Identification of (R)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-1-tosylpiperidine-2-carboxamide, ML277, as a novel, potent and selective K(v)7.1 (KCNQ1) potassium channel activator

A high-throughput screen utilizing a depolarization-triggered thallium influx through KCNQ1 channels was developed and used to screen the MLSMR collection of over 300,000 compounds. An iterative medicinal chemistry approach was initiated and from this effort, ML277 was identified as a potent activat...

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Główni autorzy: Mattmann, Margrith E., Yu, Haibo, Lin, Zhihong, Xu, Kaiping, Huang, Xiaofang, Long, Shunyou, Wu, Meng, McManus, Owen B., Engers, Darren W., Le, Uyen M., Li, Min, Lindsley, Craig W., Hopkins, Corey R.
Format: Artigo
Język:Inglês
Wydane: 2012
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Article
Dostęp online:https://ncbi.nlm.nih.gov/pmc/articles/PMC3433560/
https://ncbi.nlm.nih.gov/pubmed/22910039
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2012.07.060
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