期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 54, 期 7, 页码 2255-2265出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm101423y
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The development of a new series of p38 alpha inhibitors resulted in the identification of two clinical candidates, one of which was advanced into a phase 2 clinical study for rheumatoid arthritis. The original lead, an lck inhibitor that also potently inhibited p38a, was a screening hit from our kinase inhibitor library. This manuscript describes the optimization of the lead to p38-selective examples with good pharmacokinetic properties.
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