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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
21
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pubmed:dateCreated |
2008-11-7
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pubmed:abstractText |
The identification of a new class of potent and selective ROCK-II inhibitors is presented. Compound 5 (SR-3677) had an IC 50 of approximately 3 nM in enzyme and cell based assays and had an off-target hit rate of 1.4% against 353 kinases, and inhibited only 3 out of 70 nonkinase enzymes and receptors. Pharmacology studies showed that 5 was efficacious in both, increasing ex vivo aqueous humor outflow in porcine eyes and inhibiting myosin light chain phosphorylation.
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pubmed:grant |
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Nov
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pubmed:issn |
1520-4804
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pubmed:author |
pubmed-author:CameronMichael DMD,
pubmed-author:FengYangboY,
pubmed-author:GriffinEvelynE,
pubmed-author:InoueToshihiroT,
pubmed-author:JooFF,
pubmed-author:LograssoPhilipP,
pubmed-author:RaoP VasanthPV,
pubmed-author:RuizClaudiaC,
pubmed-author:SchürerStephan CSC,
pubmed-author:SchröterThomasT,
pubmed-author:WeiserAmieeA,
pubmed-author:XieZ RZR
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pubmed:issnType |
Electronic
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pubmed:day |
13
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pubmed:volume |
51
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
6642-5
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pubmed:meshHeading |
pubmed-meshheading:18834107-Amides,
pubmed-meshheading:18834107-Animals,
pubmed-meshheading:18834107-Dioxanes,
pubmed-meshheading:18834107-Drug Evaluation, Preclinical,
pubmed-meshheading:18834107-Models, Molecular,
pubmed-meshheading:18834107-Molecular Structure,
pubmed-meshheading:18834107-Protein Kinase Inhibitors,
pubmed-meshheading:18834107-Pyrazoles,
pubmed-meshheading:18834107-Rats,
pubmed-meshheading:18834107-Structure-Activity Relationship,
pubmed-meshheading:18834107-Swine,
pubmed-meshheading:18834107-rho-Associated Kinases
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pubmed:year |
2008
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pubmed:articleTitle |
Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors.
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pubmed:affiliation |
Department of Molecular Therapeutics, and Translational Research Institute, The Scripps Research Institute, Florida, 5353 Parkside Drive, Jupiter, Florida 33458, USA.
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pubmed:publicationType |
Journal Article,
Research Support, N.I.H., Extramural
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