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 (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 | 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 | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + [IkappaB protein] | Homo sapiens | - |
ADP + [IkappaB phosphoprotein] | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + [IkappaB protein] | - |
Homo sapiens | ADP + [IkappaB phosphoprotein] | - |
? |
Synonyms | Comment | Organism |
---|---|---|
IkappaB kinase | - |
Homo sapiens |
IKK | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
22 | - |
activity assay at room temperature | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.4 | - |
activity assay | Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
ATP | - |
Homo sapiens |
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 | Comment | Organism |
---|---|---|
physiological function | IKK is a central regulator of NF-kappaB transcription factors | Homo sapiens |