lysine demethylase 5A | 1.14.11.- Histone demethylases | IUPHAR/BPS Guide to PHARMACOLOGY

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lysine demethylase 5A

Target not currently curated in GtoImmuPdb

Target id: 2680

Nomenclature: lysine demethylase 5A

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 - 1690 12p13.33 KDM5A lysine demethylase 5A
Mouse - 1690 6 F1 Kdm5a lysine (K)-specific demethylase 5A
Rat - 1690 4q42 Kdm5a lysine demethylase 5A
Previous and Unofficial Names
JARID1A | Jumonji/ARID domain-containing protein 1A | lysine (K)-specific demethylase 5A
Database Links
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia

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 Value Parameter Reference
KDM5 inhibitor N71 Hs Irreversible inhibition 6.5 pIC50 2
pIC50 6.5 (IC50 3.2x10-7 M) [2]
Description: AlphaLISA derived IC50 values of the inhibition of KDM5A-mediated histone demethylation.
PBIT Hs Inhibition 5.2 pIC50 3
pIC50 5.2 (IC50 6x10-6 M) [3]
GSK-J1 Hs Inhibition 5.2 pIC50 1
pIC50 5.2 (IC50 6.8x10-6 M) [1]

References

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1. Heinemann B, Nielsen JM, Hudlebusch HR, Lees MJ, Larsen DV, Boesen T, Labelle M, Gerlach LO, Birk P, Helin K. (2014) Inhibition of demethylases by GSK-J1/J4. Nature, 514 (7520): E1-2. [PMID:25279926]

2. 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]

3. Sayegh J, Cao J, Zou MR, Morales A, Blair LP, Norcia M, Hoyer D, Tackett AJ, Merkel JS, Yan Q. (2013) Identification of small molecule inhibitors of Jumonji AT-rich interactive domain 1B (JARID1B) histone demethylase by a sensitive high throughput screen. J. Biol. Chem., 288 (13): 9408-17. [PMID:23408432]

How to cite this page

1.14.11.- Histone demethylases: lysine demethylase 5A. Last modified on 20/11/2018. Accessed on 12/11/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2680.