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Assay Detail

CHEMBL4024503

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

Binding
Inhibition of ARID/PHD1 domain truncated human N-terminal His-SUMO-tagged KDM5A (1 to 588 residues) expressed in Escherichia coli using H3K4me3 as substrate preincubated for 15 mins followed by substrate addition measured after 15 mins in presence of 0.1 mM alpha-KG by FDH coupled assat
2
Total Activities
2
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 5A (CHEMBL2424504)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Insights into the Action of Inhibitor Enantiomers against Histone Lysine Demethylase 5A.
Horton JR, Liu X, Wu L, Zhang K, Shanks J, Zhang X, Rai G, Mott BT, Jansen DJ, Kales SC, Henderson MJ, Pohida K, Fang Y, Hu X, Jadhav A, Maloney DJ, Hall MD, Simeonov A, Fu H, Vertino PM, Yan Q, Cheng X.
J Med Chem (2018) 61 : 3193 -3208
PubMed 29537847 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.29 5.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4088737 1 5.62
CHEMBL4067490 1 4.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4088737 IC50 = 2400.0 nM 5.62
CHEMBL4067490 IC50 = 11000.0 nM 4.96