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lysine demethylase 4E

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Target not currently curated in GtoImmuPdb

Target id: 2679

Nomenclature: lysine demethylase 4E

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 - 506 11q21 KDM4E lysine demethylase 4E
Previous and Unofficial Names Click here for help
lysine-specific demethylase 4D-like | KDM4DL | JMJD2E | lysine (K)-specific demethylase 4E
Database Links Click here for help
Alphafold B2RXH2 (Hs)
ChEMBL Target CHEMBL1293226 (Hs)
Ensembl Gene ENSG00000235268 (Hs)
Entrez Gene 390245 (Hs)
Human Protein Atlas ENSG00000235268 (Hs)
KEGG Gene hsa:390245 (Hs)
Pharos B2RXH2 (Hs)
RefSeq Nucleotide NM_001161630 (Hs)
RefSeq Protein NP_001155102 (Hs)
SynPHARM 82695 (in complex with compound 6a [PMID: 18942826])
UniProtKB B2RXH2 (Hs)
Wikipedia KDM4E (Hs)

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
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 1
⤷ pIC50 6.0 (IC50 9.2x10-7 M) [1]
compound 6a [PMID: 18942826] Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 5.8 pIC50 2
⤷ pIC50 5.8 (IC50 1.4x10-6 M) [2]
Description: FDH (formaldehyde dehydrogenase) coupled assay.

References

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1. 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]

2. 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 4E. Last modified on 25/05/2017. Accessed on 11/09/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2679.