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Literature summary for 2.7.11.24 extracted from

  • Shin, Y.; Chen, W.; Habel, J.; Duckett, D.; Ling, Y.Y.; Koenig, M.; He, Y.; Vojkovsky, T.; LoGrasso, P.; Kamenecka, T.M.
    Synthesis and SAR of piperazine amides as novel c-jun N-terminal kinase (JNK) inhibitors (2009), Bioorg. Med. Chem. Lett., 19, 3344-3347.
    View publication on PubMedView publication on EuropePMC

Activating Compound

Activating Compound Comment Organism Structure
additional information JNK can be activated in response to various stimuli such as environmental stress, cytokines and fatty acids Homo sapiens

Application

Application Comment Organism
medicine JNK3 may be a promising target for the treatment of neurodegenerative diseases such as Parkinsons disease, Alzheimers disease and other CNS disorders Homo sapiens
medicine therapeutic inhibition of JNK1 may provide a potential solution in type-2 diabetes mellitus Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2-bromo-N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-1,3-thiazole-5-carboxamide
-
Homo sapiens
3-bromo-N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]benzamide
-
Homo sapiens
4-bromo-N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-1,3-thiazole-2-carboxamide
-
Homo sapiens
5-(acetylamino)-N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]furan-2-carboxamide
-
Homo sapiens
5-(difluoromethyl)-N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]furan-2-carboxamide
-
Homo sapiens
5-benzyl-N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]furan-2-carboxamide
-
Homo sapiens
5-bromo-N-(3-chloro-2-piperazin-1-ylphenyl)furan-2-carboxamide
-
Homo sapiens
5-bromo-N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]furan-2-carboxamide
-
Homo sapiens
5-bromo-N-[2-(4-prop-2-en-1-ylpiperazin-1-yl)-3-(trifluoromethyl)phenyl]furan-2-carboxamide
-
Homo sapiens
5-bromo-N-[2-(4-prop-2-en-1-ylpiperazin-1-yl)biphenyl-3-yl]furan-2-carboxamide
-
Homo sapiens
5-bromo-N-[3-(phenylamino)-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
-
Homo sapiens
5-bromo-N-[3-bromo-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
-
Homo sapiens
5-bromo-N-[3-chloro-2-(4-cyclopropylpiperazin-1-yl)phenyl]furan-2-carboxamide
-
Homo sapiens
5-bromo-N-[3-chloro-2-(4-ethylpiperazin-1-yl)phenyl]furan-2-carboxamide
-
Homo sapiens
5-bromo-N-[3-chloro-2-(4-methylpiperazin-1-yl)phenyl]furan-2-carboxamide
-
Homo sapiens
5-bromo-N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
-
Homo sapiens
5-bromo-N-[3-chloro-2-(4-prop-2-yn-1-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
-
Homo sapiens
5-bromo-N-[3-chloro-2-(4-propylpiperazin-1-yl)phenyl]furan-2-carboxamide
-
Homo sapiens
5-bromo-N-[3-chloro-2-(4-pyridin-2-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
-
Homo sapiens
5-bromo-N-[3-chloro-2-[4-(1-methylethyl)piperazin-1-yl]phenyl]furan-2-carboxamide
-
Homo sapiens
5-bromo-N-[3-chloro-2-[4-(2-methylprop-2-en-1-yl)piperazin-1-yl]phenyl]furan-2-carboxamide
-
Homo sapiens
5-bromo-N-[3-chloro-2-[4-(2-phenylethyl)piperazin-1-yl]phenyl]furan-2-carboxamide
-
Homo sapiens
5-bromo-N-[3-chloro-2-[4-(furan-2-ylmethyl)piperazin-1-yl]phenyl]furan-2-carboxamide
-
Homo sapiens
5-bromo-N-[3-chloro-2-[4-(trifluoroacetyl)piperazin-1-yl]phenyl]furan-2-carboxamide
-
Homo sapiens
5-bromo-N-[3-fluoro-2-(4-prop-2-yn-1-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
-
Homo sapiens
5-bromo-N-[3-methyl-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
-
Homo sapiens
5-chloro-N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]furan-2-carboxamide
-
Homo sapiens
5-cyano-N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]furan-2-carboxamide
-
Homo sapiens
6-bromo-N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]pyridine-2-carboxamide
-
Homo sapiens
N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]-5-(phenylamino)furan-2-carboxamide
-
Homo sapiens
N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]-5-ethylfuran-2-carboxamide
-
Homo sapiens
N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]-5-fluorofuran-2-carboxamide
-
Homo sapiens
N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]-5-methoxyfuran-2-carboxamide
-
Homo sapiens
N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]-5-methylfuran-2-carboxamide
-
Homo sapiens
N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]-5-prop-1-yn-1-ylfuran-2-carboxamide
-
Homo sapiens
N-[2-(4-acetylpiperazin-1-yl)-3-chlorophenyl]-5-bromofuran-2-carboxamide
-
Homo sapiens
N-[2-(4-benzylpiperazin-1-yl)-3-chlorophenyl]-5-bromofuran-2-carboxamide
-
Homo sapiens
N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-1,3-thiazole-4-carboxamide
-
Homo sapiens
N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-1H-pyrrole-2-carboxamide
-
Homo sapiens
N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-2-methyl-1,3-thiazole-4-carboxamide
-
Homo sapiens
N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-5-cyanopyridine-2-carboxamide
-
Homo sapiens
N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-6-methylpyridine-2-carboxamide
-
Homo sapiens
N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]isoxazole-5-carboxamide
-
Homo sapiens
N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]pyrimidine-2-carboxamide
-
Homo sapiens
tert-butyl 4-(2-[[(5-bromofuran-2-yl)carbonyl]amino]-6-chlorophenyl)piperazine-1-carboxylate
-
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
-
-
-
Homo sapiens P53779
-
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
c-jun N-terminal kinase 1
-
Homo sapiens
c-Jun N-terminal kinase 3
-
Homo sapiens
JNK1
-
Homo sapiens
JNK3
-
Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00004
-
-
Homo sapiens 5-chloro-N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]furan-2-carboxamide
0.00006
-
-
Homo sapiens 5-bromo-N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]furan-2-carboxamide
0.00008
-
-
Homo sapiens 5-chloro-N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]furan-2-carboxamide
0.00009
-
-
Homo sapiens 5-bromo-N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]furan-2-carboxamide
0.00011
-
-
Homo sapiens 5-bromo-N-[3-fluoro-2-(4-prop-2-yn-1-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
0.00011
-
-
Homo sapiens N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]-5-prop-1-yn-1-ylfuran-2-carboxamide
0.00014
-
-
Homo sapiens 5-bromo-N-[3-chloro-2-(4-prop-2-yn-1-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
0.00016
-
-
Homo sapiens 5-bromo-N-[3-chloro-2-(4-prop-2-yn-1-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
0.00018
-
-
Homo sapiens 5-bromo-N-[3-chloro-2-(4-cyclopropylpiperazin-1-yl)phenyl]furan-2-carboxamide
0.00018
-
-
Homo sapiens 5-bromo-N-[3-methyl-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
0.0002
-
-
Homo sapiens 5-bromo-N-[3-methyl-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
0.00021
-
-
Homo sapiens 5-cyano-N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]furan-2-carboxamide
0.00021
-
-
Homo sapiens N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]-5-fluorofuran-2-carboxamide
0.00023
-
-
Homo sapiens 5-cyano-N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]furan-2-carboxamide
0.00024
-
-
Homo sapiens 5-bromo-N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
0.00025
-
-
Homo sapiens 5-bromo-N-[3-chloro-2-[4-(furan-2-ylmethyl)piperazin-1-yl]phenyl]furan-2-carboxamide
0.00026
-
-
Homo sapiens 5-(difluoromethyl)-N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]furan-2-carboxamide
0.00027
-
-
Homo sapiens 5-bromo-N-[3-chloro-2-[4-(furan-2-ylmethyl)piperazin-1-yl]phenyl]furan-2-carboxamide
0.00029
-
-
Homo sapiens 5-bromo-N-[3-fluoro-2-(4-prop-2-yn-1-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
0.00031
-
-
Homo sapiens 2-bromo-N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-1,3-thiazole-5-carboxamide
0.00033
-
-
Homo sapiens 2-bromo-N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-1,3-thiazole-5-carboxamide
0.00033
-
-
Homo sapiens 5-bromo-N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
0.00033
-
-
Homo sapiens N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]-5-methylfuran-2-carboxamide
0.00035
-
-
Homo sapiens 5-(difluoromethyl)-N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]furan-2-carboxamide
0.00036
-
-
Homo sapiens 5-bromo-N-[3-chloro-2-(4-ethylpiperazin-1-yl)phenyl]furan-2-carboxamide
0.00036
-
-
Homo sapiens 5-bromo-N-[3-chloro-2-(4-methylpiperazin-1-yl)phenyl]furan-2-carboxamide
0.0004
-
-
Homo sapiens 5-bromo-N-[3-chloro-2-[4-(2-methylprop-2-en-1-yl)piperazin-1-yl]phenyl]furan-2-carboxamide
0.00041
-
-
Homo sapiens N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]-5-fluorofuran-2-carboxamide
0.00045
-
-
Homo sapiens N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]-5-methoxyfuran-2-carboxamide
0.00053
-
-
Homo sapiens N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]-5-methylfuran-2-carboxamide
0.00054
-
-
Homo sapiens 5-bromo-N-[3-chloro-2-[4-(2-methylprop-2-en-1-yl)piperazin-1-yl]phenyl]furan-2-carboxamide
0.0006
-
-
Homo sapiens N-[2-(4-acetylpiperazin-1-yl)-3-chlorophenyl]-5-bromofuran-2-carboxamide
0.00062
-
-
Homo sapiens N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]-5-methoxyfuran-2-carboxamide
0.00063
-
-
Homo sapiens 5-bromo-N-[3-chloro-2-(4-propylpiperazin-1-yl)phenyl]furan-2-carboxamide
0.00081
-
-
Homo sapiens N-[2-(4-acetylpiperazin-1-yl)-3-chlorophenyl]-5-bromofuran-2-carboxamide
0.00088
-
-
Homo sapiens N-[2-(4-benzylpiperazin-1-yl)-3-chlorophenyl]-5-bromofuran-2-carboxamide
0.0009
-
-
Homo sapiens 5-bromo-N-[3-chloro-2-(4-propylpiperazin-1-yl)phenyl]furan-2-carboxamide
0.0009
-
-
Homo sapiens 5-bromo-N-[3-chloro-2-[4-(2-phenylethyl)piperazin-1-yl]phenyl]furan-2-carboxamide
0.00096
-
-
Homo sapiens 5-bromo-N-[3-chloro-2-(4-cyclopropylpiperazin-1-yl)phenyl]furan-2-carboxamide
0.001
-
-
Homo sapiens 5-bromo-N-[3-chloro-2-(4-pyridin-2-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
0.001
-
-
Homo sapiens N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]-5-ethylfuran-2-carboxamide
0.0011
-
-
Homo sapiens 5-bromo-N-[3-chloro-2-(4-ethylpiperazin-1-yl)phenyl]furan-2-carboxamide
0.0011
-
-
Homo sapiens N-[2-(4-benzylpiperazin-1-yl)-3-chlorophenyl]-5-bromofuran-2-carboxamide
0.0012
-
-
Homo sapiens 5-bromo-N-[3-chloro-2-(4-methylpiperazin-1-yl)phenyl]furan-2-carboxamide
0.0012
-
-
Homo sapiens 5-bromo-N-[3-chloro-2-(4-pyridin-2-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
0.0014
-
-
Homo sapiens 5-bromo-N-[3-chloro-2-[4-(2-phenylethyl)piperazin-1-yl]phenyl]furan-2-carboxamide
0.0014
-
-
Homo sapiens N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]-5-ethylfuran-2-carboxamide
0.0015
-
-
Homo sapiens 5-bromo-N-[3-chloro-2-[4-(1-methylethyl)piperazin-1-yl]phenyl]furan-2-carboxamide
0.0018
-
-
Homo sapiens 4-bromo-N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-1,3-thiazole-2-carboxamide
0.0018
-
-
Homo sapiens N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-6-methylpyridine-2-carboxamide
0.002
-
-
Homo sapiens N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-6-methylpyridine-2-carboxamide
0.002
-
-
Homo sapiens 6-bromo-N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]pyridine-2-carboxamide
0.0022
-
-
Homo sapiens 5-bromo-N-[3-chloro-2-[4-(1-methylethyl)piperazin-1-yl]phenyl]furan-2-carboxamide
0.0023
-
-
Homo sapiens N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-1,3-thiazole-4-carboxamide
0.0032
-
-
Homo sapiens 5-benzyl-N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]furan-2-carboxamide
0.0041
-
-
Homo sapiens 5-bromo-N-(3-chloro-2-piperazin-1-ylphenyl)furan-2-carboxamide
0.0045
-
-
Homo sapiens N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-1H-pyrrole-2-carboxamide
0.0048
-
-
Homo sapiens 5-benzyl-N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]furan-2-carboxamide
0.005
-
-
Homo sapiens N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]isoxazole-5-carboxamide
0.0058
-
-
Homo sapiens 5-(acetylamino)-N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]furan-2-carboxamide
0.0058
-
-
Homo sapiens N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-2-methyl-1,3-thiazole-4-carboxamide
0.0063
-
-
Homo sapiens tert-butyl 4-(2-[[(5-bromofuran-2-yl)carbonyl]amino]-6-chlorophenyl)piperazine-1-carboxylate
0.0064
-
-
Homo sapiens 3-bromo-N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]benzamide
0.0071
-
-
Homo sapiens 3-bromo-N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]benzamide
0.0089
-
-
Homo sapiens N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-1H-pyrrole-2-carboxamide
0.0099
-
-
Homo sapiens 5-bromo-N-(3-chloro-2-piperazin-1-ylphenyl)furan-2-carboxamide
0.011
-
-
Homo sapiens 5-(acetylamino)-N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]furan-2-carboxamide
0.02
-
larger than 0.020 Homo sapiens 5-bromo-N-[2-(4-prop-2-en-1-ylpiperazin-1-yl)-3-(trifluoromethyl)phenyl]furan-2-carboxamide
0.02
-
larger than 0.020 Homo sapiens 5-bromo-N-[2-(4-prop-2-en-1-ylpiperazin-1-yl)biphenyl-3-yl]furan-2-carboxamide
0.02
-
larger than 0.020 Homo sapiens 5-bromo-N-[3-(phenylamino)-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
0.02
-
larger than 0.020 Homo sapiens 5-bromo-N-[3-bromo-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
0.02
-
larger than 0.020 Homo sapiens 5-bromo-N-[3-chloro-2-[4-(trifluoroacetyl)piperazin-1-yl]phenyl]furan-2-carboxamide
0.02
-
larger than 0.020 Homo sapiens N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]-5-(phenylamino)furan-2-carboxamide
0.02
-
larger than 0.020 Homo sapiens N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-5-cyanopyridine-2-carboxamide
0.02
-
larger than 0.020 Homo sapiens N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]pyrimidine-2-carboxamide
0.02
-
larger than 0.020 Homo sapiens tert-butyl 4-(2-[[(5-bromofuran-2-yl)carbonyl]amino]-6-chlorophenyl)piperazine-1-carboxylate

General Information

General Information Comment Organism
physiological function JNK1 has been suggested to play a central role in the development of obesity-induced insulin resistance Homo sapiens
physiological function JNK3 has been shown to mediate neuronal apoptosis Homo sapiens