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Assay Detail

CHEMBL4256952

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

Binding
Inhibition of recombinant human N-terminal His-tagged JMJD2A (1 to 350 residues) expressed in Escherichia coli using H3K9me3-biotin peptide as substrate after 30 mins in presence of alpha-ketoglutaric acid by LANCE TR-FRET assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Lysine-specific demethylase 4A (CHEMBL5896)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Histone demethylase inhibitors
(2016)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.71 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4287561 1 7.00
CHEMBL4288884 1 7.00
CHEMBL4289921 1 7.00
CHEMBL4283926 1 7.00
CHEMBL4290069 1 7.00
CHEMBL4281202 1 7.00
CHEMBL4228384 1 7.00
CHEMBL4228902 1 7.00
CHEMBL4293252 1 7.00
CHEMBL4227799 1 7.00
CHEMBL4281159 1 6.00
CHEMBL4288934 1 6.00
CHEMBL4289695 1 6.00
CHEMBL4287296 1 6.00
CHEMBL4225358 1 -
CHEMBL4287890 1 -
CHEMBL4284863 1 -
CHEMBL4277650 1 -
CHEMBL4292495 1 -
CHEMBL4286778 1 -
CHEMBL4290497 1 -
CHEMBL4277439 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4287561 IC50 = 100.0 nM 7.00
CHEMBL4288884 IC50 = 100.0 nM 7.00
CHEMBL4289921 IC50 = 100.0 nM 7.00
CHEMBL4283926 IC50 = 100.0 nM 7.00
CHEMBL4290069 IC50 = 100.0 nM 7.00
CHEMBL4281202 IC50 = 100.0 nM 7.00
CHEMBL4228384 IC50 = 100.0 nM 7.00
CHEMBL4228902 IC50 = 100.0 nM 7.00
CHEMBL4293252 IC50 = 100.0 nM 7.00
CHEMBL4227799 IC50 = 100.0 nM 7.00
CHEMBL4281159 IC50 = 1000.0 nM 6.00
CHEMBL4288934 IC50 = 1000.0 nM 6.00
CHEMBL4289695 IC50 = 1000.0 nM 6.00
CHEMBL4287296 IC50 = 1000.0 nM 6.00
CHEMBL4225358 IC50 <= 100.0 nM -
CHEMBL4287890 IC50 > 10000.0 nM -
CHEMBL4284863 IC50 > 10000.0 nM -
CHEMBL4277650 IC50 > 10000.0 nM -
CHEMBL4292495 IC50 > 10000.0 nM -
CHEMBL4286778 IC50 > 10000.0 nM -
CHEMBL4290497 IC50 > 10000.0 nM -
CHEMBL4277439 IC50 > 10000.0 nM -