Structure-activity relationships of triazolopyridine oxazole p38 inhibitors: identification of candidates for clinical development.

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McClure KF, Letavic MA, Kalgutkar AS, Gabel CA, Audoly L, Barberia JT, Braganza JF, Carter D, Carty TJ, Cortina SR, Dombroski MA, Donahue KM, Elliott NC, Gibbons CP, Jordan CK, Kuperman AV, Labasi JM, Laliberte RE, McCoy JM, Naiman BM, Nelson KL, Nguyen HT, Peese KM, Sweeney FJ, Taylor TJ, Trebino CE, Abramov YA, Laird ER, Volberg WA, Zhou J, Bach J, Lombardo F

Structure-activity relationships of triazolopyridine oxazole p38 inhibitors: identification of candidates for clinical development.

Bioorg Med Chem Lett. 2006 Aug 15;16(16):4339-44. Epub 2006 Jun 12.

PubMed ID
16759861 [ View in PubMed
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Abstract

The synthesis, structure-activity relationship, in vivo activity, and metabolic profile for a series of triazolopyridine-oxazole based p38 inhibitors are described. The deficiencies of the lead structure in the series, CP-808844, were overcome by changes to the C4 aryl group and the triazole side-chain culminating in the identification of several potential clinical candidates.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
TriazolopyridineMitogen-activated protein kinase 14IC 50 (nM)57.230Details