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Found 9 Enz. Inhib. hit(s) for PDB: 5IW0
TargetLysine-specific demethylase 5A(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM191600(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
Affinity DataIC50:  13nMAssay Description:Inhibition of KDM5A (unknown origin) preincubated with enzymeMore data for this Ligand-Target Pair
TargetLysine-specific demethylase 5A(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM191600(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
Affinity DataIC50: <100nMAssay Description:Inhibition of KDM5A in human ZR-75-1 cells assessed as reduction in H3K4me3 demethylation incubated for 72 hrs by fluorometric immunoassayMore data for this Ligand-Target Pair
TargetLysine-specific demethylase 5A(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM191600(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
Affinity DataIC50: <100nMAssay Description:The enzymatic assay of Jarid1A activity is based upon Time Resolved-Fluorescence Resonance Energy Transfer (TR-FRET) detection. The ability of test c...More data for this Ligand-Target Pair
TargetLysine-specific demethylase 5A(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM191600(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
Affinity DataIC50: <100nMAssay Description:Inhibition of recombinant human C-terminal FLAG-tagged KDM5A (1 to 1090 residues) expressed in baculovirus infected sf9 cells using biotin-H3K4me3 su...More data for this Ligand-Target Pair
TargetLysine-specific demethylase 5A [1-1090](Homo sapiens (Human))
Emory University

LigandPNGBDBM191600(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
Affinity DataIC50:  240nMpH: 7.2 T: 2°CAssay Description:Reactions were performed in 50 mM HEPES [pH 7.2 for KDM5 or pH 7.5 for KDM4A(1-350)] containing 0.01% BSA and 0.01% Tween-20. To each well, 3 μL...More data for this Ligand-Target Pair
TargetLysine-specific demethylase 5A [1-739](Homo sapiens (Human))
Emory University

LigandPNGBDBM191600(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
Affinity DataIC50:  5.00E+3nMT: 2°CAssay Description:For inhibition assays, powders of inhibitor compounds were dissolved in 100% (v/v) DMSO to give a 20 or 50 mM concentration and stored at -20 °C unti...More data for this Ligand-Target Pair
TargetLysine-specific demethylase 5A/5B(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM191600(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
Affinity DataEC50:  90nMAssay Description:Inhibition of KDM5A/KDM5B in human ZR-75-1 cells assessed as increase in H3K4me3 level after 72 hrs by fluorometric immunoassayMore data for this Ligand-Target Pair
TargetLysine-specific demethylase 5B [1-604](Homo sapiens (Human))
Emory University

LigandPNGBDBM191600(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
Affinity DataKd:  70nMAssay Description:ITC experiments were carried out at an enzyme [E] concentration of 25-50 μM with 0.25-1 mM compound [I] concentration in the KDM5 storage buffer...More data for this Ligand-Target Pair
TargetLysine-specific demethylase 5A [1-588](Homo sapiens (Human))
Emory University

LigandPNGBDBM191600(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
Affinity DataKd:  60nMAssay Description:ITC experiments were carried out at an enzyme [E] concentration of 25-50 μM with 0.25-1 mM compound [I] concentration in the KDM5 storage buffer...More data for this Ligand-Target Pair