cas 356560-84-4, 1-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-2-(6-methylpyridin-2-yl)ethane-1,2-dione | Articles data ｜lookchem

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356560-84-4

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4-([1,2,4]Triazolo[1,5-a]pyridin-6-yl)-5(3)-(6-methylpyridin-2-yl)imidazole and -pyrazole derivatives as potent and selective inhibitors of transforming growth factor-β type i receptor kinase
A series of 4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5(3)-(6-methylpyridin-2- yl)imidazoles and -pyrazoles 14a-c, 15a-c, 16a, 16b, 19a-d, 21a, and 21b has been synthesized and evaluated for their ALK5 inhibitory activity in an enzyme assay and in a cell-based luciferase reporter assay. Among them, the pyrazole derivative 21b inhibited ALK5 phosphorylation with an IC50 value of 0.018 μM and showed 95% inhibition at 0.03 μM in a luciferase reporter assay using HaCaT cells permanently transfected with p3TP-luc reporter construct. The 21b showed a high selectivity index of 284 against p38α MAP kinase. The binding pose of 21b generated by docking analysis reveals that it fits well into the ATP binding cavity of ALK5 by forming several hydrogen bond interactions.
Jin, Cheng Hua,Krishnaiah, Maddeboina,Sreenu, Domalapally,Subrahmanyam, Vura Bala,Park, Hyun-Ju,Park, So-Jung,Sheen, Yhun Yhong,Kim, Dae-Kee
p. 2724 - 2732
(2014/05/06)

2-pyridyl substituted imidazoles as therapeutic ALK5 and/or ALK4 inhibitors
This invention relates to 2-pyridyl substituted imidazoles which are inhibitors of the transforming growth factor-β (TGF-β) type I receptor (ALK5) and/or the activin type I receptor (ALK4), methods for their preparation, and their use in medicine, specifically in the treatment and prevention of a disease state mediated by these receptors.
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(2012/01/04)

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Chemical Properties

Density: 1.39±0.1 g/cm3(Predicted)
Storage Temp.:Sealed in dry,Room Temperature
PKA: 0.85±0.10(Predicted)
PSA: 77.22000
LogP: 1.49830

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