221675-35-0Relevant articles and documents
Substituted indoles as selective protease activated receptor 4 (PAR-4) antagonists: Discovery and SAR of ML354
Wen, Wandong,Young, Summer E.,Duvernay, Matthew T.,Schulte, Michael L.,Nance, Kellie D.,Melancon, Bruce J.,Engers, Julie,Locuson, Charles W.,Wood, Michael R.,Daniels, J. Scott,Wu, Wenjun,Lindsley, Craig W.,Hamm, Heidi E.,Stauffer, Shaun R.
, p. 4708 - 4713 (2014)
Herein we report the discovery and SAR of an indole-based protease activated receptor-4 (PAR-4) antagonist scaffold derived from a similarity search of the Vanderbilt HTS collection, leading to MLPCN probe ML354 (VU0099704). Using a novel PAC-1 fluorescent αIIbβ3 activation assay this probe molecule antagonist was found to have an IC50of 140 nM for PAR-4 with 71-fold selectivity versus PAR-1 (PAR-1IC50= 10 μM).
HETEROCYCLIC COMPOUNDS AS PAD INHIBITORS
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Paragraph 000295, (2019/04/16)
Heterocyclic compounds of Formula (I), (II), and (III) are described herein along with their polymorphs, stereoisomers, prodrugs, solvates, co-crystals, intermediates, pharmaceutically acceptable salts, and metabolites thereof. The compounds described herein, their polymorphs, stereoisomers, prodrugs, solvates, co-crystals, intermediates, pharmaceutically acceptable salts, and metabolites thereof are PAD4 inhibitors and may be useful in the treatment of various disorders, for example rheumatoid arthritis, vasculitis, systemic lupus erythematosis, cutaneous lupus erythematosis, ulcerative colitis, cancer, cystic fibrosis, asthma, multiple sclerosis and psoriasis.
Synthesis, biological evaluation and molecular modeling of a novel series of 7-azaindole based tri-heterocyclic compounds as potent CDK2/Cyclin E inhibitors
Baltus, Christine B.,Jorda, Radek,Marot, Christophe,Berka, Karel,Bazgier, Václav,Kry?tof, Vladimír,Prié, Gildas,Viaud-Massuard, Marie-Claude
, p. 701 - 719 (2016/01/09)
From four molecules, inspired by the structural features of fascaplysin, with an interesting potential to inhibit cyclin-dependent kinases (CDKs), we designed a new series of tri-heterocyclic derivatives based on 1H-pyrrolo[2,3-b]pyridine (7-azaindole) an