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Compile Data Set for Download or QSAR
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
(change energy unit to
kcal/mol
)
Found
36
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Target
Lysine-specific demethylase 5B
(Homo sapiens (Human))
Zhengzhou University
Curated by
ChEMBL
Ligand
BDBM191600
(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
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Affinity Data
IC50: 2nM
Assay Description:
Inhibition of full length human KDM5B expressed in baculovirus expression system using (ARTK(me3)QTARKSTGGKAPRKQLA peptide subst
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Target
Lysine-specific demethylase 5B
(Homo sapiens (Human))
Zhengzhou University
Curated by
ChEMBL
Ligand
BDBM191600
(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
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Affinity Data
IC50: 2nM
Assay Description:
Inhibition of KDM5B (unknown origin) preincubated with enzyme
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Target
Lysine-specific demethylase 5A
(Homo sapiens (Human))
Celgene
Curated by
ChEMBL
Ligand
BDBM191600
(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
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Affinity Data
IC50: 13nM
Assay Description:
Inhibition of KDM5A (unknown origin) preincubated with enzyme
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Target
Lysine-specific demethylase 4C
(Homo sapiens (Human))
Celgene
Curated by
ChEMBL
Ligand
BDBM191600
(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
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Affinity Data
IC50: 35nM
Assay Description:
Inhibition of KDM4C (unknown origin) preincubated with enzyme
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Target
Lysine-specific demethylase 4A
(Homo sapiens (Human))
Celgene
Curated by
ChEMBL
Ligand
BDBM191600
(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
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Affinity Data
IC50: 99nM
Assay Description:
Inhibition of KDM4A (unknown origin)
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Target
Lysine-specific demethylase 5A
(Homo sapiens (Human))
Celgene
Curated by
ChEMBL
Ligand
BDBM191600
(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
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Affinity Data
IC50: <100nM
Assay Description:
Inhibition of KDM5A in human ZR-75-1 cells assessed as reduction in H3K4me3 demethylation incubated for 72 hrs by fluorometric immunoassay
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Target
Lysine-specific demethylase 5B
(Homo sapiens (Human))
Zhengzhou University
Curated by
ChEMBL
Ligand
BDBM191600
(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
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Affinity Data
IC50: <100nM
Assay Description:
The ability of test compounds to inhibit the activity of Jarid1B was determined in 384-well plate format under the following reaction conditions: 0.8...
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Target
Lysine-specific demethylase 5A
(Homo sapiens (Human))
Celgene
Curated by
ChEMBL
Ligand
BDBM191600
(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
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Affinity Data
IC50: <100nM
Assay Description:
The enzymatic assay of Jarid1A activity is based upon Time Resolved-Fluorescence Resonance Energy Transfer (TR-FRET) detection. The ability of test c...
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Target
Lysine-specific demethylase 5B
(Homo sapiens (Human))
Zhengzhou University
Curated by
ChEMBL
Ligand
BDBM191600
(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
Copy SMILES
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Affinity Data
IC50: <100nM
Assay Description:
Inhibition of recombinant human N-terminal His-FLAG-tagged KDM5B (2 to 751 residues) expressed in baculovirus infected sf9 cells using biotin-H3K4me3...
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Target
Lysine-specific demethylase 5A
(Homo sapiens (Human))
Celgene
Curated by
ChEMBL
Ligand
BDBM191600
(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
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Affinity Data
IC50: <100nM
Assay Description:
Inhibition of recombinant human C-terminal FLAG-tagged KDM5A (1 to 1090 residues) expressed in baculovirus infected sf9 cells using biotin-H3K4me3 su...
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Target
Lysine-specific demethylase 5B
(Homo sapiens (Human))
Zhengzhou University
Curated by
ChEMBL
Ligand
BDBM191600
(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
Copy SMILES
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Affinity Data
IC50: <100nM
Assay Description:
Inhibition of KDM5B in human ZR-75-1 cells assessed as reduction in H3K4me3 demethylation incubated for 72 hrs by fluorometric immunoassay
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Target
Lysine-specific demethylase 2B
(Homo sapiens (Human))
University Of Oxford
Curated by
ChEMBL
Ligand
BDBM191600
(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
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Affinity Data
IC50: 100nM
Assay Description:
Inhibition of recombinant human C-terminal FLAG-tagged KDM2B (1 to 650 residues) expressed in baculovirus infected sf9 cells using biotin-H3K36me2 su...
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Target
Lysine-specific demethylase 4C
(Homo sapiens (Human))
Celgene
Curated by
ChEMBL
Ligand
BDBM191600
(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
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Affinity Data
IC50: 100nM
Assay Description:
Inhibition of recombinant human N-terminal GST-tagged KDM4C (2 to 372 residues) expressed in baculovirus infected sf9 cells using biotin-H3K9me3 subs...
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Target
Lysine-specific demethylase 4D
(Homo sapiens (Human))
Celgene
Curated by
ChEMBL
Ligand
BDBM191600
(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
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Affinity Data
IC50: 110nM
Assay Description:
Inhibition of KDM4D (unknown origin)
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Target
Lysine-specific demethylase 4E
(Homo sapiens (Human))
Celgene
Curated by
ChEMBL
Ligand
BDBM191600
(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
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Affinity Data
IC50: 160nM
Assay Description:
Inhibition of KDM4E (unknown origin)
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Target
Lysine-specific demethylase 4B
(Homo sapiens (Human))
Celgene
Curated by
ChEMBL
Ligand
BDBM191600
(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
Copy SMILES
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Affinity Data
IC50: 170nM
Assay Description:
Inhibition of KDM4B (unknown origin)
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Target
Lysine-specific demethylase 5B
(Homo sapiens (Human))
Zhengzhou University
Curated by
ChEMBL
Ligand
BDBM191600
(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
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Affinity Data
IC50: 175nM
pH: 7.2 T: 2°C
Assay 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...
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Target
Lysine-specific demethylase 5A [1-1090]
(Homo sapiens (Human))
Emory University
Ligand
BDBM191600
(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
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Affinity Data
IC50: 240nM
pH: 7.2 T: 2°C
Assay 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...
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Target
Lysine-specific demethylase 2B
(Homo sapiens (Human))
University Of Oxford
Curated by
ChEMBL
Ligand
BDBM191600
(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
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Affinity Data
IC50: 550nM
Assay Description:
The ability of test compounds to inhibit the activity of FBXL10 was determined in 384-well plate format under the following reaction conditions: 0.3 ...
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Target
Lysine-specific demethylase 4C
(Homo sapiens (Human))
Celgene
Curated by
ChEMBL
Ligand
BDBM191600
(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
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Affinity Data
IC50: 550nM
Assay Description:
The ability of test compounds to inhibit the activity of JMJD2C was determined in 384-well plate format under the following reaction conditions: 0.3 ...
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Target
Lysine-specific demethylase 2B
(Homo sapiens (Human))
University Of Oxford
Curated by
ChEMBL
Ligand
BDBM191600
(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
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Affinity Data
IC50: 630nM
Assay Description:
Inhibition of KDM2B (unknown origin)
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Target
Lysine-specific demethylase 5C
(Homo sapiens (Human))
Emory University
Ligand
BDBM191600
(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
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Affinity Data
IC50: 800nM
pH: 7.2 T: 2°C
Assay 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...
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Target
Lysine-specific demethylase 2A
(Homo sapiens (Human))
Celgene
Curated by
ChEMBL
Ligand
BDBM191600
(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
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Affinity Data
IC50: 820nM
Assay Description:
Inhibition of KDM2A (unknown origin)
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Target
Lysine-specific demethylase 5B [1-755]
(Homo sapiens (Human))
Emory University
Ligand
BDBM191600
(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
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Affinity Data
IC50: 1.00E+3nM
T: 2°C
Assay 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...
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Target
Lysine-specific demethylase 5B
(Homo sapiens (Human))
Zhengzhou University
Curated by
ChEMBL
Ligand
BDBM191600
(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
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Affinity Data
IC50: 1.00E+3nM
Assay Description:
Inhibition of N-terminal his6-tagged human KDM5B (1 to 769 residues) expressed in sf9 insect cells incubated for 20 mins by Alphascreen assay
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Target
Lysine-specific demethylase 6B
(Homo sapiens (Human))
Celgene
Curated by
ChEMBL
Ligand
BDBM191600
(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
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IC50: 2.30E+3nM
Assay Description:
Inhibition of KDM6B (unknown origin)
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Target
Lysine-specific demethylase 3A
(Homo sapiens (Human))
Celgene
Curated by
ChEMBL
Ligand
BDBM191600
(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
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Affinity Data
IC50: 2.30E+3nM
Assay Description:
Inhibition of KDM3A (unknown origin)
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Target
Lysine-specific demethylase 5A
(Homo sapiens (Human))
Celgene
Curated by
ChEMBL
Ligand
BDBM191600
(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
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Affinity Data
IC50: 5.00E+3nM
Assay Description:
Inhibition of N-terminal his6-tagged human KDM5A (1 to 797 residues) expressed in sf9 insect cells incubated for 20 mins by Alphascreen assay
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Target
Lysine-specific demethylase 5A [1-739]
(Homo sapiens (Human))
Emory University
Ligand
BDBM191600
(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
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Affinity Data
IC50: 5.00E+3nM
T: 2°C
Assay 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...
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Target
Lysine-specific demethylase 5D [1-760]
(Homo sapiens (Human))
Emory University
Ligand
BDBM191600
(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
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Affinity Data
IC50: 1.10E+4nM
T: 2°C
Assay 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...
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Target
Lysine-specific demethylase 5C [1-789]
(Homo sapiens (Human))
Emory University
Ligand
BDBM191600
(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
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Affinity Data
IC50: 1.70E+4nM
T: 2°C
Assay 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...
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Target
Lysine-specific demethylase 4C
(Homo sapiens (Human))
Celgene
Curated by
ChEMBL
Ligand
BDBM191600
(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
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Affinity Data
IC50: 1.70E+4nM
Assay Description:
Inhibition of KDM4C (unknown origin) incubated for 20 mins by Alphascreen assay
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Target
Lysine-specific histone demethylase 1A
(Homo sapiens (Human))
Celgene
Curated by
ChEMBL
Ligand
BDBM191600
(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
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Affinity Data
IC50: >4.00E+4nM
Assay Description:
Inhibition of KDM1A (unknown origin)
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Target
Lysine-specific demethylase 5A [1-588]
(Homo sapiens (Human))
Emory University
Ligand
BDBM191600
(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
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Affinity Data
Kd: 60nM
Assay 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...
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Target
Lysine-specific demethylase 5B [1-604]
(Homo sapiens (Human))
Emory University
Ligand
BDBM191600
(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
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Affinity Data
Kd: 70nM
Assay 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...
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In Depth
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Article
PubMed
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3D Structure (crystal)
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Target
Lysine-specific demethylase 5A/5B
(Homo sapiens (Human))
Celgene
Curated by
ChEMBL
Ligand
BDBM191600
(2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl...)
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Affinity Data
EC50: 90nM
Assay Description:
Inhibition of KDM5A/KDM5B in human ZR-75-1 cells assessed as increase in H3K4me3 level after 72 hrs by fluorometric immunoassay
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Target Info
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Reactome pathway
UniProtKB/SwissProt
antibodypedia
GoogleScholar
Ligand Info
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PDB
In Depth
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Article
PubMed
PDB
3D Structure (crystal)
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