Literature summary for 2.1.1.319 extracted from

Eram, M.S.; Shen, Y.; Szewczyk, M.; Wu, H.; Senisterra, G.; Li, F.; Butler, K.V.; Kaniskan, H.U.e.; Speed, B.A.; Dela Sena, C.; Dong, A.; Zeng, H.; Schapira, M.; Brown, P.J.; Arrowsmith, C.H.; Barsyte-Lovejoy, D.; Liu, J.; Vedadi, M.; Jin, J.
A potent, selective, and cell-active inhibitor of human type I protein arginine methyltransferases (2016), ACS Chem. Biol., 11, 772-781 .

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Inhibitors

Inhibitors	Comment	Organism	Structure
N1-methyl-N1-([4-[3-(trifluoromethyl)phenyl]-1H-pyrrol-3-yl]methyl)ethane-1,2-diamine	-	Homo sapiens
N1-methyl-N1-([5-[3-(trifluoromethyl)phenyl]-2H-1,2,3-triazol-4-yl]methyl)ethane-1,2-diamine	the inhibitor is inactive against PRMT1, 3 and 4	Homo sapiens
N1-methyl-N1-[(4-[4-[(propan-2-yl)oxy]phenyl]-1H-pyrrol-3-yl)methyl]ethane-1,2-diamine	the inhibitor displays high potency for type I PRMTs including PRMT1, 3, 4, 6 and 8, but is completely inactive against type II and type III PRMTs, protein lysine methyltransferases and DNA methyltransferases. The inhibitor potently decreases cellular levels of histone arginine asymmetric dimethylation. MS094, a close analog of MS023, is developed which is inactive in biochemical and cellular assays, as a negative control for chemical biology studies. MS023 and MS094 are useful chemical tools for investigating the role of type I PRMTs in health and disease; the inhibitor displays high potency for type I PRMTs including PRMT1, 3, 4, 6 and 8, but is completely inactive against type II and type III PRMTs, protein lysine methyltransferases and DNA methyltransferases. The inhibitor potently decreases cellular levels of histone arginine asymmetric dimethylation. MS094, a close analog of MS023, is developed which is inactive in biochemical and cellular assays, as a negative control for chemical biology studies. MS023 and MS094 are useful chemical tools for investigating the role of type I PRMTs in health and disease; the inhibitor displays high potency for type I PRMTs including PRMT1, 3, 4, 6 and 8, but is completely inactive against type II and type III PRMTs, protein lysine methyltransferases and DNA methyltransferases. The inhibitor potently decreases cellular levels of histone arginine asymmetric dimethylation. MS094, a close analog of MS023, is developed which is inactive in biochemical and cellular assays, as a negative control for chemical biology studies. MS023 and MS094 are useful chemical tools for investigating the role of type I PRMTs in health and disease; the inhibitor displays high potency for type I PRMTs including PRMT1, 3, 4, 6 and 8, but is completely inactive against type II and type III PRMTs, protein lysine methyltransferases and DNA methyltransferases. The inhibitor potently decreases cellular levels of histone arginine asymmetric dimethylation. MS094, a close analog of MS023, is developed which is inactive in biochemical and cellular assays, as a negative control for chemical biology studies. MS023 and MS094 are useful chemical tools for investigating the role of type I PRMTs in health and disease	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	O60678	-	-
Homo sapiens	Q86X55	-	-
Homo sapiens	Q96LA8	-	-
Homo sapiens	Q99873	-	-
Homo sapiens	Q9NR22	-	-

Synonyms

Synonyms	Comment	Organism
PRMT3	-	Homo sapiens
PRMT4	-	Homo sapiens
PRMT6	-	Homo sapiens
PRMT8	-	Homo sapiens
type I protein arginine methyltransferase	-	Homo sapiens

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.000004	-	pH and temperature not specified in the publication	Homo sapiens	N1-methyl-N1-[(4-[4-[(propan-2-yl)oxy]phenyl]-1H-pyrrol-3-yl)methyl]ethane-1,2-diamine
0.000009	-	pH and temperature not specified in the publication	Homo sapiens	N1-methyl-N1-([4-[3-(trifluoromethyl)phenyl]-1H-pyrrol-3-yl]methyl)ethane-1,2-diamine
0.00003	-	pH and temperature not specified in the publication	Homo sapiens	N1-methyl-N1-[(4-[4-[(propan-2-yl)oxy]phenyl]-1H-pyrrol-3-yl)methyl]ethane-1,2-diamine
0.000119	-	pH and temperature not specified in the publication	Homo sapiens	N1-methyl-N1-[(4-[4-[(propan-2-yl)oxy]phenyl]-1H-pyrrol-3-yl)methyl]ethane-1,2-diamine
0.00023	-	pH and temperature not specified in the publication	Homo sapiens	N1-methyl-N1-([5-[3-(trifluoromethyl)phenyl]-2H-1,2,3-triazol-4-yl]methyl)ethane-1,2-diamine
0.00025	-	pH and temperature not specified in the publication	Homo sapiens	N1-methyl-N1-([4-[3-(trifluoromethyl)phenyl]-1H-pyrrol-3-yl]methyl)ethane-1,2-diamine
0.00111	-	pH and temperature not specified in the publication	Homo sapiens	N1-methyl-N1-([4-[3-(trifluoromethyl)phenyl]-1H-pyrrol-3-yl]methyl)ethane-1,2-diamine

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Release 2023.1 (January 2023)