Discovery of AMG 369, a Thiazolo[5,4-b]pyridine Agonist of S1P1 and S1P5.
Thousand Oaks, United States. In Acs Med Chem Lett, 2011
These efforts resulted in the discovery of 1-(3-fluoro-4-(5-(1-phenylcyclopropyl)thiazolo-[5,4-b]pyridin-2-yl)benzyl)azetidine-3-carboxylic acid (5d, AMG 369), a potent dual S1P1/S1P5 agonist with limited activity at S1P3 and no activity at S1P2/S1P4.
Identification of a Novel Agonist of the Sphingosine 1-phosphate Receptor 4 (S1P4)
Bethesda, United States. In Unknown Journal, 0001
ML248 activates S1P4 receptor with a half maximal effective concentration (EC50) of 37.7 nM–79.1 nM, and is inactive as an agonist against other members of the receptor family, with EC50s > 25 μM against S1P1, S1P2, and S1P3 receptors, and an EC50 of 2.1 μM against the S1P5 receptor.