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Discovery and characterization of NVP-QAV680, a potent and selective CRTh2 receptor antagonist suitable for clinical testing in allergic diseases

journal contribution
posted on 2023-06-08, 19:29 authored by David A Sandham, Nicola Arnold, Heinrich Aschauer, Kamlesh Bala, Lucy Barker, Lyndon Brown, Zarin Brown, David Budd, Brian Cox, Cerys Docx, Gerald Dubois, Nicholas Duggan, Karen England, Brian Everatt, Marcus Furegati, Edward Hall, Frank Kalthoff, Anna King, Catherine J Leblanc, Jodie Manini, Josef Meingassner, Rachael Profit, Alfred Schmidt, Jennifer Simmons, Bindi Sohal, Rowan Stringer, Matthew Thomas, Katharine L Turner, Christoph Walker, Simon J Watson, John Westwick, Jennifer Willis, Gareth Williams, Caroline Wilson
Optimization of a 7-azaindole-3-acetic acid CRTh2 receptor antagonist chemotype derived from high throughput screening furnished a highly selective compound NVP-QAV680 with low nM functional potency for inhibition of CRTh2 driven human eosinophil and Th2 lymphocyte activation in vitro. The molecule exhibited good oral bioavailability in the rat, combined with efficacy in rodent CRTh2-dependent mechanistic and allergic disease models and was suitable for clinical development.

History

Publication status

  • Published

Journal

Bioorganic and Medicinal Chemistry

ISSN

0968-0896

Publisher

Elsevier

Issue

21

Volume

21

Page range

6582-6591

Department affiliated with

  • Chemistry Publications

Full text available

  • No

Peer reviewed?

  • Yes

Legacy Posted Date

2015-01-12

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