Application | Comment | Organism |
---|---|---|
medicine | inhibitors of IKK2 could be effective in the treatment of autoimmune and inflammatory disorders such as rheumatoid arrthritis, inflammatory bowel disease, lupus and multiple sclerosis | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
2-(4-fluorophenyl)-8-methyl-N-[2-(piperidin-1-yl)ethyl]-8H-imidazo[4,5-d][1,3]thiazolo[5,4-b]pyridin-5-amine | - |
Homo sapiens | |
2-methanesulfonyl-4-methyl-7-methylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine | - |
Homo sapiens | |
4-methyl-7-methylamino-2-(azepan-1-yl)-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine | - |
Homo sapiens | |
4-methyl-7-methylamino-2-(methylthio)-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine | - |
Homo sapiens | |
4-methyl-7-methylamino-2-benzylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine | - |
Homo sapiens | |
4-methyl-7-methylamino-2-cyclopentylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine | - |
Homo sapiens | |
4-methyl-7-methylamino-2-diethylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine | - |
Homo sapiens | |
4-methyl-7-methylamino-2-ethylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine | - |
Homo sapiens | |
4-methyl-7-methylamino-2-hydroxyethylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine | - |
Homo sapiens | |
4-methyl-7-methylamino-2-methylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine | - |
Homo sapiens | |
4-methyl-7-methylamino-2-methylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine | - |
Homo sapiens | |
4-methyl-7-methylamino-2-piperidine-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine | - |
Homo sapiens | |
4-methyl-7-methylamino-2-thienylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine | - |
Homo sapiens | |
4-methyl-7-methylamino-2-[1,2,3,6-tetrahydropyridine]-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine | - |
Homo sapiens | |
8-methyl-2-(4-fluorophenyl)-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-amine | - |
Homo sapiens | |
acetamide,N-[2-[[2-(4-fluorophenyl)-8-methyl-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-yl]amino]ethyl] | - |
Homo sapiens | |
ethanol,N-[2-[[2-(4-fluorophenyl)-8-methyl-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-yl]amino]ethyl] | - |
Homo sapiens | |
N,1-dimethyl-7-phenyl-1H-pyrazolo[5,1-b]purin-4-amine | - |
Homo sapiens | |
N-(1,8-dimethylimidazo[1,2-a]quinoxalin-4-yl)ethane-1,2-diamine | - |
Homo sapiens | |
N-(8-methyl-2-phenylimidazo[1,2-a]thieno[3,2-e]pyrazin-5-yl)ethane-1,2-diamine | - |
Homo sapiens | |
N-ethyl-2-(4-fluorophenyl)-N-methyl-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-amine | - |
Homo sapiens | |
N-methyl-2-(4-fluorophenyl)-8-methyl-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-amine | - |
Homo sapiens | |
N-[5-[4-(cyclopropylamino)-1-methyl-1H-pyrazolo[5,1-b]purin-7-yl]-2-fluorobenzyl]acetamide | - |
Homo sapiens | |
N-[[2-fluoro-5-[8-methyl-5-methylamino-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]acetamide | - |
Homo sapiens | |
N-[[2-fluoro-5-[8-methyl-5-methylamino-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]methanesulfonamide | - |
Homo sapiens | |
N-[[3-[8-methyl-5-(methylamino)-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]-1,2,3-thiadiazole-5-amide | - |
Homo sapiens | |
N-[[3-[8-methyl-5-(methylamino)-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]acetamide | - |
Homo sapiens | |
N-[[3-[8-methyl-5-(methylamino)-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]isoxazole-5-amide | - |
Homo sapiens | |
N-[[3-[8-methyl-5-(methylamino)-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]methanesulfonamide | - |
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 + GST-IkappaBalpha | activity assay | Homo sapiens | ADP + GST-IkappaBalpha phosphoprotein | - |
? | |
ATP + [IkappaB protein] | - |
Homo sapiens | ADP + [IkappaB phosphoprotein] | - |
? |
Subunits | Comment | Organism |
---|---|---|
oligomer | the IkappaB kinase complex comprises two catalytic subunits, IKK1 and IKK2, also termed IKKalpha and IKKbeta, respectively | Homo sapiens |
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 |
---|---|---|---|
7.5 | - |
activity assay | Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
ATP | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.000005 | - |
IKK-2 | Homo sapiens | N-[[3-[8-methyl-5-(methylamino)-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]methanesulfonamide | |
0.000006 | - |
IKK-2 | Homo sapiens | 4-methyl-7-methylamino-2-phenyl-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine | |
0.000011 | - |
IKK-2 | Homo sapiens | 4-methyl-7-methylamino-2-phenyl-4H-imidazo[4,5-d]oxazolo[5,4-b]pyridine | |
0.000015 | - |
IKK-2 | Homo sapiens | 4-methyl-7-methylamino-2-methylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine | |
0.000015 | - |
IKK-2 | Homo sapiens | 4-methyl-7-methylamino-2-ethylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine | |
0.000015 | - |
IKK-2 | Homo sapiens | 4-methyl-7-methylamino-2-thienylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine | |
0.000016 | - |
IKK-2 | Homo sapiens | N-[[3-[8-methyl-5-(methylamino)-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]-1,2,3-thiadiazole-5-amide | |
0.000019 | - |
IKK-2 | Homo sapiens | N-(8-methyl-2-phenylimidazo[1,2-a]thieno[3,2-e]pyrazin-5-yl)ethane-1,2-diamine | |
0.000022 | - |
IKK-2 | Homo sapiens | N-[[3-[8-methyl-5-(methylamino)-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]acetamide | |
0.000025 | - |
IKK-2 | Homo sapiens | N-[[3-[8-methyl-5-(methylamino)-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]isoxazole-5-amide | |
0.000026 | - |
IKK-2 | Homo sapiens | N-methyl-2-(4-fluorophenyl)-8-methyl-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-amine | |
0.000028 | - |
IKK-2 | Homo sapiens | 4-methyl-7-methylamino-2-(methylthio)-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine | |
0.000032 | - |
IKK-2 | Homo sapiens | N-[[2-fluoro-5-[8-methyl-5-methylamino-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]methanesulfonamide | |
0.000033 | - |
IKK-2 | Homo sapiens | 4-methyl-7-methylamino-2-[1,2,3,6-tetrahydropyridine]-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine | |
0.000033 | - |
IKK-2 | Homo sapiens | acetamide,N-[2-[[2-(4-fluorophenyl)-8-methyl-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-yl]amino]ethyl] | |
0.000034 | - |
IKK-2 | Homo sapiens | N,1-dimethyl-7-phenyl-1H-pyrazolo[5,1-b]purin-4-amine | |
0.000039 | - |
IKK-2 | Homo sapiens | N-ethyl-2-(4-fluorophenyl)-N-methyl-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-amine | |
0.000053 | - |
IKK-2 | Homo sapiens | N-[[2-fluoro-5-[8-methyl-5-methylamino-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]acetamide | |
0.000056 | - |
IKK-2 | Homo sapiens | 2-(4-fluorophenyl)-8-methyl-N-[2-(piperidin-1-yl)ethyl]-8H-imidazo[4,5-d][1,3]thiazolo[5,4-b]pyridin-5-amine | |
0.000075 | - |
IKK-2 | Homo sapiens | ethanol,N-[2-[[2-(4-fluorophenyl)-8-methyl-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-yl]amino]ethyl] | |
0.000081 | - |
IKK-2 | Homo sapiens | 2-methanesulfonyl-4-methyl-7-methylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine | |
0.00013 | - |
IKK-2 | Homo sapiens | 4-methyl-7-methylamino-2-(azepan-1-yl)-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine | |
0.00016 | - |
IKK-2 | Homo sapiens | 4-methyl-7-methylamino-2-cyclopentylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine | |
0.00018 | - |
IKK-2 | Homo sapiens | 8-methyl-2-(4-fluorophenyl)-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-amine | |
0.00021 | - |
IKK-2 | Homo sapiens | 4-methyl-7-methylamino-2-piperidine-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine | |
0.00027 | - |
IKK-1 | Homo sapiens | 4-methyl-7-methylamino-2-phenyl-4H-imidazo[4,5-d]oxazolo[5,4-b]pyridine | |
0.00028 | - |
IKK-2 | Homo sapiens | N-[5-[4-(cyclopropylamino)-1-methyl-1H-pyrazolo[5,1-b]purin-7-yl]-2-fluorobenzyl]acetamide | |
0.0003 | - |
IKK-2 | Homo sapiens | N-(1,8-dimethylimidazo[1,2-a]quinoxalin-4-yl)ethane-1,2-diamine | |
0.0003 | - |
IKK-2 | Homo sapiens | 4-methyl-7-methylamino-2-hydroxyethylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine | |
0.0004 | - |
IKK-1 | Homo sapiens | N-(8-methyl-2-phenylimidazo[1,2-a]thieno[3,2-e]pyrazin-5-yl)ethane-1,2-diamine | |
0.00052 | - |
IKK-2 | Homo sapiens | 1,4-dimethyl-7-methylamino-2-phenyl-4H-imidazo[4,5-d]imidazo[5,4-b]pyridine | |
0.00084 | - |
IKK-1 | Homo sapiens | 4-methyl-7-methylamino-2-methylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine | |
0.00092 | - |
IKK-2 | Homo sapiens | 4-methyl-7-methylamino-2-methylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine | |
0.00099 | - |
IKK-1 | Homo sapiens | N,1-dimethyl-7-phenyl-1H-pyrazolo[5,1-b]purin-4-amine | |
0.001 | - |
IKK-1 | Homo sapiens | N-[[3-[8-methyl-5-(methylamino)-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]methanesulfonamide | |
0.001 | - |
IKK-1 | Homo sapiens | N-[[3-[8-methyl-5-(methylamino)-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]-1,2,3-thiadiazole-5-amide | |
0.0011 | - |
IKK-1 | Homo sapiens | 4-methyl-7-methylamino-2-ethylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine | |
0.0014 | - |
IKK-1 | Homo sapiens | N-[[3-[8-methyl-5-(methylamino)-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]isoxazole-5-amide | |
0.0015 | - |
IKK-2 | Homo sapiens | 4-methyl-7-methylamino-2-benzylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine | |
0.0019 | - |
IKK-1 | Homo sapiens | N-[[3-[8-methyl-5-(methylamino)-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]acetamide | |
0.0025 | - |
IKK-2 | Homo sapiens | 4-methyl-7-methylamino-2-diethylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine | |
0.0026 | - |
IKK-1 | Homo sapiens | 4-methyl-7-methylamino-2-(methylthio)-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine | |
0.0031 | - |
IKK-1 | Homo sapiens | N-methyl-2-(4-fluorophenyl)-8-methyl-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-amine | |
0.0034 | - |
IKK-1 | Homo sapiens | 4-methyl-7-methylamino-2-methylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine | |
0.0034 | - |
IKK-1 | Homo sapiens | N-ethyl-2-(4-fluorophenyl)-N-methyl-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-amine | |
0.0035 | - |
IKK-1 | Homo sapiens | N-[[2-fluoro-5-[8-methyl-5-methylamino-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]acetamide | |
0.0035 | - |
IKK-1 | Homo sapiens | 4-methyl-7-methylamino-2-phenyl-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine | |
0.004 | - |
IKK-1 | Homo sapiens | N-(1,8-dimethylimidazo[1,2-a]quinoxalin-4-yl)ethane-1,2-diamine | |
0.0042 | - |
IKK-1 | Homo sapiens | N-[[2-fluoro-5-[8-methyl-5-methylamino-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]methanesulfonamide | |
0.0043 | - |
IKK-1 | Homo sapiens | 1,4-dimethyl-7-methylamino-2-phenyl-4H-imidazo[4,5-d]imidazo[5,4-b]pyridine | |
0.005 | - |
IKK-1 | Homo sapiens | acetamide,N-[2-[[2-(4-fluorophenyl)-8-methyl-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-yl]amino]ethyl] | |
0.0061 | - |
IKK-1 | Homo sapiens | 4-methyl-7-methylamino-2-piperidine-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine | |
0.0076 | - |
IKK-1 | Homo sapiens | 2-methanesulfonyl-4-methyl-7-methylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine | |
0.0081 | - |
IKK-1 | Homo sapiens | 4-methyl-7-methylamino-2-[1,2,3,6-tetrahydropyridine]-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine | |
0.0083 | - |
IKK-1 | Homo sapiens | 2-(4-fluorophenyl)-8-methyl-N-[2-(piperidin-1-yl)ethyl]-8H-imidazo[4,5-d][1,3]thiazolo[5,4-b]pyridin-5-amine | |
0.0086 | - |
IKK-1 | Homo sapiens | ethanol,N-[2-[[2-(4-fluorophenyl)-8-methyl-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-yl]amino]ethyl] | |
0.0097 | - |
IKK-1 | Homo sapiens | N-[5-[4-(cyclopropylamino)-1-methyl-1H-pyrazolo[5,1-b]purin-7-yl]-2-fluorobenzyl]acetamide | |
0.02 | - |
IKK-1 | Homo sapiens | 4-methyl-7-methylamino-2-diethylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine | |
0.02 | - |
IKK-1, larger than 0.020 | Homo sapiens | 8-methyl-2-(4-fluorophenyl)-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-amine |
General Information | Comment | Organism |
---|---|---|
physiological function | IKK is a central regulator of NF-kappaB transcription factors | Homo sapiens |