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
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
RefSeq Nucleotide
RefSeq Protein

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

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]


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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 27/05/2020. IUPHAR/BPS Guide to PHARMACOLOGY,