Discovery of 5-substituted-N-arylpyridazinones as inhibitors of p38 MAP kinase.

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Jerome KD, Hepperle ME, Walker JK, Xing L, Devraj RV, Benson AG, Baldus JE, Selness SR

Discovery of 5-substituted-N-arylpyridazinones as inhibitors of p38 MAP kinase.

Bioorg Med Chem Lett. 2010 May 15;20(10):3146-9. doi: 10.1016/j.bmcl.2010.03.088. Epub 2010 Mar 31.

PubMed ID

20395140 [ View in PubMed

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Abstract

The synthesis, structure-activity relationship and modeling of a series of 5-substituted-N-aryl pyridazinone based p38alpha inhibitors are described. In comparing the series to the similar N-aryl pyridinone series, it was found that the pyridazinones maintained a weaker interaction to the p38 enzyme, and therefore showed generally weaker binding than the pyridinones.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
PH-797804	Mitogen-activated protein kinase 14	IC 50 (nM)	5.8	N/A	N/A	Details