title: Identification of non-amidine inhibitors of acid-sensing ion channel-3 (ASIC3).
abstract: A series of benzothiophene methyl amines were examined in an effort to identify non-amidine chemotypes with reduced polypharmacology from existing leads with the goal of finding potent ASIC3 channel blockers to advance the therapeutic evaluation of ASIC3 inhibition.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, Sumneytown Pike, PO Box 4, West Point, PA 19486, USA. scott_d_kuduk@merck.com
authors.forename: Scott D
authors.initials: SD
authors.lastname: Kuduk
authors.forename: Ronald K
authors.initials: RK
authors.lastname: Chang
authors.forename: Christina N
authors.initials: CN
authors.lastname: Di Marco
authors.forename: Robert M
authors.initials: RM
authors.lastname: Dipardo
authors.forename: Sean P
authors.initials: SP
authors.lastname: Cook
authors.forename: Matthew J
authors.initials: MJ
authors.lastname: Cato
authors.forename: Aneta
authors.initials: A
authors.lastname: Jovanovska
authors.forename: Mark O
authors.initials: MO
authors.lastname: Urban
authors.forename: Michael
authors.initials: M
authors.lastname: Leitl
authors.forename: Robert H
authors.initials: RH
authors.lastname: Spencer
authors.forename: Stefanie A
authors.initials: SA
authors.lastname: Kane
authors.forename: George D
authors.initials: GD
authors.lastname: Hartman
authors.forename: Mark T
authors.initials: MT
authors.lastname: Bilodeau
mesh_terms: D062565:Acid Sensing Ion Channels; D000578:Amidines / Q000737:chemistry; D000584:Amiloride / Q000737:chemistry; D000818:Animals; D009419:Nerve Tissue Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D051381:Rats; D026941:Sodium Channel Blockers / Q000737:chemistry* / Q000494:pharmacology; D015222:Sodium Channels / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: C568269:ASIC3 protein, rat; D062565:Acid Sensing Ion Channels; D000578:Amidines; D009419:Nerve Tissue Proteins; D026941:Sodium Channel Blockers; D015222:Sodium Channels; D000584:Amiloride