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lysine demethylase 4A

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Target not currently curated in GtoImmuPdb

Target id: 2675

Nomenclature: lysine demethylase 4A

Family: 1.14.11.- Histone demethylases

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1064 1p34.2-p34.1 KDM4A lysine demethylase 4A
Mouse - 1064 4 54.31 cM Kdm4a lysine (K)-specific demethylase 4A
Rat - 971 5q36 Kdm4a lysine demethylase 4A
Previous and Unofficial Names Click here for help
JMJD2 | JMJD2A | jumonji domain containing 2 | TDRD14A | lysine (K)-specific demethylase 4A
Database Links Click here for help
BRENDA
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Enzyme Reaction Click here for help
EC Number: 1.14.11.-

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Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
compound 6a [PMID: 18942826] Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.2 pIC50 3
pIC50 6.2 (IC50 7x10-7 M) [3]
Description: FDH (formaldehyde dehydrogenase) coupled assay.
ML324 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition >6.0 pIC50 2
pIC50 >6.0 (IC50 <1x10-6 M) [2]
KDM5 inhibitor N71 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.3 pIC50 1
pIC50 5.3 (IC50 5.3x10-6 M) [1]

References

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1. Horton JR, Woodcock CB, Chen Q, Liu X, Zhang X, Shanks J, Rai G, Mott BT, Jansen DJ, Kales SC et al.. (2018) Structure-Based Engineering of Irreversible Inhibitors against Histone Lysine Demethylase KDM5A. J. Med. Chem., 61 (23): 10588-10601. [PMID:30392349]

2. Rai G, Kawamura A, Tumber A, Liang Y, Vogel JL, Arbuckle JH, Rose NR, Dexheimer TS, Foley TL, King ON et al.. (2010) Discovery of ML324, a JMJD2 demethylase inhibitor with demonstrated antiviral activity. Probe Reports from the NIH Molecular Libraries Program,. [PMID:24260783]

3. Rose NR, Ng SS, Mecinović J, Liénard BM, Bello SH, Sun Z, McDonough MA, Oppermann U, Schofield CJ. (2008) Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases. J. Med. Chem., 51 (22): 7053-6. [PMID:18942826]

How to cite this page

1.14.11.- Histone demethylases: lysine demethylase 4A. Last modified on 20/11/2018. Accessed on 01/03/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2675.