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Literature summary extracted from

  • De, S.K.; Stebbins, J.L.; Chen, L.H.; Riel-Mehan, M.; Machleidt, T.; Dahl, R.; Yuan, H.; Emdadi, A.; Barile, E.; Chen, V.; Murphy, R.; Pellecchia, M.
    Design, synthesis, and structure-activity relationship of substrate competitive, selective, and in vivo active triazole and thiadiazole inhibitors of the c-Jun N-terminal kinase (2009), J. Med. Chem., 52, 1943-1952.
    View publication on PubMedView publication on EuropePMC

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.11.24 2,2'-(1,3,4-thiadiazole-2,5-diyl)bis(sulfanediyl)dithiazole-5-carboxylic acid
-
 Mammalia
2.7.11.24 2,5-bis(3-nitrobenzylthio)-1,3,4-thiadiazole
-
 Mammalia
2.7.11.24 2,5-bis(4-fluorobenzylthio)-1,3,4-thiadiazole
-
 Mammalia
2.7.11.24 2,5-bis(4-methoxybenzylthio)-1,3,4-thiadiazole
-
 Mammalia
2.7.11.24 2,5-bis(4-nitrobenzylthio)-1,3,4-thiadiazole
-
 Mammalia
2.7.11.24 2,5-bis(5-nitrothiazol-2-ylthio)-1,3,4-thiadiazole
-
 Mammalia
2.7.11.24 2,5-bis(benzylthio)-1,3,4-thiadiazole
-
 Mammalia
2.7.11.24 2-(4-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-5-phenyl-4H-1,2,4-triazol-3-ylthio)-5-nitrothiazole
-
 Mammalia
2.7.11.24 2-(4-(2,4-dichlorophenyl)-5-(1-methyl-1H-pyrrol-2-yl)-4H-1,2,4-triazol-3-ylthio)-5-nitrothiazole
-
 Mammalia
2.7.11.24 2-(4-(3-methoxyphenyl)-5-phenyl-4H-1,2,4-triazol-3-ylthio)-5-nitrothiazole
-
 Mammalia
2.7.11.24 2-(4-(furan-2-ylmethyl)-5-(naphthalen-1-yl)-4H-1,2,4-triazol-3-ylthio)-5-nitrothiazole
-
 Mammalia
2.7.11.24 4-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-5-(nitrothiazol-2-ylthio)-4H-1,2,4-triazol-3-ol
-
 Mammalia
2.7.11.24 4-(2,4-dimethoxyphenyl)-5-(5-nitrothiazol-2-ylthio)-4H-1,2,4-triazol-3-ol
-
 Mammalia
2.7.11.24 4-(2,5-dimethoxyphenyl)-5-(5-nitrothiazol-2-ylthio)-4H-1,2,4-triazol-3-ol
-
 Mammalia
2.7.11.24 4-(2-methoxyphenyl)-5-(5-nitrothiazol-2-ylthio)-4H-1,2,4-triazol-3-ol
-
 Mammalia
2.7.11.24 4-(3,4-difluorophenyl)-5-(5-nitrothiazol-2-ylthio)-4H-1,2,4-triazol-3-ol
-
 Mammalia
2.7.11.24 4-(3,4-dimethoxyphenyl)-5-(5-nitrothiazol-2-ylthio)-4H-1,2,4-triazol-3-ol
-
 Mammalia
2.7.11.24 4-(3,5-dimethoxyphenyl)-5-(5-nitrothiazol-2-ylthio)-4H-1,2,4-triazol-3-ol
-
 Mammalia
2.7.11.24 4-(3-fluorophenyl)-5-(5-nitrothiazol-2-ylthio)-4H-1,2,4-triazol-3-ol
-
 Mammalia
2.7.11.24 4-(3-methoxyphenyl)-5-(5-nitrothiazol-2-ylthio)-4H-1,2,4-triazol-3-ol
-
 Mammalia
2.7.11.24 4-(4-fluorophenyl)-5-(5-nitrothiazol-2-ylthio)-4H-1,2,4-triazol-3-ol
-
 Mammalia
2.7.11.24 4-(4-methoxyphenyl)-5-(5-nitrothiazol-2-ylthio)-4H-1,2,4-triazol-3-ol
-
 Mammalia
2.7.11.24 4-(4-nitrophenyl)-5-(5-nitrothiazol-2-ylthio)-4H-1,2,4-triazol-3-ol
-
 Mammalia
2.7.11.24 4-(4-tert-butylphenyl)-5-(5-nitrothiazol-2-ylthio)-4H-1,2,4-triazol-3-ol
-
 Mammalia
2.7.11.24 4-(benzo[d][1,3]dioxol-5-yl)-5-(5-nitrothiazol-2-ylthio)-4H-1,2,4-triazol-3-ol
-
 Mammalia
2.7.11.24 4-(naphthalen-1-yl)-5-(5-nitrothiazol-2-ylthio)-4H-1,2,4-triazol-3-ol
-
 Mammalia
2.7.11.24 4-cyclohexyl-5-(5-nitrothiazol-2-ylthio)-4H-1,2,4-triazol-3-ol
-
 Mammalia
2.7.11.24 4-fluoro-N-(5-(5-nitrothiazol-2-ylthio)-1,3,4-thiadiazol-2-yl)benzamide
-
 Mammalia
2.7.11.24 5-((4-methyl-5-(5-nitrothiazol-2-ylthio)-4H-1,2,4-triazol-3-yl)methyl)-3-(pyrazin-2-yl)-1,2,4-oxadiazole
-
 Mammalia
2.7.11.24 5-(5-nitrothiazol-2-ylthio)-1,3,4-thiadiazol-2-amine
-
 Mammalia
2.7.11.24 5-(5-nitrothiazol-2-ylthio)-4-(3-(trifluoromethyl)phenyl)-4H-1,2,4-triazol-3-ol
-
 Mammalia
2.7.11.24 5-(5-nitrothiazol-2-ylthio)-4-(4-(trifluoromethoxy)phenyl)-4H-1,2,4-triazol-3-ol
-
 Mammalia
2.7.11.24 5-(5-nitrothiazol-2-ylthio)-4-(4-(trifluoromethyl)phenyl)-4H-1,2,4-triazol-3-ol
-
 Mammalia
2.7.11.24 5-(5-nitrothiophen-2-ylthio)-4-phenyl-4H-1,2,4-triazol-3-ol
-
 Mammalia
2.7.11.24 5-(benzylthio)-1,3,4-thiadiazol-2-amine
-
 Mammalia
2.7.11.24 5-(butylthio)-4-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-4H-1,2,4-triazol-3-ol
-
 Mammalia
2.7.11.24 5-(butylthio)-4-phenyl-4H-1,2,4-triazol-3-ol
-
 Mammalia
2.7.11.24 5-(ethylthio)-4-phenyl-4H-1,2,4-triazol-3-ol
-
 Mammalia
2.7.11.24 5-nitro-2-(4-phenyl-5-(pyridin-4-yl)-4H-1,2,4-triazol-3-ylthio)-thiazole
-
 Mammalia
2.7.11.24 5-nitro-2-(4-phenyl-5-(thiophen-2-yl)-4H-1,2,4-triazol-3-ylthio)-thiazole
-
 Mammalia

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.11.24 ATP + a protein Mammalia
-
 ADP + a phosphoprotein
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.11.24 Mammalia
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.11.24 ATP + a protein
-
 Mammalia ADP + a phosphoprotein
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.7.11.24 c-Jun N-terminal kinase
-
 Mammalia
2.7.11.24 JNK
-
 Mammalia
2.7.11.24 MAP kinase
-
 Mammalia
2.7.11.24 mitogen-activated kinase
-
 Mammalia

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.11.24 ATP
-
 Mammalia

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.11.24 additional information
-
 the inhibitors are tested in LanthaScreen kinase activity assays and pepJIP1 DELFIA displacement assays Mammalia additional information