Activating Compound | Comment | Organism | Structure |
---|---|---|---|
additional information | IKK is induced by TNFalpha | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
1-(6-chloro-9H-beta-carbolin-8-yl)-3-methylurea | inhibits IKK with IC50 of 0.02 mM | Homo sapiens | |
5,6-dibromo-beta-carboline | inhibits IKK with IC50 of 600 nM | Homo sapiens | |
5-bromo-6-chloro-beta-carboline | inhibits IKK with IC50 of 600 nM | Homo sapiens | |
5-bromo-6-cyano-beta-carboline | inhibits IKK with IC50 of 0.0011 mM | Homo sapiens | |
5-bromo-6-fluoro-beta-carboline | inhibits IKK with IC50 of 0.002 mM | Homo sapiens | |
5-bromo-6-methoxy-beta-carboline | nonspecific inhibitor of IKK, inhibits IKK with IC50 of 0.004 mM | Homo sapiens | |
5-bromo-6-trifluoromethyl-beta-carboline | inhibits IKK with IC50 of 0.0011 mM | Homo sapiens | |
5-bromo-beta-carboline | inhibits IKK with IC50 of 0.015 mM | Homo sapiens | |
6,8-dichloro-7-(cyclohexylmethoxy)-9H-beta-carboline | inhibits IKK with IC50 of 0.003 mM | Homo sapiens | |
6,8-dichloro-7-ethoxy-9H-beta-carboline | inhibits IKK with IC50 of 140 nM | Homo sapiens | |
6,8-dichloro-7-methoxy-9H-beta-carboline | inhibits IKK with IC50 of 170 nM | Homo sapiens | |
6,8-dichloro-9H-beta-carbolin-7-yl morpholine-4-carboxylate | inhibits IKK with IC50 of 0.0032 mM | Homo sapiens | |
6,8-dichloro-beta-carboline | inhibits IKK with IC50 of 200 nM | Homo sapiens | |
7-(OCH2CH(CH2CH2))-6,8-dichloro-beta-carboline | inhibits IKK with IC50 of 80 nM | Homo sapiens | |
7-hydroxy-6,8-dichloro-beta-carboline | inhibits IKK with IC50 of 0.011 mM | Homo sapiens | |
8-amino-6-chloro-beta-carboline | inhibits IKK with IC50 of 0.0013 mM | Homo sapiens | |
8-dimethylamino-6-chloro-beta-carboline | inhibits IKK with IC50 of 0.0018 mM | Homo sapiens | |
8-methylamino-6-chloro-beta-carboline | inhibits IKK with IC50 of 0.0018 mM | Homo sapiens | |
8-nitro-6-chloro-beta-carboline | inhibits IKK with IC50 of 0.004 mM | Homo sapiens | |
methyl (6-chloro-9H-beta-carbolin-8-yl)carbamate | inhibits IKK with IC50 of 700 nM | Homo sapiens | |
N-(6-chloro-9H-beta-carbolin-8-yl)-2-(pyridin-2-yl)acetamide | inhibits IKK with IC50 of 0.003 mM | Homo sapiens | |
N-(6-chloro-9H-beta-carbolin-8-yl)-2-methoxybenzamide | inhibits IKK with IC50 of 0.02 mM | Homo sapiens | |
N-(6-chloro-9H-beta-carbolin-8-yl)-3-methoxybenzamide | inhibits IKK with IC50 of 600 nM | Homo sapiens | |
N-(6-chloro-9H-beta-carbolin-8-yl)-4-hydroxybutanamide | inhibits IKK with IC50 of 0.02 mM | Homo sapiens | |
N-(6-chloro-9H-beta-carbolin-8-yl)-4-methoxybenzamide | inhibits IKK with IC50 of 0.0013 mM | Homo sapiens | |
N-(6-chloro-9H-beta-carbolin-8-yl)acetamide | inhibits IKK with IC50 of 600 nM | Homo sapiens | |
N-(6-chloro-9H-beta-carbolin-8-yl)benzamide | inhibits IKK with IC50 of 700 nM | Homo sapiens | |
N-(6-chloro-9H-beta-carbolin-8-yl)benzenesulfonamide | inhibits IKK with IC50 of 0.02 mM | Homo sapiens | |
N-(6-chloro-9H-beta-carbolin-8-yl)methanesulfonamide | inhibits IKK with IC50 of 0.0083 mM | Homo sapiens | |
N-(6-chloro-9H-beta-carbolin-8-yl)morpholine-4-carboxamide | inhibits IKK with IC50 of 0.02 mM | Homo sapiens | |
N-(6-chloro-9H-beta-carbolin-8-yl)pyridine-2-carboxamide | inhibits IKK with IC50 of 0.001 mM | Homo sapiens | |
N-(6-chloro-9H-beta-carbolin-8-yl)pyridine-4-carboxamide | inhibits IKK with IC50 of 300 nM | Homo sapiens | |
N-benzyl-6-chloro-9H-beta-carbolin-8-amine | inhibits IKK with IC50 of 0.02 mM | Homo sapiens | |
PS-1145 | i.e. 8-(NHC(O)-3'-pyridyl)-6-chloro-beta-carboline, inhibits IKK with IC50 of 100 nM in vitro, blocks phosphorylation of IkappaBalpha and subsequent activation of NFkappaB in vivo | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + [IkappaBalpha protein] | Homo sapiens | enzyme is involved in activation of pro-inflammation signalling | ADP + [IkappaBalpha phosphoprotein] | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
isozymes IKK1 and IKK2 | - |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
HeLa cell | induced by TNFalpha | Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + [GST-IkappaBalpha protein] | - |
Homo sapiens | ADP + [GST-IkappaBalpha phosphoprotein] | - |
? | |
ATP + [IkappaBalpha protein] | enzyme is involved in activation of pro-inflammation signalling | Homo sapiens | ADP + [IkappaBalpha phosphoprotein] | - |
? |
Synonyms | Comment | Organism |
---|---|---|
IKK | - |
Homo sapiens |
IKK complex | - |
Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
ATP | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00008 | - |
inhibits IKK with IC50 of 80 nM | Homo sapiens | 7-(OCH2CH(CH2CH2))-6,8-dichloro-beta-carboline | |
0.0001 | - |
i.e. 8-(NHC(O)-3'-pyridyl)-6-chloro-beta-carboline, inhibits IKK with IC50 of 100 nM in vitro, blocks phosphorylation of IkappaBalpha and subsequent activation of NFkappaB in vivo | Homo sapiens | PS-1145 | |
0.00014 | - |
inhibits IKK with IC50 of 140 nM | Homo sapiens | 6,8-dichloro-7-ethoxy-9H-beta-carboline | |
0.00017 | - |
inhibits IKK with IC50 of 170 nM | Homo sapiens | 6,8-dichloro-7-methoxy-9H-beta-carboline | |
0.0002 | - |
inhibits IKK with IC50 of 200 nM | Homo sapiens | 6,8-dichloro-beta-carboline | |
0.0003 | - |
inhibits IKK with IC50 of 300 nM | Homo sapiens | N-(6-chloro-9H-beta-carbolin-8-yl)pyridine-4-carboxamide | |
0.0006 | - |
inhibits IKK with IC50 of 600 nM | Homo sapiens | N-(6-chloro-9H-beta-carbolin-8-yl)acetamide | |
0.0006 | - |
inhibits IKK with IC50 of 600 nM | Homo sapiens | N-(6-chloro-9H-beta-carbolin-8-yl)-3-methoxybenzamide | |
0.0006 | - |
inhibits IKK with IC50 of 600 nM | Homo sapiens | 5,6-dibromo-beta-carboline | |
0.0006 | - |
inhibits IKK with IC50 of 600 nM | Homo sapiens | 5-bromo-6-chloro-beta-carboline | |
0.0007 | - |
inhibits IKK with IC50 of 700 nM | Homo sapiens | N-(6-chloro-9H-beta-carbolin-8-yl)benzamide | |
0.0007 | - |
inhibits IKK with IC50 of 700 nM | Homo sapiens | methyl (6-chloro-9H-beta-carbolin-8-yl)carbamate | |
0.001 | - |
inhibits IKK with IC50 of 0.001 mM | Homo sapiens | N-(6-chloro-9H-beta-carbolin-8-yl)pyridine-2-carboxamide | |
0.0011 | - |
inhibits IKK with IC50 of 0.0011 mM | Homo sapiens | 5-bromo-6-trifluoromethyl-beta-carboline | |
0.0011 | - |
inhibits IKK with IC50 of 0.0011 mM | Homo sapiens | 5-bromo-6-cyano-beta-carboline | |
0.0013 | - |
inhibits IKK with IC50 of 0.0013 mM | Homo sapiens | 8-amino-6-chloro-beta-carboline | |
0.0013 | - |
inhibits IKK with IC50 of 0.0013 mM | Homo sapiens | N-(6-chloro-9H-beta-carbolin-8-yl)-4-methoxybenzamide | |
0.0018 | - |
inhibits IKK with IC50 of 0.0018 mM | Homo sapiens | 8-methylamino-6-chloro-beta-carboline | |
0.0018 | - |
inhibits IKK with IC50 of 0.0018 mM | Homo sapiens | 8-dimethylamino-6-chloro-beta-carboline | |
0.002 | - |
inhibits IKK with IC50 of 0.002 mM | Homo sapiens | 5-bromo-6-fluoro-beta-carboline | |
0.003 | - |
inhibits IKK with IC50 of 0.003 mM | Homo sapiens | N-(6-chloro-9H-beta-carbolin-8-yl)-2-(pyridin-2-yl)acetamide | |
0.003 | - |
inhibits IKK with IC50 of 0.003 mM | Homo sapiens | 6,8-dichloro-7-(cyclohexylmethoxy)-9H-beta-carboline | |
0.0032 | - |
inhibits IKK with IC50 of 0.0032 mM | Homo sapiens | 6,8-dichloro-9H-beta-carbolin-7-yl morpholine-4-carboxylate | |
0.004 | - |
inhibits IKK with IC50 of 0.004 mM | Homo sapiens | 8-nitro-6-chloro-beta-carboline | |
0.004 | - |
nonspecific inhibitor of IKK, inhibits IKK with IC50 of 0.004 mM | Homo sapiens | 5-bromo-6-methoxy-beta-carboline | |
0.0083 | - |
inhibits IKK with IC50 of 0.0083 mM | Homo sapiens | N-(6-chloro-9H-beta-carbolin-8-yl)methanesulfonamide | |
0.011 | - |
inhibits IKK with IC50 of 0.011 mM | Homo sapiens | 7-hydroxy-6,8-dichloro-beta-carboline | |
0.015 | - |
inhibits IKK with IC50 of 0.015 mM | Homo sapiens | 5-bromo-beta-carboline | |
0.02 | - |
inhibits IKK with IC50 of 0.02 mM | Homo sapiens | N-benzyl-6-chloro-9H-beta-carbolin-8-amine | |
0.02 | - |
inhibits IKK with IC50 of 0.02 mM | Homo sapiens | N-(6-chloro-9H-beta-carbolin-8-yl)-4-hydroxybutanamide | |
0.02 | - |
inhibits IKK with IC50 of 0.02 mM | Homo sapiens | N-(6-chloro-9H-beta-carbolin-8-yl)-2-methoxybenzamide | |
0.02 | - |
inhibits IKK with IC50 of 0.02 mM | Homo sapiens | N-(6-chloro-9H-beta-carbolin-8-yl)benzenesulfonamide | |
0.02 | - |
inhibits IKK with IC50 of 0.02 mM | Homo sapiens | 1-(6-chloro-9H-beta-carbolin-8-yl)-3-methylurea | |
0.02 | - |
inhibits IKK with IC50 of 0.02 mM | Homo sapiens | N-(6-chloro-9H-beta-carbolin-8-yl)morpholine-4-carboxamide |