coactivator associated arginine methyltransferase 1 | 2.1.1.- Protein arginine N-methyltransferases | IUPHAR/BPS Guide to PHARMACOLOGY

Top ▲

coactivator associated arginine methyltransferase 1

Target not currently curated in GtoImmuPdb

Target id: 1255

Nomenclature: coactivator associated arginine methyltransferase 1

Abbreviated Name: PRMT4

Family: 2.1.1.- Protein arginine N-methyltransferases

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 - 607 19p13.2 CARM1 coactivator associated arginine methyltransferase 1
Mouse - 608 9 7.82 cM Carm1 coactivator-associated arginine methyltransferase 1
Rat - 651 8q13 Carm1 coactivator-associated arginine methyltransferase 1
Previous and Unofficial Names
Histone-arginine methyltransferase CARM1 | protein arginine N-methyltransferase 4
Database Links
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Coactivator-associated arginine methyltransferase 1 (PRMT4) crystalised with inhibitor TP-064.
PDB Id:  5U4X
Ligand:  TP-064
Resolution:  1.88Å
Species:  Human
Enzyme Reaction
EC Number:

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
MS049 Hs Inhibition 7.0 pKd 5
pKd 7.0 (Kd 1x10-7 M) [5]
Description: Isothermal titration calorimetry (ITC) in the presence of SAH
MS023 Hs Inhibition 7.6 pKi 1
pKi 7.6 (Ki 2.3x10-8 M) [1]
BIIB021 Hs Inhibition >8.0 pIC50 4
pIC50 >8.0 (IC50 <1x10-8 M) [4]
Description: In vitro methylation of H3 (1-25).
MS049 Hs Inhibition 7.5 pIC50 5
pIC50 7.5 (IC50 3.4x10-8 M) [5]
BMS pyrazole inhibitor 7f Hs Inhibition 7.4 pIC50 3
pIC50 7.4 (IC50 4x10-8 M) [3]
SGC2085 Hs Inhibition 7.3 pIC50 2
pIC50 7.3 (IC50 5x10-8 M) [2]
compound 17f [PMID: 19632837] Hs Inhibition 7.2 pIC50 6
pIC50 7.2 (IC50 7x10-8 M) [6]
Inhibitor Comments
BMS pyrazole inhibitor 7f appears to be selective for PRMT4 (CARM1) across a panel of tested proteins [3].


Show »

1. Eram MS, Shen Y, Szewczyk MM, Wu H, Senisterra G, Li F, Butler KV, Kaniskan U, Speed BA, dela Sena C et al.. (2015) A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases. ACS Chemical Biology., Just Accepted Manuscript.

2. Ferreira de Freitas R, Eram MS, Smil D, Szewczyk MM, Kennedy S, Brown PJ, Santhakumar V, Barsyte-Lovejoy D, Arrowsmith CH, Vedadi M et al.. (2016) Discovery of a Potent and Selective Coactivator Associated Arginine Methyltransferase 1 (CARM1) Inhibitor by Virtual Screening. J. Med. Chem., 59 (14): 6838-47. [PMID:27390919]

3. Huynh T, Chen Z, Pang S, Geng J, Bandiera T, Bindi S, Vianello P, Roletto F, Thieffine S, Galvani A et al.. (2009) Optimization of pyrazole inhibitors of Coactivator Associated Arginine Methyltransferase 1 (CARM1). Bioorg. Med. Chem. Lett., 19 (11): 2924-7. [PMID:19419866]

4. SGC. TP-064 A Chemical Probe For PRMT4. Accessed on 05/04/2017. Modified on 05/04/2017.,

5. Shen Y, Szewczyk MM, Eram MS, Smil D, Kaniskan HÜ, Ferreira de Freitas R, Senisterra G, Li F, Schapira M, Brown PJ et al.. (2016) Discovery of a Potent, Selective, and Cell-Active Dual Inhibitor of Protein Arginine Methyltransferase 4 and Protein Arginine Methyltransferase 6. J. Med. Chem., 59 (19): 9124-9139. [PMID:27584694]

6. Wan H, Huynh T, Pang S, Geng J, Vaccaro W, Poss MA, Trainor GL, Lorenzi MV, Gottardis M, Jayaraman L et al.. (2009) Benzo[d]imidazole inhibitors of Coactivator Associated Arginine Methyltransferase 1 (CARM1)--Hit to Lead studies. Bioorg. Med. Chem. Lett., 19 (17): 5063-6. [PMID:19632837]

How to cite this page

2.1.1.- Protein arginine N-methyltransferases: coactivator associated arginine methyltransferase 1. Last modified on 05/04/2017. Accessed on 26/01/2020. IUPHAR/BPS Guide to PHARMACOLOGY,