title: Aminomethyl tetrahydronaphthalene biphenyl carboxamide MCH-R1 antagonists--Increasing selectivity over hERG.
abstract: Aminomethyl tetrahydronaphthalene biphenyl carboxamide MCH-R1 antagonists with greater selectivity over hERG were identified. SAR studies addressing two distinct alternatives for structural modifications leading to improve hERG selectivity are described.
authors.affiliation: Procter & Gamble Pharmaceuticals, 8700 Mason-Montgomery Road, Mason, OH 45039, USA.
authors.forename: Kenneth M
authors.initials: KM
authors.lastname: Meyers
authors.forename: Nicholas
authors.initials: N
authors.lastname: Kim
authors.forename: José L
authors.initials: JL
authors.lastname: Méndez-Andino
authors.forename: X Eric
authors.initials: XE
authors.lastname: Hu
authors.forename: Rashid N
authors.initials: RN
authors.lastname: Mumin
authors.forename: Sean R
authors.initials: SR
authors.lastname: Klopfenstein
authors.forename: John A
authors.initials: JA
authors.lastname: Wos
authors.forename: Maria C
authors.initials: MC
authors.lastname: Mitchell
authors.forename: Jennifer L
authors.initials: JL
authors.lastname: Paris
authors.forename: David C
authors.initials: DC
authors.lastname: Ackley
authors.forename: Jerry K
authors.initials: JK
authors.lastname: Holbert
authors.forename: Scott W
authors.initials: SW
authors.lastname: Mittelstadt
authors.forename: Ofer
authors.initials: O
authors.lastname: Reizes
mesh_terms: D001713:Biphenyl Compounds / Q000138:chemical synthesis / Q000494:pharmacology*; D000072237:ERG1 Potassium Channel; D004873:Ergolines / Q000494:pharmacology; D051638:Ether-A-Go-Go Potassium Channels / Q000187:drug effects*; D006801:Humans; D007202:Indicators and Reagents; D008803:Mianserin / Q000494:pharmacology; D009281:Naphthalenes / Q000138:chemical synthesis / Q000494:pharmacology*; D026902:Potassium Channel Blockers / Q000494:pharmacology*; D044405:Receptor, Serotonin, 5-HT2C / Q000187:drug effects; D017481:Receptors, Somatostatin / Q000037:antagonists & inhibitors*; D012702:Serotonin Antagonists / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D001713:Biphenyl Compounds; D000072237:ERG1 Potassium Channel; D004873:Ergolines; D051638:Ether-A-Go-Go Potassium Channels; D007202:Indicators and Reagents; C000606913:KCNH2 protein, human; C103263:MCHR1 protein, human; D009281:Naphthalenes; D026902:Potassium Channel Blockers; D044405:Receptor, Serotonin, 5-HT2C; D017481:Receptors, Somatostatin; D012702:Serotonin Antagonists; C518530:aminomethyl tetrahydronaphthalene biphenyl carboxamide; D008803:Mianserin; C031649:mesulergine