1490436-00-4Relevant academic research and scientific papers
Thieno[2,3-b]pyridines as negative allosteric modulators of metabotropic GluR5 receptors: Hit-to-lead optimization
Nógrádi, Katalin,Wágner, Gábor,Domány, Gy?rgy,Bobok, Amrita,Magdó, Ildikó,Kiss, Béla,Kolok, Sándor,Fónagy, Katalin,Gyertyán, István,Háda, Viktor,Kóti, János,Gál, Krisztina,Farkas, Sándor,Keseru, Gy?rgy M.,Greiner, István,Szombathelyi, Zsolt
, p. 3845 - 3849 (2014/09/03)
An HTS campaign of our corporate compound library resulted in thieno[2,3-b]pyridines derivative hits with mGluR5 negative allosteric modulator effects. During the hit-to-lead development our objective was to improve affinity, and to keep the ligand efficiency values at an acceptable level. After different modifications of the linker resulted in a 2-sulfonyl-thieno[2,3-b] pyridines derivative, which fulfilled the lead criteria.
