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Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

GNE-886

Target

CECR2

Action

inhibitors

Mechanism

CECR2 inhibitors(CECR2 histone acetyl-lysine reader inhibitors)

Therapeutic Areas-

Active Indication-

Inactive Indication-

Originator Organization

Genentech, Inc.

Active Organization-

Inactive Organization

Genentech, Inc.

License Organization-

Drug Highest PhasePendingPreclinical

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC28H30N6O3

InChIKeyZKIRTFGYQVXNGL-UHFFFAOYSA-N

CAS Registry2101957-05-3

Author: Neiss, Arianne ; Jayaram, Hariharan ; Murray, Jeremy ; Romero, F. Anthony ; Duplessis, Martin ; Zhu, Xiaoqin ; Cochran, Andrea G. ; Wang, Yongyun ; Jiang, Ying ; Joshi, Shivangi ; Pardo, Eneida ; Côté, Alexandre ; Flynn, E. Megan ; Tang, Yong ; Albrecht, Brian K. ; Magnuson, Steven R. ; Kiefer, James R. ; Tsui, Vickie ; Taylor, Alexander M. ; Nasveschuk, Christopher G. ; Crawford, Terry D. ; Wang, Shumei ; Bellon, Steve ; Zawadzke, Laura ; Audia, James E. ; Cummings, Richard T. ; Wang, Jian ; Huang, Hon-Ren ; Sandy, Peter ; Burdick, Daniel J. ; Hewitt, Michael ; Sims, Robert J. ; Xu, Zhaowu ; Bommi-Reddy, Archana

The biological function of bromodomains, epigenetic readers of acetylated lysine residues, remains largely unknown. Herein we report our efforts to discover a potent and selective inhibitor of the bromodomain of cat eye syndrome chromosome region candidate 2 (CECR2). Screening of our internal medicinal chemistry collection led to the identification of a pyrrolopyridone chemical lead, and subsequent structure-based drug design led to a potent and selective CECR2 bromodomain inhibitor (GNE-886) suitable for use as an in vitro tool compound.

100 Deals associated with GNE-886

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