{"id":"https://openalex.org/W1967080628","doi":"https://doi.org/10.1177/1087057110380455","title":"Fragment-Based Screening by Biochemical Assays: Systematic Feasibility Studies with Trypsin and MMP12","display_name":"Fragment-Based Screening by Biochemical Assays: Systematic Feasibility Studies with Trypsin and MMP12","publication_year":2010,"publication_date":"2010-09-21","ids":{"openalex":"https://openalex.org/W1967080628","doi":"https://doi.org/10.1177/1087057110380455","mag":"1967080628","pmid":"https://pubmed.ncbi.nlm.nih.gov/20855559"},"language":"en","primary_location":{"id":"doi:10.1177/1087057110380455","doi":"https://doi.org/10.1177/1087057110380455","is_oa":true,"landing_page_url":"https://doi.org/10.1177/1087057110380455","pdf_url":null,"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://doi.org/10.1177/1087057110380455","any_repository_has_fulltext":false},"authorships":[{"author_position":"first","author":{"id":"https://openalex.org/A5076264327","display_name":"Andreas Boettcher","orcid":"https://orcid.org/0000-0002-6548-1015","observed_orcids":["https://orcid.org/0000-0002-6548-1015"]},"institutions":[{"id":"https://openalex.org/I1283582996","display_name":"Novartis (Switzerland)","ror":"https://ror.org/02f9zrr09","country_code":"CH","type":"company","lineage":["https://openalex.org/I1283582996"]},{"id":"https://openalex.org/I4400600974","display_name":"Novartis Institutes for BioMedical Research","ror":"https://ror.org/053gv2m95","country_code":"CH","type":"funder","lineage":["https://openalex.org/I1283582996","https://openalex.org/I4400600974"]}],"countries":["CH"],"is_corresponding":false,"raw_author_name":"Andreas Boettcher","raw_affiliation_strings":["Novartis Institutes for BioMedical Research, Expertise Platform Proteases, Novartis Pharma AG, Basel, Switzerland"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Novartis Institutes for BioMedical Research, Expertise Platform Proteases, Novartis Pharma AG, Basel, Switzerland","institution_ids":["https://openalex.org/I1283582996","https://openalex.org/I4400600974"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5052240609","display_name":"Simon R\u00fcdisser","orcid":"https://orcid.org/0000-0002-1107-6196","observed_orcids":["https://orcid.org/0000-0002-1107-6196"]},"institutions":[{"id":"https://openalex.org/I1283582996","display_name":"Novartis (Switzerland)","ror":"https://ror.org/02f9zrr09","country_code":"CH","type":"company","lineage":["https://openalex.org/I1283582996"]},{"id":"https://openalex.org/I4400600974","display_name":"Novartis Institutes for BioMedical Research","ror":"https://ror.org/053gv2m95","country_code":"CH","type":"funder","lineage":["https://openalex.org/I1283582996","https://openalex.org/I4400600974"]}],"countries":["CH"],"is_corresponding":false,"raw_author_name":"Simon Ruedisser","raw_affiliation_strings":["Novartis Institutes for BioMedical Research (NIBR), Expertise Platform Proteases (EPP), Novartis Pharma AG, Basel, Switzerland"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Novartis Institutes for BioMedical Research (NIBR), Expertise Platform Proteases (EPP), Novartis Pharma AG, Basel, Switzerland","institution_ids":["https://openalex.org/I1283582996","https://openalex.org/I4400600974"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5080513503","display_name":"Paul J. A. Erbel","orcid":"https://orcid.org/0000-0002-6336-3445","observed_orcids":["https://orcid.org/0000-0002-6336-3445"]},"institutions":[{"id":"https://openalex.org/I1283582996","display_name":"Novartis (Switzerland)","ror":"https://ror.org/02f9zrr09","country_code":"CH","type":"company","lineage":["https://openalex.org/I1283582996"]},{"id":"https://openalex.org/I4400600974","display_name":"Novartis Institutes for BioMedical Research","ror":"https://ror.org/053gv2m95","country_code":"CH","type":"funder","lineage":["https://openalex.org/I1283582996","https://openalex.org/I4400600974"]}],"countries":["CH"],"is_corresponding":false,"raw_author_name":"Paulus Erbel","raw_affiliation_strings":["Novartis Institutes for BioMedical Research (NIBR), Expertise Platform Proteases (EPP), Novartis Pharma AG, Basel, Switzerland"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Novartis Institutes for BioMedical Research (NIBR), Expertise Platform Proteases (EPP), Novartis Pharma AG, Basel, Switzerland","institution_ids":["https://openalex.org/I1283582996","https://openalex.org/I4400600974"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5006048785","display_name":"D. Vinzenz","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I1283582996","display_name":"Novartis (Switzerland)","ror":"https://ror.org/02f9zrr09","country_code":"CH","type":"company","lineage":["https://openalex.org/I1283582996"]},{"id":"https://openalex.org/I4400600974","display_name":"Novartis Institutes for BioMedical Research","ror":"https://ror.org/053gv2m95","country_code":"CH","type":"funder","lineage":["https://openalex.org/I1283582996","https://openalex.org/I4400600974"]}],"countries":["CH"],"is_corresponding":false,"raw_author_name":"Daniela Vinzenz","raw_affiliation_strings":["Novartis Institutes for BioMedical Research (NIBR), Expertise Platform Proteases (EPP), Novartis Pharma AG, Basel, Switzerland"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Novartis Institutes for BioMedical Research (NIBR), Expertise Platform Proteases (EPP), Novartis Pharma AG, Basel, Switzerland","institution_ids":["https://openalex.org/I1283582996","https://openalex.org/I4400600974"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5000642677","display_name":"Nikolaus Schiering","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I1283582996","display_name":"Novartis (Switzerland)","ror":"https://ror.org/02f9zrr09","country_code":"CH","type":"company","lineage":["https://openalex.org/I1283582996"]},{"id":"https://openalex.org/I4400600974","display_name":"Novartis Institutes for BioMedical Research","ror":"https://ror.org/053gv2m95","country_code":"CH","type":"funder","lineage":["https://openalex.org/I1283582996","https://openalex.org/I4400600974"]}],"countries":["CH"],"is_corresponding":false,"raw_author_name":"Nikolaus Schiering","raw_affiliation_strings":["Novartis Institutes for BioMedical Research (NIBR), Expertise Platform Proteases (EPP), Novartis Pharma AG, Basel, Switzerland"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Novartis Institutes for BioMedical Research (NIBR), Expertise Platform Proteases (EPP), Novartis Pharma AG, Basel, Switzerland","institution_ids":["https://openalex.org/I1283582996","https://openalex.org/I4400600974"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5061595074","display_name":"Ulrich Hassiepen","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I1283582996","display_name":"Novartis (Switzerland)","ror":"https://ror.org/02f9zrr09","country_code":"CH","type":"company","lineage":["https://openalex.org/I1283582996"]},{"id":"https://openalex.org/I4400600974","display_name":"Novartis Institutes for BioMedical Research","ror":"https://ror.org/053gv2m95","country_code":"CH","type":"funder","lineage":["https://openalex.org/I1283582996","https://openalex.org/I4400600974"]}],"countries":["CH"],"is_corresponding":false,"raw_author_name":"Ulrich Hassiepen","raw_affiliation_strings":["Novartis Institutes for BioMedical Research (NIBR), Expertise Platform Proteases (EPP), Novartis Pharma AG, Basel, Switzerland"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Novartis Institutes for BioMedical Research (NIBR), Expertise Platform Proteases (EPP), Novartis Pharma AG, Basel, Switzerland","institution_ids":["https://openalex.org/I1283582996","https://openalex.org/I4400600974"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5053646331","display_name":"Pascal Rigollier","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I1283582996","display_name":"Novartis (Switzerland)","ror":"https://ror.org/02f9zrr09","country_code":"CH","type":"company","lineage":["https://openalex.org/I1283582996"]},{"id":"https://openalex.org/I4400600974","display_name":"Novartis Institutes for BioMedical Research","ror":"https://ror.org/053gv2m95","country_code":"CH","type":"funder","lineage":["https://openalex.org/I1283582996","https://openalex.org/I4400600974"]}],"countries":["CH"],"is_corresponding":false,"raw_author_name":"Pascal Rigollier","raw_affiliation_strings":["Novartis Institutes for BioMedical Research (NIBR), Expertise Platform Proteases (EPP), Novartis Pharma AG, Basel, Switzerland"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Novartis Institutes for BioMedical Research (NIBR), Expertise Platform Proteases (EPP), Novartis Pharma AG, Basel, Switzerland","institution_ids":["https://openalex.org/I1283582996","https://openalex.org/I4400600974"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5051647746","display_name":"Lorenz M. Mayr","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I1283582996","display_name":"Novartis (Switzerland)","ror":"https://ror.org/02f9zrr09","country_code":"CH","type":"company","lineage":["https://openalex.org/I1283582996"]},{"id":"https://openalex.org/I4400600974","display_name":"Novartis Institutes for BioMedical Research","ror":"https://ror.org/053gv2m95","country_code":"CH","type":"funder","lineage":["https://openalex.org/I1283582996","https://openalex.org/I4400600974"]}],"countries":["CH"],"is_corresponding":false,"raw_author_name":"Lorenz M. Mayr","raw_affiliation_strings":["Novartis Institutes for BioMedical Research (NIBR), Expertise Platform Proteases (EPP), Novartis Pharma AG, Basel, Switzerland"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Novartis Institutes for BioMedical Research (NIBR), Expertise Platform Proteases (EPP), Novartis Pharma AG, Basel, Switzerland","institution_ids":["https://openalex.org/I1283582996","https://openalex.org/I4400600974"]}]},{"author_position":"last","author":{"id":"https://openalex.org/A5001392363","display_name":"Julian Woelcke","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I1283582996","display_name":"Novartis (Switzerland)","ror":"https://ror.org/02f9zrr09","country_code":"CH","type":"company","lineage":["https://openalex.org/I1283582996"]},{"id":"https://openalex.org/I4400600974","display_name":"Novartis Institutes for BioMedical Research","ror":"https://ror.org/053gv2m95","country_code":"CH","type":"funder","lineage":["https://openalex.org/I1283582996","https://openalex.org/I4400600974"]}],"countries":["CH"],"is_corresponding":true,"raw_author_name":"Julian Woelcke","raw_affiliation_strings":["Novartis Institutes for BioMedical Research (NIBR), Expertise Platform Proteases (EPP), Novartis Pharma AG, Basel, Switzerland"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Novartis Institutes for BioMedical Research (NIBR), Expertise Platform Proteases (EPP), Novartis Pharma AG, Basel, Switzerland","institution_ids":["https://openalex.org/I1283582996","https://openalex.org/I4400600974"]}]}],"institutions":[],"countries_distinct_count":1,"institutions_distinct_count":2,"corresponding_author_ids":["https://openalex.org/A5001392363"],"corresponding_institution_ids":["https://openalex.org/I1283582996","https://openalex.org/I4400600974"],"apc_list":{"value":2070,"currency":"USD","value_usd":2070},"apc_paid":{"value":2070,"currency":"USD","value_usd":2070},"fwci":2.1298,"has_fulltext":false,"cited_by_count":46,"citation_normalized_percentile":{"value":0.86488169,"is_in_top_1_percent":false,"is_in_top_10_percent":false},"cited_by_percentile_year":{"min":88,"max":99},"biblio":{"volume":"15","issue":"9","first_page":"1029","last_page":"1041"},"is_retracted":false,"is_paratext":false,"is_xpac":false,"primary_topic":{"id":"https://openalex.org/T10211","display_name":"Computational Drug Discovery Methods","score":0.6503999829292297,"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":0.6503999829292297,"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/T10911","display_name":"Chemical Synthesis and Analysis","score":0.09059999883174896,"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"}},{"id":"https://openalex.org/T10620","display_name":"Protease and Inhibitor Mechanisms","score":0.08349999785423279,"subfield":{"id":"https://openalex.org/subfields/1306","display_name":"Cancer Research"},"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/fragment-based-screening","display_name":"fragment screening","score":0.9940000176429749},{"id":"https://openalex.org/keywords/trypsin","display_name":"trypsin","score":0.8579999804496765},{"id":"https://openalex.org/keywords/mmp-12","display_name":"MMP-12","score":0.8820000290870667},{"id":"https://openalex.org/keywords/serine-protease","display_name":"serine protease","score":0.6200000047683716},{"id":"https://openalex.org/keywords/matrix-metalloproteinases","display_name":"matrix metalloproteinases","score":0.9409999847412109},{"id":"https://openalex.org/keywords/false-positive-rate","display_name":"false positive rate","score":0.6359999775886536},{"id":"https://openalex.org/keywords/false-negative-rate","display_name":"false negative rate","score":0.9800000190734863},{"id":"https://openalex.org/keywords/mobility-shift-assay","display_name":"mobility shift assay","score":0.8999999761581421},{"id":"https://openalex.org/keywords/surface-plasmon-resonance","display_name":"surface plasmon resonance","score":0.8809999823570251},{"id":"https://openalex.org/keywords/protease-assay","display_name":"protease activity assay","score":0.5669999718666077},{"id":"https://openalex.org/keywords/drug-discovery","display_name":"drug discovery","score":0.6209999918937683}],"concepts":[{"id":"https://openalex.org/C2776714187","wikidata":"https://www.wikidata.org/wiki/Q212410","display_name":"Protease","level":3,"score":0.6744553446769714},{"id":"https://openalex.org/C2777807008","wikidata":"https://www.wikidata.org/wiki/Q87324999","display_name":"Serine protease","level":4,"score":0.615730881690979},{"id":"https://openalex.org/C2780340462","wikidata":"https://www.wikidata.org/wiki/Q127450","display_name":"Trypsin","level":3,"score":0.5898935794830322},{"id":"https://openalex.org/C185592680","wikidata":"https://www.wikidata.org/wiki/Q2329","display_name":"Chemistry","level":0,"score":0.5890070796012878},{"id":"https://openalex.org/C106847996","wikidata":"https://www.wikidata.org/wiki/Q898756","display_name":"Surface plasmon resonance","level":3,"score":0.5451116561889648},{"id":"https://openalex.org/C51323132","wikidata":"https://www.wikidata.org/wiki/Q626251","display_name":"High-throughput screening","level":2,"score":0.50014328956604},{"id":"https://openalex.org/C2909000736","wikidata":"https://www.wikidata.org/wiki/Q87324999","display_name":"Serine Proteinase Inhibitors","level":5,"score":0.4482359290122986},{"id":"https://openalex.org/C74187038","wikidata":"https://www.wikidata.org/wiki/Q1418791","display_name":"Drug discovery","level":2,"score":0.4466693699359894},{"id":"https://openalex.org/C43617362","wikidata":"https://www.wikidata.org/wiki/Q170050","display_name":"Chromatography","level":1,"score":0.42104193568229675},{"id":"https://openalex.org/C193244246","wikidata":"https://www.wikidata.org/wiki/Q5432696","display_name":"False discovery rate","level":3,"score":0.4142473042011261},{"id":"https://openalex.org/C181199279","wikidata":"https://www.wikidata.org/wiki/Q8047","display_name":"Enzyme","level":2,"score":0.3774232566356659},{"id":"https://openalex.org/C55493867","wikidata":"https://www.wikidata.org/wiki/Q7094","display_name":"Biochemistry","level":1,"score":0.3762325048446655},{"id":"https://openalex.org/C171250308","wikidata":"https://www.wikidata.org/wiki/Q11468","display_name":"Nanotechnology","level":1,"score":0.0942118763923645},{"id":"https://openalex.org/C192562407","wikidata":"https://www.wikidata.org/wiki/Q228736","display_name":"Materials science","level":0,"score":0.08286029100418091},{"id":"https://openalex.org/C104317684","wikidata":"https://www.wikidata.org/wiki/Q7187","display_name":"Gene","level":2,"score":0.0},{"id":"https://openalex.org/C155672457","wikidata":"https://www.wikidata.org/wiki/Q61231","display_name":"Nanoparticle","level":2,"score":0.0}],"mesh":[{"descriptor_ui":"D000818","descriptor_name":"Animals","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D001681","descriptor_name":"Biological Assay","qualifier_ui":"Q000379","qualifier_name":"methods","is_major_topic":true},{"descriptor_ui":"D002417","descriptor_name":"Cattle","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D002853","descriptor_name":"Chromatography, Liquid","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D004353","descriptor_name":"Drug Evaluation, Preclinical","qualifier_ui":"Q000379","qualifier_name":"methods","is_major_topic":true},{"descriptor_ui":"D005188","descriptor_name":"False Negative Reactions","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D005189","descriptor_name":"False Positive Reactions","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D005240","descriptor_name":"Feasibility Studies","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D005453","descriptor_name":"Fluorescence","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":"D007700","descriptor_name":"Kinetics","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D008027","descriptor_name":"Light","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D009682","descriptor_name":"Magnetic Resonance Spectroscopy","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D010446","descriptor_name":"Peptide Fragments","qualifier_ui":"Q000032","qualifier_name":"analysis","is_major_topic":true},{"descriptor_ui":"D010446","descriptor_name":"Peptide Fragments","qualifier_ui":"Q000737","qualifier_name":"chemistry","is_major_topic":false},{"descriptor_ui":"D012542","descriptor_name":"Scattering, Radiation","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D012995","descriptor_name":"Solubility","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D013058","descriptor_name":"Mass Spectrometry","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D014357","descriptor_name":"Trypsin","qualifier_ui":"Q000378","qualifier_name":"metabolism","is_major_topic":true},{"descriptor_ui":"D020349","descriptor_name":"Surface Plasmon Resonance","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D053508","descriptor_name":"Matrix Metalloproteinase 12","qualifier_ui":"Q000378","qualifier_name":"metabolism","is_major_topic":true}],"locations_count":2,"locations":[{"id":"doi:10.1177/1087057110380455","doi":"https://doi.org/10.1177/1087057110380455","is_oa":true,"landing_page_url":"https://doi.org/10.1177/1087057110380455","pdf_url":null,"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:20855559","doi":null,"is_oa":false,"landing_page_url":"https://pubmed.ncbi.nlm.nih.gov/20855559","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 biomolecular screening","raw_type":"Journal Article"}],"best_oa_location":{"id":"doi:10.1177/1087057110380455","doi":"https://doi.org/10.1177/1087057110380455","is_oa":true,"landing_page_url":"https://doi.org/10.1177/1087057110380455","pdf_url":null,"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":[],"study_designs":[],"awards":[],"funders":[{"id":"https://openalex.org/F4320314605","display_name":"Astex Pharmaceuticals","ror":"https://ror.org/05fx1fs38"}],"has_content":{"grobid_xml":false,"pdf":false},"content_urls":null,"referenced_works_count":39,"referenced_works":["https://openalex.org/W200948446","https://openalex.org/W207689782","https://openalex.org/W1966496513","https://openalex.org/W1968826906","https://openalex.org/W1971553338","https://openalex.org/W1996100382","https://openalex.org/W2000909785","https://openalex.org/W2011395093","https://openalex.org/W2017040371","https://openalex.org/W2019351126","https://openalex.org/W2024705685","https://openalex.org/W2028816469","https://openalex.org/W2044905153","https://openalex.org/W2046258407","https://openalex.org/W2047710091","https://openalex.org/W2047756206","https://openalex.org/W2050535564","https://openalex.org/W2056326723","https://openalex.org/W2056960294","https://openalex.org/W2065511203","https://openalex.org/W2076755375","https://openalex.org/W2079919603","https://openalex.org/W2082124210","https://openalex.org/W2111530399","https://openalex.org/W2125920799","https://openalex.org/W2127313625","https://openalex.org/W2134375419","https://openalex.org/W2135732933","https://openalex.org/W2139827114","https://openalex.org/W2140011931","https://openalex.org/W2143827494","https://openalex.org/W2147131626","https://openalex.org/W2151028167","https://openalex.org/W2159701165","https://openalex.org/W2166199238","https://openalex.org/W2166704869","https://openalex.org/W2167291273","https://openalex.org/W2414546912","https://openalex.org/W2497379199"],"related_works":["https://openalex.org/W2000909785","https://openalex.org/W2126765139","https://openalex.org/W2079919603","https://openalex.org/W2182673671","https://openalex.org/W4385374891","https://openalex.org/W2318264392","https://openalex.org/W2411101090","https://openalex.org/W2159701165","https://openalex.org/W2139827114","https://openalex.org/W2558224536"],"abstract_inverted_index":{"Fragment-based":[0],"screening":[1,40,130,162],"(FBS)":[2],"has":[3],"gained":[4],"acceptance":[5],"in":[6,26,47,51],"the":[7,15,37,58,62,80,99,117,145,161,179,184,196],"pharmaceutical":[8],"industry":[9],"as":[10,32,105],"an":[11],"attractive":[12],"approach":[13],"for":[14,22,129,172],"identification":[16],"of":[17,41,65,131,167,192],"new":[18],"chemical":[19],"starting":[20],"points":[21],"drug":[23],"discovery":[24],"programs":[25],"addition":[27],"to":[28,141,176,203],"classical":[29],"strategies":[30],"such":[31],"high-throughput":[33],"screening.":[34],"There":[35],"is":[36],"concern":[38],"that":[39,153],"fragments":[42,112,132,155],"at":[43],"high":[44],"\u00b5M":[45],"concentrations":[46],"biochemical":[48,122,180],"assays":[49,78,181],"results":[50],"increased":[52],"false-positive":[53,138],"and":[54,75,88,98,136,194],"false-negative":[55,135],"rates.":[56],"Here":[57],"authors":[59],"systematically":[60],"compare":[61],"data":[63,81,118],"quality":[64,82],"FBS":[66,173,186],"obtained":[67],"by":[68,165,188,199],"enzyme":[69],"activity-based":[70],"fluorescence":[71,73],"intensity,":[72],"lifetime,":[74],"mobility":[76],"shift":[77],"with":[79,133,144,156],"from":[83],"surface":[84],"plasmon":[85],"resonance":[86,91],"(SPR)":[87],"nuclear":[89],"magnetic":[90],"(NMR)":[92],"methods.":[93],"The":[94],"serine":[95],"protease":[96,123,197],"trypsin":[97],"matrix":[100],"metalloprotease":[101],"MMP12":[102],"were":[103,113],"selected":[104,114],"model":[106],"systems.":[107],"For":[108],"both":[109],"studies,":[110],"352":[111],"each.":[115],"From":[116],"generated,":[119],"all":[120],"3":[121],"assay":[124],"methods":[125],"can":[126,149],"be":[127,151,170],"used":[128,171],"low":[134,137],"rates,":[139],"comparable":[140],"those":[142],"achieved":[143],"SPR-based":[146],"assays.":[147],"It":[148],"also":[150],"concluded":[152],"only":[154],"a":[157,190],"solubility":[158],"higher":[159],"than":[160],"concentration":[163],"determined":[164],"means":[166],"NMR":[168,204],"should":[169],"purposes.":[174],"Extrapolated":[175],"10,000":[177],"fragments,":[178],"speed":[182],"up":[183],"primary":[185],"process":[187],"approximately":[189,200],"factor":[191],"10":[193],"reduce":[195],"consumption":[198],"10,000-fold":[201],"compared":[202],"protein":[205],"observation":[206],"experiments.":[207]},"counts_by_year":[{"year":2026,"cited_by_count":6},{"year":2025,"cited_by_count":2},{"year":2024,"cited_by_count":1},{"year":2023,"cited_by_count":1},{"year":2021,"cited_by_count":2},{"year":2020,"cited_by_count":1},{"year":2019,"cited_by_count":3},{"year":2018,"cited_by_count":2},{"year":2017,"cited_by_count":2},{"year":2016,"cited_by_count":3},{"year":2015,"cited_by_count":3},{"year":2014,"cited_by_count":5},{"year":2013,"cited_by_count":6},{"year":2012,"cited_by_count":4}],"updated_date":"2026-11-07T11:25:07.637180","created_date":"2016-06-24T00:00:00"}
