Application | Comment | Organism |
---|---|---|
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 (Comment) | Organism |
---|---|
a GST-IkappaBalpha fusion protein is generated | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
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 | |
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 | |
3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzonitrile | - |
Homo sapiens | |
7-(2-fluorophenyl)-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine | - |
Homo sapiens | |
7-(3-fluorophenyl)-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine | - |
Homo sapiens | |
7-(3-methoxyphenyl)-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine | - |
Homo sapiens | |
7-(4-fluorophenyl)-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine | - |
Homo sapiens | |
7-[3-(aminomethyl)phenyl]-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine | - |
Homo sapiens | |
N,1-dimethyl-7-phenyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine | - |
Homo sapiens | |
N,3,8-trimethyl-2-phenyl-3,8-dihydrodiimidazo[4,5-b:4',5'-d]pyridin-5-amine | - |
Homo sapiens | |
N,8-dimethyl-2-phenyl-8H-imidazo[4,5-d][1,3]oxazolo[5,4-b]pyridin-5-amine | - |
Homo sapiens | |
N,8-dimethyl-2-phenyl-8H-imidazo[4,5-d][1,3]thiazolo[5,4-b]pyridin-5-amine | - |
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 | - |
Homo sapiens | |
N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]acetamide | - |
Homo sapiens | |
N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]butanediamide | - |
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 | - |
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 | O14920 | - |
- |
Homo sapiens | Q15111 | - |
- |
Purification (Comment) | Organism |
---|---|
- |
Homo sapiens |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
peripheral blood mononuclear cell | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + [IkappaB protein] | - |
Homo sapiens | ADP + [IkappaB phosphoprotein] | - |
? |
Subunits | Comment | Organism |
---|---|---|
oligomer | two catalytic subunits, IKK1 and IKK2 | Homo sapiens |
Synonyms | Comment | Organism |
---|---|---|
IkappaB kinase-1 | - |
Homo sapiens |
IkappaB kinase-2 | - |
Homo sapiens |
IKK-1 | - |
Homo sapiens |
IKK-2 | - |
Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
ATP | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.000006 | - |
- |
Homo sapiens | N,8-dimethyl-2-phenyl-8H-imidazo[4,5-d][1,3]thiazolo[5,4-b]pyridin-5-amine | |
0.000007 | - |
- |
Homo sapiens | 7-(3-fluorophenyl)-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine | |
0.000007 | - |
- |
Homo sapiens | 3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzonitrile | |
0.000008 | - |
- |
Homo sapiens | 7-(3-methoxyphenyl)-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine | |
0.000011 | - |
- |
Homo sapiens | N,8-dimethyl-2-phenyl-8H-imidazo[4,5-d][1,3]oxazolo[5,4-b]pyridin-5-amine | |
0.000011 | - |
- |
Homo sapiens | 7-[3-(aminomethyl)phenyl]-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine | |
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 | |
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 | |
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 | |
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 | |
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 | |
0.00004 | - |
- |
Homo sapiens | N,1-dimethyl-7-phenyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine | |
0.000043 | - |
- |
Homo sapiens | 7-(4-fluorophenyl)-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine | |
0.000044 | - |
- |
Homo sapiens | 7-(2-fluorophenyl)-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine | |
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 | |
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 | |
0.00027 | - |
- |
Homo sapiens | N,8-dimethyl-2-phenyl-8H-imidazo[4,5-d][1,3]oxazolo[5,4-b]pyridin-5-amine | |
0.00052 | - |
- |
Homo sapiens | N,3,8-trimethyl-2-phenyl-3,8-dihydrodiimidazo[4,5-b:4',5'-d]pyridin-5-amine | |
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 | |
0.00167 | - |
- |
Homo sapiens | N,1-dimethyl-7-phenyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine | |
0.00173 | - |
- |
Homo sapiens | 7-(4-fluorophenyl)-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine | |
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 | |
0.0035 | - |
- |
Homo sapiens | N,8-dimethyl-2-phenyl-8H-imidazo[4,5-d][1,3]thiazolo[5,4-b]pyridin-5-amine | |
0.00428 | - |
- |
Homo sapiens | N,3,8-trimethyl-2-phenyl-3,8-dihydrodiimidazo[4,5-b:4',5'-d]pyridin-5-amine |
General Information | Comment | Organism |
---|---|---|
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 |