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Updated: Dec 25, 2025
Author Spotlight: Advancing Cellular and Protein Engineering to Control Biological Functions and Develop Novel Therapies
Published on: September 27, 2024
Discovery of 2-aminoimidazopyridine adenosine A(2A) receptor antagonists
Brian F McGuinness1, Andrew G Cole, Guizhen Dong
1Ligand Pharmaceuticals, Inc., 3000 Eastpark Boulevard, Cranbury, NJ 08512, USA. bmcguinness@venenumbiodesign.com
Abstract:
A novel series of adenosine A(2A) receptor antagonists was identified by high-throughput screening of an encoded combinatorial compound collection. The initial hits were optimized for A(2A) binding affinity, A(1) selectivity, and in vitro microsomal stability generating orally available 2-aminoimidazo[4,5-b]pyridine-based A(2A) antagonist leads.
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