{"id":"https://openalex.org/W2000749166","doi":"https://doi.org/10.1021/jm500342d","title":"Optimization of an Imidazopyridazine Series of Inhibitors of Plasmodium falciparum Calcium-Dependent Protein Kinase 1 (PfCDPK1)","display_name":"Optimization of an Imidazopyridazine Series of Inhibitors of Plasmodium falciparum Calcium-Dependent Protein Kinase 1 (PfCDPK1)","publication_year":2014,"publication_date":"2014-04-01","ids":{"openalex":"https://openalex.org/W2000749166","doi":"https://doi.org/10.1021/jm500342d","mag":"2000749166","pmid":"https://pubmed.ncbi.nlm.nih.gov/24689770","pmcid":"https://www.ncbi.nlm.nih.gov/pmc/articles/4024065"},"language":"en","primary_location":{"id":"doi:10.1021/jm500342d","doi":"https://doi.org/10.1021/jm500342d","is_oa":true,"landing_page_url":"https://doi.org/10.1021/jm500342d","pdf_url":"https://pubs.acs.org/doi/pdf/10.1021/jm500342d","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":"cc-by","license_id":"https://openalex.org/licenses/cc-by","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":true,"oa_status":"hybrid","oa_url":"https://pubs.acs.org/doi/pdf/10.1021/jm500342d","any_repository_has_fulltext":true},"authorships":[{"author_position":"first","author":{"id":"https://openalex.org/A5034830599","display_name":"Timothy M. Chapman","orcid":"https://orcid.org/0000-0002-7396-0569","observed_orcids":["https://orcid.org/0000-0002-7396-0569"]},"institutions":[{"id":"https://openalex.org/I109541847","display_name":"LifeArc","ror":"https://ror.org/01dqb0q37","country_code":"GB","type":"nonprofit","lineage":["https://openalex.org/I109541847"]}],"countries":["GB"],"is_corresponding":true,"raw_author_name":"Timothy M. Chapman","raw_affiliation_strings":["Centre for Therapeutics Discovery, MRC Technology, 1-3 Burtonhole Lane, Mill Hill, London NW7 1AD, U.K"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Centre for Therapeutics Discovery, MRC Technology, 1-3 Burtonhole Lane, Mill Hill, London NW7 1AD, U.K","institution_ids":["https://openalex.org/I109541847"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5020419534","display_name":"Simon A. Osborne","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I109541847","display_name":"LifeArc","ror":"https://ror.org/01dqb0q37","country_code":"GB","type":"nonprofit","lineage":["https://openalex.org/I109541847"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"Simon A. Osborne","raw_affiliation_strings":["Centre\rfor Therapeutics Discovery, MRC Technology, 1-3 Burtonhole Lane, Mill Hill, London NW7 1AD, U.K","Centre#R#for Therapeutics Discovery, MRC Technology, 1-3 Burtonhole Lane, Mill Hill, London NW7 1AD, U.K"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Centre\rfor Therapeutics Discovery, MRC Technology, 1-3 Burtonhole Lane, Mill Hill, London NW7 1AD, U.K","institution_ids":["https://openalex.org/I109541847"]},{"raw_affiliation_string":"Centre#R#for Therapeutics Discovery, MRC Technology, 1-3 Burtonhole Lane, Mill Hill, London NW7 1AD, U.K","institution_ids":["https://openalex.org/I109541847"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5042648219","display_name":"Claire Wallace","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I109541847","display_name":"LifeArc","ror":"https://ror.org/01dqb0q37","country_code":"GB","type":"nonprofit","lineage":["https://openalex.org/I109541847"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"Claire Wallace","raw_affiliation_strings":["Centre\rfor Therapeutics Discovery, MRC Technology, 1-3 Burtonhole Lane, Mill Hill, London NW7 1AD, U.K","Centre#R#for Therapeutics Discovery, MRC Technology, 1-3 Burtonhole Lane, Mill Hill, London NW7 1AD, U.K"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Centre\rfor Therapeutics Discovery, MRC Technology, 1-3 Burtonhole Lane, Mill Hill, London NW7 1AD, U.K","institution_ids":["https://openalex.org/I109541847"]},{"raw_affiliation_string":"Centre#R#for Therapeutics Discovery, MRC Technology, 1-3 Burtonhole Lane, Mill Hill, London NW7 1AD, U.K","institution_ids":["https://openalex.org/I109541847"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5059606387","display_name":"Kristian Birchall","orcid":"https://orcid.org/0000-0001-9992-2555","observed_orcids":["https://orcid.org/0000-0001-9992-2555"]},"institutions":[{"id":"https://openalex.org/I109541847","display_name":"LifeArc","ror":"https://ror.org/01dqb0q37","country_code":"GB","type":"nonprofit","lineage":["https://openalex.org/I109541847"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"Kristian Birchall","raw_affiliation_strings":["Centre\rfor Therapeutics Discovery, MRC Technology, 1-3 Burtonhole Lane, Mill Hill, London NW7 1AD, U.K","Centre#R#for Therapeutics Discovery, MRC Technology, 1-3 Burtonhole Lane, Mill Hill, London NW7 1AD, U.K"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Centre\rfor Therapeutics Discovery, MRC Technology, 1-3 Burtonhole Lane, Mill Hill, London NW7 1AD, U.K","institution_ids":["https://openalex.org/I109541847"]},{"raw_affiliation_string":"Centre#R#for Therapeutics Discovery, MRC Technology, 1-3 Burtonhole Lane, Mill Hill, London NW7 1AD, U.K","institution_ids":["https://openalex.org/I109541847"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5081575824","display_name":"Nathalie S. Bouloc","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I109541847","display_name":"LifeArc","ror":"https://ror.org/01dqb0q37","country_code":"GB","type":"nonprofit","lineage":["https://openalex.org/I109541847"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"Nathalie Bouloc","raw_affiliation_strings":["Centre\rfor Therapeutics Discovery, MRC Technology, 1-3 Burtonhole Lane, Mill Hill, London NW7 1AD, U.K","Centre#R#for Therapeutics Discovery, MRC Technology, 1-3 Burtonhole Lane, Mill Hill, London NW7 1AD, U.K"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Centre\rfor Therapeutics Discovery, MRC Technology, 1-3 Burtonhole Lane, Mill Hill, London NW7 1AD, U.K","institution_ids":["https://openalex.org/I109541847"]},{"raw_affiliation_string":"Centre#R#for Therapeutics Discovery, MRC Technology, 1-3 Burtonhole Lane, Mill Hill, London NW7 1AD, U.K","institution_ids":["https://openalex.org/I109541847"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5055807167","display_name":"Hayley M. Jones","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I109541847","display_name":"LifeArc","ror":"https://ror.org/01dqb0q37","country_code":"GB","type":"nonprofit","lineage":["https://openalex.org/I109541847"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"Hayley M. Jones","raw_affiliation_strings":["Centre\rfor Therapeutics Discovery, MRC Technology, 1-3 Burtonhole Lane, Mill Hill, London NW7 1AD, U.K","Centre#R#for Therapeutics Discovery, MRC Technology, 1-3 Burtonhole Lane, Mill Hill, London NW7 1AD, U.K"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Centre\rfor Therapeutics Discovery, MRC Technology, 1-3 Burtonhole Lane, Mill Hill, London NW7 1AD, U.K","institution_ids":["https://openalex.org/I109541847"]},{"raw_affiliation_string":"Centre#R#for Therapeutics Discovery, MRC Technology, 1-3 Burtonhole Lane, Mill Hill, London NW7 1AD, U.K","institution_ids":["https://openalex.org/I109541847"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5035686174","display_name":"Keith H. Ansell","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I109541847","display_name":"LifeArc","ror":"https://ror.org/01dqb0q37","country_code":"GB","type":"nonprofit","lineage":["https://openalex.org/I109541847"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"Keith H. Ansell","raw_affiliation_strings":["Centre\rfor Therapeutics Discovery, MRC Technology, 1-3 Burtonhole Lane, Mill Hill, London NW7 1AD, U.K","Centre#R#for Therapeutics Discovery, MRC Technology, 1-3 Burtonhole Lane, Mill Hill, London NW7 1AD, U.K"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Centre\rfor Therapeutics Discovery, MRC Technology, 1-3 Burtonhole Lane, Mill Hill, London NW7 1AD, U.K","institution_ids":["https://openalex.org/I109541847"]},{"raw_affiliation_string":"Centre#R#for Therapeutics Discovery, MRC Technology, 1-3 Burtonhole Lane, Mill Hill, London NW7 1AD, U.K","institution_ids":["https://openalex.org/I109541847"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5110847838","display_name":"Debra L. Taylor","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I109541847","display_name":"LifeArc","ror":"https://ror.org/01dqb0q37","country_code":"GB","type":"nonprofit","lineage":["https://openalex.org/I109541847"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"Debra L. Taylor","raw_affiliation_strings":["Centre\rfor Therapeutics Discovery, MRC Technology, 1-3 Burtonhole Lane, Mill Hill, London NW7 1AD, U.K","Centre#R#for Therapeutics Discovery, MRC Technology, 1-3 Burtonhole Lane, Mill Hill, London NW7 1AD, U.K"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Centre\rfor Therapeutics Discovery, MRC Technology, 1-3 Burtonhole Lane, Mill Hill, London NW7 1AD, U.K","institution_ids":["https://openalex.org/I109541847"]},{"raw_affiliation_string":"Centre#R#for Therapeutics Discovery, MRC Technology, 1-3 Burtonhole Lane, Mill Hill, London NW7 1AD, U.K","institution_ids":["https://openalex.org/I109541847"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5069594586","display_name":"Barbara Clough","orcid":"https://orcid.org/0000-0002-3235-6170","observed_orcids":["https://orcid.org/0000-0002-3235-6170"]},"institutions":[{"id":"https://openalex.org/I4405285715","display_name":"National Institute for Medical Research","ror":"https://ror.org/00146rb91","country_code":"GB","type":"facility","lineage":["https://openalex.org/I2801081054","https://openalex.org/I4210087105","https://openalex.org/I4405285715","https://openalex.org/I90344618"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"Barbara Clough","raw_affiliation_strings":["Division\rof Parasitology, MRC National Institute for Medical Research, The Ridgeway, Mill Hill, London NW7 1AA, U.K","Division#R#of Parasitology, MRC National Institute for Medical Research, The Ridgeway, Mill, Hill, London NW7 1AA, U.K"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Division\rof Parasitology, MRC National Institute for Medical Research, The Ridgeway, Mill Hill, London NW7 1AA, U.K","institution_ids":["https://openalex.org/I4405285715"]},{"raw_affiliation_string":"Division#R#of Parasitology, MRC National Institute for Medical Research, The Ridgeway, Mill, Hill, London NW7 1AA, U.K","institution_ids":["https://openalex.org/I4405285715"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5049161625","display_name":"Judith L. Green","orcid":"https://orcid.org/0000-0001-6825-9404","observed_orcids":["https://orcid.org/0000-0001-6825-9404"]},"institutions":[{"id":"https://openalex.org/I4405285715","display_name":"National Institute for Medical Research","ror":"https://ror.org/00146rb91","country_code":"GB","type":"facility","lineage":["https://openalex.org/I2801081054","https://openalex.org/I4210087105","https://openalex.org/I4405285715","https://openalex.org/I90344618"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"Judith L. Green","raw_affiliation_strings":["Division\rof Parasitology, MRC National Institute for Medical Research, The Ridgeway, Mill Hill, London NW7 1AA, U.K","Division#R#of Parasitology, MRC National Institute for Medical Research, The Ridgeway, Mill, Hill, London NW7 1AA, U.K"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Division\rof Parasitology, MRC National Institute for Medical Research, The Ridgeway, Mill Hill, London NW7 1AA, U.K","institution_ids":["https://openalex.org/I4405285715"]},{"raw_affiliation_string":"Division#R#of Parasitology, MRC National Institute for Medical Research, The Ridgeway, Mill, Hill, London NW7 1AA, U.K","institution_ids":["https://openalex.org/I4405285715"]}]},{"author_position":"last","author":{"id":"https://openalex.org/A5076699881","display_name":"Anthony A. Holder","orcid":"https://orcid.org/0000-0002-8490-6058","observed_orcids":["https://orcid.org/0000-0002-8490-6058"]},"institutions":[{"id":"https://openalex.org/I4405285715","display_name":"National Institute for Medical Research","ror":"https://ror.org/00146rb91","country_code":"GB","type":"facility","lineage":["https://openalex.org/I2801081054","https://openalex.org/I4210087105","https://openalex.org/I4405285715","https://openalex.org/I90344618"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"Anthony A. Holder","raw_affiliation_strings":["Division\rof Parasitology, MRC National Institute for Medical Research, The Ridgeway, Mill Hill, London NW7 1AA, U.K","Division#R#of Parasitology, MRC National Institute for Medical Research, The Ridgeway, Mill, Hill, London NW7 1AA, U.K"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Division\rof Parasitology, MRC National Institute for Medical Research, The Ridgeway, Mill Hill, London NW7 1AA, U.K","institution_ids":["https://openalex.org/I4405285715"]},{"raw_affiliation_string":"Division#R#of Parasitology, MRC National Institute for Medical Research, The Ridgeway, Mill, Hill, London NW7 1AA, U.K","institution_ids":["https://openalex.org/I4405285715"]}]}],"institutions":[],"countries_distinct_count":1,"institutions_distinct_count":2,"corresponding_author_ids":["https://openalex.org/A5034830599"],"corresponding_institution_ids":["https://openalex.org/I109541847"],"apc_list":{"value":4500,"currency":"USD","value_usd":4500},"apc_paid":{"value":4500,"currency":"USD","value_usd":4500},"fwci":5.4953,"has_fulltext":false,"cited_by_count":53,"citation_normalized_percentile":{"value":0.95869707,"is_in_top_1_percent":false,"is_in_top_10_percent":true},"cited_by_percentile_year":{"min":88,"max":99},"biblio":{"volume":"57","issue":"8","first_page":"3570","last_page":"3587"},"is_retracted":false,"is_paratext":false,"is_xpac":false,"primary_topic":{"id":"https://openalex.org/T10091","display_name":"Malaria Research and Control","score":0.9657999873161316,"subfield":{"id":"https://openalex.org/subfields/2739","display_name":"Public Health, Environmental and Occupational Health"},"field":{"id":"https://openalex.org/fields/27","display_name":"Medicine"},"domain":{"id":"https://openalex.org/domains/4","display_name":"Health Sciences"}},"topics":[{"id":"https://openalex.org/T10091","display_name":"Malaria Research and Control","score":0.9657999873161316,"subfield":{"id":"https://openalex.org/subfields/2739","display_name":"Public Health, Environmental and Occupational Health"},"field":{"id":"https://openalex.org/fields/27","display_name":"Medicine"},"domain":{"id":"https://openalex.org/domains/4","display_name":"Health Sciences"}},{"id":"https://openalex.org/T10211","display_name":"Computational Drug Discovery Methods","score":0.027300000190734863,"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/T14099","display_name":"Synthesis and Characterization of Heterocyclic Compounds","score":0.00139999995008111,"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/imidazopyridazines","display_name":"imidazopyridazines","score":0.8410000205039978},{"id":"https://openalex.org/keywords/plasmodium-falciparum","display_name":"Plasmodium falciparum","score":0.9559999704360962},{"id":"https://openalex.org/keywords/calcium-dependent-protein-kinase-1","display_name":"CDPK1","score":0.9020000100135803},{"id":"https://openalex.org/keywords/antimalarial-drugs","display_name":"antimalarial drugs","score":0.8930000066757202},{"id":"https://openalex.org/keywords/kinase-inhibitors","display_name":"kinase inhibitors","score":0.7710000276565552},{"id":"https://openalex.org/keywords/structure-guided-design","display_name":"structure-guided design","score":0.847000002861023},{"id":"https://openalex.org/keywords/homology-modeling","display_name":"homology modeling","score":0.8790000081062317},{"id":"https://openalex.org/keywords/adme-properties","display_name":"ADME properties","score":0.9049999713897705},{"id":"https://openalex.org/keywords/membrane-permeability","display_name":"membrane permeability","score":0.7120000123977661},{"id":"https://openalex.org/keywords/in-vivo-efficacy","display_name":"in vivo efficacy","score":0.6579999923706055},{"id":"https://openalex.org/keywords/murine-malaria-model","display_name":"murine malaria model","score":0.6830000281333923},{"id":"https://openalex.org/keywords/medication-optimization","display_name":"medication optimization","score":0.4269999861717224}],"concepts":[{"id":"https://openalex.org/C69366308","wikidata":"https://www.wikidata.org/wiki/Q2272286","display_name":"ADME","level":3,"score":0.9599089622497559},{"id":"https://openalex.org/C2778371730","wikidata":"https://www.wikidata.org/wiki/Q311383","display_name":"Plasmodium falciparum","level":3,"score":0.8839787244796753},{"id":"https://openalex.org/C57992300","wikidata":"https://www.wikidata.org/wiki/Q2066956","display_name":"Potency","level":3,"score":0.8065998554229736},{"id":"https://openalex.org/C185592680","wikidata":"https://www.wikidata.org/wiki/Q2329","display_name":"Chemistry","level":0,"score":0.7620822191238403},{"id":"https://openalex.org/C207001950","wikidata":"https://www.wikidata.org/wiki/Q141124","display_name":"In vivo","level":2,"score":0.7440750598907471},{"id":"https://openalex.org/C202751555","wikidata":"https://www.wikidata.org/wiki/Q221681","display_name":"In vitro","level":2,"score":0.6545968055725098},{"id":"https://openalex.org/C98274493","wikidata":"https://www.wikidata.org/wiki/Q128406","display_name":"Pharmacology","level":1,"score":0.5118557810783386},{"id":"https://openalex.org/C2777752497","wikidata":"https://www.wikidata.org/wiki/Q286779","display_name":"IC50","level":3,"score":0.48215052485466003},{"id":"https://openalex.org/C96529984","wikidata":"https://www.wikidata.org/wiki/Q286136","display_name":"EC50","level":3,"score":0.4478609263896942},{"id":"https://openalex.org/C181199279","wikidata":"https://www.wikidata.org/wiki/Q8047","display_name":"Enzyme","level":2,"score":0.44340837001800537},{"id":"https://openalex.org/C55493867","wikidata":"https://www.wikidata.org/wiki/Q7094","display_name":"Biochemistry","level":1,"score":0.4363417327404022},{"id":"https://openalex.org/C2778048844","wikidata":"https://www.wikidata.org/wiki/Q12156","display_name":"Malaria","level":2,"score":0.22286292910575867},{"id":"https://openalex.org/C86803240","wikidata":"https://www.wikidata.org/wiki/Q420","display_name":"Biology","level":0,"score":0.13350674510002136},{"id":"https://openalex.org/C203014093","wikidata":"https://www.wikidata.org/wiki/Q101929","display_name":"Immunology","level":1,"score":0.0893997848033905},{"id":"https://openalex.org/C150903083","wikidata":"https://www.wikidata.org/wiki/Q7108","display_name":"Biotechnology","level":1,"score":0.0}],"mesh":[{"descriptor_ui":"D000818","descriptor_name":"Animals","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D000962","descriptor_name":"Antimalarials","qualifier_ui":"Q000138","qualifier_name":"chemical synthesis","is_major_topic":true},{"descriptor_ui":"D000962","descriptor_name":"Antimalarials","qualifier_ui":"Q000494","qualifier_name":"pharmacology","is_major_topic":false},{"descriptor_ui":"D010963","descriptor_name":"Plasmodium falciparum","qualifier_ui":"Q000187","qualifier_name":"drug effects","is_major_topic":true},{"descriptor_ui":"D010963","descriptor_name":"Plasmodium falciparum","qualifier_ui":"Q000201","qualifier_name":"enzymology","is_major_topic":false},{"descriptor_ui":"D011494","descriptor_name":"Protein Kinases","qualifier_ui":"Q000737","qualifier_name":"chemistry","is_major_topic":false},{"descriptor_ui":"D011724","descriptor_name":"Pyridazines","qualifier_ui":"Q000138","qualifier_name":"chemical synthesis","is_major_topic":true},{"descriptor_ui":"D011724","descriptor_name":"Pyridazines","qualifier_ui":"Q000494","qualifier_name":"pharmacology","is_major_topic":false},{"descriptor_ui":"D013329","descriptor_name":"Structure-Activity Relationship","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D015800","descriptor_name":"Protozoan Proteins","qualifier_ui":"Q000037","qualifier_name":"antagonists & inhibitors","is_major_topic":true},{"descriptor_ui":"D015800","descriptor_name":"Protozoan Proteins","qualifier_ui":"Q000737","qualifier_name":"chemistry","is_major_topic":false},{"descriptor_ui":"D047428","descriptor_name":"Protein Kinase Inhibitors","qualifier_ui":"Q000138","qualifier_name":"chemical synthesis","is_major_topic":true},{"descriptor_ui":"D047428","descriptor_name":"Protein Kinase Inhibitors","qualifier_ui":"Q000494","qualifier_name":"pharmacology","is_major_topic":false},{"descriptor_ui":"D051379","descriptor_name":"Mice","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false}],"locations_count":6,"locations":[{"id":"doi:10.1021/jm500342d","doi":"https://doi.org/10.1021/jm500342d","is_oa":true,"landing_page_url":"https://doi.org/10.1021/jm500342d","pdf_url":"https://pubs.acs.org/doi/pdf/10.1021/jm500342d","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":"cc-by","license_id":"https://openalex.org/licenses/cc-by","version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Journal of Medicinal Chemistry","raw_type":"journal-article"},{"id":"pmh:oai:europepmc.org:3000757","doi":null,"is_oa":true,"landing_page_url":"https://www.ncbi.nlm.nih.gov/pmc/articles/4024065","pdf_url":null,"source":{"id":"https://openalex.org/S4306400806","display_name":"Europe PMC (PubMed Central)","issn_l":null,"issn":null,"is_oa":false,"is_in_doaj":false,"is_core":false,"listed_in":[],"host_organization":"https://openalex.org/I1303153112","host_organization_name":"European Bioinformatics Institute","host_organization_lineage":["https://openalex.org/I1303153112"],"host_organization_lineage_names":[],"type":"repository"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":null,"raw_type":"Text"},{"id":"pmh:oai:pubmedcentral.nih.gov:4024065","doi":null,"is_oa":true,"landing_page_url":"https://www.ncbi.nlm.nih.gov/pmc/articles/4024065","pdf_url":null,"source":{"id":"https://openalex.org/S2764455111","display_name":"PubMed Central","issn_l":null,"issn":null,"is_oa":true,"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":"J Med Chem","raw_type":"Text"},{"id":"pmid:24689770","doi":null,"is_oa":false,"landing_page_url":"https://pubmed.ncbi.nlm.nih.gov/24689770","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"},{"id":"pmh:oai:CiteSeerX.psu:10.1.1.777.82","doi":null,"is_oa":false,"landing_page_url":"http://citeseerx.ist.psu.edu/viewdoc/summary?doi=10.1.1.777.82","pdf_url":null,"source":null,"license":null,"license_id":null,"version":"submittedVersion","is_accepted":false,"is_published":false,"raw_source_name":"ftp://ftp.ncbi.nlm.nih.gov/pub/pmc/92/78/jm500342d.PMC4024065.pdf","raw_type":"text"},{"id":"pmh:oai:pure.atira.dk:openaire_cris_publications/4bcdd409-dfd7-4a22-9095-c3d8eeb6838c","doi":null,"is_oa":true,"landing_page_url":"https://research.birmingham.ac.uk/en/publications/4bcdd409-dfd7-4a22-9095-c3d8eeb6838c","pdf_url":null,"source":{"id":"https://openalex.org/S4306402634","display_name":"University of Birmingham Research Portal (University of Birmingham)","issn_l":null,"issn":null,"is_oa":false,"is_in_doaj":false,"is_core":false,"listed_in":[],"host_organization":"https://openalex.org/I79619799","host_organization_name":"University of Birmingham","host_organization_lineage":["https://openalex.org/I79619799"],"host_organization_lineage_names":[],"type":"repository"},"license":"other-oa","license_id":"https://openalex.org/licenses/other-oa","version":"submittedVersion","is_accepted":false,"is_published":false,"raw_source_name":"Chapman , T M , Osborne , S A , Wallace , C , Birchall , K , Bouloc , N , Jones , H M , Ansell , K H , Taylor , D L , Clough , B , Green , J L & Holder , A A 2014 , ' Optimization of an imidazopyridazine series of inhibitors of plasmodium falciparum calcium-dependent protein kinase 1 (Pf CDPK1) ' , Journal of Medicinal Chemistry , vol. 57 , no. 8 , pp. 3570-3587 . https://doi.org/10.1021/jm500342d","raw_type":"article"}],"best_oa_location":{"id":"doi:10.1021/jm500342d","doi":"https://doi.org/10.1021/jm500342d","is_oa":true,"landing_page_url":"https://doi.org/10.1021/jm500342d","pdf_url":"https://pubs.acs.org/doi/pdf/10.1021/jm500342d","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":"cc-by","license_id":"https://openalex.org/licenses/cc-by","version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Journal of Medicinal Chemistry","raw_type":"journal-article"},"sustainable_development_goals":[{"id":"https://metadata.un.org/sdg/3","display_name":"Good health and well-being","score":0.9391000270843506}],"study_designs":[],"awards":[{"id":"https://openalex.org/G1697524021","display_name":"Expansion of MRCTs Drug Discovery Group (DDG)","funder_award_id":"MC_G1000806","funder_id":"https://openalex.org/F4320334626","funder_display_name":"Medical Research Council"}],"funders":[{"id":"https://openalex.org/F4320334626","display_name":"Medical Research Council","ror":"https://ror.org/03x94j517"}],"has_content":{"pdf":true,"grobid_xml":false},"content_urls":{"pdf":"https://content.openalex.org/works/W2000749166.pdf"},"referenced_works_count":23,"referenced_works":["https://openalex.org/W1490630327","https://openalex.org/W1607470432","https://openalex.org/W1930237957","https://openalex.org/W1984276710","https://openalex.org/W2000106654","https://openalex.org/W2002487680","https://openalex.org/W2004388457","https://openalex.org/W2016500542","https://openalex.org/W2019102860","https://openalex.org/W2025636478","https://openalex.org/W2028765092","https://openalex.org/W2035032966","https://openalex.org/W2038073476","https://openalex.org/W2052295239","https://openalex.org/W2053732861","https://openalex.org/W2056883627","https://openalex.org/W2074004956","https://openalex.org/W2080463096","https://openalex.org/W2092890873","https://openalex.org/W2093012648","https://openalex.org/W2111127068","https://openalex.org/W2130533265","https://openalex.org/W2297954266"],"related_works":["https://openalex.org/W7098950007","https://openalex.org/W2035032966","https://openalex.org/W2002487680","https://openalex.org/W6903165927","https://openalex.org/W2620348215","https://openalex.org/W2211322663","https://openalex.org/W2901637517","https://openalex.org/W3213452177","https://openalex.org/W1984276710","https://openalex.org/W3213027411"],"abstract_inverted_index":{"A":[0],"structure-guided":[1],"design":[2],"approach":[3],"using":[4],"a":[5,23,74,100,115],"homology":[6],"model":[7,117],"of":[8,22,25,118,124,146,154],"Plasmodium":[9],"falciparum":[10,51],"calcium-dependent":[11],"protein":[12],"kinase":[13],"1":[14],"(PfCDPK1)":[15],"was":[16],"used":[17],"to":[18,56,68,80,107,128],"improve":[19],"the":[20,82,104,136,144,152],"potency":[21],"series":[24],"imidazopyridazine":[26],"inhibitors":[27],"as":[28],"potential":[29],"antimalarial":[30],"agents.":[31],"This":[32],"resulted":[33,140],"in":[34,48,70,73,85,93,103,112,114,130],"high":[35,122],"affinity":[36],"compounds":[37,61],"with":[38],"PfCDPK1":[39],"enzyme":[40],"IC50":[41],"values":[42,54],"less":[43],"than":[44],"10":[45],"nM":[46],"and":[47,135],"vitro":[49,131],"P.":[50],"antiparasite":[52,94],"EC50":[53],"down":[55],"12":[57],"nM,":[58],"although":[59],"these":[60],"did":[62],"not":[63],"have":[64],"suitable":[65],"ADME":[66,83],"properties":[67],"show":[69],"vivo":[71,113],"efficacy":[72,119,138],"mouse":[75],"model.":[76],"Structural":[77],"modifications":[78],"designed":[79],"address":[81],"issues,":[84],"particular":[86],"permeability,":[87],"were":[88,133],"initially":[89],"accompanied":[90],"by":[91],"losses":[92],"potency,":[95],"but":[96],"further":[97],"optimization":[98],"allowed":[99],"good":[101],"balance":[102],"compound":[105,125],"profile":[106],"be":[108],"achieved.":[109],"Upon":[110],"testing":[111],"murine":[116],"against":[120],"malaria,":[121],"levels":[123],"exposure":[126],"relative":[127],"their":[129],"activities":[132],"achieved,":[134],"modest":[137],"that":[139,148],"raises":[141],"questions":[142],"about":[143],"level":[145],"effect":[147],"is":[149],"achievable":[150],"through":[151],"targeting":[153],"PfCDPK1.":[155]},"counts_by_year":[{"year":2026,"cited_by_count":2},{"year":2025,"cited_by_count":3},{"year":2024,"cited_by_count":4},{"year":2023,"cited_by_count":1},{"year":2022,"cited_by_count":2},{"year":2021,"cited_by_count":4},{"year":2020,"cited_by_count":10},{"year":2019,"cited_by_count":3},{"year":2018,"cited_by_count":6},{"year":2017,"cited_by_count":5},{"year":2016,"cited_by_count":2},{"year":2015,"cited_by_count":5},{"year":2014,"cited_by_count":5}],"updated_date":"2026-11-07T11:25:07.637180","created_date":"2016-06-24T00:00:00"}