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From UTP to AR-C118925, the discovery of a potent non nucleotide antagonist of the P2Y2 receptor

Kindon, Nicholas; Davis, Andrew; Dougall, Iain; Dixon, John; Johnson, Timothy; Walters, Iain; Thom, Steve; McKechnie, Kenneth; Meghani, Premji; Stocks, Michael


Andrew Davis

Iain Dougall

John Dixon

Timothy Johnson

Iain Walters

Steve Thom

Kenneth McKechnie

Premji Meghani

Professor of Medicinal Chemistry and Drug Discovery


The G protein-coupled P2Y2 receptor, activated by ATP and UTP has been reported as a potential drug target for a wide range of important clinical conditions, such as tumor metastasis, kidney disorders, and in the treatment of inflammatory conditions. However, pharmacological studies on this receptor have been impeded by the limited reported availability of stable, potent and selective P2Y2R antagonists. This article describes the design and synthesis of AR-C118925, a potent and selective non-nucleotide antagonist of the P2Y2 receptor discovered using the endogenous P2Y2R agonist UTP as the chemical starting point.


Kindon, N., Davis, A., Dougall, I., Dixon, J., Johnson, T., Walters, I., …Stocks, M. (2017). From UTP to AR-C118925, the discovery of a potent non nucleotide antagonist of the P2Y2 receptor. Bioorganic and Medicinal Chemistry Letters, 27(21), 4849-4853.

Journal Article Type Article
Acceptance Date Sep 20, 2017
Online Publication Date Sep 21, 2017
Publication Date Nov 1, 2017
Deposit Date Sep 27, 2017
Journal Bioorganic & Medicinal Chemistry Letters
Electronic ISSN 1464-3405
Publisher Elsevier
Peer Reviewed Peer Reviewed
Volume 27
Issue 21
Pages 4849-4853
Keywords P2Y2; Purinergic; AR-C118925; P2; Antagonist
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