{"id":"https://openalex.org/W2610073351","doi":"https://doi.org/10.1177/2472555217695080","title":"A High-Throughput Method for Measuring Drug Residence Time Using the Transcreener ADP Assay","display_name":"A High-Throughput Method for Measuring Drug Residence Time Using the Transcreener ADP Assay","publication_year":2017,"publication_date":"2017-05-26","ids":{"openalex":"https://openalex.org/W2610073351","doi":"https://doi.org/10.1177/2472555217695080","mag":"2610073351","pmid":"https://pubmed.ncbi.nlm.nih.gov/28346107"},"language":"en","primary_location":{"id":"doi:10.1177/2472555217695080","doi":"https://doi.org/10.1177/2472555217695080","is_oa":true,"landing_page_url":"https://doi.org/10.1177/2472555217695080","pdf_url":"https://journals.sagepub.com/doi/pdf/10.1177/2472555217695080","source":{"id":"https://openalex.org/S4387277810","display_name":"SLAS DISCOVERY","issn_l":"2472-5552","issn":["2472-5552","2472-5560"],"is_oa":false,"is_in_doaj":true,"is_core":true,"listed_in":["cwts-core","doaj","dongbi-b","jufo-1","ki-jl-1","medline","norway-1","oarl","poland-40"],"host_organization":"https://openalex.org/P4310320990","host_organization_name":"Elsevier BV","host_organization_lineage":["https://openalex.org/P4310320990"],"host_organization_lineage_names":["Elsevier BV"],"type":"journal"},"license":"cc-by-nc-nd","license_id":"https://openalex.org/licenses/cc-by-nc-nd","version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"SLAS Discovery","raw_type":"journal-article"},"volume":null,"type":"article","is_traditional":true,"indexed_in":["crossref","doaj","pubmed"],"open_access":{"is_oa":true,"oa_status":"hybrid","oa_url":"https://journals.sagepub.com/doi/pdf/10.1177/2472555217695080","any_repository_has_fulltext":false},"authorships":[{"author_position":"first","author":{"id":"https://openalex.org/A5042211627","display_name":"Meera Ajeet Kumar","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210162091","display_name":"Bellbrook Labs (United States)","ror":"https://ror.org/05eewjw07","country_code":"US","type":"company","lineage":["https://openalex.org/I4210162091"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Meera Kumar","raw_affiliation_strings":["1 BellBrook Labs, Madison, WI, USA","BellBrook Labs, Madison, WI, USA"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"1 BellBrook Labs, Madison, WI, USA","institution_ids":["https://openalex.org/I4210162091"]},{"raw_affiliation_string":"BellBrook Labs, Madison, WI, USA","institution_ids":["https://openalex.org/I4210162091"]}]},{"author_position":"last","author":{"id":"https://openalex.org/A5048290877","display_name":"Robert G. Lowery","orcid":"https://orcid.org/0009-0009-5322-7165","observed_orcids":["https://orcid.org/0009-0009-5322-7165"]},"institutions":[{"id":"https://openalex.org/I4210162091","display_name":"Bellbrook Labs (United States)","ror":"https://ror.org/05eewjw07","country_code":"US","type":"company","lineage":["https://openalex.org/I4210162091"]}],"countries":["US"],"is_corresponding":true,"raw_author_name":"Robert G. Lowery","raw_affiliation_strings":["1 BellBrook Labs, Madison, WI, USA","BellBrook Labs, Madison, WI, USA"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"1 BellBrook Labs, Madison, WI, USA","institution_ids":["https://openalex.org/I4210162091"]},{"raw_affiliation_string":"BellBrook Labs, Madison, WI, USA","institution_ids":["https://openalex.org/I4210162091"]}]}],"institutions":[],"countries_distinct_count":1,"institutions_distinct_count":1,"corresponding_author_ids":["https://openalex.org/A5048290877"],"corresponding_institution_ids":["https://openalex.org/I4210162091"],"apc_list":{"value":2070,"currency":"USD","value_usd":2070},"apc_paid":{"value":2070,"currency":"USD","value_usd":2070},"fwci":0.5909,"has_fulltext":true,"cited_by_count":27,"citation_normalized_percentile":{"value":0.64141311,"is_in_top_1_percent":false,"is_in_top_10_percent":false},"cited_by_percentile_year":{"min":88,"max":99},"biblio":{"volume":"22","issue":"7","first_page":"915","last_page":"922"},"is_retracted":false,"is_paratext":false,"is_xpac":false,"primary_topic":{"id":"https://openalex.org/T10211","display_name":"Computational Drug Discovery Methods","score":0.6654999852180481,"subfield":{"id":"https://openalex.org/subfields/3002","display_name":"Drug Discovery"},"field":{"id":"https://openalex.org/fields/30","display_name":"Pharmacology, Toxicology and Pharmaceutics"},"domain":{"id":"https://openalex.org/domains/1","display_name":"Life Sciences"}},"topics":[{"id":"https://openalex.org/T10211","display_name":"Computational Drug Discovery Methods","score":0.6654999852180481,"subfield":{"id":"https://openalex.org/subfields/3002","display_name":"Drug Discovery"},"field":{"id":"https://openalex.org/fields/30","display_name":"Pharmacology, Toxicology and Pharmaceutics"},"domain":{"id":"https://openalex.org/domains/1","display_name":"Life Sciences"}},{"id":"https://openalex.org/T10169","display_name":"Protein Kinase Regulation and GTPase Signaling","score":0.0544000007212162,"subfield":{"id":"https://openalex.org/subfields/1312","display_name":"Molecular Biology"},"field":{"id":"https://openalex.org/fields/13","display_name":"Biochemistry, Genetics and Molecular Biology"},"domain":{"id":"https://openalex.org/domains/1","display_name":"Life Sciences"}},{"id":"https://openalex.org/T12412","display_name":"Enzyme function and inhibition","score":0.037700001150369644,"subfield":{"id":"https://openalex.org/subfields/1312","display_name":"Molecular Biology"},"field":{"id":"https://openalex.org/fields/13","display_name":"Biochemistry, Genetics and Molecular Biology"},"domain":{"id":"https://openalex.org/domains/1","display_name":"Life Sciences"}}],"keywords":[{"id":"https://openalex.org/keywords/drug-residence-time","display_name":"drug residence time","score":0.9070000052452087},{"id":"https://openalex.org/keywords/dissociation-rate-constant","display_name":"dissociation rate constant","score":0.8240000009536743},{"id":"https://openalex.org/keywords/kinase-inhibitors","display_name":"kinase inhibitors","score":0.7200000286102295},{"id":"https://openalex.org/keywords/high-throughput-screening","display_name":"high-throughput screening","score":0.871999979019165},{"id":"https://openalex.org/keywords/epidermal-growth-factor-receptor","display_name":"epidermal growth factor receptor","score":0.8169999718666077},{"id":"https://openalex.org/keywords/c-abl","display_name":"c-Abl","score":0.8949999809265137},{"id":"https://openalex.org/keywords/aurora-kinases","display_name":"Aurora kinases","score":0.9959999918937683},{"id":"https://openalex.org/keywords/compound-prioritization","display_name":"compound prioritization","score":0.7770000100135803},{"id":"https://openalex.org/keywords/fluorescence-polarization","display_name":"fluorescence polarization","score":0.7940000295639038},{"id":"https://openalex.org/keywords/fluorescence-intensity","display_name":"fluorescence intensity","score":0.9020000100135803}],"concepts":[{"id":"https://openalex.org/C185592680","wikidata":"https://www.wikidata.org/wiki/Q2329","display_name":"Chemistry","level":0,"score":0.5903940796852112},{"id":"https://openalex.org/C184235292","wikidata":"https://www.wikidata.org/wiki/Q421851","display_name":"Kinase","level":2,"score":0.5772922039031982},{"id":"https://openalex.org/C96305047","wikidata":"https://www.wikidata.org/wiki/Q367473","display_name":"F\u00f6rster resonance energy transfer","level":3,"score":0.5466930270195007},{"id":"https://openalex.org/C74187038","wikidata":"https://www.wikidata.org/wiki/Q1418791","display_name":"Drug discovery","level":2,"score":0.5316762328147888},{"id":"https://openalex.org/C2775913793","wikidata":"https://www.wikidata.org/wiki/Q3030793","display_name":"Residence time (fluid dynamics)","level":2,"score":0.4903883934020996},{"id":"https://openalex.org/C2780035454","wikidata":"https://www.wikidata.org/wiki/Q8386","display_name":"Drug","level":2,"score":0.47654634714126587},{"id":"https://openalex.org/C111357860","wikidata":"https://www.wikidata.org/wiki/Q903807","display_name":"Fluorescence anisotropy","level":3,"score":0.4501308798789978},{"id":"https://openalex.org/C51323132","wikidata":"https://www.wikidata.org/wiki/Q626251","display_name":"High-throughput screening","level":2,"score":0.4408086836338043},{"id":"https://openalex.org/C12554922","wikidata":"https://www.wikidata.org/wiki/Q7100","display_name":"Biophysics","level":1,"score":0.3267281651496887},{"id":"https://openalex.org/C91881484","wikidata":"https://www.wikidata.org/wiki/Q191807","display_name":"Fluorescence","level":2,"score":0.29098501801490784},{"id":"https://openalex.org/C55493867","wikidata":"https://www.wikidata.org/wiki/Q7094","display_name":"Biochemistry","level":1,"score":0.2558135986328125},{"id":"https://openalex.org/C98274493","wikidata":"https://www.wikidata.org/wiki/Q128406","display_name":"Pharmacology","level":1,"score":0.25028955936431885},{"id":"https://openalex.org/C86803240","wikidata":"https://www.wikidata.org/wiki/Q420","display_name":"Biology","level":0,"score":0.1754056215286255},{"id":"https://openalex.org/C121332964","wikidata":"https://www.wikidata.org/wiki/Q413","display_name":"Physics","level":0,"score":0.09025654196739197},{"id":"https://openalex.org/C187320778","wikidata":"https://www.wikidata.org/wiki/Q1349130","display_name":"Geotechnical engineering","level":1,"score":0.0},{"id":"https://openalex.org/C41625074","wikidata":"https://www.wikidata.org/wiki/Q176088","display_name":"Membrane","level":2,"score":0.0},{"id":"https://openalex.org/C127413603","wikidata":"https://www.wikidata.org/wiki/Q11023","display_name":"Engineering","level":0,"score":0.0},{"id":"https://openalex.org/C62520636","wikidata":"https://www.wikidata.org/wiki/Q944","display_name":"Quantum mechanics","level":1,"score":0.0}],"mesh":[{"descriptor_ui":"D000244","descriptor_name":"Adenosine Diphosphate","qualifier_ui":"Q000378","qualifier_name":"metabolism","is_major_topic":false},{"descriptor_ui":"D001681","descriptor_name":"Biological Assay","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D006801","descriptor_name":"Humans","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D008024","descriptor_name":"Ligands","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D025181","descriptor_name":"ATP Synthetase Complexes","qualifier_ui":"Q000037","qualifier_name":"antagonists & inhibitors","is_major_topic":false},{"descriptor_ui":"D025181","descriptor_name":"ATP Synthetase Complexes","qualifier_ui":"Q000378","qualifier_name":"metabolism","is_major_topic":true},{"descriptor_ui":"D031541","descriptor_name":"Fluorescence Resonance Energy Transfer","qualifier_ui":"Q000379","qualifier_name":"methods","is_major_topic":false},{"descriptor_ui":"D047428","descriptor_name":"Protein Kinase Inhibitors","qualifier_ui":"Q000494","qualifier_name":"pharmacology","is_major_topic":false},{"descriptor_ui":"D057166","descriptor_name":"High-Throughput Screening Assays","qualifier_ui":"Q000379","qualifier_name":"methods","is_major_topic":false},{"descriptor_ui":"D066246","descriptor_name":"ErbB Receptors","qualifier_ui":"Q000378","qualifier_name":"metabolism","is_major_topic":false}],"locations_count":2,"locations":[{"id":"doi:10.1177/2472555217695080","doi":"https://doi.org/10.1177/2472555217695080","is_oa":true,"landing_page_url":"https://doi.org/10.1177/2472555217695080","pdf_url":"https://journals.sagepub.com/doi/pdf/10.1177/2472555217695080","source":{"id":"https://openalex.org/S4387277810","display_name":"SLAS DISCOVERY","issn_l":"2472-5552","issn":["2472-5552","2472-5560"],"is_oa":false,"is_in_doaj":true,"is_core":true,"listed_in":["cwts-core","doaj","dongbi-b","jufo-1","ki-jl-1","medline","norway-1","oarl","poland-40"],"host_organization":"https://openalex.org/P4310320990","host_organization_name":"Elsevier BV","host_organization_lineage":["https://openalex.org/P4310320990"],"host_organization_lineage_names":["Elsevier BV"],"type":"journal"},"license":"cc-by-nc-nd","license_id":"https://openalex.org/licenses/cc-by-nc-nd","version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"SLAS Discovery","raw_type":"journal-article"},{"id":"pmid:28346107","doi":null,"is_oa":false,"landing_page_url":"https://pubmed.ncbi.nlm.nih.gov/28346107","pdf_url":null,"source":{"id":"https://openalex.org/S4306525036","display_name":"PubMed","issn_l":null,"issn":null,"is_oa":false,"is_in_doaj":false,"is_core":false,"listed_in":[],"host_organization":"https://openalex.org/I1299303238","host_organization_name":"National Institutes of Health","host_organization_lineage":["https://openalex.org/I1299303238"],"host_organization_lineage_names":[],"type":"repository"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"SLAS discovery : advancing life sciences R & D","raw_type":"Journal Article"}],"best_oa_location":{"id":"doi:10.1177/2472555217695080","doi":"https://doi.org/10.1177/2472555217695080","is_oa":true,"landing_page_url":"https://doi.org/10.1177/2472555217695080","pdf_url":"https://journals.sagepub.com/doi/pdf/10.1177/2472555217695080","source":{"id":"https://openalex.org/S4387277810","display_name":"SLAS DISCOVERY","issn_l":"2472-5552","issn":["2472-5552","2472-5560"],"is_oa":false,"is_in_doaj":true,"is_core":true,"listed_in":["cwts-core","doaj","dongbi-b","jufo-1","ki-jl-1","medline","norway-1","oarl","poland-40"],"host_organization":"https://openalex.org/P4310320990","host_organization_name":"Elsevier BV","host_organization_lineage":["https://openalex.org/P4310320990"],"host_organization_lineage_names":["Elsevier BV"],"type":"journal"},"license":"cc-by-nc-nd","license_id":"https://openalex.org/licenses/cc-by-nc-nd","version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"SLAS Discovery","raw_type":"journal-article"},"sustainable_development_goals":[{"score":0.5683000087738037,"id":"https://metadata.un.org/sdg/3","display_name":"Good health and well-being"}],"study_designs":[],"awards":[],"funders":[],"has_content":{"grobid_xml":true,"pdf":true},"content_urls":{"pdf":"https://content.openalex.org/works/W2610073351.pdf","grobid_xml":"https://content.openalex.org/works/W2610073351.grobid-xml"},"referenced_works_count":21,"referenced_works":["https://openalex.org/W1526377515","https://openalex.org/W1967676836","https://openalex.org/W1997362383","https://openalex.org/W2000899552","https://openalex.org/W2003586687","https://openalex.org/W2005517577","https://openalex.org/W2025038506","https://openalex.org/W2030718808","https://openalex.org/W2040680919","https://openalex.org/W2073263185","https://openalex.org/W2093247413","https://openalex.org/W2106776993","https://openalex.org/W2120234899","https://openalex.org/W2128307445","https://openalex.org/W2138851777","https://openalex.org/W2146643640","https://openalex.org/W2207535250","https://openalex.org/W2412135520","https://openalex.org/W2567139825","https://openalex.org/W2917868259","https://openalex.org/W6639649577"],"related_works":["https://openalex.org/W2010497812","https://openalex.org/W2992557879","https://openalex.org/W2803500509","https://openalex.org/W1996773464","https://openalex.org/W2898157327","https://openalex.org/W3139510775","https://openalex.org/W1525851782","https://openalex.org/W2575009204","https://openalex.org/W4386726159","https://openalex.org/W2607348308"],"abstract_inverted_index":{"Analysis":[0],"of":[1,28,36,51,84,109,145,194],"drug\u2013target":[2],"residence":[3,122,195],"times":[4,123],"during":[5],"drug":[6,208],"development":[7],"can":[8,22],"result":[9],"in":[10,206],"improved":[11],"efficacy,":[12],"increased":[13],"therapeutic":[14],"window,":[15],"and":[16,136,139,176,203],"reduced":[17],"side":[18],"effects.":[19],"Residence":[20],"time":[21,196],"be":[23],"estimated":[24],"as":[25,100,112,197],"the":[26,29,94,107,113,129,142,166,192],"reciprocal":[27],"dissociation":[30],"rate":[31],"(":[32],"k":[33,47,85,147],"off":[34,48,86,148],")":[35],"an":[37,60,67],"inhibitor":[38,90,146],"from":[39,116],"its":[40],"target.":[41],"The":[42],"traditional":[43],"methods":[44],"for":[45,82,88,124,200],"measuring":[46],"require":[49],"synthesis":[50],"labeled":[52],"ligands":[53],"or":[54],"low-throughput":[55],"label-free":[56],"methods.":[57],"To":[58],"provide":[59],"alternative":[61],"that":[62,127,141],"is":[63],"better":[64],"suited":[65],"to":[66,105],"automated":[68],"high-throughput":[69],"screening":[70],"(HTS)":[71],"environment,":[72],"we":[73],"adapted":[74],"a":[75,101,198],"classic":[76],"\"jump":[77],"dilution\"":[78],"catalytic":[79],"assay":[80,99,168,188],"method":[81,104,189],"determination":[83],"values":[87,149,153],"kinase":[89,110,207],"drugs.":[91],"We":[92,120],"used":[93],"Transcreener":[95,167],"ADP":[96],"2":[97],"Kinase":[98],"universal,":[102],"homogenous":[103],"monitor":[106],"recovery":[108],"activity":[111],"drugs":[114,126],"dissociated":[115],"preformed":[117],"inhibitor\u2013kinase":[118],"complexes.":[119],"measured":[121],"several":[125],"bind":[128],"epidermal":[130],"growth":[131],"factor":[132],"receptor":[133],"(EGFR),":[134],"ABL1,":[135],"Aurora":[137],"kinases":[138],"found":[140],"rank":[143],"ordering":[144],"correlated":[150],"with":[151,169],"literature":[152],"determined":[154],"using":[155,165],"ligand":[156],"binding":[157],"assays.":[158],"Moreover,":[159],"very":[160],"similar":[161],"results":[162],"were":[163],"obtained":[164],"fluorescence":[170,173],"polarization":[171],"(FP),":[172],"intensity":[174],"(FI),":[175],"time-resolved":[177],"F\u00f6rster":[178],"resonance":[179],"energy":[180],"transfer":[181],"(TR-FRET)":[182],"detection":[183],"modes.":[184],"This":[185],"HTS-compatible,":[186],"generic":[187],"should":[190],"facilitate":[191],"use":[193],"parameter":[199],"compound":[201],"prioritization":[202],"optimization":[204],"early":[205],"discovery":[209],"programs.":[210]},"counts_by_year":[{"year":2026,"cited_by_count":3},{"year":2025,"cited_by_count":7},{"year":2024,"cited_by_count":3},{"year":2023,"cited_by_count":1},{"year":2022,"cited_by_count":6},{"year":2021,"cited_by_count":2},{"year":2020,"cited_by_count":1},{"year":2019,"cited_by_count":1},{"year":2018,"cited_by_count":3}],"updated_date":"2026-11-07T11:25:07.637180","created_date":"2017-05-05T00:00:00"}
