pubmed-article:21251828 | rdf:type | pubmed:Citation | lld:pubmed |
pubmed-article:21251828 | lifeskim:mentions | umls-concept:C0243077 | lld:lifeskim |
pubmed-article:21251828 | lifeskim:mentions | umls-concept:C1705938 | lld:lifeskim |
pubmed-article:21251828 | lifeskim:mentions | umls-concept:C1527178 | lld:lifeskim |
pubmed-article:21251828 | pubmed:issue | 4 | lld:pubmed |
pubmed-article:21251828 | pubmed:dateCreated | 2011-2-7 | lld:pubmed |
pubmed-article:21251828 | pubmed:abstractText | Rho kinase is an important target implicated in a variety of cardiovascular diseases. Herein, we report the optimisation of the fragment derived ATP-competitive ROCK inhibitors 1 and 2 into lead compound 14A. The initial goal of improving ROCK-I potency relative to 1, whilst maintaining a good PK profile, was achieved through removal of the aminoisoquinoline basic centre. Lead 14A was equipotent against both ROCK-I and ROCK-II, showed good in vivo efficacy in the spontaneous hypertensive rat model, and was further optimised to demonstrate the scope for improving selectivity over PKA versus hydroxy Fasudil 3. | lld:pubmed |
pubmed-article:21251828 | pubmed:language | eng | lld:pubmed |
pubmed-article:21251828 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:21251828 | pubmed:citationSubset | IM | lld:pubmed |
pubmed-article:21251828 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:21251828 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:21251828 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:21251828 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:21251828 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:21251828 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:21251828 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:21251828 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:21251828 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:21251828 | pubmed:status | MEDLINE | lld:pubmed |
pubmed-article:21251828 | pubmed:month | Feb | lld:pubmed |
pubmed-article:21251828 | pubmed:issn | 1464-3405 | lld:pubmed |
pubmed-article:21251828 | pubmed:author | pubmed-author:JonesPhilP | lld:pubmed |
pubmed-article:21251828 | pubmed:author | pubmed-author:WrightJaneJ | lld:pubmed |
pubmed-article:21251828 | pubmed:author | pubmed-author:YorkMarkM | lld:pubmed |
pubmed-article:21251828 | pubmed:author | pubmed-author:SherborneBrad... | lld:pubmed |
pubmed-article:21251828 | pubmed:author | pubmed-author:RayPeterP | lld:pubmed |
pubmed-article:21251828 | pubmed:author | pubmed-author:SherryLorcanL | lld:pubmed |
pubmed-article:21251828 | pubmed:author | pubmed-author:EpemoluOlaO | lld:pubmed |
pubmed-article:21251828 | pubmed:author | pubmed-author:FletcherDanD | lld:pubmed |
pubmed-article:21251828 | pubmed:author | pubmed-author:MorphyRichard... | lld:pubmed |
pubmed-article:21251828 | pubmed:author | pubmed-author:WestwoodPaulP | lld:pubmed |
pubmed-article:21251828 | pubmed:author | pubmed-author:AdamJuliaJ | lld:pubmed |
pubmed-article:21251828 | pubmed:author | pubmed-author:BlackDarceyD | lld:pubmed |
pubmed-article:21251828 | pubmed:author | pubmed-author:BoucharensSyl... | lld:pubmed |
pubmed-article:21251828 | pubmed:author | pubmed-author:HuggettMargar... | lld:pubmed |
pubmed-article:21251828 | pubmed:author | pubmed-author:BrownAngus... | lld:pubmed |
pubmed-article:21251828 | pubmed:author | pubmed-author:LaatsStevenS | lld:pubmed |
pubmed-article:21251828 | pubmed:author | pubmed-author:LyonsAmandaA | lld:pubmed |
pubmed-article:21251828 | pubmed:author | pubmed-author:de ManJosJ | lld:pubmed |
pubmed-article:21251828 | pubmed:author | pubmed-author:StratenNicole... | lld:pubmed |
pubmed-article:21251828 | pubmed:copyrightInfo | Copyright © 2010 Elsevier Ltd. All rights reserved. | lld:pubmed |
pubmed-article:21251828 | pubmed:issnType | Electronic | lld:pubmed |
pubmed-article:21251828 | pubmed:day | 15 | lld:pubmed |
pubmed-article:21251828 | pubmed:volume | 21 | lld:pubmed |
pubmed-article:21251828 | pubmed:owner | NLM | lld:pubmed |
pubmed-article:21251828 | pubmed:authorsComplete | Y | lld:pubmed |
pubmed-article:21251828 | pubmed:pagination | 1084-8 | lld:pubmed |
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pubmed-article:21251828 | pubmed:year | 2011 | lld:pubmed |
pubmed-article:21251828 | pubmed:articleTitle | Optimisation of 6-substituted isoquinolin-1-amine based ROCK-I inhibitors. | lld:pubmed |
pubmed-article:21251828 | pubmed:affiliation | Discovery Research, MSD, Newhouse, Lanarkshire, ML1 5SH Scotland, UK. p.ray@btinternet.com | lld:pubmed |
pubmed-article:21251828 | pubmed:publicationType | Journal Article | lld:pubmed |
http://linkedlifedata.com/r... | http://linkedlifedata.com/r... | pubmed-article:21251828 | lld:chembl |