| pubmed-article:17201416 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:17201416 | lifeskim:mentions | umls-concept:C0020792 | lld:lifeskim |
| pubmed-article:17201416 | lifeskim:mentions | umls-concept:C0076552 | lld:lifeskim |
| pubmed-article:17201416 | lifeskim:mentions | umls-concept:C0231491 | lld:lifeskim |
| pubmed-article:17201416 | pubmed:issue | 1 | lld:pubmed |
| pubmed-article:17201416 | pubmed:dateCreated | 2007-1-4 | lld:pubmed |
| pubmed-article:17201416 | pubmed:abstractText | The metabolism of our prototypical thrombin receptor antagonist 1, Ki = 2.7 nM, was studied and three major metabolites (2, 4, and 5) were found. The structures of the metabolites were verified independently by synthesis. Compound 4 was shown to be a potent antagonist of the thrombin receptor with a Ki = 11 nM. Additionally, compound 4 showed a 3-fold improvement in potency with respect to 1 in an agonist-induced ex-vivo platelet aggregation assay in cynomolgus monkeys after oral administration; this activity was sustained with 60% inhibition observed at 24 h post-dose. Compound 4 was highly active in functional assays and showed excellent oral bioavailability in rats and monkeys. Compound 4 showed a superior rat enzyme induction profile relative to compound 1, allowing it to replace compound 1 as a development candidate. | lld:pubmed |
| pubmed-article:17201416 | pubmed:language | eng | lld:pubmed |
| pubmed-article:17201416 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:17201416 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:17201416 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:17201416 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:17201416 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:17201416 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:17201416 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:17201416 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:17201416 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:17201416 | pubmed:month | Jan | lld:pubmed |
| pubmed-article:17201416 | pubmed:issn | 0022-2623 | lld:pubmed |
| pubmed-article:17201416 | pubmed:author | pubmed-author:OrrV BVB | lld:pubmed |
| pubmed-article:17201416 | pubmed:author | pubmed-author:HsiehYunsheng... | lld:pubmed |
| pubmed-article:17201416 | pubmed:author | pubmed-author:Chackalamanni... | lld:pubmed |
| pubmed-article:17201416 | pubmed:author | pubmed-author:GreenleeWilli... | lld:pubmed |
| pubmed-article:17201416 | pubmed:author | pubmed-author:LauJaniceJ | lld:pubmed |
| pubmed-article:17201416 | pubmed:author | pubmed-author:KaoGraceG | lld:pubmed |
| pubmed-article:17201416 | pubmed:author | pubmed-author:BryantMatthew... | lld:pubmed |
| pubmed-article:17201416 | pubmed:author | pubmed-author:FosterCarolyn... | lld:pubmed |
| pubmed-article:17201416 | pubmed:author | pubmed-author:YanXiaX | lld:pubmed |
| pubmed-article:17201416 | pubmed:author | pubmed-author:PalamandaJair... | lld:pubmed |
| pubmed-article:17201416 | pubmed:author | pubmed-author:ChintalaMadhu... | lld:pubmed |
| pubmed-article:17201416 | pubmed:author | pubmed-author:Smith-TorhanA... | lld:pubmed |
| pubmed-article:17201416 | pubmed:author | pubmed-author:AhnHo-SamHS | lld:pubmed |
| pubmed-article:17201416 | pubmed:author | pubmed-author:BoykowGeorgeG | lld:pubmed |
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| pubmed-article:17201416 | pubmed:author | pubmed-author:DollerDarioD | lld:pubmed |
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| pubmed-article:17201416 | pubmed:author | pubmed-author:TsaiHsinganH | lld:pubmed |
| pubmed-article:17201416 | pubmed:author | pubmed-author:Agans-Fantuzz... | lld:pubmed |
| pubmed-article:17201416 | pubmed:author | pubmed-author:ClasbyMartin... | lld:pubmed |
| pubmed-article:17201416 | pubmed:author | pubmed-author:EagenKeithK | lld:pubmed |
| pubmed-article:17201416 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:17201416 | pubmed:day | 11 | lld:pubmed |
| pubmed-article:17201416 | pubmed:volume | 50 | lld:pubmed |
| pubmed-article:17201416 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:17201416 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:17201416 | pubmed:pagination | 129-38 | lld:pubmed |
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| pubmed-article:17201416 | pubmed:meshHeading | pubmed-meshheading:17201416... | lld:pubmed |
| pubmed-article:17201416 | pubmed:meshHeading | pubmed-meshheading:17201416... | lld:pubmed |
| pubmed-article:17201416 | pubmed:meshHeading | pubmed-meshheading:17201416... | lld:pubmed |
| pubmed-article:17201416 | pubmed:meshHeading | pubmed-meshheading:17201416... | lld:pubmed |
| pubmed-article:17201416 | pubmed:year | 2007 | lld:pubmed |
| pubmed-article:17201416 | pubmed:articleTitle | Metabolism-based identification of a potent thrombin receptor antagonist. | lld:pubmed |
| pubmed-article:17201416 | pubmed:affiliation | Central Nervous System and Cardiovascular Chemical Research, Schering-Plough Research Institute, Kenilworth, New Jersey 07033, USA. | lld:pubmed |
| pubmed-article:17201416 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:17201416 | pubmed:publicationType | In Vitro | lld:pubmed |
| http://linkedlifedata.com/r... | http://linkedlifedata.com/r... | pubmed-article:17201416 | lld:chembl |
