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Literature summary for 2.1.1.320 extracted from

  • Wang, Y.; Hu, W.; Yuan, Y.
    Protein arginine methyltransferase 5 (PRMT5) as an anticancer target and its inhibitor discovery (2018), J. Med. Chem., 61, 9429-9441 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
1-(6-bromo-9-ethyl-9H-carbazol-3-yl)-N-[(2-methoxyphenyl)methyl]methanamine
-
Homo sapiens
2-([[2-(benzyloxy)-1,4-dihydronaphthalen-1-yl]methyl]amino)-1-phenylethan-1-ol
-
Homo sapiens
7-[(5R)-5-C-phenyl-beta-D-ribofuranosyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine
-
Homo sapiens
dehydrosinefungin
-
Homo sapiens
methyl 2-[2-[(6-methoxy-1H-benzimidazol-2-yl)sulfanyl]acetamido]benzoate
-
Homo sapiens
N-[(2S)-3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl]-6-[(oxetan-3-yl)amino]pyrimidine-4-carboxamide
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens O14744
-
-

Source Tissue

Source Tissue Comment Organism Textmining
A-375 cell
-
Homo sapiens
-
MCF-7 cell
-
Homo sapiens
-
MV4-11 cell
-
Homo sapiens
-
Th1 cell
-
Homo sapiens
-
Th2 cell
-
Homo sapiens
-

Synonyms

Synonyms Comment Organism
PRMT5
-
Homo sapiens
protein arginine methyltransferase 5
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000022
-
pH and temperature not specified in the publication Homo sapiens N-[(2S)-3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl]-6-[(oxetan-3-yl)amino]pyrimidine-4-carboxamide
0.000026
-
pH and temperature not specified in the publication Homo sapiens 7-[(5R)-5-C-phenyl-beta-D-ribofuranosyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine
0.000035
-
pH and temperature not specified in the publication Homo sapiens dehydrosinefungin
0.00033
-
pH and temperature not specified in the publication Homo sapiens methyl 2-[2-[(6-methoxy-1H-benzimidazol-2-yl)sulfanyl]acetamido]benzoate
0.000517
-
pH and temperature not specified in the publication Homo sapiens 1-(6-bromo-9-ethyl-9H-carbazol-3-yl)-N-[(2-methoxyphenyl)methyl]methanamine
0.0028
-
pH and temperature not specified in the publication Homo sapiens 2-([[2-(benzyloxy)-1,4-dihydronaphthalen-1-yl]methyl]amino)-1-phenylethan-1-ol

General Information

General Information Comment Organism
drug target targeting PRMT5 offers a great opportunity to combat cancer in an efficient and selective way Homo sapiens
physiological function the enzyme (PRMT5) is a major enzyme responsible for symmetric dimethylation of arginine residues on both histone and non-histone proteins, regulating many biological pathways in mammalian cells Homo sapiens