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Found 15 Enz. Inhib. hit(s) with Target = 'Lysine-specific histone demethylase 1A' and Ligand = 'BDBM50158869'
TargetLysine-specific histone demethylase 1A(Homo sapiens (Human))
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50158869(CHEMBL3786182 | US10836743, Compound GSK-2879552 |...)
Affinity DataKi:  9.60nMAssay Description:Time dependant inhibition of recombinant N-terminal His-tagged LSD1 (unknown origin) expressed in Escherichia coli expression system assessed as inhi...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLysine-specific histone demethylase 1A(Homo sapiens (Human))
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50158869(CHEMBL3786182 | US10836743, Compound GSK-2879552 |...)
Affinity DataKi:  1.70E+3nMAssay Description:Inhibition of KDM1A (unknown origin) by peroxidase coupled assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLysine-specific histone demethylase 1A(Homo sapiens (Human))
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50158869(CHEMBL3786182 | US10836743, Compound GSK-2879552 |...)
Affinity DataKi:  1.70E+3nMAssay Description:Inhibition of LSD1 (unknown origin) using H3K4(diMe) peptide as substrate measured after 60 mins by amplex red dye based HRP-coupled assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLysine-specific histone demethylase 1A(Homo sapiens (Human))
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50158869(CHEMBL3786182 | US10836743, Compound GSK-2879552 |...)
Affinity DataIC50:  24nMAssay Description:Dissociation constant against galectin-3 using competitive fluorescence polarizationMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLysine-specific histone demethylase 1A(Homo sapiens (Human))
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50158869(CHEMBL3786182 | US10836743, Compound GSK-2879552 |...)
Affinity DataIC50:  24nMAssay Description:Inhibition of full length recombinant LSD1 (unknown origin) expressed in Escherichia coli BL21(DE3) using H3K4me2 as substrate after 30 mins in prese...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLysine-specific histone demethylase 1A(Homo sapiens (Human))
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50158869(CHEMBL3786182 | US10836743, Compound GSK-2879552 |...)
Affinity DataIC50:  24nMAssay Description:Inhibition of LSD1 (unknown origin) using H3K4(diMe) peptide as substrate measured after 60 mins by amplex red dye based HRP-coupled assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLysine-specific histone demethylase 1A(Homo sapiens (Human))
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50158869(CHEMBL3786182 | US10836743, Compound GSK-2879552 |...)
Affinity DataIC50:  41nMAssay Description:Inhibition of full length recombinant LSD1 (unknown origin) expressed in Escherichia coli BL21(DE) using H3K4me2 as substrate by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLysine-specific histone demethylase 1A(Homo sapiens (Human))
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50158869(CHEMBL3786182 | US10836743, Compound GSK-2879552 |...)
Affinity DataIC50:  160nMAssay Description:Inhibition of human LSD1 using H3K4Me2 peptide as substrate incubated for 60 min by horseradish peroxidase coupled assayMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetLysine-specific histone demethylase 1A(Homo sapiens (Human))
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50158869(CHEMBL3786182 | US10836743, Compound GSK-2879552 |...)
Affinity DataIC50:  212nMAssay Description:Inhibition of recombinant N-terminal His-tagged LSD1 (unknown origin) expressed in Escherichia coli expression system using ART-K(Me1)-QTARKSTGGKAPRK...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLysine-specific histone demethylase 1A(Homo sapiens (Human))
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50158869(CHEMBL3786182 | US10836743, Compound GSK-2879552 |...)
Affinity DataIC50:  311nMAssay Description:The biochemical inhibition activity of the synthesized compounds on LSD1 was measured. The activity measurement was performed using LSD1 fluorescence...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetLysine-specific histone demethylase 1A(Homo sapiens (Human))
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50158869(CHEMBL3786182 | US10836743, Compound GSK-2879552 |...)
Affinity DataIC50:  404nMAssay Description:Principle: LSD1 specifically removes the methylation modification at K4 lysine on H3 polypeptide substrate, making it a substrate without methylation...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetLysine-specific histone demethylase 1A(Homo sapiens (Human))
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50158869(CHEMBL3786182 | US10836743, Compound GSK-2879552 |...)
Affinity DataIC50:  1.20E+3nMAssay Description:Inhibition of recombinant human LSD1 (172 to 852 residues) using biotin-labelled H3K4me2 (1 to 24 residues) after 1 hr by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLysine-specific histone demethylase 1A(Homo sapiens (Human))
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50158869(CHEMBL3786182 | US10836743, Compound GSK-2879552 |...)
Affinity DataIC50:  1.22E+3nMAssay Description:Screening method: lysine-specific demethylase 1 (LSD1) activity screeningInstrument: microplate reader Envision™ (PerkinElmer, USA).MATERIALS: Human ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetLysine-specific histone demethylase 1A(Homo sapiens (Human))
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50158869(CHEMBL3786182 | US10836743, Compound GSK-2879552 |...)
Affinity DataIC50:  4.04E+5nMAssay Description:Inhibition of N-terminal His/GST-tagged human LSD1 (172 to 852 residues) expressed in expressed in baculovirus infected insect cells using biotinylat...More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetLysine-specific histone demethylase 1A(Homo sapiens (Human))
Constellation Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50158869(CHEMBL3786182 | US10836743, Compound GSK-2879552 |...)
Affinity DataEC50:  54nMAssay Description:Inhibition of LSD1 in human MV4-11 cells assessed as induction of LY96 mRNA expression incubated for 16 hrs by chemiluminescent methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed