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Literature summary for 2.7.11.10 extracted from

  • Christopher, J.A.; Bamborough, P.; Alder, C.; Campbell, A.; Cutler, G.J.; Down, K.; Hamadi, A.M.; Jolly, A.M.; Kerns, J.K.; Lucas, F.S.; Mellor, G.W.; Miller, D.D.; Morse, M.A.; Pancholi, K.D.; Rumsey, W.; Solanke, Y.E.; Williamson, R.
    Discovery of 6-aryl-7-alkoxyisoquinoline inhibitors of IkappaB kinase-beta (IKK-beta) (2009), J. Med. Chem., 52, 3098-3102.
    View publication on PubMed
Search for more literature for 2.7.11.10

Application

Application Comment Organism
pharmacology aberrant kinase activity is implicated in many diseases and makes this target class attractive for the pharmaceutical industry Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
recombinant human IKK-beta, residues 1-737, is expressed in Baculovirus as a C-terminal GST-tagged fusion protein, a 6-His-tagged full length IKK-alpha construct is used Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1-[3-[7-(piperidin-4-yloxy)isoquinolin-6-yl]phenyl]methanamine
-
 Homo sapiens
1-[4-[7-(piperidin-4-yloxy)isoquinolin-6-yl]phenyl]methanamine
-
 Homo sapiens
1-[4-[7-(piperidin-4-yloxy)isoquinolin-6-yl]phenyl]methanesulfonamide
-
 Homo sapiens
3-[7-(benzyloxy)isoquinolin-6-yl]benzenesulfonamide
-
 Homo sapiens
3-[7-(piperidin-4-yloxy)isoquinolin-6-yl]benzenesulfonamide
-
 Homo sapiens
4'-amino-4-chloro-4''-sulfamoyl-1,1':3',1''-terphenyl-5'-carboxamide
-
 Homo sapiens
4-(7-[[1-(ethylsulfonyl)piperidin-4-yl]oxy]isoquinolin-6-yl)benzenesulfonamide
-
 Homo sapiens
4-[7-(benzyloxy)isoquinolin-6-yl]benzenesulfonamide
-
 Homo sapiens
4-[7-(piperidin-3-ylmethoxy)isoquinolin-6-yl]benzenesulfonamide
-
 Homo sapiens
4-[7-(piperidin-3-yloxy)isoquinolin-6-yl]benzenesulfonamide
-
 Homo sapiens
4-[7-(piperidin-4-ylmethoxy)isoquinolin-6-yl]benzenesulfonamide
-
 Homo sapiens
4-[7-(piperidin-4-yloxy)isoquinolin-6-yl]benzenesulfonamide
-
 Homo sapiens
4-[7-[(1-acetylpiperidin-4-yl)oxy]isoquinolin-6-yl]benzenesulfonamide
-
 Homo sapiens
6-bromo-7-(piperidin-4-yloxy)isoquinoline
-
 Homo sapiens
6-bromo-7-[[1-(ethylsulfonyl)piperidin-4-yl]oxy]isoquinoline
-
 Homo sapiens
6-phenyl-7-(piperidin-3-ylmethoxy)isoquinoline
-
 Homo sapiens
6-phenyl-7-(piperidin-3-yloxy)isoquinoline
-
 Homo sapiens
6-phenyl-7-(piperidin-4-ylmethoxy)isoquinoline
-
 Homo sapiens
6-phenyl-7-(piperidin-4-yloxy)isoquinoline
-
 Homo sapiens
6-phenyl-7-(pyridin-3-ylmethoxy)isoquinoline
-
 Homo sapiens
6-phenyl-7-(pyridin-4-ylmethoxy)isoquinoline
-
 Homo sapiens
7-(piperidin-4-yloxy)isoquinoline
-
 Homo sapiens
7-[(1-acetylpiperidin-4-yl)oxy]-6-bromoisoquinoline
-
 Homo sapiens
7-[(1-acetylpiperidin-4-yl)oxy]-6-phenylisoquinoline
-
 Homo sapiens
7-[[1-(ethylsulfonyl)piperidin-4-yl]methoxy]-6-phenylisoquinoline
-
 Homo sapiens
7-[[1-(ethylsulfonyl)piperidin-4-yl]oxy]-6-phenylisoquinoline
-
 Homo sapiens
N,N-dimethyl-3-[(4-[[(6-phenylisoquinolin-7-yl)oxy]methyl]piperidin-1-yl)sulfonyl]propan-1-amine
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + [IkappaB protein]
-
 Homo sapiens ADP + [IkappaB phosphoprotein]
-
 ?

Synonyms

Synonyms Comment Organism
IkappaB kinase
-
 Homo sapiens
IKK
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
22
-
 activity assay at room temperature Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
 activity assay Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0001
-
 IKK-beta Homo sapiens 4-[7-(piperidin-4-yloxy)isoquinolin-6-yl]benzenesulfonamide
0.0001
-
 IKK-beta Homo sapiens 1-[4-[7-(piperidin-4-yloxy)isoquinolin-6-yl]phenyl]methanamine
0.0001
-
 IKK-beta Homo sapiens 6-phenyl-7-(piperidin-4-yloxy)isoquinoline
0.0002
-
 IKK-beta Homo sapiens 6-phenyl-7-(piperidin-3-ylmethoxy)isoquinoline
0.0004
-
 IKK-beta Homo sapiens 1-[4-[7-(piperidin-4-yloxy)isoquinolin-6-yl]phenyl]methanesulfonamide
0.0004
-
 IKK-beta Homo sapiens 6-bromo-7-(piperidin-4-yloxy)isoquinoline
0.0006
-
 IKK-beta Homo sapiens 6-phenyl-7-(piperidin-3-yloxy)isoquinoline
0.0006
-
 IKK-beta Homo sapiens 4-[7-(piperidin-4-ylmethoxy)isoquinolin-6-yl]benzenesulfonamide
0.0008
-
 IKK-beta Homo sapiens 1-[3-[7-(piperidin-4-yloxy)isoquinolin-6-yl]phenyl]methanamine
0.0008
-
 IKK-beta Homo sapiens 4-[7-(piperidin-3-yloxy)isoquinolin-6-yl]benzenesulfonamide
0.0008
-
 IKK-beta Homo sapiens 4-[7-(piperidin-3-ylmethoxy)isoquinolin-6-yl]benzenesulfonamide
0.001
-
 IKK-beta Homo sapiens 4-(7-[[1-(ethylsulfonyl)piperidin-4-yl]oxy]isoquinolin-6-yl)benzenesulfonamide
0.0013
-
 IKK-beta Homo sapiens 3-[7-(piperidin-4-yloxy)isoquinolin-6-yl]benzenesulfonamide
0.0013
-
 IKK-beta Homo sapiens 4-[7-[(1-acetylpiperidin-4-yl)oxy]isoquinolin-6-yl]benzenesulfonamide
0.0013
-
 IKK-beta Homo sapiens 6-phenyl-7-(piperidin-4-ylmethoxy)isoquinoline
0.0013
-
 IKK-beta Homo sapiens N,N-dimethyl-3-[(4-[[(6-phenylisoquinolin-7-yl)oxy]methyl]piperidin-1-yl)sulfonyl]propan-1-amine
0.0016
-
 IKK-alpha Homo sapiens 7-[(1-acetylpiperidin-4-yl)oxy]-6-phenylisoquinoline
0.0016
-
 IKK-alpha Homo sapiens 4-[7-(piperidin-4-ylmethoxy)isoquinolin-6-yl]benzenesulfonamide
0.002
-
 IKK-beta Homo sapiens 7-[[1-(ethylsulfonyl)piperidin-4-yl]oxy]-6-phenylisoquinoline
0.0025
-
 IKK-alpha Homo sapiens 6-phenyl-7-(piperidin-4-yloxy)isoquinoline
0.0025
-
 IKK-beta Homo sapiens 7-[[1-(ethylsulfonyl)piperidin-4-yl]methoxy]-6-phenylisoquinoline
0.0032
-
 IKK-alpha Homo sapiens 6-phenyl-7-(piperidin-3-ylmethoxy)isoquinoline
0.0032
-
 IKK-beta Homo sapiens 4-[7-(benzyloxy)isoquinolin-6-yl]benzenesulfonamide
0.0032
-
 IKK-beta Homo sapiens 7-[(1-acetylpiperidin-4-yl)oxy]-6-phenylisoquinoline
0.004
-
 IKK-alpha Homo sapiens 1-[4-[7-(piperidin-4-yloxy)isoquinolin-6-yl]phenyl]methanesulfonamide
0.004
-
 IKK-alpha Homo sapiens 6-phenyl-7-(piperidin-3-yloxy)isoquinoline
0.004
-
 IKK-beta Homo sapiens 6-phenyl-7-(pyridin-3-ylmethoxy)isoquinoline
0.005
-
 IKK-alpha Homo sapiens 4-[7-(piperidin-3-ylmethoxy)isoquinolin-6-yl]benzenesulfonamide
0.005
-
 IKK-beta Homo sapiens 6-bromo-7-[[1-(ethylsulfonyl)piperidin-4-yl]oxy]isoquinoline
0.005
-
 IKK-beta Homo sapiens 7-(piperidin-4-yloxy)isoquinoline
0.005
-
 IKK-beta Homo sapiens 6-phenyl-7-(pyridin-4-ylmethoxy)isoquinoline
0.0063
-
 IKK-alpha Homo sapiens 1-[4-[7-(piperidin-4-yloxy)isoquinolin-6-yl]phenyl]methanamine
0.0079
-
 IKK-alpha Homo sapiens 3-[7-(piperidin-4-yloxy)isoquinolin-6-yl]benzenesulfonamide
0.0079
-
 IKK-alpha Homo sapiens 4-[7-(piperidin-4-yloxy)isoquinolin-6-yl]benzenesulfonamide
0.0079
-
 IKK-beta Homo sapiens 3-[7-(benzyloxy)isoquinolin-6-yl]benzenesulfonamide
0.01
-
 IKK-alpha Homo sapiens 6-bromo-7-(piperidin-4-yloxy)isoquinoline
0.01
-
 IKK-alpha Homo sapiens 6-phenyl-7-(piperidin-4-ylmethoxy)isoquinoline
0.01
-
 IKK-alpha Homo sapiens N,N-dimethyl-3-[(4-[[(6-phenylisoquinolin-7-yl)oxy]methyl]piperidin-1-yl)sulfonyl]propan-1-amine
0.0126
-
 IKK-alpha Homo sapiens 1-[3-[7-(piperidin-4-yloxy)isoquinolin-6-yl]phenyl]methanamine
0.0126
-
 IKK-alpha Homo sapiens 7-[[1-(ethylsulfonyl)piperidin-4-yl]oxy]-6-phenylisoquinoline
0.0126
-
 IKK-alpha Homo sapiens 4-[7-(piperidin-3-yloxy)isoquinolin-6-yl]benzenesulfonamide
0.0126
-
 IKK-beta Homo sapiens 7-[(1-acetylpiperidin-4-yl)oxy]-6-bromoisoquinoline
0.02
-
 IKK-alpha Homo sapiens 7-[[1-(ethylsulfonyl)piperidin-4-yl]methoxy]-6-phenylisoquinoline
0.0251
-
-
 Homo sapiens 4-(7-[[1-(ethylsulfonyl)piperidin-4-yl]oxy]isoquinolin-6-yl)benzenesulfonamide
0.0251
-
 IKK-alpha, less than 0.0251 Homo sapiens 3-[7-(benzyloxy)isoquinolin-6-yl]benzenesulfonamide
0.0251
-
 IKK-alpha, less than 0.0251 Homo sapiens 4-[7-(benzyloxy)isoquinolin-6-yl]benzenesulfonamide
0.0251
-
 IKK-alpha, less than 0.0251 Homo sapiens 6-bromo-7-[[1-(ethylsulfonyl)piperidin-4-yl]oxy]isoquinoline
0.0251
-
 IKK-alpha, less than 0.0251 Homo sapiens 7-[(1-acetylpiperidin-4-yl)oxy]-6-bromoisoquinoline
0.0251
-
 IKK-alpha, less than 0.0251 Homo sapiens 4-[7-[(1-acetylpiperidin-4-yl)oxy]isoquinolin-6-yl]benzenesulfonamide
0.0251
-
 IKK-alpha, less than 0.0251 Homo sapiens 7-(piperidin-4-yloxy)isoquinoline
0.0251
-
 IKK-alpha, less than 0.0251 Homo sapiens 6-phenyl-7-(pyridin-3-ylmethoxy)isoquinoline
0.0251
-
 IKK-alpha, less than 0.0251 Homo sapiens 6-phenyl-7-(pyridin-4-ylmethoxy)isoquinoline

General Information

General Information Comment Organism
physiological function IKK is a central regulator of NF-kappaB transcription factors Homo sapiens