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Literature summary for 2.7.11.24 extracted from

  • Lumeras, W.; Caturla, F.; Vidal, L.; Esteve, C.; Balague, C.; Orellana, A.; Dominguez, M.; Roca, R.; Huerta, J.M.; Godessart, N.; Vidal, B.
    Design, synthesis, and structure-activity relationships of aminopyridine N-oxides, a novel scaffold for the potent and selective inhibition of p38 mitogen activated protein kinase (2009), J. Med. Chem., 52, 5531-5545.
    View publication on PubMed
Search for more literature for 2.7.11.24

Activating Compound

Activating Compound Comment Organism Structure
MKK3 activation of p38alpha occurs through bisphosphorylation by the dual-specificity Ser/Thr MAP kinases MKK3 and MKK6 on the Thr180-Gly181-Tyr182 motif located on the activation loop Homo sapiens
MKK6 activation of p38alpha occurs through bisphosphorylation by the dual-specificity Ser/Thr MAP kinases MKK3 and MKK6 on the Thr180-Gly181-Tyr182 motif located on the activation loop Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(3-amino-1-oxido-2-phenylpyridin-4-yl)(phenyl)methanone
-
 Homo sapiens
4-[3-amino-4-(2,4-difluorobenzoyl)-1-oxidopyridin-2-yl]-3-methyl-N-(2-morpholin-4-ylethyl)benzamide
-
 Homo sapiens
4-[3-amino-4-(2,4-difluorobenzoyl)-1-oxidopyridin-2-yl]-3-methylbenzoic acid
-
 Homo sapiens
4-[3-amino-4-(2,4-difluorobenzoyl)-1-oxidopyridin-2-yl]-N-(2-methoxyethyl)-3-methylbenzamide
-
 Homo sapiens
[3-amino-2-(1,3-benzodioxol-4-yl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
-
 Homo sapiens
[3-amino-2-(2,3-dimethoxyphenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
-
 Homo sapiens
[3-amino-2-(2,4-difluorophenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
-
 Homo sapiens
[3-amino-2-(2,6-dichlorophenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
-
 Homo sapiens
[3-amino-2-(2,6-difluoro-4-methoxyphenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
-
 Homo sapiens
[3-amino-2-(2,6-difluorophenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
-
 Homo sapiens
[3-amino-2-(2,6-dimethoxyphenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
-
 Homo sapiens
[3-amino-2-(2,6-dimethylphenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
-
 Homo sapiens
[3-amino-2-(2-chlorophenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
-
 Homo sapiens
[3-amino-2-(2-chlorophenyl)-1-oxidopyridin-4-yl](2-chlorophenyl)methanone
-
 Homo sapiens
[3-amino-2-(2-chlorophenyl)-1-oxidopyridin-4-yl](2-methoxyphenyl)methanone
-
 Homo sapiens
[3-amino-2-(2-chlorophenyl)-1-oxidopyridin-4-yl](2-trifluoromethylphenyl)methanone
-
 Homo sapiens
[3-amino-2-(2-chlorophenyl)-1-oxidopyridin-4-yl](phenyl)methanone
-
 Homo sapiens
[3-amino-2-(2-isopropylphenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
-
 Homo sapiens
[3-amino-2-(2-methoxyphenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
-
 Homo sapiens
[3-amino-2-(2-methylphenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
-
 Homo sapiens
[3-amino-2-(2-methylphenyl)-1-oxidopyridin-4-yl](phenyl)methanone
-
 Homo sapiens
[3-amino-2-(3-chlorophenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
-
 Homo sapiens
[3-amino-2-(4-chloro-2-methylphenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
-
 Homo sapiens
[3-amino-2-(4-chlorophenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
-
 Homo sapiens
[3-amino-2-(4-chlorophenyl)-1-oxidopyridin-4-yl](phenyl)methanone
-
 Homo sapiens
[3-amino-2-(4-hydroxy-2-methylphenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
-
 Homo sapiens
[3-amino-2-[2-methyl-4-(2-morpholin-4-ylethoxy)phenyl]-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
-
 Homo sapiens
[3-amino-2-[4-(2-methoxyethoxy)-2-methylphenyl]-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
-
 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 Q16539
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
phosphoprotein
-
 Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
blood whole blood assay Homo sapiens
-
THP-1 cell THP-1 assay 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 assay, biotinylated ATF2 Homo sapiens ADP + a phosphorylated ATF2
-
 ?

Synonyms

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

pH Optimum

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

Cofactor

Cofactor Comment Organism Structure
ATP
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000005
-
-
 Homo sapiens [3-amino-2-(2,6-difluoro-4-methoxyphenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
0.000008
-
-
 Homo sapiens [3-amino-2-(4-hydroxy-2-methylphenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
0.000009
-
-
 Homo sapiens [3-amino-2-(2,6-dichlorophenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
0.000014
-
-
 Homo sapiens [3-amino-2-[2-methyl-4-(2-morpholin-4-ylethoxy)phenyl]-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
0.000015
-
-
 Homo sapiens [3-amino-2-(2,6-dimethoxyphenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
0.000017
-
-
 Homo sapiens [3-amino-2-(2,6-difluorophenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
0.000017
-
-
 Homo sapiens [3-amino-2-(2,6-dimethylphenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
0.00002
-
-
 Homo sapiens [3-amino-2-[4-(2-methoxyethoxy)-2-methylphenyl]-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
0.000021
-
-
 Homo sapiens [3-amino-2-(2-methylphenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
0.000023
-
-
 Homo sapiens [3-amino-2-(2-methoxyphenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
0.000024
-
-
 Homo sapiens [3-amino-2-(2-chlorophenyl)-1-oxidopyridin-4-yl](2-chlorophenyl)methanone
0.000024
-
-
 Homo sapiens [3-amino-2-(1,3-benzodioxol-4-yl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
0.000037
-
-
 Homo sapiens [3-amino-2-(2,3-dimethoxyphenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
0.000038
-
-
 Homo sapiens [3-amino-2-(4-chloro-2-methylphenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
0.000039
-
-
 Homo sapiens [3-amino-2-(2-chlorophenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
0.000042
-
-
 Homo sapiens 4-[3-amino-4-(2,4-difluorobenzoyl)-1-oxidopyridin-2-yl]-3-methyl-N-(2-morpholin-4-ylethyl)benzamide
0.00007
-
-
 Homo sapiens 4-[3-amino-4-(2,4-difluorobenzoyl)-1-oxidopyridin-2-yl]-N-(2-methoxyethyl)-3-methylbenzamide
0.000126
-
-
 Homo sapiens [3-amino-2-(2,4-difluorophenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
0.000149
-
-
 Homo sapiens [3-amino-2-(2-chlorophenyl)-1-oxidopyridin-4-yl](2-methoxyphenyl)methanone
0.000174
-
-
 Homo sapiens [3-amino-2-(2-chlorophenyl)-1-oxidopyridin-4-yl](phenyl)methanone
0.000208
-
-
 Homo sapiens [3-amino-2-(2-isopropylphenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
0.000228
-
-
 Homo sapiens [3-amino-2-(3-chlorophenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
0.000411
-
-
 Homo sapiens [3-amino-2-(2-methylphenyl)-1-oxidopyridin-4-yl](phenyl)methanone
0.000491
-
-
 Homo sapiens 4-[3-amino-4-(2,4-difluorobenzoyl)-1-oxidopyridin-2-yl]-3-methylbenzoic acid
0.000802
-
-
 Homo sapiens [3-amino-2-(4-chlorophenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
0.000967
-
-
 Homo sapiens (3-amino-1-oxido-2-phenylpyridin-4-yl)(phenyl)methanone
0.001655
-
-
 Homo sapiens [3-amino-2-(2-chlorophenyl)-1-oxidopyridin-4-yl](2-trifluoromethylphenyl)methanone
0.00253
-
-
 Homo sapiens [3-amino-2-(4-chlorophenyl)-1-oxidopyridin-4-yl](phenyl)methanone