Application | Comment | Organism |
---|---|---|
medicine | PHA-408 is efficacious in a chronic model of arthritis with no adverse effects | Rattus norvegicus |
medicine | PHA-408 is efficacious in a chronic model of arthritis with no adverse effects | Homo sapiens |
Cloned (Comment) | Organism |
---|---|
- |
Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
8-(5-chloro-2-(4-methylpiperazin-1-yl)isonicotinamido)-1-(4-fluorophenyl)-4,5-dihydro-1H-benzo[g]indazole-3-carboxamide | PHA-408, ATP-competitive, selective IKK-2 inhibitor; PHA-408, ATP-competitive, selective IKK-2 inhibitor | Homo sapiens | |
8-(5-chloro-2-(4-methylpiperazin-1-yl)isonicotinamido)-1-(4-fluorophenyl)-4,5-dihydro-1H-benzo[g]indazole-3-carboxamide | PHA-408, ATP-competitive, selective IKK-2 inhibitor | Rattus norvegicus |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + [IkappaB protein] | Rattus norvegicus | - |
ADP + [IkappaB phosphoprotein] | - |
? | |
ATP + [IkappaB protein] | Homo sapiens | - |
ADP + [IkappaB phosphoprotein] | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | O14920 | - |
- |
Homo sapiens | Q15111 | - |
- |
Rattus norvegicus | - |
- |
- |
Purification (Comment) | Organism |
---|---|
- |
Homo sapiens |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
blood | - |
Homo sapiens | - |
liver | - |
Rattus norvegicus | - |
paw | - |
Rattus norvegicus | - |
peripheral blood mononuclear cell | - |
Homo sapiens | - |
rheumatoid arthritis disease specific synovial fibroblast | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + [IkappaB protein] | - |
Rattus norvegicus | ADP + [IkappaB phosphoprotein] | - |
? | |
ATP + [IkappaB protein] | - |
Homo sapiens | ADP + [IkappaB phosphoprotein] | - |
? |
Synonyms | Comment | Organism |
---|---|---|
IkappaB kinase-1 | - |
Homo sapiens |
IkappaB kinase-2 | - |
Rattus norvegicus |
IkappaB kinase-2 | - |
Homo sapiens |
IKK-1 | - |
Homo sapiens |
IKK-2 | - |
Rattus norvegicus |
IKK-2 | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
25 | - |
activity assay | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.6 | - |
activity assay | Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
ATP | - |
Rattus norvegicus | |
ATP | - |
Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.000006 | - |
8-(5-chloro-2-(4-methylpiperazin-1-yl)isonicotinamido)-1-(4-fluorophenyl)-4,5-dihydro-1H-benzo[g]indazole-3-carboxamide | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00004 | - |
- |
Homo sapiens | 8-(5-chloro-2-(4-methylpiperazin-1-yl)isonicotinamido)-1-(4-fluorophenyl)-4,5-dihydro-1H-benzo[g]indazole-3-carboxamide | |
0.0141 | - |
- |
Homo sapiens | 8-(5-chloro-2-(4-methylpiperazin-1-yl)isonicotinamido)-1-(4-fluorophenyl)-4,5-dihydro-1H-benzo[g]indazole-3-carboxamide |