A uHTS approach for the identification of beta-adrenoceptor ligands.

Tasler S, Baumgartner R, Aschenbrenner A, Ammendola A, Wolf K, Wieber T, Schachtner J, Blisse M, Quotschalla U, Ney P


4SC AG, Planegg-Martinsried, Germany. UCB pharma S. A., Brain l'Alleud, Belgium.

Bioorg Med Chem Lett. 2010;20(11):3399-404.

Using a vHTS based on a pharmacophore alignment on known beta3-adrenoceptor ligands, a set of intriguing beta-adrenoceptor ligands was identified, optimization of which resulted in a selective and potent human beta2-AR antagonist.

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