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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

Contents:

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
Alphafold O75164 (Hs), Q8BW72 (Mm)
BRENDA 1.14.11.-
CATH/Gene3D 3.30.40.10
ChEMBL Target CHEMBL5896 (Hs)
Ensembl Gene ENSG00000066135 (Hs), ENSMUSG00000033326 (Mm), ENSRNOG00000019956 (Rn)
Entrez Gene 9682 (Hs), 230674 (Mm), 313539 (Rn)
Human Protein Atlas ENSG00000066135 (Hs)
KEGG Enzyme 1.14.11.-
KEGG Gene hsa:9682 (Hs), mmu:230674 (Mm), rno:313539 (Rn)
OMIM 609764 (Hs)
Pharos O75164 (Hs)
RefSeq Nucleotide NM_014663 (Hs), NM_001161823 (Mm), NM_001107966 (Rn)
RefSeq Protein NP_055478 (Hs), NP_001155295 (Mm), NP_001101436 (Rn)
SynPHARM 82694 (in complex with compound 6a [PMID: 18942826])
UniProtKB O75164 (Hs), Q8BW72 (Mm)
Wikipedia KDM4A (Hs)
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 Guide to Malaria Pharmacology 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 11/09/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2675.