https://m2.mtmt.hu/ hun 2026-10-23 19:34 JournalArticle 31428111 VALIDATED true 0 false 2026-10-20T15:50:12.660+0000 2020-12-06T02:42:29.721+0000 2020-08-26T03:53:06.871+0000 true 565 WoS import /api/admin/565 Admin true 2025-05-08T14:58:54.618+0000 2020-09-02T06:06:49.158+0000 true 565 WoS import /api/admin/565 Admin true Admin 10023792 /api/admin/10023792 Suchanek-Lukács Margit true 10023792 true Admin 10067876 /api/admin/10067876 Ladányi Gusztáv true true 2024-10-17T16:35:19.342+0000 true false true 24 24 /api/publicationtype/24 PublicationType 1 true 24 JournalArticle true 1134514 Survey paper true 24 24 /api/publicationtype/24 PublicationType 1 true 24 JournalArticle /api/subtype/1134514 Összefoglaló cikk SubType 102 true 1134514 true 1 /api/category/1 Category true 1 Keeley, Aaron Covalent fragment libraries in drug discovery true true /api/journal/11965 REVIEWED true false 11965 false 11965 true 1359-6446 1878-5832 Journal FOREIGN 25 6 983 996 983 14 2020 Targeted covalent inhibitors and chemical probes have become integral parts of drug discovery approaches. Given the advantages of fragment-based drug discovery, screening electrophilic fragments emerged as a promising alternative to discover and validate novel targets and to generate viable chemical starting points even for targets that are barely tractable. In this review, we present recent principles and considerations in the design of electrophilic fragment libraries from the selection of the appropriate covalent warhead through the design of the covalent fragment to the compilation of the library. We then summarize recent screening methodologies of covalent fragments against surrogate models, proteins, and the whole proteome, or living cells. Finally, we highlight recent drug discovery applications of covalent fragment libraries. 2020 true true true false false NONE 2026-10-20 false 80 0 80 71 8 80 80 80 55 80 80 71 71 71 9 0 80 71 80 71 0 6 6 Folyóiratcikk Journal Article 24 79 Könyvrészlet Chapter in Book 25 1 Könyv Book 23 0 Egyéb konferenciaközlemény Conference paper 31 0 Egyéb konferenciakötet Conference proceedings 32 0 Oltalmi formák Protection forms 26 0 Disszertáció Thesis 28 0 Egyéb Miscellaneous 29 0 Alkotás Achievement 22 0 Kutatási adat Research data 33 0 Folyóiratcikk Journal Article 24 0 0 0 Könyvrészlet Chapter in Book 25 0 0 0 Könyv Book 23 0 0 0 Egyéb konferenciaközlemény Conference paper 31 0 0 0 Egyéb konferenciakötet Conference proceedings 32 0 0 0 Oltalmi formák Protection forms 26 0 0 0 Disszertáció Thesis 28 0 0 0 Egyéb Miscellaneous 29 0 0 0 Alkotás Achievement 22 0 0 0 Kutatási adat Research data 33 0 0 0 2020 0 5 4 5 4 2021 0 16 14 16 14 2022 0 17 15 17 15 2023 0 13 13 13 13 2024 0 12 11 12 11 2025 0 7 7 7 7 2026 0 10 7 10 7 D1 false 10053848 false false false 2020-11-26T11:44:30.895+0000 Gyógyszerkémiai Kutatócsoport (HRN TTK / SZKI) 4 19 1 4 0 true 10023792 10067876 Language 10002 /api/language/10002 Angol English true 2 true PersonAuthorship 92461024 /api/authorship/92461024 1 0.25 true false false Author 10061376 /api/author/10061376 Keeley Aaron Brian true 10061376 true Keeley Aaron true false false AuthorshipType 1 /api/authorshiptype/1 0 true 0 true false true PersonAuthorship 92461025 /api/authorship/92461025 2 0.25 false false false Author 10053848 /api/author/10053848 Petri László true 10053848 true Petri Laszlo true false false AuthorshipType 1 /api/authorshiptype/1 0 true 0 true false true PersonAuthorship 92461026 /api/authorship/92461026 3 0.25 false false false Author 10042926 /api/author/10042926 Ábrányi-Balogh Péter true 10042926 true Abranyi-Balogh Peter true false false AuthorshipType 1 /api/authorshiptype/1 0 true 0 true false true PersonAuthorship 92461027 /api/authorship/92461027 4 0.25 false true true Author 10001451 /api/author/10001451 Keserű György Miklós true 10001451 true Keseru Gyorgy M. true false false AuthorshipType 1 /api/authorshiptype/1 0 true 0 true false true PublicationIdentifier 17191055 /api/publicationidentifier/17191055 PlainSource 6 /api/publicationsource/6 PublicationSourceType 10001 /api/publicationsourcetype/10001 true true true DOI DOI https://doi.org/@@@ true true 6 true IDENTICAL 10.1016/j.drudis.2020.03.016 https://doi.org/10.1016/j.drudis.2020.03.016 false true PublicationIdentifier 17191054 /api/publicationidentifier/17191054 PlainSource 1 /api/publicationsource/1 PublicationSourceType 10003 /api/publicationsourcetype/10003 false true true WoS WoS https://www.webofscience.com/wos/woscc/full-record/@@@ true true 1 true IDENTICAL 000545311000009 https://www.webofscience.com/wos/woscc/full-record/000545311000009 false true PublicationIdentifier 17191056 /api/publicationidentifier/17191056 PlainSource 3 /api/publicationsource/3 PublicationSourceType 10003 /api/publicationsourcetype/10003 false true true Scopus Scopus http://www.scopus.com/record/display.url?origin=inward&eid=2-s2.0-@@@ true true 3 true IDENTICAL 85084119035 http://www.scopus.com/record/display.url?origin=inward&eid=2-s2.0-85084119035 false true PublicationIdentifier 17191057 /api/publicationidentifier/17191057 PlainSource 17 /api/publicationsource/17 PublicationSourceType 10003 /api/publicationsourcetype/10003 false true true PubMed PubMed http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=@@@&dopt=Abstract true true 17 true 32298798 http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=32298798&dopt=Abstract false true Classification 12125 /api/classification/12125 true true Classification 10398 /api/classification/10398 true true Classification 10293 /api/classification/10293 true true SjrRating 10782004 /api/sjrrating/10782004 14 0.1 journal RatingType 10002 /api/ratingtype/10002 sjr true true ClassificationExternal 3002 /api/classificationexternal/3002 true 3002 true D1 DIRECT true true /api/publication/31428111 <div class="JournalArticle Publication long-list"> <div class="authors"> <img title="Forrásközlemény" style="float: left" src="/frontend/resources/grid/publication-core-icon.png"> <img title="Idézőközlemény" style="float: left" src="/frontend/resources/grid/publication-citation-icon.png"> <div class="autype autype0"> <span class="author-name" mtid="10061376"><a href="/gui2/?type=authors&mode=browse&sel=10061376" target="_blank">Keeley Aaron (<span class="authorship-author-name">Keeley Aaron Brian</span> <span class="authorAux-mtmt"> kémiai tudományok</span>) </a> </span> <span class="author-affil"><span title="Természettudományi Kutatóközpont">TTK</span>/<span title="Szerves Kémiai Intézet">SZKI</span>/Gyógyszerkémiai Kutatócsoport</span> ;&nbsp;&nbsp;&nbsp; <span class="author-name" mtid="10053848"><a href="/gui2/?type=authors&mode=browse&sel=10053848" target="_blank">Petri Laszlo (<span class="authorship-author-name">Petri László</span> <span class="authorAux-mtmt"> szerves kémia, gyógyszerkémia</span>) </a> </span> <span class="author-affil"><span title="Természettudományi Kutatóközpont">TTK</span>/<span title="Szerves Kémiai Intézet">SZKI</span>/Gyógyszerkémiai Kutatócsoport</span> ;&nbsp;&nbsp;&nbsp; <span class="author-name" mtid="10042926"><a href="/gui2/?type=authors&mode=browse&sel=10042926" target="_blank">Abranyi-Balogh Peter (<span class="authorship-author-name">Ábrányi-Balogh Péter</span> <span class="authorAux-mtmt"> szerves kémia</span>) </a> </span> <span class="author-affil"><span title="Természettudományi Kutatóközpont">TTK</span>/<span title="Szerves Kémiai Intézet">SZKI</span>/Gyógyszerkémiai Kutatócsoport</span> ;&nbsp;&nbsp;&nbsp; <span class="author-name" mtid="10001451"><a href="/gui2/?type=authors&mode=browse&sel=10001451" target="_blank">Keseru Gyorgy M. ✉ (<span class="authorship-author-name">Keserű György Miklós</span> <span class="authorAux-mtmt"> Gyógyszerkémia, gyógyszertervezés</span>) </a> </span> <span class="author-affil"><span title="Természettudományi Kutatóközpont">TTK</span>/<span title="Szerves Kémiai Intézet">SZKI</span>/Gyógyszerkémiai Kutatócsoport</span> </div> </div> <div class="title"><a href="/gui2/?mode=browse&params=publication;31428111" target="_blank">Covalent fragment libraries in drug discovery</a></div> <div> <span class="journal-title">DRUG DISCOVERY TODAY</span> <span class="journal-issn">(<a target="_blank" href="https://portal.issn.org/resource/ISSN/1359-6446">1359-6446</a> <a target="_blank" href="https://portal.issn.org/resource/ISSN/1878-5832">1878-5832</a>)</span>: <span class="journal-volume">25</span> <span class="journal-issue">6</span> <span class="page"> pp 983-996 </span> <span class="year">(2020)</span> </div> <div class="pub-footer"> <span class="language" xmlns="http://www.w3.org/1999/html">Nyelv: Angol | </span> <span class="identifiers"> <span class="id identifier oa_none" title="none"> <a style="color:blue" title="10.1016/j.drudis.2020.03.016" target="_blank" href="https://doi.org/10.1016/j.drudis.2020.03.016"> DOI </a> </span> <span class="id identifier oa_none" title="none"> <a style="color:blue" title="000545311000009" target="_blank" href="https://www.webofscience.com/wos/woscc/full-record/000545311000009"> WoS </a> </span> <span class="id identifier oa_none" title="none"> <a style="color:blue" title="85084119035" target="_blank" href="http://www.scopus.com/record/display.url?origin=inward&eid=2-s2.0-85084119035"> Scopus </a> </span> <span class="id identifier oa_none" title="none"> <a style="color:black" title="32298798" target="_blank" href="http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=32298798&dopt=Abstract"> PubMed </a> </span> </span> <OnlyViewableByAuthor><div class="ratings"> <div class="journal-subject">Folyóirat szakterülete: Scopus - Drug Discovery&nbsp;&nbsp;&nbsp;SJR indikátor:&nbsp;D1</div> <div class="journal-subject">Folyóirat szakterülete: Scopus - Pharmacology&nbsp;&nbsp;&nbsp;SJR indikátor:&nbsp;Q1</div> </div></OnlyViewableByAuthor> <div class="publication-citation" style="margin-left: 0.5cm;"> <span title="Nyilvános idézőközlemények összesen, említések nélkül" class="citingPub-count">Nyilvános idéző összesen: 80</span> | Független: 71 | Függő: 9 | Nem jelölt: 0 | WoS jelölt: 80 | Scopus jelölt:&nbsp;55 | WoS/Scopus jelölt:&nbsp;80 | DOI jelölt:&nbsp;80 </div> <div class="publication-citation"> <a target="_blank" href="/api/publication?cond=citations.related;eq;31428111&sort=publishedYear,desc&sort=title"> Idézett közlemények száma: 6 </a> </div> <div class="mtid"><span class="long-pub-mtid">Közlemény: 31428111</span> | <span class="status-data status-VALIDATED"> Egyeztetett </span> Forrás Idéző | <span class="type-subtype">Folyóiratcikk ( Összefoglaló cikk ) </span> | <span class="pub-category">Tudományos</span> | <span class="publication-sourceOfData">WoS-XML</span> </div> <div class="lastModified">Utolsó módosítás: 2020.12.06. 03:42 WoS import (admin) </div> <div class="lockedBy">Központi kezelésű 2024.10.17. 18:35 Suchanek-Lukács Margit (Admin 3, admin) Ladányi Gusztáv (MTMT API user, admin) </div> </div></div>