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Literature summary for 2.7.11.24 extracted from

  • Humphries, P.S.; Lafontaine, J.A.; Agree, C.S.; Alexander, D.; Chen, P.; Do, Q.Q.; Li, L.Y.; Lunney, E.A.; Rajapakse, R.J.; Siegel, K.; Timofeevski, S.L.; Wang, T.; Wilhite, D.M.
    Synthesis and SAR of 4-substituted-2-aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors (2009), Bioorg. Med. Chem. Lett., 19, 2099-2102.
    View publication on PubMed

Application

Application Comment Organism
medicine JNK1 has emerged as an attractive target for diabetes therapy, since JNK1 is believed to play a key role in linking obesity and insulin resistance Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(3R)-3-([4-[3-(4-chlorophenyl)-1H-pyrazol-4-yl]pyrimidin-2-yl]amino)butanoic acid
-
Homo sapiens
3-([4-[3-(tetrahydro-2H-pyran-3-yl)-1H-pyrazol-4-yl]pyrimidin-2-yl]amino)cyclohexanol
-
Homo sapiens
4-[3-(4-chlorophenyl)-1H-pyrazol-4-yl]-N-(1-methylethyl)pyrimidin-2-amine
-
Homo sapiens
4-[3-(4-chlorophenyl)-1H-pyrazol-4-yl]-N-(1-methylpiperidin-4-yl)pyrimidin-2-amine
-
Homo sapiens
4-[3-(4-chlorophenyl)-1H-pyrazol-4-yl]-N-cyclohexylpyrimidin-2-amine
-
Homo sapiens
4-[3-(4-chlorophenyl)-1H-pyrazol-4-yl]-N-cyclopentylpyrimidin-2-amine
-
Homo sapiens
4-[3-(4-chlorophenyl)-1H-pyrazol-4-yl]-N-cyclopropylpyrimidin-2-amine
-
Homo sapiens
4-[3-(4-chlorophenyl)-1H-pyrazol-4-yl]-N-methylpyrimidin-2-amine
-
Homo sapiens
N-(1-methylethyl)-4-(1H-pyrazol-4-yl)pyrimidin-2-amine
-
Homo sapiens
N-(1-methylethyl)-4-(3-piperidin-3-yl-1H-pyrazol-4-yl)pyrimidin-2-amine
-
Homo sapiens
N-(1-methylethyl)-4-[3-(6-methylpyridin-3-yl)-1H-pyrazol-4-yl]pyrimidin-2-amine
-
Homo sapiens
N-(1-methylethyl)-4-[3-(tetrahydro-2H-pyran-2-yl)-1H-pyrazol-4-yl]pyrimidin-2-amine
-
Homo sapiens
N-(1-methylethyl)-4-[3-(tetrahydro-2H-pyran-3-yl)-1H-pyrazol-4-yl]pyrimidin-2-amine
-
Homo sapiens
N-(1-methylethyl)-4-[3-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl]pyrimidin-2-amine
-
Homo sapiens
N-(1-methylethyl)-4-[3-[1-(methylsulfonyl)piperidin-4-yl]-1H-pyrazol-4-yl]pyrimidin-2-amine
-
Homo sapiens
N-cyclopentyl-4-[3-(tetrahydro-2H-pyran-3-yl)-1H-pyrazol-4-yl]pyrimidin-2-amine
-
Homo sapiens
N-[trans-4-([4-[3-(tetrahydro-2H-pyran-3-yl)-1H-pyrazol-4-yl]pyrimidin-2-yl]amino)cyclohexyl]acetamide
-
Homo sapiens
N-[trans-4-([4-[3-(tetrahydro-2H-pyran-3-yl)-1H-pyrazol-4-yl]pyrimidin-2-yl]amino)cyclohexyl]methanesulfonamide
-
Homo sapiens
trans-4-([4-[3-(tetrahydro-2H-pyran-3-yl)-1H-pyrazol-4-yl]pyrimidin-2-yl]amino)cyclohexanol
-
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
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
Hep-G2 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 + IRS-1 phosphorylation of the insulin receptor substrate IRS-1 at serine 307 Homo sapiens ADP + phosphorylated IRS-1
-
?

Synonyms

Synonyms Comment Organism
c-Jun N-terminal kinase
-
Homo sapiens
c-Jun N-terminal kinase 2
-
Homo sapiens
c-Jun N-terminal kinase 3
-
Homo sapiens
JNK
-
Homo sapiens
JNK1
-
Homo sapiens
JNK2
-
Homo sapiens
JNK3
-
Homo sapiens
MAP kinase
-
Homo sapiens
mitogen-activated kinase
-
Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000009
-
N-[trans-4-([4-[3-(tetrahydro-2H-pyran-3-yl)-1H-pyrazol-4-yl]pyrimidin-2-yl]amino)cyclohexyl]methanesulfonamide
-
Homo sapiens
0.000012
-
trans-4-([4-[3-(tetrahydro-2H-pyran-3-yl)-1H-pyrazol-4-yl]pyrimidin-2-yl]amino)cyclohexanol
-
Homo sapiens
0.000012
-
N-cyclopentyl-4-[3-(tetrahydro-2H-pyran-3-yl)-1H-pyrazol-4-yl]pyrimidin-2-amine
-
Homo sapiens
0.000016
-
trans-4-([4-[3-(tetrahydro-2H-pyran-3-yl)-1H-pyrazol-4-yl]pyrimidin-2-yl]amino)cyclohexanol
-
Homo sapiens
0.000017
-
trans-4-([4-[3-(tetrahydro-2H-pyran-3-yl)-1H-pyrazol-4-yl]pyrimidin-2-yl]amino)cyclohexanol
-
Homo sapiens
0.000026
-
4-[3-(4-chlorophenyl)-1H-pyrazol-4-yl]-N-cyclopentylpyrimidin-2-amine
-
Homo sapiens
0.000027
-
4-[3-(4-chlorophenyl)-1H-pyrazol-4-yl]-N-cyclohexylpyrimidin-2-amine
-
Homo sapiens
0.000028
-
N-[trans-4-([4-[3-(tetrahydro-2H-pyran-3-yl)-1H-pyrazol-4-yl]pyrimidin-2-yl]amino)cyclohexyl]acetamide
-
Homo sapiens
0.000036
-
3-([4-[3-(tetrahydro-2H-pyran-3-yl)-1H-pyrazol-4-yl]pyrimidin-2-yl]amino)cyclohexanol
-
Homo sapiens
0.000043
-
N-(1-methylethyl)-4-[3-(tetrahydro-2H-pyran-3-yl)-1H-pyrazol-4-yl]pyrimidin-2-amine
-
Homo sapiens
0.000048
-
4-[3-(4-chlorophenyl)-1H-pyrazol-4-yl]-N-(1-methylethyl)pyrimidin-2-amine
-
Homo sapiens
0.000101
-
N-(1-methylethyl)-4-[3-[1-(methylsulfonyl)piperidin-4-yl]-1H-pyrazol-4-yl]pyrimidin-2-amine
-
Homo sapiens
0.000151
-
4-[3-(4-chlorophenyl)-1H-pyrazol-4-yl]-N-cyclopropylpyrimidin-2-amine
-
Homo sapiens
0.000162
-
N-(1-methylethyl)-4-[3-(6-methylpyridin-3-yl)-1H-pyrazol-4-yl]pyrimidin-2-amine
-
Homo sapiens
0.000169
-
N-(1-methylethyl)-4-[3-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl]pyrimidin-2-amine
-
Homo sapiens
0.000315
-
(3R)-3-([4-[3-(4-chlorophenyl)-1H-pyrazol-4-yl]pyrimidin-2-yl]amino)butanoic acid
-
Homo sapiens
0.000381
-
N-(1-methylethyl)-4-[3-(tetrahydro-2H-pyran-2-yl)-1H-pyrazol-4-yl]pyrimidin-2-amine
-
Homo sapiens
0.00053
-
N-(1-methylethyl)-4-(3-piperidin-3-yl-1H-pyrazol-4-yl)pyrimidin-2-amine
-
Homo sapiens
0.00157
-
4-[3-(4-chlorophenyl)-1H-pyrazol-4-yl]-N-(1-methylpiperidin-4-yl)pyrimidin-2-amine
-
Homo sapiens
0.00206
-
4-[3-(4-chlorophenyl)-1H-pyrazol-4-yl]-N-methylpyrimidin-2-amine
-
Homo sapiens
0.00273
-
N-(1-methylethyl)-4-(1H-pyrazol-4-yl)pyrimidin-2-amine
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000098
-
-
Homo sapiens trans-4-([4-[3-(tetrahydro-2H-pyran-3-yl)-1H-pyrazol-4-yl]pyrimidin-2-yl]amino)cyclohexanol
0.000114
-
-
Homo sapiens N-[trans-4-([4-[3-(tetrahydro-2H-pyran-3-yl)-1H-pyrazol-4-yl]pyrimidin-2-yl]amino)cyclohexyl]methanesulfonamide
0.000209
-
-
Homo sapiens 3-([4-[3-(tetrahydro-2H-pyran-3-yl)-1H-pyrazol-4-yl]pyrimidin-2-yl]amino)cyclohexanol
0.000221
-
-
Homo sapiens N-(1-methylethyl)-4-[3-[1-(methylsulfonyl)piperidin-4-yl]-1H-pyrazol-4-yl]pyrimidin-2-amine
0.000245
-
-
Homo sapiens N-cyclopentyl-4-[3-(tetrahydro-2H-pyran-3-yl)-1H-pyrazol-4-yl]pyrimidin-2-amine
0.000299
-
-
Homo sapiens N-[trans-4-([4-[3-(tetrahydro-2H-pyran-3-yl)-1H-pyrazol-4-yl]pyrimidin-2-yl]amino)cyclohexyl]acetamide
0.000357
-
-
Homo sapiens N-(1-methylethyl)-4-[3-(tetrahydro-2H-pyran-3-yl)-1H-pyrazol-4-yl]pyrimidin-2-amine
0.00046
-
-
Homo sapiens 4-[3-(4-chlorophenyl)-1H-pyrazol-4-yl]-N-cyclopentylpyrimidin-2-amine
0.000814
-
-
Homo sapiens N-(1-methylethyl)-4-[3-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl]pyrimidin-2-amine
0.00084
-
-
Homo sapiens 4-[3-(4-chlorophenyl)-1H-pyrazol-4-yl]-N-cyclopropylpyrimidin-2-amine
0.00092
-
-
Homo sapiens 4-[3-(4-chlorophenyl)-1H-pyrazol-4-yl]-N-(1-methylethyl)pyrimidin-2-amine
0.0011
-
-
Homo sapiens 4-[3-(4-chlorophenyl)-1H-pyrazol-4-yl]-N-cyclohexylpyrimidin-2-amine
0.0035
-
-
Homo sapiens N-(1-methylethyl)-4-[3-(tetrahydro-2H-pyran-2-yl)-1H-pyrazol-4-yl]pyrimidin-2-amine
0.00602
-
-
Homo sapiens N-(1-methylethyl)-4-[3-(6-methylpyridin-3-yl)-1H-pyrazol-4-yl]pyrimidin-2-amine

Expression

Organism Comment Expression
Homo sapiens JNK activity is elevated in adipocytes of type 2 diabetic patients up

General Information

General Information Comment Organism
physiological function JNK1 disrupts the insulin signaling cascade via phosphorylation of the insulin receptor substrate IRS-1, which leads to the degradation of IRS-1 Homo sapiens