lysine demethylase 4A | 1.14.11.- Histone demethylases | IUPHAR/BPS Guide to PHARMACOLOGY

Top ▲

lysine demethylase 4A

Target not currently curated in GtoImmuPdb

Target id: 2675

Nomenclature: lysine demethylase 4A

Family: 1.14.11.- Histone demethylases

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1064 1p34.1 KDM4A lysine demethylase 4A
Mouse - 1064 4 D2.1 Kdm4a lysine (K)-specific demethylase 4A
Rat - 971 5q36 Kdm4a lysine demethylase 4A
Previous and Unofficial Names
JMJD2 | JMJD2A | jumonji domain containing 2 | TDRD14A | lysine (K)-specific demethylase 4A
Database Links
BRENDA
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 1.14.11.-

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Parameter Reference
compound 6a [PMID: 18942826] Hs Inhibition 6.2 pIC50 3
pIC50 6.2 (IC50 7x10-7 M) [3]
Description: FDH (formaldehyde dehydrogenase) coupled assay.
ML324 Hs Inhibition >6.0 pIC50 2
pIC50 >6.0 (IC50 <1x10-6 M) [2]
KDM5 inhibitor N71 Hs Inhibition 5.3 pIC50 1
pIC50 5.3 (IC50 5.3x10-6 M) [1]

References

Show »

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., [Epub ahead of print]. [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 24/04/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2675.