title: Highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.
abstract: We report the SAR around a series of 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase. 2-Aminophenethyl analogs demonstrate excellent potency but moderate kinase selectivity, while 2-aminobenzyl analogs that fill the Ala571 subpocket exhibit good inhibition activity and excellent kinase selectivity.
authors: Pfizer Global Research & Development, Michigan Laboratories, Ann Arbor, MI 48105, USA. napowell@comcast.net
authors: Noel A
authors: NA
authors: Powell
authors: Jennifer K
authors: JK
authors: Hoffman
authors: Fred L
authors: FL
authors: Ciske
authors: Michael D
authors: MD
authors: Kaufman
authors: Jeffrey T
authors: JT
authors: Kohrt
authors: John
authors: J
authors: Quin
authors: Derek J
authors: DJ
authors: Sheehan
authors: Amy
authors: A
authors: Delaney
authors: Sangita M
authors: SM
authors: Baxi
authors: Cornel
authors: C
authors: Catana
authors: Patrick
authors: P
authors: McConnell
authors: Jeff
authors: J
authors: Ohren
authors: Lisa A
authors: LA
authors: Perrin
authors: Jeremy J
authors: JJ
authors: Edmunds
mesh_terms: D000577:Amides / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D006801:Humans; D051379:Mice; D047428:Protein Kinase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D011743:Pyrimidines / Q000737:chemistry* / Q000494:pharmacology*; D020794:Receptor Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D013379:Substrate Specificity
chemical_list: D000577:Amides; D047428:Protein Kinase Inhibitors; D011743:Pyrimidines; C017205:2,4-diaminopyrimidine; D020794:Receptor Protein-Tyrosine Kinases; C084944:TYRO3 protein, human