Abstract：
:The explored kinome was extended with broad profiling using the DiscoveRx and Millipore assay panels. The analysis of the profiling of 3368 selected inhibitors on 456 kinases in the DiscoveRx format delivered several insights. First, the coverage depended on the threshold of the selectivity parameter. Second, the relation between hit confirmation rates and inhibitor selectivity showed unexpectedly that higher selectivity can increase the likelihood of false positives. Third, comparing the coverage of a focused to that of a random library showed that the design based on a maximum number of scaffolds was superior to a limited number of scaffolds. Therefore, selective compounds can be used in target validation, enable the jumpstarting of new kinase drug discovery projects, and chart new biological space via phenotypic screening.
journal_name
Drug Discov Todayjournal_title
Drug discovery todayauthors
Jacoby E,Tresadern G,Bembenek S,Wroblowski B,Buyck C,Neefs JM,Rassokhin D,Poncelet A,Hunt J,van Vlijmen Hdoi
10.1016/j.drudis.2015.01.002subject
Has Abstractpub_date
2015-06-01 00:00:00pages
652-8issue
6eissn
1359-6446issn
1878-5832pii
S1359-6446(15)00020-3journal_volume
20pub_type
杂志文章,评审abstract：:Identification and validation of viable targets is an important first step in drug discovery and new methods, and integrated approaches are continuously explored to improve the discovery rate and exploration of new drug targets. An in silico machine learning method, support vector machines, has been explored as a new ...
journal_title：Drug discovery today
pub_type： 杂志文章,评审
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journal_title：Drug discovery today
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journal_title：Drug discovery today
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journal_title：Drug discovery today
pub_type： 杂志文章,评审
doi：10.1016/j.drudis.2009.09.014
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abstract：:Denosumab (Dmab) was the first monoclonal antibody (mAb) approved for the treatment of osteoporosis. It blocks the receptor activator for nuclear factor κB ligand (RANKL) and acts as a potent antiresorptive agent. In contrast to classic antiresorptive agents, Dmab treatment leads to a progressive increase in bone mass...
journal_title：Drug discovery today
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journal_title：Drug discovery today
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journal_title：Drug discovery today
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journal_title：Drug discovery today
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journal_title：Drug discovery today
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journal_title：Drug discovery today
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journal_title：Drug discovery today
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journal_title：Drug discovery today
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journal_title：Drug discovery today
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journal_title：Drug discovery today
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journal_title：Drug discovery today
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journal_title：Drug discovery today
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journal_title：Drug discovery today
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journal_title：Drug discovery today
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journal_title：Drug discovery today
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journal_title：Drug discovery today
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journal_title：Drug discovery today
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journal_title：Drug discovery today
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journal_title：Drug discovery today
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journal_title：Drug discovery today
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journal_title：Drug discovery today
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journal_title：Drug discovery today
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journal_title：Drug discovery today
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journal_title：Drug discovery today
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