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lysine demethylase 5A

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Target not currently curated in GtoImmuPdb

Target id: 2680

Nomenclature: lysine demethylase 5A

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 - 1690 12p13.33 KDM5A lysine demethylase 5A
Mouse - 1690 6 56.95 cM Kdm5a lysine demethylase 5A
Rat - 1690 4q42 Kdm5a lysine demethylase 5A
Previous and Unofficial Names Click here for help
JARID1A | Jumonji/ARID domain-containing protein 1A | lysine (K)-specific demethylase 5A
Database Links Click here for help
Alphafold P29375 (Hs), Q3UXZ9 (Mm)
CATH/Gene3D 3.30.40.10
ChEMBL Target CHEMBL2424504 (Hs), CHEMBL3707461 (Mm)
Ensembl Gene ENSG00000073614 (Hs), ENSMUSG00000030180 (Mm), ENSRNOG00000010591 (Rn)
Entrez Gene 5927 (Hs), 214899 (Mm), 312678 (Rn)
Human Protein Atlas ENSG00000073614 (Hs)
KEGG Gene hsa:5927 (Hs), mmu:214899 (Mm), rno:312678 (Rn)
OMIM 180202 (Hs)
Pharos P29375 (Hs)
RefSeq Nucleotide NM_001042603 (Hs), NM_145997 (Mm), NM_001277177 (Rn)
RefSeq Protein NP_001036068 (Hs), NP_666109 (Mm), NP_001264106 (Rn)
UniProtKB P29375 (Hs), Q3UXZ9 (Mm)
Wikipedia KDM5A (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
KDM5 inhibitor N71 Small molecule or natural product Primary target of this compound Click here for species-specific activity table 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 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.2 pIC50 3
⤷ pIC50 5.2 (IC50 6x10-6 M) [3]
GSK-J1 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand 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 08/10/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2680.