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Literature summary for 2.1.1.319 extracted from

  • Sun, Y.; Wang, Z.; Yang, H.; Zhu, X.; Wu, H.; Ma, L.; Xu, F.; Hong, W.; Wang, H.
    The Development of tetrazole derivatives as protein arginine methyltransferase I (PRMT I) inhibitors (2019), Int. J. Mol. Sci., 20, 3840 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.1.1.319

Inhibitors

Inhibitors Comment Organism Structure
N,N'-dimethyl-N'-(1-(4-(2,2,2-trifluoroethoxy)phenyl)-1H-tetrazol-5-yl-methyl)ethylenediamine hydrochloride
-
 Homo sapiens
N,N'-dimethyl-N'-(1-(4-isopropoxyphenyl)-1H-tetrazol-5-yl-methyl)ethylenediamine hydrochloride non-competitive inhibition pattern with respect to either S-adenosyl-L-methionine or substrate arginine. Potent PRMT1 inhibitor, which can be used as lead compound for further drug discovery Homo sapiens
N,N'-dimethyl-N'-(1-(4-trifluoromethoxyphenyl)-1H-tetrazol-5-yl-methyl)ethylenediamine hydrochloride
-
 Homo sapiens
N-(1-(4-isopropoxyphenyl)-1H-tetrazol-5-yl-methyl)-N-methyl-ethylenediamine hydrochloride
-
 Homo sapiens
N-aminoethyl-N'-(1-(4-isopropoxyphenyl)-1H-tetrazol-5-yl-methyl)-piperazinehydrochloride
-
 Homo sapiens
S-adenosyl-L-homocysteine
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q99873
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2 S-adenosyl-L-methionine + [histone H4 peptide]-L-arginine
-
 Homo sapiens 2 S-adenosyl-L-homocysteine + [histone H4 peptide]-Nomega,Nomega-dimethyl-L-arginine
-
 ?

Synonyms

Synonyms Comment Organism
PRMT I
-
 Homo sapiens
protein arginine methyltransferase I
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00049
-
 pH and temperature not specified in the publication Homo sapiens S-adenosyl-L-homocysteine
0.0035
-
 pH and temperature not specified in the publication Homo sapiens N,N'-dimethyl-N'-(1-(4-isopropoxyphenyl)-1H-tetrazol-5-yl-methyl)ethylenediamine hydrochloride
0.01
-
 pH and temperature not specified in the publication Homo sapiens N-(1-(4-isopropoxyphenyl)-1H-tetrazol-5-yl-methyl)-N-methyl-ethylenediamine hydrochloride
0.0199
-
 pH and temperature not specified in the publication Homo sapiens N,N'-dimethyl-N'-(1-(4-(2,2,2-trifluoroethoxy)phenyl)-1H-tetrazol-5-yl-methyl)ethylenediamine hydrochloride
0.0238
-
 pH and temperature not specified in the publication Homo sapiens N,N'-dimethyl-N'-(1-(4-trifluoromethoxyphenyl)-1H-tetrazol-5-yl-methyl)ethylenediamine hydrochloride
0.029
-
 pH and temperature not specified in the publication Homo sapiens N-aminoethyl-N'-(1-(4-isopropoxyphenyl)-1H-tetrazol-5-yl-methyl)-piperazinehydrochloride

General Information

General Information Comment Organism
physiological function dysregulation of PRMT1 is involved in a diverse range of diseases, including cancer Homo sapiens