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http://purl.uniprot.org/citations/38228402http://www.w3.org/1999/02/22-rdf-syntax-ns#typehttp://purl.uniprot.org/core/Journal_Citation
http://purl.uniprot.org/citations/38228402http://www.w3.org/2000/01/rdf-schema#comment"Interleukin-1 receptor-associated kinase 4 (IRAK4) plays a critical role in innate inflammatory processes. Here, we describe the discovery of two clinical candidate IRAK4 inhibitors, BAY1834845 (zabedosertib) and BAY1830839, starting from a high-throughput screening hit derived from Bayer's compound library. By exploiting binding site features distinct to IRAK4 using an in-house docking model, liabilities of the original hit could surprisingly be overcome to confer both candidates with a unique combination of good potency and selectivity. Favorable DMPK profiles and activity in animal inflammation models led to the selection of these two compounds for clinical development in patients."xsd:string
http://purl.uniprot.org/citations/38228402http://purl.org/dc/terms/identifier"doi:10.1021/acs.jmedchem.3c01714"xsd:string
http://purl.uniprot.org/citations/38228402http://purl.uniprot.org/core/author"Lange M."xsd:string
http://purl.uniprot.org/citations/38228402http://purl.uniprot.org/core/author"Sutter A."xsd:string
http://purl.uniprot.org/citations/38228402http://purl.uniprot.org/core/author"Schmidt N."xsd:string
http://purl.uniprot.org/citations/38228402http://purl.uniprot.org/core/author"Eberspacher U."xsd:string
http://purl.uniprot.org/citations/38228402http://purl.uniprot.org/core/author"Nubbemeyer R."xsd:string
http://purl.uniprot.org/citations/38228402http://purl.uniprot.org/core/author"Peters M."xsd:string
http://purl.uniprot.org/citations/38228402http://purl.uniprot.org/core/author"Steuber H."xsd:string
http://purl.uniprot.org/citations/38228402http://purl.uniprot.org/core/author"Ring S."xsd:string
http://purl.uniprot.org/citations/38228402http://purl.uniprot.org/core/author"Schafer M."xsd:string
http://purl.uniprot.org/citations/38228402http://purl.uniprot.org/core/author"Siebeneicher H."xsd:string
http://purl.uniprot.org/citations/38228402http://purl.uniprot.org/core/author"Zollner T.M."xsd:string
http://purl.uniprot.org/citations/38228402http://purl.uniprot.org/core/author"Gunther J."xsd:string
http://purl.uniprot.org/citations/38228402http://purl.uniprot.org/core/author"Denner K."xsd:string
http://purl.uniprot.org/citations/38228402http://purl.uniprot.org/core/author"Bomer U."xsd:string
http://purl.uniprot.org/citations/38228402http://purl.uniprot.org/core/author"Steinmeyer A."xsd:string
http://purl.uniprot.org/citations/38228402http://purl.uniprot.org/core/author"Rausch A."xsd:string
http://purl.uniprot.org/citations/38228402http://purl.uniprot.org/core/author"Wengner A.M."xsd:string
http://purl.uniprot.org/citations/38228402http://purl.uniprot.org/core/author"Platzek J."xsd:string
http://purl.uniprot.org/citations/38228402http://purl.uniprot.org/core/author"Himmel H."xsd:string
http://purl.uniprot.org/citations/38228402http://purl.uniprot.org/core/author"Bothe U."xsd:string
http://purl.uniprot.org/citations/38228402http://purl.uniprot.org/core/author"Guimond N."xsd:string
http://purl.uniprot.org/citations/38228402http://purl.uniprot.org/core/author"Terebesi I."xsd:string