In Retrospect: Root-Cause Analysis of Structure–Activity Relationships in IRAK4 Inhibitor Zimlovisertib (PF-06650833)
Author:
Affiliation:
1. Medicine Design, Pfizer Inc., 445 Eastern Point Rd, Groton, Connecticut 06340, United States
2. Inflammation and Immunology Research Unit, Pfizer Inc., 1 Portland Street, Cambridge, Massachusetts 02139, United States
Publisher
American Chemical Society (ACS)
Link
https://pubs.acs.org/doi/pdf/10.1021/acsmedchemlett.4c00036
Reference23 articles.
1. Discovery of Clinical Candidate 1-{[(2S,3S,4S)-3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl]methoxy}-7-methoxyisoquinoline-6-carboxamide (PF-06650833), a Potent, Selective Inhibitor of Interleukin-1 Receptor Associated Kinase 4 (IRAK4), by Fragment-Based Drug Design
2. Safety, tolerability, pharmacokinetics, and pharmacodynamics of PF-06650833, a selective interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor, in single and multiple ascending dose randomized phase 1 studies in healthy subjects
3. The Interleukin‐1 Receptor–Associated Kinase 4 Inhibitor PF‐06650833 Blocks Inflammation in Preclinical Models of Rheumatic Disease and in Humans Enrolled in a Randomized Clinical Trial
4. IRAK-4 and MyD88 deficiencies impair IgM responses against T-independent bacterial antigens
5. A Critical Role for the Innate Immune Signaling Molecule IRAK-4 in T Cell Activation
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