title: Benzo[d]imidazole inhibitors of Coactivator Associated Arginine Methyltransferase 1 (CARM1)--Hit to Lead studies.
abstract: Hit to Lead optimization and SAR development led to the identification of the potent and selective benzo[d]imidazole inhibitor (17b) of Co-activator Associated Arginine Methyltransferase (CARM1).
authors.affiliation: Bristol-Myers Squibb Pharmaceutical Research and Development, Princeton, NJ 08543, USA. Honghe.wan@bms.com
authors.forename: Honghe
authors.initials: H
authors.lastname: Wan
authors.forename: Tram
authors.initials: T
authors.lastname: Huynh
authors.forename: Suhong
authors.initials: S
authors.lastname: Pang
authors.forename: Jieping
authors.initials: J
authors.lastname: Geng
authors.forename: Wayne
authors.initials: W
authors.lastname: Vaccaro
authors.forename: Michael A
authors.initials: MA
authors.lastname: Poss
authors.forename: George L
authors.initials: GL
authors.lastname: Trainor
authors.forename: Matthew V
authors.initials: MV
authors.lastname: Lorenzi
authors.forename: Marco
authors.initials: M
authors.lastname: Gottardis
authors.forename: Lata
authors.initials: L
authors.lastname: Jayaraman
authors.forename: Ashok V
authors.initials: AV
authors.lastname: Purandare
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D001562:Benzimidazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D010880:Piperidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D011484:Protein-Arginine N-Methyltransferases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D001562:Benzimidazoles; D004791:Enzyme Inhibitors; D010880:Piperidines; D011484:Protein-Arginine N-Methyltransferases; C119966:coactivator-associated arginine methyltransferase 1