{"database":"LINCS","file_versions":[{"headers":{"Content-Type":["application/json"]},"body":{"files":{"Other":["http://lincsportal.ccs.miami.edu/dcic/api/download?path=LINCS_Data/HMS_LINCS&file=LDS-1149.tar.gz"]},"type":"primary"},"statusCode":"OK","statusCodeValue":200}],"scores":null,"additional":{"omics_type":["Multiomics"],"submitter":["Mindy Davis"],"funding":["1U54HG006097-01"],"technology_type":["KINOMEscan","Fluorescence 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LINCS (Harvard Medical School)"],"sample_protocol":["The KINOMEscan assay platform is based on a competition binding assay that is run for a compound of interest against each of a panel of 442 kinases. The assay has three components: a kinase-tagged phage, a test compound, and an immobilized ligand that the compound competes with to displace the kinase. The amount of kinase bound to the immobilized ligand is determined using quantitative PCR of the DNA tag. Kd values (nM) reported for each compound were determined using 11 serial threefold dilutions of test compound and a DMSO control. A null result means no inhibition of kinase binding to the ligand in the presence of the compound and low Kd means strong inhibition."],"repository":["LINCS"],"data_protocol":[""],"pubmed_abstract":["We tested the interaction of 72 kinase inhibitors with 442 kinases covering >80% of the human catalytic protein kinome. Our data show that, as a class, type II inhibitors are more selective than type I inhibitors, but that there are important exceptions to this trend. The data further illustrate that selective inhibitors have been developed against the majority of kinases targeted by the compounds tested. Analysis of the interaction patterns reveals a class of 'group-selective' inhibitors broadly active against a single subfamily of kinases, but selective outside that subfamily. The data set suggests compounds to use as tools to study kinases for which no dedicated inhibitors exist. It also provides a foundation for further exploring kinase inhibitor biology and toxicity, as well as for studying the structural basis of the observed interaction patterns. Our findings will help to realize the direct enabling potential of genomics for drug development and basic research about cellular signaling."],"pubmed_title":["Comprehensive analysis of kinase inhibitor selectivity."],"pubmed_authors":["Davis Mindy I MI, Hunt Jeremy P JP, Herrgard Sanna S, Ciceri Pietro P, Wodicka Lisa M LM, Pallares Gabriel G, Hocker Michael M, Treiber Daniel K DK, Zarrinkar Patrick P PP"],"additional_accession":[]},"is_claimable":false,"name":"TKI-258 KINOMEscan","description":"-","dates":{"publication":"2016-06-03","updated":"2016-06-03"},"accession":"LDS-1149","cross_references":{"pubmed":["22037378"]}}