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Literature summary for 2.7.11.24 extracted from

  • De, S.K.; Chen, V.; Stebbins, J.L.; Chen, L.H.; Cellitti, J.F.; Machleidt, T.; Barile, E.; Riel-Mehan, M.; Dahl, R.; Yang, L.; Emdadi, A.; Murphy, R.; Pellecchia, M.
    Synthesis and optimization of thiadiazole derivatives as a novel class of substrate competitive c-Jun N-terminal kinase inhibitors (2010), Bioorg. Med. Chem., 18, 590-596.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.7.11.24

Activating Compound

Activating Compound Comment Organism Structure
additional information activated by a range of stress stimuli Homo sapiens

Application

Application Comment Organism
medicine JNK inhibitors are expected to be effective therapeutic agents against a variety of diseases Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
4-(2,3-dihydro-1,4-benzodioxin-6-yl)-5-[(5-nitro-1,3,4-thiadiazol-2-yl)sulfanyl]-4H-1,2,4-triazol-3-ol
-
 Homo sapiens
5-(5-nitrothiazol-2-ylthio)-N-((tetrahydrofuran-2-yl)methyl)-1,3,4-thiadiazol-2-amine
-
 Homo sapiens
5-(5-nitrothiazol-2-ylthio)-N-propyl-1,3,4-thiadiazol-2-amine
-
 Homo sapiens
N-(2-methoxyethyl)-5-(5-nitrothiazol-2-ylthio)-1,3,4-thiadiazol-2-amine
-
 Homo sapiens
N-(3,4-dimethoxyphenethyl)-5-(5-nitrothiazol-2-ylthio)-1,3,4-thiadiazol-2-amine
-
 Homo sapiens
N-(4-methoxybenzyl)-5-(5-nitrothiazol-2-ylthio)-1,3,4-thiadiazol-2-amine
-
 Homo sapiens
N-ethyl-5-(5-nitrothiazol-2-ylthio)-1,3,4-thiadiazol-2-amine
-
 Homo sapiens
N-sec-butyl-5-(5-nitrothiazol-2-ylthio)-1,3,4-thiadiazol-2-amine
-
 Homo sapiens

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
45000
-
 JNK1 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + a protein Homo sapiens
-
 ADP + a phosphoprotein
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
HeLa cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + a protein
-
 Homo sapiens ADP + a phosphoprotein
-
 ?
ATP + ATF2 substrate in in vitro kinase assay, LanthaScreen Homo sapiens ADP + phosphorylated ATF2
-
 ?
ATP + c-Jun transcription factor JNK phosphorylates the N-terminal transactivation domain of c-Jun transcription factor Homo sapiens ADP + phosphorylated c-Jun transcription factor
-
 ?

Synonyms

Synonyms Comment Organism
c-Jun N-terminal kinase
-
 Homo sapiens
JNK
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
22
-
 in vitro kinase assay at room temperature Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
 in vitro kinase assay Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0001
-
 pepJIP1 displacement assay DELFIA, GST-JNK2 is applied Homo sapiens N-(4-methoxybenzyl)-5-(5-nitrothiazol-2-ylthio)-1,3,4-thiadiazol-2-amine
0.0001
-
 pepJIP1 displacement assay DELFIA, GST-JNK2 is applied Homo sapiens N-(3,4-dimethoxyphenethyl)-5-(5-nitrothiazol-2-ylthio)-1,3,4-thiadiazol-2-amine
0.0001
-
 pepJIP1 displacement assay DELFIA, GST-JNK2 is applied Homo sapiens N-ethyl-5-(5-nitrothiazol-2-ylthio)-1,3,4-thiadiazol-2-amine
0.00014
-
 pepJIP1 displacement assay DELFIA, GST-JNK2 is applied Homo sapiens N-sec-butyl-5-(5-nitrothiazol-2-ylthio)-1,3,4-thiadiazol-2-amine
0.00016
-
 pepJIP1 displacement assay DELFIA, GST-JNK2 is applied Homo sapiens N-(2-methoxyethyl)-5-(5-nitrothiazol-2-ylthio)-1,3,4-thiadiazol-2-amine
0.00028
-
 JNK1 kinase inhibition assay LANTHA Homo sapiens 4-(2,3-dihydro-1,4-benzodioxin-6-yl)-5-[(5-nitro-1,3,4-thiadiazol-2-yl)sulfanyl]-4H-1,2,4-triazol-3-ol
0.00029
-
 pepJIP1 displacement assay DELFIA, GST-JNK2 is applied Homo sapiens 5-(5-nitrothiazol-2-ylthio)-N-propyl-1,3,4-thiadiazol-2-amine
0.00047
-
 pepJIP1 displacement assay DELFIA, GST-JNK2 is applied Homo sapiens 5-(5-nitrothiazol-2-ylthio)-N-((tetrahydrofuran-2-yl)methyl)-1,3,4-thiadiazol-2-amine
0.0005
-
-
 Homo sapiens 4-(2,3-dihydro-1,4-benzodioxin-6-yl)-5-[(5-nitro-1,3,4-thiadiazol-2-yl)sulfanyl]-4H-1,2,4-triazol-3-ol
0.003
-
 JNK1 kinase inhibition assay LANTHA Homo sapiens N-sec-butyl-5-(5-nitrothiazol-2-ylthio)-1,3,4-thiadiazol-2-amine
0.0048
-
 JNK1 kinase inhibition assay LANTHA Homo sapiens N-(2-methoxyethyl)-5-(5-nitrothiazol-2-ylthio)-1,3,4-thiadiazol-2-amine
0.0057
-
 JNK1 kinase inhibition assay LANTHA Homo sapiens N-(3,4-dimethoxyphenethyl)-5-(5-nitrothiazol-2-ylthio)-1,3,4-thiadiazol-2-amine
0.0067
-
 JNK1 kinase inhibition assay LANTHA Homo sapiens 5-(5-nitrothiazol-2-ylthio)-N-propyl-1,3,4-thiadiazol-2-amine
0.0091
-
 JNK1 kinase inhibition assay LANTHA Homo sapiens N-(4-methoxybenzyl)-5-(5-nitrothiazol-2-ylthio)-1,3,4-thiadiazol-2-amine
0.01
-
 JNK1 kinase inhibition assay LANTHA Homo sapiens 5-(5-nitrothiazol-2-ylthio)-N-((tetrahydrofuran-2-yl)methyl)-1,3,4-thiadiazol-2-amine
0.1
-
 JNK1 kinase inhibition assay LANTHA Homo sapiens N-ethyl-5-(5-nitrothiazol-2-ylthio)-1,3,4-thiadiazol-2-amine

Expression

Organism Comment Expression
Homo sapiens up-regulation of JNK activity is associated with a number of disease states such as type-2 diabetes, obesity, cancer, inflammation, and stroke up