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Bioorg Med Chem Lett. 2010 Sep 15;20(18):5426-30. doi: 10.1016/j.bmcl.2010.07.108. Epub 2010 Jul 29.

Pyrido pyrimidinones as selective agonists of the high affinity niacin receptor GPR109A: optimization of in vitro activity.

Author information

1
Pharma Research, F. Hoffmann-La Roche Ltd, 4070 Basel, Switzerland.

Abstract

Pyrido pyrimidinones are selective agonists of the human high affinity niacin receptor GPR109A (HM74A). They show no activity on the highly homologous low affinity receptor GPR109B (HM74). Starting from a high throughput screening hit the in vitro activity of the pyrido pyrimidinones was significantly improved providing lead compounds suitable for further optimization.

PMID:
20724150
DOI:
10.1016/j.bmcl.2010.07.108
[Indexed for MEDLINE]

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