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Literature summary extracted from

  • Kempson, J.; Spergel, S.H.; Guo, J.; Quesnelle, C.; Gill, P.; Belanger, D.; Dyckman, A.J.; Li, T.; Watterson, S.H.; Langevine, C.M.; Das, J.; Moquin, R.V.; Furch, J.A.; Marinier, A.; Dodier, M.; Martel, A.; Nirschl, D.; Van Kirk, K.; Burke, J.R.; Pattoli, M.A.; Gillooly, K.; McIntyre, K.W.; Chen, L.; Yang, Z.
    Novel tricyclic inhibitors of IkappaB kinase (2009), J. Med. Chem., 52, 1994-2005.
    View publication on PubMed

Application

EC Number Application Comment Organism
2.7.11.10 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

EC Number Inhibitors Comment Organism Structure
2.7.11.10 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
2.7.11.10 2-methanesulfonyl-4-methyl-7-methylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
-
 Homo sapiens
2.7.11.10 4-methyl-7-methylamino-2-(azepan-1-yl)-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
-
 Homo sapiens
2.7.11.10 4-methyl-7-methylamino-2-(methylthio)-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
-
 Homo sapiens
2.7.11.10 4-methyl-7-methylamino-2-benzylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
-
 Homo sapiens
2.7.11.10 4-methyl-7-methylamino-2-cyclopentylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
-
 Homo sapiens
2.7.11.10 4-methyl-7-methylamino-2-diethylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
-
 Homo sapiens
2.7.11.10 4-methyl-7-methylamino-2-ethylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
-
 Homo sapiens
2.7.11.10 4-methyl-7-methylamino-2-hydroxyethylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
-
 Homo sapiens
2.7.11.10 4-methyl-7-methylamino-2-methylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
-
 Homo sapiens
2.7.11.10 4-methyl-7-methylamino-2-methylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
-
 Homo sapiens
2.7.11.10 4-methyl-7-methylamino-2-piperidine-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
-
 Homo sapiens
2.7.11.10 4-methyl-7-methylamino-2-thienylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
-
 Homo sapiens
2.7.11.10 4-methyl-7-methylamino-2-[1,2,3,6-tetrahydropyridine]-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
-
 Homo sapiens
2.7.11.10 8-methyl-2-(4-fluorophenyl)-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-amine
-
 Homo sapiens
2.7.11.10 acetamide,N-[2-[[2-(4-fluorophenyl)-8-methyl-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-yl]amino]ethyl]
-
 Homo sapiens
2.7.11.10 ethanol,N-[2-[[2-(4-fluorophenyl)-8-methyl-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-yl]amino]ethyl]
-
 Homo sapiens
2.7.11.10 N,1-dimethyl-7-phenyl-1H-pyrazolo[5,1-b]purin-4-amine
-
 Homo sapiens
2.7.11.10 N-(1,8-dimethylimidazo[1,2-a]quinoxalin-4-yl)ethane-1,2-diamine
-
 Homo sapiens
2.7.11.10 N-(8-methyl-2-phenylimidazo[1,2-a]thieno[3,2-e]pyrazin-5-yl)ethane-1,2-diamine
-
 Homo sapiens
2.7.11.10 N-ethyl-2-(4-fluorophenyl)-N-methyl-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-amine
-
 Homo sapiens
2.7.11.10 N-methyl-2-(4-fluorophenyl)-8-methyl-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-amine
-
 Homo sapiens
2.7.11.10 N-[5-[4-(cyclopropylamino)-1-methyl-1H-pyrazolo[5,1-b]purin-7-yl]-2-fluorobenzyl]acetamide
-
 Homo sapiens
2.7.11.10 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
2.7.11.10 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
2.7.11.10 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
2.7.11.10 N-[[3-[8-methyl-5-(methylamino)-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]acetamide
-
 Homo sapiens
2.7.11.10 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
2.7.11.10 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/ Products (Substrates)

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

Organism

EC Number Organism UniProt Comment Textmining
2.7.11.10 Homo sapiens
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.11.10 ATP + GST-IkappaBalpha activity assay Homo sapiens ADP + GST-IkappaBalpha phosphoprotein
-
 ?
2.7.11.10 ATP + [IkappaB protein]
-
 Homo sapiens ADP + [IkappaB phosphoprotein]
-
 ?

Subunits

EC Number Subunits Comment Organism
2.7.11.10 oligomer the IkappaB kinase complex comprises two catalytic subunits, IKK1 and IKK2, also termed IKKalpha and IKKbeta, respectively Homo sapiens

Synonyms

EC Number Synonyms Comment Organism
2.7.11.10 IkappaB kinase
-
 Homo sapiens
2.7.11.10 IKK
-
 Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.7.11.10 22
-
 activity assay at room temperature Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.7.11.10 7.5
-
 activity assay Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.11.10 ATP
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.11.10 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
2.7.11.10 0.000006
-
 IKK-2 Homo sapiens 4-methyl-7-methylamino-2-phenyl-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
2.7.11.10 0.000011
-
 IKK-2 Homo sapiens 4-methyl-7-methylamino-2-phenyl-4H-imidazo[4,5-d]oxazolo[5,4-b]pyridine
2.7.11.10 0.000015
-
 IKK-2 Homo sapiens 4-methyl-7-methylamino-2-methylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
2.7.11.10 0.000015
-
 IKK-2 Homo sapiens 4-methyl-7-methylamino-2-ethylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
2.7.11.10 0.000015
-
 IKK-2 Homo sapiens 4-methyl-7-methylamino-2-thienylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
2.7.11.10 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
2.7.11.10 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
2.7.11.10 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
2.7.11.10 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
2.7.11.10 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
2.7.11.10 0.000028
-
 IKK-2 Homo sapiens 4-methyl-7-methylamino-2-(methylthio)-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
2.7.11.10 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
2.7.11.10 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
2.7.11.10 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]
2.7.11.10 0.000034
-
 IKK-2 Homo sapiens N,1-dimethyl-7-phenyl-1H-pyrazolo[5,1-b]purin-4-amine
2.7.11.10 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
2.7.11.10 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
2.7.11.10 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
2.7.11.10 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]
2.7.11.10 0.000081
-
 IKK-2 Homo sapiens 2-methanesulfonyl-4-methyl-7-methylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
2.7.11.10 0.00013
-
 IKK-2 Homo sapiens 4-methyl-7-methylamino-2-(azepan-1-yl)-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
2.7.11.10 0.00016
-
 IKK-2 Homo sapiens 4-methyl-7-methylamino-2-cyclopentylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
2.7.11.10 0.00018
-
 IKK-2 Homo sapiens 8-methyl-2-(4-fluorophenyl)-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-amine
2.7.11.10 0.00021
-
 IKK-2 Homo sapiens 4-methyl-7-methylamino-2-piperidine-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
2.7.11.10 0.00027
-
 IKK-1 Homo sapiens 4-methyl-7-methylamino-2-phenyl-4H-imidazo[4,5-d]oxazolo[5,4-b]pyridine
2.7.11.10 0.00028
-
 IKK-2 Homo sapiens N-[5-[4-(cyclopropylamino)-1-methyl-1H-pyrazolo[5,1-b]purin-7-yl]-2-fluorobenzyl]acetamide
2.7.11.10 0.0003
-
 IKK-2 Homo sapiens N-(1,8-dimethylimidazo[1,2-a]quinoxalin-4-yl)ethane-1,2-diamine
2.7.11.10 0.0003
-
 IKK-2 Homo sapiens 4-methyl-7-methylamino-2-hydroxyethylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
2.7.11.10 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
2.7.11.10 0.00052
-
 IKK-2 Homo sapiens 1,4-dimethyl-7-methylamino-2-phenyl-4H-imidazo[4,5-d]imidazo[5,4-b]pyridine
2.7.11.10 0.00084
-
 IKK-1 Homo sapiens 4-methyl-7-methylamino-2-methylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
2.7.11.10 0.00092
-
 IKK-2 Homo sapiens 4-methyl-7-methylamino-2-methylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
2.7.11.10 0.00099
-
 IKK-1 Homo sapiens N,1-dimethyl-7-phenyl-1H-pyrazolo[5,1-b]purin-4-amine
2.7.11.10 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
2.7.11.10 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
2.7.11.10 0.0011
-
 IKK-1 Homo sapiens 4-methyl-7-methylamino-2-ethylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
2.7.11.10 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
2.7.11.10 0.0015
-
 IKK-2 Homo sapiens 4-methyl-7-methylamino-2-benzylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
2.7.11.10 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
2.7.11.10 0.0025
-
 IKK-2 Homo sapiens 4-methyl-7-methylamino-2-diethylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
2.7.11.10 0.0026
-
 IKK-1 Homo sapiens 4-methyl-7-methylamino-2-(methylthio)-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
2.7.11.10 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
2.7.11.10 0.0034
-
 IKK-1 Homo sapiens 4-methyl-7-methylamino-2-methylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
2.7.11.10 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
2.7.11.10 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
2.7.11.10 0.0035
-
 IKK-1 Homo sapiens 4-methyl-7-methylamino-2-phenyl-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
2.7.11.10 0.004
-
 IKK-1 Homo sapiens N-(1,8-dimethylimidazo[1,2-a]quinoxalin-4-yl)ethane-1,2-diamine
2.7.11.10 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
2.7.11.10 0.0043
-
 IKK-1 Homo sapiens 1,4-dimethyl-7-methylamino-2-phenyl-4H-imidazo[4,5-d]imidazo[5,4-b]pyridine
2.7.11.10 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]
2.7.11.10 0.0061
-
 IKK-1 Homo sapiens 4-methyl-7-methylamino-2-piperidine-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
2.7.11.10 0.0076
-
 IKK-1 Homo sapiens 2-methanesulfonyl-4-methyl-7-methylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
2.7.11.10 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
2.7.11.10 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
2.7.11.10 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]
2.7.11.10 0.0097
-
 IKK-1 Homo sapiens N-[5-[4-(cyclopropylamino)-1-methyl-1H-pyrazolo[5,1-b]purin-7-yl]-2-fluorobenzyl]acetamide
2.7.11.10 0.02
-
 IKK-1 Homo sapiens 4-methyl-7-methylamino-2-diethylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
2.7.11.10 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

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