| pubmed-article:20541404 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:20541404 | lifeskim:mentions | umls-concept:C0054874 | lld:lifeskim |
| pubmed-article:20541404 | lifeskim:mentions | umls-concept:C0559956 | lld:lifeskim |
| pubmed-article:20541404 | lifeskim:mentions | umls-concept:C0243077 | lld:lifeskim |
| pubmed-article:20541404 | pubmed:issue | 14 | lld:pubmed |
| pubmed-article:20541404 | pubmed:dateCreated | 2010-7-8 | lld:pubmed |
| pubmed-article:20541404 | pubmed:abstractText | A pyridazin-4-one fragment 4 (hCatS IC(50)=170 microM) discovered through Tethering was modeled into cathepsin S and predicted to overlap in S2 with the tetrahydropyridinepyrazole core of a previously disclosed series of CatS inhibitors. This fragment served as a template to design pyridazin-3-one 12 (hCatS IC(50)=430 nM), which also incorporates P3 and P5 binding elements. A crystal structure of 12 bound to Cys25Ser CatS led to the synthesis of the potent diazinone isomers 22 (hCatS IC(50)=60 nM) and 27 (hCatS IC(50)=40 nM). | lld:pubmed |
| pubmed-article:20541404 | pubmed:language | eng | lld:pubmed |
| pubmed-article:20541404 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:20541404 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:20541404 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:20541404 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:20541404 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:20541404 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:20541404 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:20541404 | pubmed:month | Jul | lld:pubmed |
| pubmed-article:20541404 | pubmed:issn | 1464-3405 | lld:pubmed |
| pubmed-article:20541404 | pubmed:author | pubmed-author:KarlssonLarsL | lld:pubmed |
| pubmed-article:20541404 | pubmed:author | pubmed-author:ZhuJianJ | lld:pubmed |
| pubmed-article:20541404 | pubmed:author | pubmed-author:ThurmondRobin... | lld:pubmed |
| pubmed-article:20541404 | pubmed:author | pubmed-author:PurkeyHans... | lld:pubmed |
| pubmed-article:20541404 | pubmed:author | pubmed-author:StakerBart... | lld:pubmed |
| pubmed-article:20541404 | pubmed:author | pubmed-author:GebauerDamara... | lld:pubmed |
| pubmed-article:20541404 | pubmed:author | pubmed-author:ChoongIngrid... | lld:pubmed |
| pubmed-article:20541404 | pubmed:author | pubmed-author:BurdettMatthe... | lld:pubmed |
| pubmed-article:20541404 | pubmed:author | pubmed-author:EdwardsJames... | lld:pubmed |
| pubmed-article:20541404 | pubmed:author | pubmed-author:SunSiquanS | lld:pubmed |
| pubmed-article:20541404 | pubmed:author | pubmed-author:GuYinY | lld:pubmed |
| pubmed-article:20541404 | pubmed:author | pubmed-author:BembenekScott... | lld:pubmed |
| pubmed-article:20541404 | pubmed:author | pubmed-author:AmeriksMichae... | lld:pubmed |
| pubmed-article:20541404 | pubmed:copyrightInfo | 2010 Elsevier Ltd. All rights reserved. | lld:pubmed |
| pubmed-article:20541404 | pubmed:issnType | Electronic | lld:pubmed |
| pubmed-article:20541404 | pubmed:day | 15 | lld:pubmed |
| pubmed-article:20541404 | pubmed:volume | 20 | lld:pubmed |
| pubmed-article:20541404 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:20541404 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:20541404 | pubmed:pagination | 4060-4 | lld:pubmed |
| pubmed-article:20541404 | pubmed:meshHeading | pubmed-meshheading:20541404... | lld:pubmed |
| pubmed-article:20541404 | pubmed:meshHeading | pubmed-meshheading:20541404... | lld:pubmed |
| pubmed-article:20541404 | pubmed:meshHeading | pubmed-meshheading:20541404... | lld:pubmed |
| pubmed-article:20541404 | pubmed:meshHeading | pubmed-meshheading:20541404... | lld:pubmed |
| pubmed-article:20541404 | pubmed:meshHeading | pubmed-meshheading:20541404... | lld:pubmed |
| pubmed-article:20541404 | pubmed:meshHeading | pubmed-meshheading:20541404... | lld:pubmed |
| pubmed-article:20541404 | pubmed:year | 2010 | lld:pubmed |
| pubmed-article:20541404 | pubmed:articleTitle | Diazinones as P2 replacements for pyrazole-based cathepsin S inhibitors. | lld:pubmed |
| pubmed-article:20541404 | pubmed:affiliation | Johnson & Johnson Pharmaceutical Research & Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA. mameriks@its.jnj.com | lld:pubmed |
| pubmed-article:20541404 | pubmed:publicationType | Journal Article | lld:pubmed |
| http://linkedlifedata.com/r... | http://linkedlifedata.com/r... | pubmed-article:20541404 | lld:chembl |
