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Assay Detail

CHEMBL3788935

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

Binding
Inhibition of recombinant human N-terminal His-tagged KDM4A (1 to 350 residues) expressed in Escherichia coli using biotin-H3K9me3 substrate incubated for 30 mins by TR-FRET assay
5
Total Activities
5
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 4A (CHEMBL5896)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Recent Progress in Histone Demethylase Inhibitors.
McAllister TE, England KS, Hopkinson RJ, Brennan PE, Kawamura A, Schofield CJ.
J Med Chem (2016) 59 : 1308 -1329
PubMed 26710088 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.67 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3786108 1 7.00
CHEMBL3785421 1 7.00
CHEMBL3787548 1 6.00
CHEMBL3787133 1 -
CHEMBL3786225 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3786108 IC50 = 100.0 nM 7.00
CHEMBL3785421 IC50 = 100.0 nM 7.00
CHEMBL3787548 IC50 = 1000.0 nM 6.00
CHEMBL3787133 IC50 < 100.0 nM -
CHEMBL3786225 IC50 > 10000.0 nM -