Title : Structure-activity relationships of quinoxaline-based 5-HT3A and 5-HT3AB receptor-selective ligands.

Pub. Date : 2013 Jun

PMID : 23640722






3 Functional Relationships(s)
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1 During a recent fragment screen, 2-chloro-3-(4-methylpiperazin-1-yl)quinoxaline (VUF10166) was identified as a ligand that displays an 83-fold difference in [(3)H]granisetron binding affinity between 5-HT3A and 5-HT3AB receptors. 2-chloro-(4-methylpiperazine-1-yl)quinoxaline 5-hydroxytryptamine receptor 3A Homo sapiens
2 During a recent fragment screen, 2-chloro-3-(4-methylpiperazin-1-yl)quinoxaline (VUF10166) was identified as a ligand that displays an 83-fold difference in [(3)H]granisetron binding affinity between 5-HT3A and 5-HT3AB receptors. 2-chloro-(4-methylpiperazine-1-yl)quinoxaline 5-hydroxytryptamine receptor 3A Homo sapiens
3 Fragment hit exploration, initiated from VUF10166 and 3-(4-methylpiperazin-1-yl)quinoxalin-2-ol, resulted in a series of compounds with higher affinity at either 5-HT3A or 5-HT3AB receptors. 2-chloro-(4-methylpiperazine-1-yl)quinoxaline 5-hydroxytryptamine receptor 3A Homo sapiens