{"id":"https://openalex.org/W2017544644","doi":"https://doi.org/10.1021/jm101527u","title":"Structure-Based Design of Potent and Selective 3-Phosphoinositide-Dependent Kinase-1 (PDK1) Inhibitors","display_name":"Structure-Based Design of Potent and Selective 3-Phosphoinositide-Dependent Kinase-1 (PDK1) Inhibitors","publication_year":2011,"publication_date":"2011-02-22","ids":{"openalex":"https://openalex.org/W2017544644","doi":"https://doi.org/10.1021/jm101527u","mag":"2017544644","pmid":"https://pubmed.ncbi.nlm.nih.gov/21341675"},"language":"en","primary_location":{"id":"doi:10.1021/jm101527u","doi":"https://doi.org/10.1021/jm101527u","is_oa":false,"landing_page_url":"https://doi.org/10.1021/jm101527u","pdf_url":null,"source":{"id":"https://openalex.org/S162030435","display_name":"Journal of Medicinal Chemistry","issn_l":"0022-2623","issn":["0022-2623","1520-4804"],"is_oa":false,"is_in_doaj":false,"is_core":true,"listed_in":["anvur-scientific","cwts-core","dongbi-a","jufo-3","ki-jl-2","medline","norway-2","poland-200","russia-white-list-1","vabb-shw"],"host_organization":"https://openalex.org/P4310320006","host_organization_name":"American Chemical Society","host_organization_lineage":["https://openalex.org/P4310320006"],"host_organization_lineage_names":["American Chemical Society"],"type":"journal"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Journal of Medicinal Chemistry","raw_type":"journal-article"},"volume":null,"type":"article","is_traditional":true,"indexed_in":["crossref","pubmed"],"open_access":{"is_oa":false,"oa_status":"closed","oa_url":null,"any_repository_has_fulltext":false},"authorships":[{"author_position":"first","author":{"id":"https://openalex.org/A5017997650","display_name":"Jes\u00fas R. Medina","orcid":"https://orcid.org/0000-0003-0274-3257","observed_orcids":["https://orcid.org/0000-0003-0274-3257"]},"institutions":[{"id":"https://openalex.org/I4210114143","display_name":"GlaxoSmithKline (United States)","ror":"https://ror.org/025vn3989","country_code":"US","type":"company","lineage":["https://openalex.org/I188950975","https://openalex.org/I4210114143"]}],"countries":["US"],"is_corresponding":true,"raw_author_name":"Jes\u00fas R. Medina","raw_affiliation_strings":["Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States","institution_ids":["https://openalex.org/I4210114143"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5054351628","display_name":"Christopher J. Becker","orcid":"https://orcid.org/0000-0003-3414-9826","observed_orcids":["https://orcid.org/0000-0003-3414-9826"]},"institutions":[{"id":"https://openalex.org/I4210114143","display_name":"GlaxoSmithKline (United States)","ror":"https://ror.org/025vn3989","country_code":"US","type":"company","lineage":["https://openalex.org/I188950975","https://openalex.org/I4210114143"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Christopher J. Becker","raw_affiliation_strings":["Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States","institution_ids":["https://openalex.org/I4210114143"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5048262929","display_name":"Charles W. Blackledge","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210114143","display_name":"GlaxoSmithKline (United States)","ror":"https://ror.org/025vn3989","country_code":"US","type":"company","lineage":["https://openalex.org/I188950975","https://openalex.org/I4210114143"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Charles W. Blackledge","raw_affiliation_strings":["Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States","institution_ids":["https://openalex.org/I4210114143"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5060108884","display_name":"C\u00e9line Duquenne","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210114143","display_name":"GlaxoSmithKline (United States)","ror":"https://ror.org/025vn3989","country_code":"US","type":"company","lineage":["https://openalex.org/I188950975","https://openalex.org/I4210114143"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Celine Duquenne","raw_affiliation_strings":["Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States","institution_ids":["https://openalex.org/I4210114143"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5112062456","display_name":"Yanhong Feng","orcid":"https://orcid.org/0009-0002-8600-6499","observed_orcids":["https://orcid.org/0009-0002-8600-6499"]},"institutions":[{"id":"https://openalex.org/I4210114143","display_name":"GlaxoSmithKline (United States)","ror":"https://ror.org/025vn3989","country_code":"US","type":"company","lineage":["https://openalex.org/I188950975","https://openalex.org/I4210114143"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Yanhong Feng","raw_affiliation_strings":["Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States","institution_ids":["https://openalex.org/I4210114143"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5100827969","display_name":"Seth W. Grant","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210114143","display_name":"GlaxoSmithKline (United States)","ror":"https://ror.org/025vn3989","country_code":"US","type":"company","lineage":["https://openalex.org/I188950975","https://openalex.org/I4210114143"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Seth W. Grant","raw_affiliation_strings":["Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States","institution_ids":["https://openalex.org/I4210114143"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5058562680","display_name":"Dirk A. Heerding","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210114143","display_name":"GlaxoSmithKline (United States)","ror":"https://ror.org/025vn3989","country_code":"US","type":"company","lineage":["https://openalex.org/I188950975","https://openalex.org/I4210114143"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Dirk Heerding","raw_affiliation_strings":["Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States","institution_ids":["https://openalex.org/I4210114143"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5072161328","display_name":"William Ho Cheung Li","orcid":"https://orcid.org/0000-0002-2562-769X","observed_orcids":["https://orcid.org/0000-0002-2562-769X"]},"institutions":[{"id":"https://openalex.org/I4210114143","display_name":"GlaxoSmithKline (United States)","ror":"https://ror.org/025vn3989","country_code":"US","type":"company","lineage":["https://openalex.org/I188950975","https://openalex.org/I4210114143"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"William H. Li","raw_affiliation_strings":["Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States","institution_ids":["https://openalex.org/I4210114143"]}]},{"author_position":"middle","author":{"id":null,"display_name":"William H. Miller","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210114143","display_name":"GlaxoSmithKline (United States)","ror":"https://ror.org/025vn3989","country_code":"US","type":"company","lineage":["https://openalex.org/I188950975","https://openalex.org/I4210114143"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"William H. Miller","raw_affiliation_strings":["Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States","institution_ids":["https://openalex.org/I4210114143"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5059210625","display_name":"Stuart P. Romeril","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210114143","display_name":"GlaxoSmithKline (United States)","ror":"https://ror.org/025vn3989","country_code":"US","type":"company","lineage":["https://openalex.org/I188950975","https://openalex.org/I4210114143"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Stuart P. Romeril","raw_affiliation_strings":["Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States","institution_ids":["https://openalex.org/I4210114143"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5079017404","display_name":"Daryl A. Scherzer","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210114143","display_name":"GlaxoSmithKline (United States)","ror":"https://ror.org/025vn3989","country_code":"US","type":"company","lineage":["https://openalex.org/I188950975","https://openalex.org/I4210114143"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Daryl Scherzer","raw_affiliation_strings":["Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States","institution_ids":["https://openalex.org/I4210114143"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5110000314","display_name":"Arthur Y. L. Shu","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210114143","display_name":"GlaxoSmithKline (United States)","ror":"https://ror.org/025vn3989","country_code":"US","type":"company","lineage":["https://openalex.org/I188950975","https://openalex.org/I4210114143"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Arthur Shu","raw_affiliation_strings":["Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States","institution_ids":["https://openalex.org/I4210114143"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5028360982","display_name":"Mark A. Bobko","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210114143","display_name":"GlaxoSmithKline (United States)","ror":"https://ror.org/025vn3989","country_code":"US","type":"company","lineage":["https://openalex.org/I188950975","https://openalex.org/I4210114143"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Mark A. Bobko","raw_affiliation_strings":["Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States","institution_ids":["https://openalex.org/I4210114143"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5059051683","display_name":"Antony R. Chadderton","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210114143","display_name":"GlaxoSmithKline (United States)","ror":"https://ror.org/025vn3989","country_code":"US","type":"company","lineage":["https://openalex.org/I188950975","https://openalex.org/I4210114143"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Antony R. Chadderton","raw_affiliation_strings":["Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States","institution_ids":["https://openalex.org/I4210114143"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5088977059","display_name":"Melissa L. Dumble","orcid":"https://orcid.org/0009-0007-7944-4921","observed_orcids":["https://orcid.org/0009-0007-7944-4921"]},"institutions":[{"id":"https://openalex.org/I4210114143","display_name":"GlaxoSmithKline (United States)","ror":"https://ror.org/025vn3989","country_code":"US","type":"company","lineage":["https://openalex.org/I188950975","https://openalex.org/I4210114143"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Melissa Dumble","raw_affiliation_strings":["Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States","institution_ids":["https://openalex.org/I4210114143"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5036867504","display_name":"Christine M. Gardiner","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210114143","display_name":"GlaxoSmithKline (United States)","ror":"https://ror.org/025vn3989","country_code":"US","type":"company","lineage":["https://openalex.org/I188950975","https://openalex.org/I4210114143"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Christine M. Gardiner","raw_affiliation_strings":["Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States","institution_ids":["https://openalex.org/I4210114143"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5043278576","display_name":"Seth A. Gilbert","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210114143","display_name":"GlaxoSmithKline (United States)","ror":"https://ror.org/025vn3989","country_code":"US","type":"company","lineage":["https://openalex.org/I188950975","https://openalex.org/I4210114143"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Seth Gilbert","raw_affiliation_strings":["Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States","institution_ids":["https://openalex.org/I4210114143"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5100453178","display_name":"Qi Liu","orcid":"https://orcid.org/0000-0002-0839-8039","observed_orcids":["https://orcid.org/0000-0002-0839-8039"]},"institutions":[{"id":"https://openalex.org/I4210114143","display_name":"GlaxoSmithKline (United States)","ror":"https://ror.org/025vn3989","country_code":"US","type":"company","lineage":["https://openalex.org/I188950975","https://openalex.org/I4210114143"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Qi Liu","raw_affiliation_strings":["Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States","institution_ids":["https://openalex.org/I4210114143"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5076785086","display_name":"Sridhar K. Rabindran","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210114143","display_name":"GlaxoSmithKline (United States)","ror":"https://ror.org/025vn3989","country_code":"US","type":"company","lineage":["https://openalex.org/I188950975","https://openalex.org/I4210114143"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Sridhar K. Rabindran","raw_affiliation_strings":["Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States","institution_ids":["https://openalex.org/I4210114143"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5014914998","display_name":"Valery Sudakin","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210114143","display_name":"GlaxoSmithKline (United States)","ror":"https://ror.org/025vn3989","country_code":"US","type":"company","lineage":["https://openalex.org/I188950975","https://openalex.org/I4210114143"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Valery Sudakin","raw_affiliation_strings":["Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States","institution_ids":["https://openalex.org/I4210114143"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5080743064","display_name":"Hong Xiang","orcid":"https://orcid.org/0000-0001-6753-4283","observed_orcids":["https://orcid.org/0000-0001-6753-4283"]},"institutions":[{"id":"https://openalex.org/I4210114143","display_name":"GlaxoSmithKline (United States)","ror":"https://ror.org/025vn3989","country_code":"US","type":"company","lineage":["https://openalex.org/I188950975","https://openalex.org/I4210114143"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Hong Xiang","raw_affiliation_strings":["Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States","institution_ids":["https://openalex.org/I4210114143"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5056808437","display_name":"Pat G. Brady","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210114143","display_name":"GlaxoSmithKline (United States)","ror":"https://ror.org/025vn3989","country_code":"US","type":"company","lineage":["https://openalex.org/I188950975","https://openalex.org/I4210114143"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Pat G. Brady","raw_affiliation_strings":["Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States","institution_ids":["https://openalex.org/I4210114143"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5050234899","display_name":"Nino Campobasso","orcid":"https://orcid.org/0000-0003-3419-2840","observed_orcids":["https://orcid.org/0000-0003-3419-2840"]},"institutions":[{"id":"https://openalex.org/I4210114143","display_name":"GlaxoSmithKline (United States)","ror":"https://ror.org/025vn3989","country_code":"US","type":"company","lineage":["https://openalex.org/I188950975","https://openalex.org/I4210114143"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Nino Campobasso","raw_affiliation_strings":["Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States","institution_ids":["https://openalex.org/I4210114143"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5003893325","display_name":"Paris Ward","orcid":"https://orcid.org/0000-0002-6253-0379","observed_orcids":["https://orcid.org/0000-0002-6253-0379"]},"institutions":[{"id":"https://openalex.org/I4210114143","display_name":"GlaxoSmithKline (United States)","ror":"https://ror.org/025vn3989","country_code":"US","type":"company","lineage":["https://openalex.org/I188950975","https://openalex.org/I4210114143"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Paris Ward","raw_affiliation_strings":["Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States","institution_ids":["https://openalex.org/I4210114143"]}]},{"author_position":"last","author":{"id":"https://openalex.org/A5031552626","display_name":"Jeffrey M. Axten","orcid":"https://orcid.org/0000-0002-8999-3381","observed_orcids":["https://orcid.org/0000-0002-8999-3381"]},"institutions":[{"id":"https://openalex.org/I4210114143","display_name":"GlaxoSmithKline (United States)","ror":"https://ror.org/025vn3989","country_code":"US","type":"company","lineage":["https://openalex.org/I188950975","https://openalex.org/I4210114143"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Jeffrey M. Axten","raw_affiliation_strings":["Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Oncology Research and \u00a7Molecular Discovery Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, United States","institution_ids":["https://openalex.org/I4210114143"]}]}],"institutions":[],"countries_distinct_count":1,"institutions_distinct_count":1,"corresponding_author_ids":["https://openalex.org/A5017997650"],"corresponding_institution_ids":["https://openalex.org/I4210114143"],"apc_list":{"value":4500,"currency":"USD","value_usd":4500},"apc_paid":null,"fwci":2.0329,"has_fulltext":false,"cited_by_count":56,"citation_normalized_percentile":{"value":0.86925142,"is_in_top_1_percent":false,"is_in_top_10_percent":false},"cited_by_percentile_year":{"min":87,"max":99},"biblio":{"volume":"54","issue":"6","first_page":"1871","last_page":"1895"},"is_retracted":false,"is_paratext":false,"is_xpac":false,"primary_topic":{"id":"https://openalex.org/T10952","display_name":"PI3K/AKT/mTOR signaling in cancer","score":0.9916999936103821,"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"}},"topics":[{"id":"https://openalex.org/T10952","display_name":"PI3K/AKT/mTOR signaling in cancer","score":0.9916999936103821,"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/T10211","display_name":"Computational Drug Discovery Methods","score":0.005900000222027302,"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/T10274","display_name":"Heterocyclic Compound Synthesis and Bioactivity","score":0.000699999975040555,"subfield":{"id":"https://openalex.org/subfields/1605","display_name":"Organic Chemistry"},"field":{"id":"https://openalex.org/fields/16","display_name":"Chemistry"},"domain":{"id":"https://openalex.org/domains/3","display_name":"Physical Sciences"}}],"keywords":[{"id":"https://openalex.org/keywords/pdk1-inhibitors","display_name":"PDK1 inhibitors","score":0.8970000147819519},{"id":"https://openalex.org/keywords/3-phosphoinositide-dependent-kinase-1","display_name":"3-phosphoinositide-dependent kinase 1","score":0.9269999861717224},{"id":"https://openalex.org/keywords/structure-based-drug-design","display_name":"structure-based drug design","score":0.8640000224113464},{"id":"https://openalex.org/keywords/pi3k-akt-mtor-pathway","display_name":"PI3K/AKT/mTOR pathway","score":0.972000002861023},{"id":"https://openalex.org/keywords/agc-kinases","display_name":"AGC kinases","score":0.8650000095367432},{"id":"https://openalex.org/keywords/acute-myeloid-leukemia","display_name":"acute myeloid leukemia","score":0.8420000076293945},{"id":"https://openalex.org/keywords/antiproliferative-activity","display_name":"antiproliferative activity","score":0.9380000233650208},{"id":"https://openalex.org/keywords/xenograft-models","display_name":"xenograft models","score":0.5720000267028809},{"id":"https://openalex.org/keywords/anticancer-agents","display_name":"anticancer agents","score":0.6759999990463257},{"id":"https://openalex.org/keywords/kinase-substrate-phosphorylation","display_name":"kinase substrate phosphorylation","score":0.7179999947547913}],"concepts":[{"id":"https://openalex.org/C185592680","wikidata":"https://www.wikidata.org/wiki/Q2329","display_name":"Chemistry","level":0,"score":0.748289942741394},{"id":"https://openalex.org/C11960822","wikidata":"https://www.wikidata.org/wiki/Q242736","display_name":"Phosphorylation","level":2,"score":0.6343986392021179},{"id":"https://openalex.org/C86554907","wikidata":"https://www.wikidata.org/wiki/Q285613","display_name":"PI3K/AKT/mTOR pathway","level":3,"score":0.624164879322052},{"id":"https://openalex.org/C184235292","wikidata":"https://www.wikidata.org/wiki/Q421851","display_name":"Kinase","level":2,"score":0.6175718307495117},{"id":"https://openalex.org/C6929976","wikidata":"https://www.wikidata.org/wiki/Q3771881","display_name":"Regulator","level":3,"score":0.5838791728019714},{"id":"https://openalex.org/C75217442","wikidata":"https://www.wikidata.org/wiki/Q423650","display_name":"Protein kinase B","level":3,"score":0.542255699634552},{"id":"https://openalex.org/C207001950","wikidata":"https://www.wikidata.org/wiki/Q141124","display_name":"In vivo","level":2,"score":0.4940641224384308},{"id":"https://openalex.org/C97029542","wikidata":"https://www.wikidata.org/wiki/Q281417","display_name":"Protein kinase A","level":3,"score":0.4759407043457031},{"id":"https://openalex.org/C2781322055","wikidata":"https://www.wikidata.org/wiki/Q423725","display_name":"Phosphoinositide 3-kinase","level":4,"score":0.46904000639915466},{"id":"https://openalex.org/C95444343","wikidata":"https://www.wikidata.org/wiki/Q7141","display_name":"Cell biology","level":1,"score":0.4461617171764374},{"id":"https://openalex.org/C55493867","wikidata":"https://www.wikidata.org/wiki/Q7094","display_name":"Biochemistry","level":1,"score":0.385949969291687},{"id":"https://openalex.org/C62478195","wikidata":"https://www.wikidata.org/wiki/Q828130","display_name":"Signal transduction","level":2,"score":0.3555797338485718},{"id":"https://openalex.org/C502942594","wikidata":"https://www.wikidata.org/wiki/Q3421914","display_name":"Cancer research","level":1,"score":0.3442750573158264},{"id":"https://openalex.org/C86803240","wikidata":"https://www.wikidata.org/wiki/Q420","display_name":"Biology","level":0,"score":0.15009841322898865},{"id":"https://openalex.org/C150903083","wikidata":"https://www.wikidata.org/wiki/Q7108","display_name":"Biotechnology","level":1,"score":0.0},{"id":"https://openalex.org/C104317684","wikidata":"https://www.wikidata.org/wiki/Q7187","display_name":"Gene","level":2,"score":0.0}],"mesh":[{"descriptor_ui":"D000081382","descriptor_name":"Pyruvate Dehydrogenase Acetyl-Transferring Kinase","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D000818","descriptor_name":"Animals","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D000970","descriptor_name":"Antineoplastic Agents","qualifier_ui":"Q000138","qualifier_name":"chemical synthesis","is_major_topic":true},{"descriptor_ui":"D000970","descriptor_name":"Antineoplastic Agents","qualifier_ui":"Q000494","qualifier_name":"pharmacology","is_major_topic":false},{"descriptor_ui":"D000970","descriptor_name":"Antineoplastic Agents","qualifier_ui":"Q000737","qualifier_name":"chemistry","is_major_topic":false},{"descriptor_ui":"D004354","descriptor_name":"Drug Screening Assays, Antitumor","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D007191","descriptor_name":"Indazoles","qualifier_ui":"Q000138","qualifier_name":"chemical synthesis","is_major_topic":true},{"descriptor_ui":"D007191","descriptor_name":"Indazoles","qualifier_ui":"Q000494","qualifier_name":"pharmacology","is_major_topic":false},{"descriptor_ui":"D007191","descriptor_name":"Indazoles","qualifier_ui":"Q000737","qualifier_name":"chemistry","is_major_topic":false},{"descriptor_ui":"D008958","descriptor_name":"Models, Molecular","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D009025","descriptor_name":"Morpholines","qualifier_ui":"Q000138","qualifier_name":"chemical synthesis","is_major_topic":true},{"descriptor_ui":"D009025","descriptor_name":"Morpholines","qualifier_ui":"Q000494","qualifier_name":"pharmacology","is_major_topic":false},{"descriptor_ui":"D009025","descriptor_name":"Morpholines","qualifier_ui":"Q000737","qualifier_name":"chemistry","is_major_topic":false},{"descriptor_ui":"D009368","descriptor_name":"Neoplasm Transplantation","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D010766","descriptor_name":"Phosphorylation","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D010880","descriptor_name":"Piperidines","qualifier_ui":"Q000138","qualifier_name":"chemical synthesis","is_major_topic":true},{"descriptor_ui":"D010880","descriptor_name":"Piperidines","qualifier_ui":"Q000494","qualifier_name":"pharmacology","is_major_topic":false},{"descriptor_ui":"D010880","descriptor_name":"Piperidines","qualifier_ui":"Q000737","qualifier_name":"chemistry","is_major_topic":false},{"descriptor_ui":"D011485","descriptor_name":"Protein Binding","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D011743","descriptor_name":"Pyrimidines","qualifier_ui":"Q000138","qualifier_name":"chemical synthesis","is_major_topic":true},{"descriptor_ui":"D011743","descriptor_name":"Pyrimidines","qualifier_ui":"Q000494","qualifier_name":"pharmacology","is_major_topic":false},{"descriptor_ui":"D011743","descriptor_name":"Pyrimidines","qualifier_ui":"Q000737","qualifier_name":"chemistry","is_major_topic":false},{"descriptor_ui":"D013237","descriptor_name":"Stereoisomerism","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D013329","descriptor_name":"Structure-Activity Relationship","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D014183","descriptor_name":"Transplantation, Heterologous","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D015394","descriptor_name":"Molecular Structure","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D016513","descriptor_name":"Mice, SCID","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D017346","descriptor_name":"Protein Serine-Threonine Kinases","qualifier_ui":"Q000037","qualifier_name":"antagonists & inhibitors","is_major_topic":true},{"descriptor_ui":"D018360","descriptor_name":"Crystallography, X-Ray","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D045744","descriptor_name":"Cell Line, Tumor","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D051379","descriptor_name":"Mice","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false}],"locations_count":2,"locations":[{"id":"doi:10.1021/jm101527u","doi":"https://doi.org/10.1021/jm101527u","is_oa":false,"landing_page_url":"https://doi.org/10.1021/jm101527u","pdf_url":null,"source":{"id":"https://openalex.org/S162030435","display_name":"Journal of Medicinal Chemistry","issn_l":"0022-2623","issn":["0022-2623","1520-4804"],"is_oa":false,"is_in_doaj":false,"is_core":true,"listed_in":["anvur-scientific","cwts-core","dongbi-a","jufo-3","ki-jl-2","medline","norway-2","poland-200","russia-white-list-1","vabb-shw"],"host_organization":"https://openalex.org/P4310320006","host_organization_name":"American Chemical Society","host_organization_lineage":["https://openalex.org/P4310320006"],"host_organization_lineage_names":["American Chemical Society"],"type":"journal"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Journal of Medicinal Chemistry","raw_type":"journal-article"},{"id":"pmid:21341675","doi":null,"is_oa":false,"landing_page_url":"https://pubmed.ncbi.nlm.nih.gov/21341675","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":"Journal of medicinal chemistry","raw_type":"Journal Article"}],"best_oa_location":null,"sustainable_development_goals":[{"id":"https://metadata.un.org/sdg/3","score":0.8371999859809875,"display_name":"Good health and well-being"}],"study_designs":[],"awards":[],"funders":[],"has_content":{"pdf":false,"grobid_xml":false},"content_urls":null,"referenced_works_count":32,"referenced_works":["https://openalex.org/W1977405012","https://openalex.org/W1978550148","https://openalex.org/W1984621921","https://openalex.org/W1989987646","https://openalex.org/W1999283837","https://openalex.org/W2002228383","https://openalex.org/W2008312146","https://openalex.org/W2010929249","https://openalex.org/W2014172880","https://openalex.org/W2015714994","https://openalex.org/W2029633599","https://openalex.org/W2047255238","https://openalex.org/W2047973222","https://openalex.org/W2049885874","https://openalex.org/W2050395172","https://openalex.org/W2059943377","https://openalex.org/W2061293170","https://openalex.org/W2069232844","https://openalex.org/W2074952550","https://openalex.org/W2077804275","https://openalex.org/W2079741758","https://openalex.org/W2082820955","https://openalex.org/W2087861588","https://openalex.org/W2091913780","https://openalex.org/W2095960945","https://openalex.org/W2103299776","https://openalex.org/W2128555695","https://openalex.org/W2135178022","https://openalex.org/W2146157811","https://openalex.org/W2147746551","https://openalex.org/W2153677887","https://openalex.org/W2159990074"],"related_works":["https://openalex.org/W191329735","https://openalex.org/W7138864179","https://openalex.org/W4416410767","https://openalex.org/W2925031265","https://openalex.org/W2313228223","https://openalex.org/W1998926494","https://openalex.org/W1590595348","https://openalex.org/W2997767454","https://openalex.org/W6980542297","https://openalex.org/W1995401182"],"abstract_inverted_index":{"Phosphoinositide-dependent":[0],"protein":[1],"kinase-1(PDK1)":[2],"is":[3,24],"a":[4,33,62,90,136],"master":[5],"regulator":[6],"of":[7,11,17,36,51,79,81,92,99,101,118,128,135],"the":[8,18,26,116,126,131],"AGC":[9],"family":[10],"kinases":[12],"and":[13,57,69,130],"an":[14,42],"integral":[15],"component":[16],"PI3K/AKT/mTOR":[19],"pathway.":[20],"As":[21],"this":[22],"pathway":[23],"among":[25],"most":[27,67],"commonly":[28],"deregulated":[29],"across":[30],"all":[31],"cancers,":[32],"selective":[34,58,70],"inhibitor":[35],"PDK1":[37,59,82,102,129,137],"might":[38],"have":[39],"utility":[40,117],"as":[41,75,84,86,121],"anticancer":[43],"agent.":[44],"Herein":[45],"we":[46],"describe":[47],"our":[48],"lead":[49],"optimization":[50],"compound":[52],"1":[53],"toward":[54],"highly":[55],"potent":[56,68],"inhibitors":[60,71],"via":[61],"structure-based":[63],"design":[64],"strategy.":[65],"The":[66],"demonstrated":[72,105],"submicromolar":[73],"activity":[74,88],"measured":[76],"by":[77],"inhibition":[78],"phosphorylation":[80,100],"substrates":[83,103],"well":[85],"antiproliferative":[87],"against":[89],"subset":[91],"AML":[93],"cell":[94],"lines.":[95],"In":[96],"addition,":[97],"reduction":[98],"was":[104],"in":[106,108],"vivo":[107],"mice":[109],"bearing":[110],"OCl-AML2":[111],"xenografts.":[112],"These":[113],"observations":[114],"demonstrate":[115],"these":[119],"molecules":[120],"tools":[122],"to":[123],"further":[124],"delineate":[125],"biology":[127],"potential":[132],"pharmacological":[133],"uses":[134],"inhibitor.":[138]},"counts_by_year":[{"year":2026,"cited_by_count":3},{"year":2025,"cited_by_count":2},{"year":2024,"cited_by_count":3},{"year":2023,"cited_by_count":1},{"year":2022,"cited_by_count":3},{"year":2021,"cited_by_count":1},{"year":2020,"cited_by_count":4},{"year":2019,"cited_by_count":4},{"year":2018,"cited_by_count":3},{"year":2017,"cited_by_count":6},{"year":2016,"cited_by_count":3},{"year":2015,"cited_by_count":5},{"year":2014,"cited_by_count":1},{"year":2013,"cited_by_count":8},{"year":2012,"cited_by_count":8}],"updated_date":"2026-11-04T10:54:05.112534","created_date":"2016-06-24T00:00:00"}