PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 22607682-3 2012 Library preparation of related analogs allowed the establishment of additional SAR understanding and in particular the requirement for a key hydrogen bond donor motif at the 4-position of the phenyl ring in compounds such as indole 19. indole 225-231 sarcosine dehydrogenase Homo sapiens 79-82 23681056-5 2013 With the aid of co-crystal structures of two discovered inhibitors (compounds 19 and 25) with BACE1, we explored the SAR around the indole and aryl groups, and obtained several BACE1 inhibitors about 1,000-fold more potent than the initial fragment hit. indole 132-138 sarcosine dehydrogenase Homo sapiens 117-120 18308566-1 2008 We report herein the SAR studies of a series of indole- and indolizine-glyoxylamides that demonstrate substantial in vitro anti-proliferative activities against cancer cell lines, including multidrug resistance (MDR) phenotypes. indole 48-54 sarcosine dehydrogenase Homo sapiens 21-24 22104146-2 2012 Development of SAR at the C2 position of indole lead 1, a palm site inhibitor of HCV NS5B polymerase (NS5B IC(50)=0.053muM, replicon EC(50)=4.8muM), is described. indole 41-47 sarcosine dehydrogenase Homo sapiens 15-18 20074949-1 2010 SAR studies at the N(1)-position of allosteric indole-based HCV NS5B inhibitors has led to the discovery of acetamide derivatives with good cellular potency in subgenomic replicons (EC(50) <200 nM). indole 47-53 sarcosine dehydrogenase Homo sapiens 0-3 19914828-3 2010 SAR studies focused on the discovery of novel alicyclic moieties appended to an indole core to optimize potency, physical properties and off-target activities. indole 80-86 sarcosine dehydrogenase Homo sapiens 0-3 19914828-4 2010 Subsequent SAR on the N-benzyl substituent of the indole led to the discovery of compound 39 (AM679) which showed potent inhibition of leukotrienes in human blood and in a rodent bronchoalvelolar lavage (BAL) challenge model. indole 50-56 sarcosine dehydrogenase Homo sapiens 11-14 19769332-4 2009 Systematic replacement of each of the unfused carbon atoms in the phenyl ring of the indole moiety by a nitrogen atom provided four different azaindole derivatives that displayed a clear SAR for antiviral activity and all of which displayed marked improvements in pharmaceutical properties. indole 85-91 sarcosine dehydrogenase Homo sapiens 187-190 17512197-0 2007 Synthesis and SAR of selective benzothiophene, benzofuran, and indole-based peroxisome proliferator-activated receptor delta agonists. indole 63-69 sarcosine dehydrogenase Homo sapiens 14-17 17512197-4 2007 Further elucidation of the SAR led to the identification of benzofuran and indole based templates. indole 75-81 sarcosine dehydrogenase Homo sapiens 27-30 15546707-1 2004 Part 1: SAR studies of the 7-position of the indole ring. indole 45-51 sarcosine dehydrogenase Homo sapiens 8-11 15186849-3 2004 A SAR study was carried out by modification of the substitutions on the indole and benzene rings. indole 72-78 sarcosine dehydrogenase Homo sapiens 2-5 12729661-2 2003 The synthesis and SAR of indolizine, indole and pyrazolopyridine based compounds are now described. indole 37-43 sarcosine dehydrogenase Homo sapiens 18-21 31303995-2 2019 SAR exploration revealed that 5-Cl and the sulfonyl side chain of the indole scaffold are crucial for anti-RSV activity. indole 70-76 sarcosine dehydrogenase Homo sapiens 0-3