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Literature summary for 2.7.11.24 extracted from

  • Montalban, A.G.; Boman, E.; Chang, C.D.; Ceide, S.C.; Dahl, R.; Dalesandro, D.; Delaet, N.G.; Erb, E.; Ernst, J.; Gibbs, A.; Kahl, J.; Kessler, L.; Lundstroem, J.; Miller, S.; Nakanishi, H.; Roberts, E.; Saiah, E.; Sullivan, R.; Wang, Z.; Larson, C.J.
    KR-003048, a potent, orally active inhibitor of p38 mitogen-activated protein kinase (2010), Eur. J. Pharmacol., 632, 93-102.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
interleukin-I
-
Homo sapiens
lipopolysaccharide
-
Homo sapiens
additional information activated by growth factors, cellular stresses, and cytokines Homo sapiens
tumor necrosis factor-alpha
-
Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
-
Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
5-tert-butyl-N-cyclopropyl-2-methoxy-3-[2-[4-(2-morpholin-4-yl-ethoxy)-naphthalen-1-yl]-2-oxo-acetylamino]-benzamide KR-003048 Homo sapiens
BIRB796
-
Homo sapiens
SB203580
-
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
-
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
phosphoprotein
-
Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
blood
-
Homo sapiens
-
THP-1 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 + myelin basic protein substrate in in vitro kinase assay Homo sapiens ADP + phosphorylated myelin basic protein
-
?

Synonyms

Synonyms Comment Organism
MAP kinase
-
Homo sapiens
mitogen-activated kinase
-
Homo sapiens
p38 mitogen-activated protein kinase
-
Homo sapiens
p38alpha
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
25
-
kinase assay Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
kinase assay Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000022
-
-
Homo sapiens 5-tert-butyl-N-cyclopropyl-2-methoxy-3-[2-[4-(2-morpholin-4-yl-ethoxy)-naphthalen-1-yl]-2-oxo-acetylamino]-benzamide
0.000033
-
-
Homo sapiens SB203580
0.000035
-
-
Homo sapiens BIRB796

General Information

General Information Comment Organism
physiological function monocyte, macrophage production of tumor necrosis factor-alpha is largely driven by p38 mitogen-activated protein kinase Homo sapiens