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

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lysine demethylase 5B

Target not currently curated in GtoImmuPdb

Target id: 2681

Nomenclature: lysine demethylase 5B

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 - 1544 1q32.1 KDM5B lysine demethylase 5B
Mouse - 1544 1 E4 Kdm5b lysine (K)-specific demethylase 5B
Rat - 1544 13q13 Kdm5b lysine demethylase 5B
Previous and Unofficial Names
JARID1B | jumonji/ARID domain-containing protein 1B | Jumonji AT-rich interactive domain 1B | lysine (K)-specific demethylase 5B | PLU1
Database Links
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
RefSeq Nucleotide
RefSeq Protein
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of human PLU-1 (JARID1B) in complex with KDOAM25a (note that JARID1B=KDM5B).
PDB Id:  5A3N
Ligand:  KDOAM25
Resolution:  2.0Å
Species:  Human

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
GSK-J1 Hs Inhibition 6.8 pIC50 2
pIC50 6.8 (IC50 1.7x10-7 M) [2]
KDM5 inhibitor N71 Hs Irreversible inhibition 6.7 pIC50 3
pIC50 6.7 (IC50 2.2x10-7 M) [3]
Description: AlphaLISA derived IC50 values of the inhibition of KDM5B-mediated histone demethylation.
Compound 9 [doi:10.26434/chemrxiv.7072592.v1] Hs Inhibition 6.5 pIC50 5
pIC50 6.5 (IC50 3x10-7 M) [5]
PBIT Hs Inhibition 5.5 pIC50 4
pIC50 5.5 (IC50 3x10-6 M) [4]
GSK-J4 Hs Inhibition 5.0 pIC50 2
pIC50 5.0 (IC50 9.7x10-6 M) [2]
Inhibitor Comments
PBIT also inhibits KDM5A and KDM5C, with IC50 values of 6000 and 4900 nm respectively [4].
Gene Expression and Pathophysiology
Tissue or cell type: 
Pathophysiology:  Various cancers
Species:  Human
References:  1
General Comments
KDM5B is an H3K4 histone demethylase [6], belonging to a subfamily of demethylases responsible for the demethylation of H3K4me3 [4].


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1. Blair LP, Cao J, Zou MR, Sayegh J, Yan Q. (2011) Epigenetic Regulation by Lysine Demethylase 5 (KDM5) Enzymes in Cancer. Cancers (Basel), 3 (1): 1383-404. [PMID:21544224]

2. 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]

3. 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]

4. 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]

5. Vazquez-Rodriguez et al.. (2018) Design, Synthesis and Characterization of Covalent KDM5 Inhibitors. ChemRxiv, Preprint. DOI: 10.26434/chemrxiv.7072592.v1

6. Yamane K, Tateishi K, Klose RJ, Fang J, Fabrizio LA, Erdjument-Bromage H, Taylor-Papadimitriou J, Tempst P, Zhang Y. (2007) PLU-1 is an H3K4 demethylase involved in transcriptional repression and breast cancer cell proliferation. Mol. Cell, 25 (6): 801-12. [PMID:17363312]

How to cite this page

1.14.11.- Histone demethylases: lysine demethylase 5B. Last modified on 20/11/2018. Accessed on 16/10/2019. IUPHAR/BPS Guide to PHARMACOLOGY,