Activating Compound | Comment | Organism | Structure |
---|---|---|---|
mitogen-activated protein kinase kinase 6 | MKK6 | Homo sapiens |
Application | Comment | Organism |
---|---|---|
medicine | p38 MAP kinase inhibition constitutes a promising therapeutic strategy for treatment of chronic inflammatory diseases, based upon its potential to inhibit key pathways driving the inflammatory and destructive processes in these debilitating diseases | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
3-(3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl)-N,4-dimethylbenzamide | PH-797804, ATP-competitive, readily reversible inhibitor of the alpha isoform of human p38 MAP kinase | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + a protein | Homo sapiens | - |
ADP + a phosphoprotein | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Posttranslational Modification | Comment | Organism |
---|---|---|
phosphoprotein | - |
Homo sapiens |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
monocyte | - |
Homo sapiens | - |
rheumatoid arthritis synovial fibroblast | RASF | Homo sapiens | - |
synovial tissue | - |
Homo sapiens | - |
U-937 cell | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + a protein | - |
Homo sapiens | ADP + a phosphoprotein | - |
? | |
ATP + GST-c-Jun | substrate in kinase activity assay | Homo sapiens | ADP + phosphorylated GST-c-Jun | - |
? | |
ATP + protein EGFRP | epidermal growth factor receptor peptide, substrate in kinase activity assay | Homo sapiens | ADP + phosphorylated protein EGFRP | - |
? |
Synonyms | Comment | Organism |
---|---|---|
p38 mitogen-activated protein kinase | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
25 | - |
kinase activity assay | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.5 | - |
kinase activity assay | Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
ATP | - |
Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0000058 | - |
3-(3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl)-N,4-dimethylbenzamide | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.000026 | - |
- |
Homo sapiens | 3-(3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl)-N,4-dimethylbenzamide |
General Information | Comment | Organism |
---|---|---|
physiological function | signal transduction through the p38 mitogen-activated protein kinase pathway is central to the transcriptional and translational control of cytokine and inflammatory mediator production | Homo sapiens |