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protein arginine methyltransferase 5

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Target not currently curated in GtoImmuPdb

Target id: 1256

Nomenclature: protein arginine methyltransferase 5

Abbreviated Name: PRMT5

Family: 2.1.1.- Protein arginine N-methyltransferases

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 637 14q11.2 PRMT5 protein arginine methyltransferase 5
Mouse - 637 14 C2 Prmt5 protein arginine N-methyltransferase 5
Rat - - 15p13 Prmt5 protein arginine methyltransferase 5
Previous and Unofficial Names Click here for help
Histone-arginine N-methyltransferase | Jak-binding protein 1 | Jbp1 | HRMT1L5
Database Links Click here for help
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Pharos
SynPHARM
UniProtKB
Wikipedia

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
EPZ015666 Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Inhibition 8.3 pKi
pKi 8.3 (Ki 5x10-9 M)
GSK591 Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Inhibition 8.0 pIC50 4
pIC50 8.0 (IC50 1.1x10-8 M) [4]
Description: Measuring inhibition of methylation of histone H4 in an in vitro biochemical assay.
LLY-283 Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Inhibition 7.7 pIC50 2
pIC50 7.7 (IC50 2x10-8 M) [2]
Description: Inhibition of methylation of an H4R3 derived peptide substrate in vitro.
DS-437 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 5.2 pIC50 3
pIC50 5.2 (IC50 5.9x10-6 M) [3]
cmp5 [PMID: 25742700] Small molecule or natural product Primary target of this compound Hs Inhibition - - 1
[1]

References

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1. Alinari L, Mahasenan KV, Yan F, Karkhanis V, Chung JH, Smith EM, Quinion C, Smith PL, Kim L, Patton JT et al.. (2015) Selective inhibition of protein arginine methyltransferase 5 blocks initiation and maintenance of B-cell transformation. Blood, 125 (16): 2530-43. [PMID:25742700]

2. SGC. LLY-283 A Chemical Probe For PRMT5. Accessed on 05/04/2017. Modified on 05/04/2017. thesgc.org, http://www.thesgc.org/chemical-probes/LLY-283

3. Smil D, Eram MS, Li F, Kennedy S, Szewczyk MM, Brown PJ, Barsyte-Lovejoy D, Arrowsmith CH, Vedadi M, Schapira M. (2015) Discovery of a Dual PRMT5-PRMT7 Inhibitor. ACS Med Chem Lett, 6 (4): 408-12. [PMID:25893041]

4. Structural Genomics Consortium. GSK591 A chemical probe for PRMT5. Accessed on 11/12/2015. Modified on 11/12/2015. The Structural Genomics Consortium, http://www.thesgc.org/chemical-probes/GSK591

How to cite this page

2.1.1.- Protein arginine N-methyltransferases: protein arginine methyltransferase 5 . Last modified on 05/04/2017. Accessed on 26/07/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1256.