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Journal of Medicinal Chemistry|August 10, 2018
A Fragment-Derived Clinical Candidate for Antagonism of X-Linked and Cellular Inhibitor of Apoptosis Proteins: 1-(6-[(4-Fluorophenyl)methyl]-5-(hydroxymethyl)-3,3-dimethyl-1 H,2 H,3 H-pyrrolo[3,2- b]pyridin-1-yl)-2-[(2 R,5 R)-5-methyl-2-([(3R)-3-methylmorpholin-4-yl]methyl)piperazin-1-yl]ethan-1-one (ASTX660)Christopher N Johnson, Jong Sook Ahn, Ildiko M Buck, et al.Journal of Medicinal Chemistry|April 12, 2019
Structure-Activity and Structure-Conformation Relationships of Aryl Propionic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1/Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1/NRF2) Protein-Protein InteractionTom D Heightman, James F Callahan, Elisabetta Chiarparin, et al.ACS Chemical Biology|August 30, 2016
Structure of the Epigenetic Oncogene MMSET and Inhibition by N-Alkyl Sinefungin DerivativesDominic Tisi, Elisabetta Chiarparin, Emiliano Tamanini, et al.Journal of Medicinal Chemistry|February 8, 2022
Discovery of a Potent and Selective ATAD2 Bromodomain Inhibitor with Antiproliferative Activity in Breast Cancer ModelsJon J Winter-Holt, Catherine Bardelle, Elisabetta Chiarparin, et al.Nature Communications|February 27, 2025
Integrating fragment-based screening with targeted protein degradation and genetic rescue to explore eIF4E functionSwee Y Sharp, Marianna Martella, Sabrina D'Agostino, et al.Journal of Medicinal Chemistry|March 11, 2024
Development of a Series of Pyrrolopyridone MAT2A InhibitorsStephen J Atkinson, Sharan K Bagal, Argyrides Argyrou, et al.ACS Chemical Biology|October 19, 2018
Development of a Novel B-Cell Lymphoma 6 (BCL6) PROTAC To Provide Insight into Small Molecule Targeting of BCL6William McCoull, Tony Cheung, Erica Anderson, et al.Communications Biology|May 13, 2024
Metabolism-driven in vitro/in vivo disconnect of an oral ERɑ VHL-PROTACThomas G Hayhow, Beth Williamson, Mandy Lawson, et al.Nature Communications|December 19, 2018
Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemiaAdriana E Tron, Matthew A Belmonte, Ammar Adam, et al.Journal of Medicinal Chemistry|July 31, 2024
Discovery and <i>In Vivo</i> Efficacy of AZ-PRMT5i-1, a Novel PRMT5 Inhibitor with High MTA CooperativityJames M Smith, Bernard Barlaam, David Beattie, et al.Pageof 5