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Literature summary for 2.7.12.2 extracted from

  • Wallace, E.M.; Lyssikatos, J.; Blake, J.F.; Seo, J.; Yang, H.W.; Yeh, T.C.; Perrier, M.; Jarski, H.; Marsh, V.; Poch, G.; Livingston, M.G.; Otten, J.; Hingorani, G.; Woessner, R.; Lee, P.; Winkler, J.; Koch, K.
    Potent and selective mitogen-activated protein kinase kinase (MEK) 1,2 inhibitors. 4-(4-Bromo-2-fluorophenylamino)-1-methylpyridin-2(1H)-ones (2006), J. Med. Chem., 49, 441-444.
    View publication on PubMed
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Inhibitors

Inhibitors Comment Organism Structure
4-(4-bromo-2-fluorophenylamino)-1-methylpyridin-2(1H)-one selective anthranilic acid type inhibitors, residues K97, I141, M143, F129, V127, I126, L118, F209, V211, and S212 of MEK1/2 are important for interaction with the inhibitor, noncompetitive to ATP, inhibition of ERK phosphorylation by MEK1/2 by the derivatives with IC50 values of 6.8-124 nM, low cytotoxic effects, overview Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + ERK Homo sapiens ERK phosphorylation by MEK1/2 ADP + phosphorylated ERK
-
 ?
additional information Homo sapiens MEK1/2 are involved in the mitogen-activated protein kinase signaling pathway and in cancer tumorigenesis ?
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + ERK ERK phosphorylation by MEK1/2 Homo sapiens ADP + phosphorylated ERK
-
 ?
additional information MEK1/2 are involved in the mitogen-activated protein kinase signaling pathway and in cancer tumorigenesis Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
MEK 1
-
 Homo sapiens
MEK 2
-
 Homo sapiens
mitogen-activated protein kinase kinase 1
-
 Homo sapiens
mitogen-activated protein kinase kinase 2
-
 Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000068 0.000124 selective anthranilic acid type inhibitors, residues K97, I141, M143, F129, V127, I126, L118, F209, V211, and S212 of MEK1/2 are important for interaction with the inhibitor, noncompetitive to ATP, inhibition of ERK phosphorylation by MEK1/2 by the deriva Homo sapiens 4-(4-bromo-2-fluorophenylamino)-1-methylpyridin-2(1H)-one