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EC 1.14.99.66 (lysine-specific histone demethylase 1A) inhibitor

An EC 1.14.99.* (miscellaneous oxidoreductase acting on paired donors, with incorporation or reduction of molecular oxygen) inhibitor that interferes with the action of lysine-specific histone demethylase 1A (EC 1.14.99.66).

ChEBI ID: 131509

Members (1)

MemberDefinitionClass
gsk2879552A member of the class of piperidines that is piperidine substituted by (4-carboxyphenyl)methyl and {[(1R,2S)-2-phenylcyclopropyl]amino}methyl groups at positions 1 and 4, respectively. It is a potent and irreversible inhibitor of lysine specific demethylase 1 (LSD1, also known as KDM1A). It was under clinical investigation for the treatment of acute myeloid leukaemia and small cell lung carcinoma.GSK2879552

Research

Studies (29)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's18 (62.07)24.3611
2020's11 (37.93)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials2 (6.90%)5.53%
Reviews5 (17.24%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other22 (75.86%)84.16%

Protein Targets (5)

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Amine oxidase [flavin-containing] AHomo sapiens (human)IC50100.000033
Amine oxidase [flavin-containing] BHomo sapiens (human)IC50100.000033
Cytochrome P450 2C9 Homo sapiens (human)IC50100.000011
Lysine-specific histone demethylase 1AHomo sapiens (human)IC5050.698188
Lysine-specific histone demethylase 1AHomo sapiens (human)Ki1.136533
Lysine-specific histone demethylase 1BHomo sapiens (human)IC50100.000022

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Lysine-specific histone demethylase 1AHomo sapiens (human)EC500.054011