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Literature summary for 2.7.11.24 extracted from
- Pyridinylquinoxalines and pyridinylpyridopyrazines as lead compounds for novel p38 alpha mitogen-activated protein kinase inhibitors (2010), J. Med. Chem., 53, 1128-1137.
Activating Compound
| Activating Compound | Comment | Organism | Structure |
|---|---|---|---|
| additional information | activated by infection or cellular stressors such as mechanical wear, heat, or osmotic shock | Mus musculus |
Application
| Application | Comment | Organism |
|---|---|---|
| medicine | inhibition of p38 alpha mitogen-activated protein kinase is a promising therapeutic strategy for the treatment of cytokine-driven disorders like inflammatory bowel disease or rheumatoid arthritis | Mus musculus |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 2-(4-fluorophenyl)-3-(2-isopropylaminopyridin-4-yl)pyrido[2,3-b]pyrazine | - |
Mus musculus |  |
| 2-(4-fluorophenyl)-3-(pyridin-4-yl)pyrido[2,3-b]pyrazine | - |
Mus musculus | |
| 2-(4-fluorophenyl)-3-(pyridin-4-yl)quinoxaline | - |
Mus musculus | |
| 2-(4-fluorophenyl)-3-pyridin-4-ylpyrido[3,4-b]pyrazine | - |
Mus musculus | |
| 2-(4-fluorophenyl)-6,7-dimethyl-3-pyridin-4-ylquinoxaline | - |
Mus musculus | |
| 2-(4-fluorophenyl)-6-methoxy-3-(pyridin-4-yl)quinoxaline | - |
Mus musculus | |
| 3-(4-fluorophenyl)-2-(2-isopropylaminopyridin-4-yl)pyrido[2,3-b]pyrazine | - |
Mus musculus | |
| 3-(4-fluorophenyl)-2-(pyridin-4-yl)pyrido[2,3-b]pyrazine | - |
Mus musculus | |
| 3-(4-fluorophenyl)-2-pyridin-4-ylpyrido[3,4-b]pyrazine | - |
Mus musculus | |
| 3-(4-fluorophenyl)-6-methoxy-2-(pyridin-4-yl)quinoxaline | - |
Mus musculus | |
| 4-[3-(4-fluorophenyl)-6,7-dimethylquinoxalin-2-yl]-N-(1-methylethyl)pyridin-2-amine | - |
Mus musculus | |
| 4-[3-(4-fluorophenyl)quinoxalin-2-yl]-N-(1-phenylethyl)pyridin-2-amine | - |
Mus musculus | |
| 4-[3-(4-fluorophenyl)quinoxalin-2-yl]-N-(3-methylbutan-2-yl)pyridin-2-amine | - |
Mus musculus | |
| 4-[3-(4-fluorophenyl)quinoxalin-2-yl]-N-isobutylpyridin-2-amine | - |
Mus musculus | |
| 4-[3-(4-fluorophenyl)quinoxalin-2-yl]-N-isopropylpyridin-2-amine | - |
Mus musculus | |
| 4-[3-(4-fluorophenyl)quinoxalin-2-yl]-N-[(1R)-1-phenylethyl]pyridin-2-amine | - |
Mus musculus | |
| 4-[3-(4-fluorophenyl)quinoxalin-2-yl]-N-[(1S)-1-phenylethyl]pyridin-2-amine | - |
Mus musculus | |
| 4-[3-(4-fluorophenyl)quinoxalin-2-yl]-N-[(R)-3-methylbutan-2-yl]pyridin-2-amine | - |
Mus musculus | |
| 4-[3-(4-fluorophenyl)quinoxalin-2-yl]-N-[(S)-3-methylbutan-2-yl]pyridin-2-amine | - |
Mus musculus | |
| 4-[4-[3-(4-fluorophenyl)quinoxalin-2-yl]pyridin-2-ylamine]-cyclohexanol | - |
Mus musculus | |
| 4-[6,7-dichloro-3-(4-fluorophenyl)quinoxalin-2-yl]-N-(1,2-dimethylpropyl)pyridin-2-amine | - |
Mus musculus | |
| 4-[6,7-dichloro-3-(4-fluorophenyl)quinoxalin-2-yl]-N-(1-methylethyl)pyridin-2-amine | - |
Mus musculus | |
| 6,7-dichloro-2-(4-fluorophenyl)-3-pyridin-4-ylquinoxaline | - |
Mus musculus | |
| N-(1,2-dimethylpropyl)-4-[3-(4-fluorophenyl)-6,7-dimethylquinoxalin-2-yl]pyridin-2-amine | - |
Mus musculus | |
| N-benzyl-4-[3-(4-fluorophenyl)-6,7-dimethylquinoxalin-2-yl]pyridin-2-amine | - |
Mus musculus | |
| N-benzyl-4-[3-(4-fluorophenyl)quinoxalin-2-yl]pyridin-2-amine | - |
Mus musculus | |
| N-benzyl-4-[6,7-dichloro-3-(4-fluorophenyl)quinoxalin-2-yl]pyridin-2-amine | - |
Mus musculus | |
| N-sec-butyl-4-[3-(4-fluorophenyl)-6,7-dimethylquinoxalin-2-yl]pyridin-2-amine | - |
Mus musculus | |
| N-sec-butyl-4-[3-(4-fluorophenyl)quinoxalin-2-yl]pyridin-2-amine | - |
Mus musculus | |
| N-tert-butyl-4-[2-(4-fluorophenyl)pyrido[3,4-b]pyrazin-3-yl]pyridin-2-amine | - |
Mus musculus | |
| N-tert-butyl-4-[3-(4-fluorophenyl)pyrido[3,4-b]pyrazin-2-yl]pyridin-2-amine | - |
Mus musculus | |
| trans-4-([4-[3-(4-fluorophenyl)-6,7-dimethylquinoxalin-2-yl]pyridin-2-yl]amino)cyclohexanol | - |
Mus musculus | |
| trans-4-([4-[6,7-dichloro-3-(4-fluorophenyl)quinoxalin-2-yl]pyridin-2-yl]amino)cyclohexanol | - |
Mus musculus | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + a protein | Mus musculus | - |
ADP + a phosphoprotein | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Mus musculus | - |
for docking studies the X-ray structure of murine p38alpha is used | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + a protein | - |
Mus musculus | ADP + a phosphoprotein | - |
? | |
| ATP + ATF-2 | substrate in kinase assay | Mus musculus | ADP + phosphorylated ATF-2 | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| MAP kinase | - |
Mus musculus |
| mitogen-activated kinase | - |
Mus musculus |
| p38 alpha mitogen-activated protein kinase | - |
Mus musculus |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| ATP | - |
Mus musculus | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| additional information | - |
33% at 10 microM | Mus musculus | 2-(4-fluorophenyl)-6-methoxy-3-(pyridin-4-yl)quinoxaline | |
| additional information | - |
33% at 10 microM, mixture of 3-(4-fluorophenyl)-2-pyridin-4-ylpyrido[3,4-b]pyrazine and 2-(4-fluorophenyl)-3-pyridin-4-ylpyrido[3,4-b]pyrazine | Mus musculus | 2-(4-fluorophenyl)-3-pyridin-4-ylpyrido[3,4-b]pyrazine | |
| additional information | - |
33% at 10 microM, mixture of 3-(4-fluorophenyl)-2-pyridin-4-ylpyrido[3,4-b]pyrazine and 2-(4-fluorophenyl)-3-pyridin-4-ylpyrido[3,4-b]pyrazine | Mus musculus | 3-(4-fluorophenyl)-2-pyridin-4-ylpyrido[3,4-b]pyrazine | |
| additional information | - |
37% at 10 microM | Mus musculus | N-benzyl-4-[6,7-dichloro-3-(4-fluorophenyl)quinoxalin-2-yl]pyridin-2-amine | |
| additional information | - |
39% at 10 microM | Mus musculus | 6,7-dichloro-2-(4-fluorophenyl)-3-pyridin-4-ylquinoxaline | |
| additional information | - |
46% at 10 microM | Mus musculus | 2-(4-fluorophenyl)-3-(pyridin-4-yl)pyrido[2,3-b]pyrazine | |
| additional information | - |
9% at 10 microM | Mus musculus | N-benzyl-4-[3-(4-fluorophenyl)quinoxalin-2-yl]pyridin-2-amine | |
| 0.000038 | - |
- |
Mus musculus | 3-(4-fluorophenyl)-2-(2-isopropylaminopyridin-4-yl)pyrido[2,3-b]pyrazine | |
| 0.000081 | - |
- |
Mus musculus | 4-[3-(4-fluorophenyl)quinoxalin-2-yl]-N-isopropylpyridin-2-amine | |
| 0.000114 | - |
- |
Mus musculus | N-sec-butyl-4-[3-(4-fluorophenyl)quinoxalin-2-yl]pyridin-2-amine | |
| 0.000211 | - |
- |
Mus musculus | 4-[4-[3-(4-fluorophenyl)quinoxalin-2-yl]pyridin-2-ylamine]-cyclohexanol | |
| 0.000238 | - |
- |
Mus musculus | 4-[3-(4-fluorophenyl)-6,7-dimethylquinoxalin-2-yl]-N-(1-methylethyl)pyridin-2-amine | |
| 0.000259 | - |
- |
Mus musculus | trans-4-([4-[3-(4-fluorophenyl)-6,7-dimethylquinoxalin-2-yl]pyridin-2-yl]amino)cyclohexanol | |
| 0.000333 | - |
- |
Mus musculus | 2-(4-fluorophenyl)-3-(2-isopropylaminopyridin-4-yl)pyrido[2,3-b]pyrazine | |
| 0.000412 | - |
- |
Mus musculus | 4-[6,7-dichloro-3-(4-fluorophenyl)quinoxalin-2-yl]-N-(1-methylethyl)pyridin-2-amine | |
| 0.000431 | - |
- |
Mus musculus | 4-[3-(4-fluorophenyl)quinoxalin-2-yl]-N-[(1S)-1-phenylethyl]pyridin-2-amine | |
| 0.000522 | - |
mixture of N-tert-butyl-4-[3-(4-fluorophenyl)pyrido[3,4-b]pyrazin-2-yl]pyridin-2-amine and N-tert-butyl-4-[2-(4-fluorophenyl)pyrido[3,4-b]pyrazin-3-yl]pyridin-2-amine | Mus musculus | N-tert-butyl-4-[2-(4-fluorophenyl)pyrido[3,4-b]pyrazin-3-yl]pyridin-2-amine | |
| 0.000522 | - |
mixture of N-tert-butyl-4-[3-(4-fluorophenyl)pyrido[3,4-b]pyrazin-2-yl]pyridin-2-amine and N-tert-butyl-4-[2-(4-fluorophenyl)pyrido[3,4-b]pyrazin-3-yl]pyridin-2-amine | Mus musculus | N-tert-butyl-4-[3-(4-fluorophenyl)pyrido[3,4-b]pyrazin-2-yl]pyridin-2-amine | |
| 0.000595 | - |
- |
Mus musculus | N-sec-butyl-4-[3-(4-fluorophenyl)-6,7-dimethylquinoxalin-2-yl]pyridin-2-amine | |
| 0.000608 | - |
- |
Mus musculus | trans-4-([4-[6,7-dichloro-3-(4-fluorophenyl)quinoxalin-2-yl]pyridin-2-yl]amino)cyclohexanol | |
| 0.000642 | - |
- |
Mus musculus | 4-[3-(4-fluorophenyl)quinoxalin-2-yl]-N-isobutylpyridin-2-amine | |
| 0.00072 | - |
- |
Mus musculus | 4-[3-(4-fluorophenyl)quinoxalin-2-yl]-N-(1-phenylethyl)pyridin-2-amine | |
| 0.000794 | - |
- |
Mus musculus | 4-[3-(4-fluorophenyl)quinoxalin-2-yl]-N-(3-methylbutan-2-yl)pyridin-2-amine | |
| 0.00138 | - |
- |
Mus musculus | N-(1,2-dimethylpropyl)-4-[3-(4-fluorophenyl)-6,7-dimethylquinoxalin-2-yl]pyridin-2-amine | |
| 0.00153 | - |
- |
Mus musculus | N-benzyl-4-[3-(4-fluorophenyl)-6,7-dimethylquinoxalin-2-yl]pyridin-2-amine | |
| 0.00159 | - |
- |
Mus musculus | 4-[3-(4-fluorophenyl)quinoxalin-2-yl]-N-[(R)-3-methylbutan-2-yl]pyridin-2-amine | |
| 0.00315 | - |
- |
Mus musculus | 2-(4-fluorophenyl)-3-(pyridin-4-yl)quinoxaline | |
| 0.00319 | - |
- |
Mus musculus | 3-(4-fluorophenyl)-2-(pyridin-4-yl)pyrido[2,3-b]pyrazine | |
| 0.0037 | - |
- |
Mus musculus | 2-(4-fluorophenyl)-6,7-dimethyl-3-pyridin-4-ylquinoxaline | |
| 0.00479 | - |
- |
Mus musculus | 4-[3-(4-fluorophenyl)quinoxalin-2-yl]-N-[(1R)-1-phenylethyl]pyridin-2-amine | |
| 0.00576 | - |
- |
Mus musculus | 4-[3-(4-fluorophenyl)quinoxalin-2-yl]-N-[(S)-3-methylbutan-2-yl]pyridin-2-amine | |
| 0.00614 | - |
- |
Mus musculus | 3-(4-fluorophenyl)-6-methoxy-2-(pyridin-4-yl)quinoxaline | |
| 0.00946 | - |
- |
Mus musculus | 4-[6,7-dichloro-3-(4-fluorophenyl)quinoxalin-2-yl]-N-(1,2-dimethylpropyl)pyridin-2-amine | |
General Information
| General Information | Comment | Organism |
|---|---|---|
| physiological function | p38 alpha mitogen-activated protein kinase is a key component of the cascade leading to pro-inflammatory cytokines such as tumor necrosis factor-alpha and interleukin-1beta | Mus musculus |
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