Understanding of molecular substructures that contribute to hERG K + channel blockade: Synthesis and biological evaluation of E-4031 analogues

ChemMedChem

Volumn 7, Issue 1, 2012, Pages 107-113

  Vilums, Maris ^a   Overman, Jeroen ^a   Klaasse, Elisabeth ^a   Scheel, Olaf ^b   Brussee, Johannes ^a   Ijzerman, Adriaan P ^a  

^a LEIDEN UNIVERSITY   (Netherlands)

^b Cytocentrics AG   (Germany)

Author keywords

E 4031; HERG; Ion channels; Patch clamp assay; Radioligand binding; Structure activity relationships

Indexed keywords

(1 PHENETHYLPIPERIDIN 4 YL)(PHENYL)METHANONE; (4 PHENETHYLPIPERAZIN 1 YL)(PHENYL)METHANONE; 1 [2 (6 METHYL 2 PYRIDYL)ETHYL] 4 (4 METHYLSULFONYLAMINOBENZOYL)PIPERIDINE; 4 (4 CHLOROBENZOYL) 1 METHYL 1 PHENETHYLPIPERIDINIUM IODIDE; 4 BENZYL 1 PHENETHYLPIPERIDINE; CARBONYL DERIVATIVE; NITROGEN; OXYGEN; POTASSIUM CHANNEL BLOCKING AGENT; POTASSIUM CHANNEL HERG; RADIOLIGAND; UNCLASSIFIED DRUG;

ARTICLE; BINDING AFFINITY; CARDIOTOXICITY; CONTROLLED STUDY; DRUG ACTIVITY; DRUG BINDING; DRUG STRUCTURE; DRUG SYNTHESIS; HEART ARRHYTHMIA; PATCH CLAMP; PRIORITY JOURNAL; STRUCTURE ACTIVITY RELATION; SUDDEN DEATH;

ANTI-ARRHYTHMIA AGENTS; ARRHYTHMIAS, CARDIAC; ETHER-A-GO-GO POTASSIUM CHANNELS; HEK293 CELLS; HUMANS; PIPERIDINES; PYRIDINES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84555186707     PISSN: 18607179     EISSN: 18607187     Source Type: Journal    
DOI: 10.1002/cmdc.201100366     Document Type: Article

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