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Literature summary for 2.1.1.319 extracted from

  • Yu, X.R.; Tang, Y.; Wang, W.J.; Ji, S.; Ma, S.; Zhong, L.; Zhang, C.H.; Yang, J.; Wu, X.A.; Fu, Z.Y.; Li, L.L.; Yang, S.Y.
    Discovery and structure-activity analysis of 4-((5-nitropyrimidin-4-yl)amino)benzimidamide derivatives as novel protein arginine methyltransferase 1 (PRMT1) inhibitors (2015), Bioorg. Med. Chem. Lett., 25, 5449-5453 .
    View publication on PubMed
Search for more literature for 2.1.1.319

Application

Application Comment Organism
medicine potential application of PRMT1 inhibitors in cancer treatment Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
4-([6-[(2H-1,3-benzodioxol-5-yl)amino]-5-nitropyrimidin-4-yl]amino)benzene-1-carboximidamide
-
 Homo sapiens
4-[(6-amino-5-nitropyrimidin-4-yl)amino]benzene-1-carboximidamide
-
 Homo sapiens
4-[(6-anilino-5-nitropyrimidin-4-yl)amino]benzene-1-carboximidamide 0.05 mM, 9% inhibition Homo sapiens
4-[[5-nitro-6-(4-sulfamoylanilino)pyrimidin-4-yl]amino]benzene-1-carboximidamide 0.05 mM, 28% inhibition Homo sapiens
4-[[6-(4-aminoanilino)-5-nitropyrimidin-4-yl]amino]benzene-1-carboximidamide 0.05 mM, 28% inhibition Homo sapiens
4-[[6-(4-carbamimidoylanilino)-5-nitropyrimidin-4-yl]amino]benzamide
-
 Homo sapiens
4-[[6-(4-cyanoanilino)-5-nitropyrimidin-4-yl]amino]benzene-1-carboximidamide
-
 Homo sapiens
4-[[6-(4-hydroxy-3,5-dimethoxyanilino)-5-nitropyrimidin-4-yl]amino]benzene-1-carboximidamide 0.05 mM, 44% inhibition Homo sapiens
N2-[6-(4-carbamimidoylanilino)-5-nitropyrimidin-4-yl]glycinamide 0.05 mM, 49% inhibition Homo sapiens
tert-butyl (4-[[6-(4-carbamimidoylanilino)-5-nitropyrimidin-4-yl]amino]phenyl)carbamate
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2 S-adenosyl-L-methionine + [histone H4R3]-L-arginine Homo sapiens
-
 2 S-adenosyl-L-homocysteine + [histone H4R3]-Nomega,Nomega-dimethyl-L-arginine
-
 ?

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 H4R3]-L-arginine
-
 Homo sapiens 2 S-adenosyl-L-homocysteine + [histone H4R3]-Nomega,Nomega-dimethyl-L-arginine
-
 ?

Synonyms

Synonyms Comment Organism
PRMT1
-
 Homo sapiens
protein arginine methyltransferase 1
-
 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0017
-
 4-[[6-(4-cyanoanilino)-5-nitropyrimidin-4-yl]amino]benzene-1-carboximidamide pH and temperature not specified in the publication Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.002
-
 pH and temperature not specified in the publication Homo sapiens 4-[[6-(4-cyanoanilino)-5-nitropyrimidin-4-yl]amino]benzene-1-carboximidamide
0.0093
-
 pH and temperature not specified in the publication Homo sapiens 4-[[6-(4-carbamimidoylanilino)-5-nitropyrimidin-4-yl]amino]benzamide
0.013
-
 pH and temperature not specified in the publication Homo sapiens tert-butyl (4-[[6-(4-carbamimidoylanilino)-5-nitropyrimidin-4-yl]amino]phenyl)carbamate
0.025
-
 pH and temperature not specified in the publication Homo sapiens 4-([6-[(2H-1,3-benzodioxol-5-yl)amino]-5-nitropyrimidin-4-yl]amino)benzene-1-carboximidamide
0.038
-
 pH and temperature not specified in the publication Homo sapiens 4-[(6-amino-5-nitropyrimidin-4-yl)amino]benzene-1-carboximidamide

General Information

General Information Comment Organism
drug target the enzyme (PRMT1) is a promising target for the treatment of cancer Homo sapiens
physiological function overexpression or dysregulation of PRMT1 is associated with many diseases, particularly cancer Homo sapiens