Ontology highlight
ABSTRACT:
SUBMITTER: Cheung YY
PROVIDER: S-EPMC3530927 | biostudies-literature | 2012 Aug
REPOSITORIES: biostudies-literature
Journal of medicinal chemistry 20120726 15
A potent and selective inhibitor of KCNQ2, (S)-5 (ML252, IC(50) = 69 nM), was discovered after a high-throughput screen of the MLPCN library was performed. SAR studies revealed a small structural change (ethyl group to hydrogen) caused a functional shift from antagonist to agonist activity (37, EC(50) = 170 nM), suggesting an interaction at a critical site for controlling gating of KCNQ2 channels. ...[more]