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Ref Type Journal Article
PMID (29456795)
Authors Lu B, Shen X, Zhang L, Liu D, Zhang C, Cao J, Shen R, Zhang J, Wang D, Wan H, Xu Z, Ho MH, Zhang M, Zhang L, He F, Tao W
Title Discovery of EBI-2511: A Highly Potent and Orally Active EZH2 Inhibitor for the Treatment of Non-Hodgkin's Lymphoma.
Journal Vol Issue Date Pages Journal Short Title
ACS medicinal chemistry letters 9 2 2018 Feb 08 98-102 ACS Med Chem Lett
URL
Abstract Text A novel series of benzofuran derived EZH2 inhibitors were discovered through a scaffold hopping approach based on the clinical compound of EPZ-6438. Further rational structure-activity relationship exploration and optimization led to the discovery of more potent EZH2 inhibitors with oral bioavailability in mice and rats. A lead compound EBI-2511 (compound 34) demonstrated excellent in vivo efficacy in Pfeiffer tumor Xenograft models in mouse and is under preclinical development for the treatment of cancers associated with EZH2 mutations.

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Molecular Profile Treatment Approach
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
EBI-2511 EBI-2511 0 0
Drug Name Trade Name Synonyms Drug Classes Drug Description
EBI-2511 EBI2511|EBI 2511 EZH2 inhibitor 20 EBI-2511 is an inhibitor of EZH2, potentially leading to inhibition of tumor growth and tumor regression (PMID: 29456795).
Gene Variant Impact Protein Effect Variant Description Associated with drug Resistance
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References