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Literature summary for 2.7.11.24 extracted from

  • Kamenecka, T.; Habel, J.; Duckett, D.; Chen, W.; Ling, Y.Y.; Frackowiak, B.; Jiang, R.; Shin, Y.; Song, X.; LoGrasso, P.
    Structure-activity relationships and X-ray structures describing the selectivity of aminopyrazole inhibitors for c-Jun N-terminal kinase 3 (JNK3) over p38 (2009), J. Biol. Chem., 284, 12853-12861.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
a pDEST_JNK3_39-402 construct is used for the expression of the protein in Escherichia coli BL21DE3 cells Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
the structure of SR3737 and SR3451-soaked JNK3 crystals are solved at 2.20 and 2.29 A, respectively Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
SR3451
-
Homo sapiens
SR3451
-
Mammalia
SR3576
-
Homo sapiens
SR3576
-
Mammalia
SR3582
-
Homo sapiens
SR3582
-
Mammalia
SR3583
-
Homo sapiens
SR4018
-
Homo sapiens
SR4018
-
Mammalia
SR4276
-
Homo sapiens
SR4276
-
Mammalia
SR4326
-
Homo sapiens
SR4326
-
Mammalia
SR4642
-
Homo sapiens
SR4642
-
Mammalia
SR4643
-
Homo sapiens
SR4643
-
Mammalia

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Mammalia
-
-
-

Purification (Commentary)

Purification (Comment) Organism
a SP Fastflow column, a Mono S column, and a Sephacryl S200 column are used Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + a protein
-
Mammalia ADP + a phosphoprotein
-
?
ATP + a protein
-
Homo sapiens ADP + a phosphoprotein
-
?
ATP + ATF-2
-
Homo sapiens ADP + phosphorylated ATF-2
-
?
ATP + c-Jun
-
Homo sapiens ADP + phosphorylated c-Jun
-
?

Synonyms

Synonyms Comment Organism
c-jun N-terminal kinase 1
-
Mammalia
c-Jun N-terminal kinase 3
-
Homo sapiens
JNK1
-
Mammalia
JNK3
-
Homo sapiens
p38 mitogen-activated protein kinase
-
Mammalia
p38MAPK
-
Mammalia

Cofactor

Cofactor Comment Organism Structure
ATP
-
Mammalia
ATP
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000007
-
-
Homo sapiens SR3576
0.000023
-
-
Homo sapiens SR3582
0.000025
-
-
Homo sapiens SR3451
0.000055
-
-
Homo sapiens SR4326
0.00017
-
-
Mammalia SR3576
0.00035
-
-
Homo sapiens SR4276
0.0004
-
-
Mammalia SR3451
0.00048
-
-
Homo sapiens SR3583
0.00056
-
-
Mammalia SR3582
0.0014
-
-
Mammalia SR4326
0.0015
-
-
Homo sapiens SR4643
0.0021
-
-
Homo sapiens SR4018
0.0022
-
-
Homo sapiens SR4642
0.0037
-
-
Mammalia SR3451
0.02
-
larger than 0.020 Mammalia SR3582
0.02
-
larger than 0.020 Mammalia SR3576
0.02
-
larger than 0.020 Mammalia SR4326
0.02
-
larger than 0.020 Mammalia SR4642
0.02
-
larger than 0.020 Mammalia SR4643
0.02
-
larger than 0.020 Mammalia SR4018
0.02
-
larger than 0.020 Mammalia SR4276