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Literature summary extracted from

  • Kempson, J.; Guo, J.; Das, J.; Moquin, R.V.; Spergel, S.H.; Watterson, S.H.; Langevine, C.M.; Dyckman, A.J.; Pattoli, M.; Burke, J.R.; Yang, X.; Gillooly, K.M.; McIntyre, K.W.; Chen, L.; Dodd, J.H.; McKinnon, M.; Barrish, J.C.; Pitts, W.J.
    Synthesis, initial SAR and biological evaluation of 1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine derived inhibitors of IkappaB kinase (2009), Bioorg. Med. Chem. Lett., 19, 2646-2649.
    View publication on PubMed

Application

EC Number Application Comment Organism
2.7.11.10 medicine since IKK2 is vital for translating pro-inflammatory stimuli into the activation of NF-kappaB, an inhibitor of IKK2 could be effective in the treatment of autoimmune and inflammatory disorders Homo sapiens

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.7.11.10 a GST-IkappaBalpha fusion protein is generated Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.11.10 2-hydroxy-N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]acetamide
-
Homo sapiens
2.7.11.10 3-methoxy-N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]propanamide
-
Homo sapiens
2.7.11.10 3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzonitrile
-
Homo sapiens
2.7.11.10 7-(2-fluorophenyl)-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
-
Homo sapiens
2.7.11.10 7-(3-fluorophenyl)-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
-
Homo sapiens
2.7.11.10 7-(3-methoxyphenyl)-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
-
Homo sapiens
2.7.11.10 7-(4-fluorophenyl)-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
-
Homo sapiens
2.7.11.10 7-[3-(aminomethyl)phenyl]-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
-
Homo sapiens
2.7.11.10 N,1-dimethyl-7-phenyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
-
Homo sapiens
2.7.11.10 N,3,8-trimethyl-2-phenyl-3,8-dihydrodiimidazo[4,5-b:4',5'-d]pyridin-5-amine
-
Homo sapiens
2.7.11.10 N,8-dimethyl-2-phenyl-8H-imidazo[4,5-d][1,3]oxazolo[5,4-b]pyridin-5-amine
-
Homo sapiens
2.7.11.10 N,8-dimethyl-2-phenyl-8H-imidazo[4,5-d][1,3]thiazolo[5,4-b]pyridin-5-amine
-
Homo sapiens
2.7.11.10 N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]-1,2,3-thiadiazole-4-carboxamide
-
Homo sapiens
2.7.11.10 N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]acetamide
-
Homo sapiens
2.7.11.10 N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]butanediamide
-
Homo sapiens
2.7.11.10 N2,N2-dimethyl-N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]glycinamide
-
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 O14920
-
-
2.7.11.10 Homo sapiens Q15111
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.7.11.10
-
Homo sapiens

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.7.11.10 peripheral blood mononuclear cell
-
Homo sapiens
-

Substrates and Products (Substrate)

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

Subunits

EC Number Subunits Comment Organism
2.7.11.10 oligomer two catalytic subunits, IKK1 and IKK2 Homo sapiens

Synonyms

EC Number Synonyms Comment Organism
2.7.11.10 IkappaB kinase-1
-
Homo sapiens
2.7.11.10 IkappaB kinase-2
-
Homo sapiens
2.7.11.10 IKK-1
-
Homo sapiens
2.7.11.10 IKK-2
-
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 0.000006
-
-
Homo sapiens N,8-dimethyl-2-phenyl-8H-imidazo[4,5-d][1,3]thiazolo[5,4-b]pyridin-5-amine
2.7.11.10 0.000007
-
-
Homo sapiens 7-(3-fluorophenyl)-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
2.7.11.10 0.000007
-
-
Homo sapiens 3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzonitrile
2.7.11.10 0.000008
-
-
Homo sapiens 7-(3-methoxyphenyl)-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
2.7.11.10 0.000011
-
-
Homo sapiens N,8-dimethyl-2-phenyl-8H-imidazo[4,5-d][1,3]oxazolo[5,4-b]pyridin-5-amine
2.7.11.10 0.000011
-
-
Homo sapiens 7-[3-(aminomethyl)phenyl]-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
2.7.11.10 0.000012
-
-
Homo sapiens 3-methoxy-N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]propanamide
2.7.11.10 0.000014
-
-
Homo sapiens N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]acetamide
2.7.11.10 0.000022
-
-
Homo sapiens N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]butanediamide
2.7.11.10 0.000025
-
-
Homo sapiens 2-hydroxy-N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]acetamide
2.7.11.10 0.000039
-
-
Homo sapiens N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]-1,2,3-thiadiazole-4-carboxamide
2.7.11.10 0.00004
-
-
Homo sapiens N,1-dimethyl-7-phenyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
2.7.11.10 0.000043
-
-
Homo sapiens 7-(4-fluorophenyl)-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
2.7.11.10 0.000044
-
-
Homo sapiens 7-(2-fluorophenyl)-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
2.7.11.10 0.000079
-
-
Homo sapiens N2,N2-dimethyl-N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]glycinamide
2.7.11.10 0.00015
-
-
Homo sapiens N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]-1,2,3-thiadiazole-4-carboxamide
2.7.11.10 0.00027
-
-
Homo sapiens N,8-dimethyl-2-phenyl-8H-imidazo[4,5-d][1,3]oxazolo[5,4-b]pyridin-5-amine
2.7.11.10 0.00052
-
-
Homo sapiens N,3,8-trimethyl-2-phenyl-3,8-dihydrodiimidazo[4,5-b:4',5'-d]pyridin-5-amine
2.7.11.10 0.000633
-
-
Homo sapiens N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]acetamide
2.7.11.10 0.00167
-
-
Homo sapiens N,1-dimethyl-7-phenyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
2.7.11.10 0.00173
-
-
Homo sapiens 7-(4-fluorophenyl)-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
2.7.11.10 0.00262
-
-
Homo sapiens 3-methoxy-N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]propanamide
2.7.11.10 0.0035
-
-
Homo sapiens N,8-dimethyl-2-phenyl-8H-imidazo[4,5-d][1,3]thiazolo[5,4-b]pyridin-5-amine
2.7.11.10 0.00428
-
-
Homo sapiens N,3,8-trimethyl-2-phenyl-3,8-dihydrodiimidazo[4,5-b:4',5'-d]pyridin-5-amine

General Information

EC Number General Information Comment Organism
2.7.11.10 physiological function the IkappaB kinase complex catalyses the phosphorylation of IkappaBalpha at Ser32 and Ser36, essential for signaling the subsequent ubiquination and protosomal degradation of IkappaBalpha, thus leaving the NF-kappaB free to translocate to the nucleus and activate pro-inflammatory gene transcription Homo sapiens