Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
3
pubmed:dateCreated
2008-2-5
pubmed:abstractText
This article is focusing on further optimization of previously described hydroxy ethylamine (HEA) BACE-1 inhibitors obtained from a focused library with the support of X-ray crystallography. Optimization of the non-prime side of our inhibitors and introduction of a 6-membered sultam substituent binding to Asn-294 as well as a fluorine in the C-2 position led to derivatives with nanomolar potency in cell-based assays.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Feb
pubmed:issn
1464-3405
pubmed:author
pubmed-author:BeswickPaulP, pubmed-author:CharrierNicolasN, pubmed-author:ClarkeBrianB, pubmed-author:DemontEmmanuelE, pubmed-author:DingwallColinC, pubmed-author:DunsdonRachelR, pubmed-author:FallerAndrewA, pubmed-author:GleaveRobertR, pubmed-author:HawkinsJulieJ, pubmed-author:HussainIshrutI, pubmed-author:JohnsonChristopher NCN, pubmed-author:MacPhersonDavidD, pubmed-author:MaileGrahamG, pubmed-author:MaticoRosalieR, pubmed-author:MilnerPeterP, pubmed-author:MosleyJulieJ, pubmed-author:NaylorAlanA, pubmed-author:O'BrienAlistairA, pubmed-author:RedshawSallyS, pubmed-author:RiddellDavidD, pubmed-author:RowlandPaulP, pubmed-author:SkidmoreJohnJ, pubmed-author:SmithKathrine JKJ, pubmed-author:SoleilVirginieV, pubmed-author:StanwayStevenS, pubmed-author:StempGeoffreyG, pubmed-author:StuartAlistairA, pubmed-author:SweitzerSharonS, pubmed-author:TheobaldPamP, pubmed-author:VeseyDavidD, pubmed-author:WalterDaryl SDS, pubmed-author:WardJohnJ, pubmed-author:WayneGarethG
pubmed:issnType
Electronic
pubmed:day
1
pubmed:volume
18
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
1022-6
pubmed:dateRevised
2009-11-19
pubmed:meshHeading
pubmed:year
2008
pubmed:articleTitle
BACE-1 inhibitors part 3: identification of hydroxy ethylamines (HEAs) with nanomolar potency in cells.
pubmed:affiliation
Neurology and Gastrointestinal Centre of Excellence for Drug Discovery, GlaxoSmithKline R&D, New Frontiers Science Park, Third Avenue, Harlow, Essex, CM19 5AW, UK.
pubmed:publicationType
Journal Article