Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88L265P Diffuse Large B-Cell Lymphoma.

doi:10.1021/acs.jmedchem.7b01290

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Article

Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88L265P Diffuse Large B-Cell Lymphoma.

Journal of medicinal chemistry - 28 Dec 2017

Scott James S, Degorce Sébastien L, Anjum Rana, Culshaw Janet, Davies Robert D M, Davies Nichola L, Dillman Keith S, Dowling James E, Drew Lisa, Ferguson Andrew D, Groombridge Sam D, Halsall Christopher T, Hudson Julian A, Lamont Scott, Lindsay Nicola A, Marden Stacey K, Mayo Michele F, Pease J Elizabeth, Perkins David R, Pink Jennifer H, Robb Graeme R, Rosen Alan, Shen Minhui, McWhirter Claire, Wu Dedong

Abstract excerpt

Herein we report the optimization of a series of pyrrolopyrimidine inhibitors of interleukin-1 receptor associated kinase 4 (IRAK4) using X-ray crystal structures and structure based design to identify and optimize our scaffold. Compound 28 demonstrated a favorable physicochemical and kinase selectivity profile and was identified as a promising in vivo tool with which to explore the role of IRAK4 inhibition in...

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PMID: 29172502
DOI: 10.1021/acs.jmedchem.7b01290

Genes

IRAK4
BTK

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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