Title : Improvement of hERG-ROMK index of spirocyclic ROMK inhibitors through scaffold optimization and incorporation of novel pharmacophores.

Pub. Date : 2017 Jun 1

PMID : 28431879






2 Functional Relationships(s)
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1 Efforts aimed at decreasing hERG affinity within the series led to the discovery of multiple novel right-hand pharmacophores including 3-methoxythiadiazole, 2-methoxypyrimidine, and pyridazinone. 2-phenyl-3(2H)-pyridazinone ETS transcription factor ERG Homo sapiens
2 The most promising candidate is pyridazinone analog 32 that showed an improved functional hERG/ROMK potency ratio and preclinical PK profile. 2-phenyl-3(2H)-pyridazinone ETS transcription factor ERG Homo sapiens