EC Number   |
Inhibitors |
Structure |
|---|
   2.7.7.86 | (1R,2S)-2-(7-oxo-5-phenyl-4,7-dihydropyrazolo[1,5-a]pyrimidine-3-carboxamido)cyclohexane-1-carboxylic acid |
PF-06928215, a commercial inhibitor, enzyme binding structure analysis, the pyrazolopyrimidine of PF-06928215 is sandwiched between the guanidinium group of R376 and the aromatic ring of Y436, mimicking the nucleobase. The benzene is anchored in a hydrophobic subpocket lined by the side chains of F488 and L490, molecular dynamics simulations, overview |
 |
| 2.7.7.86 | (1R,2S)-2-(7-oxo-5-phenyl-4,7-dihydropyrazolo[1,5-a]pyrimidine-3-carboxamido)cyclohexane-1-carboxylic acid |
PF-06928215, a commercial inhibitor |
|
| 2.7.7.86 | (3R)-1-(pyrrolo[1,2-a]quinoxalin-4-yl)piperidine-3-carboxylic acid |
16.8% inhibition at 0.1 mM |
  |
| 2.7.7.86 | (4-amino-6-((4-fluorophenyl)(methyl)amino)-1,3,5-triazin-2-yl)methanol |
- |
|
| 2.7.7.86 | (4-amino-6-((4-fluorophenyl)amino)-1,3,5-triazin-2-yl)methanol |
- |
|
| 2.7.7.86 | 1,3-dioxo-2,3-dihydro-1H-benzo[de]isoquinoline-6,7-dicarboxylic acid |
39.9% inhibition at 0.1 mM |
|
| 2.7.7.86 | 1-[9-(6-aminopyridin-3-yl)-6,7-dichloro-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indol-2-yl]-2-hydroxyethan-1-one |
- |
|
| 2.7.7.86 | 3-[1-(6,7-dichloro-1H-benzimidazol-2-yl)-5-hydroxy-3-methyl-pyrazol-4-yl]-3H-isobenzofuran-1-one |
RU-521 or RU.521 |
|
| 2.7.7.86 | 3-[1-(6,7-dichloro-1H-benzimidazol-2-yl)-5-hydroxy-3-methyl-pyrazol-4-yl]-3H-isobenzofuran-1-one |
RU-521 or RU.521, markedly mitigates the inflammatory responses, oxidative stress and apoptosis in hearts of sepsis mice. RU.521 attenuates myocardial apoptosis in the hearts of mice with sepsis |
|
| 2.7.7.86 | 3-[5-(carboxymethyl)-3-oxo-3,5-dihydro[1,2,4]triazino[2,3-a]benzimidazol-2-yl]propanoic acid |
29.9% inhibition at 0.1 mM |
|
