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Assay Detail

CHEMBL4042091

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

Binding
Inhibition of recombinant human MAO-B assessed as reduction in 4-hydroxyquinolone production using kynuramine as substrate after 20 mins by fluorescence assay
29
Total Activities
29
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

Synthesis and evaluation of 7-substituted coumarin derivatives as multimodal monoamine oxidase-B and cholinesterase inhibitors for the treatment of Alzheimer's disease.
Joubert J, Foka GB, Repsold BP, Oliver DW, Kapp E, Malan SF.
Eur J Med Chem (2017) 125 : 853 -864
PubMed 27744252 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 7.19 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4068321 1 9.30
CHEMBL4079843 1 9.10
CHEMBL4097867 1 9.05
CHEMBL4105601 1 8.89
CHEMBL4095676 1 8.72
CHEMBL108660 1 8.70
CHEMBL4094745 1 8.68
CHEMBL4082300 1 8.66
CHEMBL145781 7-BENZYLOXYCOUMARIN 1 8.42
CHEMBL972 SELEGILINE 4.0 1 8.10
CHEMBL4060398 1 7.89
CHEMBL4069084 1 7.75
CHEMBL4090150 1 7.14
CHEMBL4087723 1 6.98
CHEMBL4067432 1 6.54
CHEMBL4088674 1 6.52
CHEMBL4078343 1 6.33
CHEMBL4096387 1 6.28
CHEMBL4089608 1 5.85
CHEMBL4104128 1 5.81
CHEMBL4066437 1 5.77
CHEMBL4091054 1 5.51
CHEMBL4086218 1 5.44
CHEMBL4093982 1 5.27
CHEMBL4061479 1 5.25
CHEMBL4063174 1 5.04
CHEMBL8706 CLORGILINE 2.0 1 -
CHEMBL502 DONEPEZIL 4.0 1 -
CHEMBL95 TACRINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4068321 IC50 = 0.5 nM 9.30
CHEMBL4079843 IC50 = 0.8 nM 9.10
CHEMBL4097867 IC50 = 0.9 nM 9.05
CHEMBL4105601 IC50 = 1.3 nM 8.89
CHEMBL4095676 IC50 = 1.9 nM 8.72
CHEMBL108660 IC50 = 2.0 nM 8.70
CHEMBL4094745 IC50 = 2.1 nM 8.68
CHEMBL4082300 IC50 = 2.2 nM 8.66
CHEMBL145781 7-BENZYLOXYCOUMARIN IC50 = 3.8 nM 8.42
CHEMBL972 SELEGILINE IC50 = 8.0 nM 8.10
CHEMBL4060398 IC50 = 13.0 nM 7.89
CHEMBL4069084 IC50 = 18.0 nM 7.75
CHEMBL4090150 IC50 = 73.0 nM 7.14
CHEMBL4087723 IC50 = 104.0 nM 6.98
CHEMBL4067432 IC50 = 290.0 nM 6.54
CHEMBL4088674 IC50 = 300.0 nM 6.52
CHEMBL4078343 IC50 = 470.0 nM 6.33
CHEMBL4096387 IC50 = 530.0 nM 6.28
CHEMBL4089608 IC50 = 1410.0 nM 5.85
CHEMBL4104128 IC50 = 1550.0 nM 5.81
CHEMBL4066437 IC50 = 1700.0 nM 5.77
CHEMBL4091054 IC50 = 3090.0 nM 5.51
CHEMBL4086218 IC50 = 3600.0 nM 5.44
CHEMBL4093982 IC50 = 5330.0 nM 5.27
CHEMBL4061479 IC50 = 5640.0 nM 5.25
CHEMBL4063174 IC50 = 9210.0 nM 5.04
CHEMBL8706 CLORGILINE IC50 - -
CHEMBL502 DONEPEZIL IC50 - -
CHEMBL95 TACRINE IC50 - -