.96 nM 4.59