All Outputs (2)

Discovery of fevipiprant (NVP-QAW039), a potent and selective DP2 receptor antagonist for treatment of asthma (2017)
Journal Article
Sandham, D. A., Barker, L., Brown, L., Brown, Z., Budd, D., Charlton, S. J., …Willis, J. (2017). Discovery of fevipiprant (NVP-QAW039), a potent and selective DP2 receptor antagonist for treatment of asthma. ACS Medicinal Chemistry Letters, 8(5), 582-586. https://doi.org/10.1021/acsmedchemlett.7b00157

Further optimization of an initial DP2 receptor antagonist clinical candidate NVPQAV680 led to the discovery of a follow-up molecule 2-(2-methyl-1-(4-(methylsulfonyl)-2- (trifluoromethyl)benzyl)-1H-pyrrolo[2,3-b]pyridin-3-yl)acetic acid (compound 11,... Read More about Discovery of fevipiprant (NVP-QAW039), a potent and selective DP2 receptor antagonist for treatment of asthma.

Uncoupling the Structure–Activity Relationships of β2 Adrenergic Receptor Ligands from Membrane Binding (2016)
Journal Article
Dickson, C. J., Hornak, V., Velez-Vega, C., McKay, D. J., Reilly, J., Sandham, D. A., …Duca, J. S. (2016). Uncoupling the Structure–Activity Relationships of β2 Adrenergic Receptor Ligands from Membrane Binding. Journal of Medicinal Chemistry, 59(12), 5780-5789. https://doi.org/10.1021/acs.jmedchem.6b00358

Ligand binding to membrane proteins may be significantly influenced by the interaction of ligands with the membrane. In particular, the microscopic ligand concentration within the membrane surface solvation layer may exceed that in bulk solvent, resu... Read More about Uncoupling the Structure–Activity Relationships of β2 Adrenergic Receptor Ligands from Membrane Binding.