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Assay Detail

CHEMBL3390925

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

Binding
Inhibition of N-terminal His-6-tagged human JMJD2E (1 to 337 residues) expressed in Escherichia coli using ARK(me3)STGGK peptide as substrate by MALDI-TOF/MS analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Lysine-specific demethylase 4E (CHEMBL1293226)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of second generation epigenetic agents
Jones P
Medchemcomm (2012) 3 : 135 -161
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.83 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1230640 1 6.70
CHEMBL1486366 1 5.96
CHEMBL1435274 1 5.70
CHEMBL1519338 1 4.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1230640 IC50 = 200.0 nM 6.70
CHEMBL1486366 IC50 = 1100.0 nM 5.96
CHEMBL1435274 IC50 = 2000.0 nM 5.70
CHEMBL1519338 IC50 = 11000.0 nM 4.96