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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 WilsonOptimization 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 ChemistryISSN
0968-0896Publisher
ElsevierExternal DOI
Issue
21Volume
21Page range
6582-6591Department affiliated with
- Chemistry Publications
Full text available
- No
Peer reviewed?
- Yes
Legacy Posted Date
2015-01-12Usage metrics
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