{"id":"https://openalex.org/W7127180263","doi":"https://doi.org/10.1111/bph.70344","title":"Covalent drug discovery: Progress against key targets, emerging strategies and lessons learnt","display_name":"Covalent drug discovery: Progress against key targets, emerging strategies and lessons learnt","publication_year":2026,"publication_date":"2026-02-24","ids":{"openalex":"https://openalex.org/W7127180263","doi":"https://doi.org/10.1111/bph.70344","pmid":"https://pubmed.ncbi.nlm.nih.gov/41736234"},"language":"en","primary_location":{"id":"doi:10.1111/bph.70344","doi":"https://doi.org/10.1111/bph.70344","is_oa":true,"landing_page_url":"https://doi.org/10.1111/bph.70344","pdf_url":null,"source":{"id":"https://openalex.org/S55107261","display_name":"British Journal of Pharmacology","issn_l":"0007-1188","issn":["0007-1188","1476-5381"],"is_oa":false,"is_in_doaj":false,"is_core":true,"listed_in":["anvur-scientific","cwts-core","dongbi-b","doyens","jufo-3","ki-jl-2","medline","norway-2","poland-140","russia-white-list-1","vabb-shw"],"host_organization":"https://openalex.org/P4310320595","host_organization_name":"Wiley","host_organization_lineage":["https://openalex.org/P4310320595"],"host_organization_lineage_names":["Wiley"],"type":"journal"},"license":"cc-by","license_id":"https://openalex.org/licenses/cc-by","version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"British Journal of Pharmacology","raw_type":"journal-article"},"volume":null,"type":"article","indexed_in":["crossref","pubmed"],"open_access":{"is_oa":true,"oa_status":"hybrid","oa_url":"https://doi.org/10.1111/bph.70344","any_repository_has_fulltext":true},"authorships":[{"author_position":"first","author":{"id":"https://openalex.org/A5124782572","display_name":"Charlie Brown","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I47508984","display_name":"Imperial College London","ror":"https://ror.org/041kmwe10","country_code":"GB","type":"education","lineage":["https://openalex.org/I47508984"]}],"countries":["GB"],"is_corresponding":true,"raw_author_name":"Charles P. Brown","raw_affiliation_strings":["Department of Chemistry, Imperial College London Molecular Sciences Research Hub  London UK","Department of Life Sciences Imperial College London  London UK"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Department of Chemistry, Imperial College London Molecular Sciences Research Hub  London UK","institution_ids":["https://openalex.org/I47508984"]},{"raw_affiliation_string":"Department of Life Sciences Imperial College London  London UK","institution_ids":["https://openalex.org/I47508984"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5022913428","display_name":"Alan Armstrong","orcid":"https://orcid.org/0000-0002-3692-3099","observed_orcids":["https://orcid.org/0000-0002-3692-3099"]},"institutions":[{"id":"https://openalex.org/I47508984","display_name":"Imperial College London","ror":"https://ror.org/041kmwe10","country_code":"GB","type":"education","lineage":["https://openalex.org/I47508984"]}],"countries":["GB"],"is_corresponding":true,"raw_author_name":"Alan Armstrong","raw_affiliation_strings":["Department of Chemistry, Imperial College London Molecular Sciences Research Hub  London UK"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Department of Chemistry, Imperial College London Molecular Sciences Research Hub  London UK","institution_ids":["https://openalex.org/I47508984"]}]},{"author_position":"last","author":{"id":"https://openalex.org/A5061447348","display_name":"David J. Mann","orcid":"https://orcid.org/0000-0003-3023-1734","observed_orcids":["https://orcid.org/0000-0003-3023-1734"]},"institutions":[{"id":"https://openalex.org/I47508984","display_name":"Imperial College London","ror":"https://ror.org/041kmwe10","country_code":"GB","type":"education","lineage":["https://openalex.org/I47508984"]}],"countries":["GB"],"is_corresponding":true,"raw_author_name":"David J. Mann","raw_affiliation_strings":["Department of Life Sciences Imperial College London  London UK"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Department of Life Sciences Imperial College London  London UK","institution_ids":["https://openalex.org/I47508984"]}]}],"institutions":[],"countries_distinct_count":1,"institutions_distinct_count":1,"corresponding_author_ids":["https://openalex.org/A5022913428","https://openalex.org/A5061447348","https://openalex.org/A5124782572"],"corresponding_institution_ids":["https://openalex.org/I47508984"],"apc_list":{"value":4780,"currency":"USD","value_usd":4780},"apc_paid":{"value":4780,"currency":"USD","value_usd":4780},"fwci":5.7824,"has_fulltext":false,"cited_by_count":3,"citation_normalized_percentile":{"value":0.95297071,"is_in_top_1_percent":false,"is_in_top_10_percent":true},"cited_by_percentile_year":{"min":97,"max":98},"biblio":{"volume":null,"issue":null,"first_page":null,"last_page":null},"is_retracted":false,"is_paratext":false,"is_xpac":false,"primary_topic":{"id":"https://openalex.org/T12534","display_name":"Protein Degradation and Inhibitors","score":0.3788999915122986,"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/T12534","display_name":"Protein Degradation and Inhibitors","score":0.3788999915122986,"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/T11440","display_name":"Click Chemistry and Applications","score":0.26809999346733093,"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/T10274","display_name":"Synthesis and biological activity","score":0.04529999941587448,"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/covalent-drug-discovery","display_name":"covalent drug discovery","score":0.9660000205039978},{"id":"https://openalex.org/keywords/covalent-inhibitors","display_name":"covalent inhibitors","score":0.8230000138282776},{"id":"https://openalex.org/keywords/kras-g12c","display_name":"KRAS G12C","score":0.8899999856948853},{"id":"https://openalex.org/keywords/egfr-l858r-mutation","display_name":"L858R mutation","score":0.9120000004768372},{"id":"https://openalex.org/keywords/egfr-t790m-mutation","display_name":"T790M mutation","score":0.9559999704360962},{"id":"https://openalex.org/keywords/bruton-tyrosine-kinase-inhibitors","display_name":"BTK inhibitors","score":0.7549999952316284},{"id":"https://openalex.org/keywords/kras-g12d","display_name":"KRAS G12D","score":0.949999988079071},{"id":"https://openalex.org/keywords/wrn-helicase","display_name":"WRN helicase","score":0.9959999918937683},{"id":"https://openalex.org/keywords/therapeutic-target","display_name":"therapeutic target","score":0.4309999942779541},{"id":"https://openalex.org/keywords/covalent-drug-design","display_name":"covalent drug design","score":0.47600001096725464}],"concepts":[{"id":"https://openalex.org/C180577832","wikidata":"https://www.wikidata.org/wiki/Q127920","display_name":"Covalent bond","level":2,"score":0.6743999719619751},{"id":"https://openalex.org/C74187038","wikidata":"https://www.wikidata.org/wiki/Q1418791","display_name":"Drug discovery","level":2,"score":0.6164000034332275},{"id":"https://openalex.org/C26517878","wikidata":"https://www.wikidata.org/wiki/Q228039","display_name":"Key (lock)","level":2,"score":0.5702999830245972},{"id":"https://openalex.org/C185592680","wikidata":"https://www.wikidata.org/wiki/Q2329","display_name":"Chemistry","level":0,"score":0.420199990272522},{"id":"https://openalex.org/C161624437","wikidata":"https://www.wikidata.org/wiki/Q1988322","display_name":"Small molecule","level":2,"score":0.40950000286102295},{"id":"https://openalex.org/C64903051","wikidata":"https://www.wikidata.org/wiki/Q2198549","display_name":"Drug development","level":3,"score":0.40459999442100525},{"id":"https://openalex.org/C171250308","wikidata":"https://www.wikidata.org/wiki/Q11468","display_name":"Nanotechnology","level":1,"score":0.400299996137619},{"id":"https://openalex.org/C2780035454","wikidata":"https://www.wikidata.org/wiki/Q8386","display_name":"Drug","level":2,"score":0.375},{"id":"https://openalex.org/C70721500","wikidata":"https://www.wikidata.org/wiki/Q177005","display_name":"Computational biology","level":1,"score":0.3357999920845032},{"id":"https://openalex.org/C3018522384","wikidata":"https://www.wikidata.org/wiki/Q127920","display_name":"Covalent binding","level":3,"score":0.328900009393692},{"id":"https://openalex.org/C171852809","wikidata":"https://www.wikidata.org/wiki/Q731154","display_name":"Chemical biology","level":2,"score":0.3188000023365021},{"id":"https://openalex.org/C2989108626","wikidata":"https://www.wikidata.org/wiki/Q904407","display_name":"Drug target","level":2,"score":0.3070000112056732},{"id":"https://openalex.org/C41008148","wikidata":"https://www.wikidata.org/wiki/Q21198","display_name":"Computer science","level":0,"score":0.2831000089645386},{"id":"https://openalex.org/C98274493","wikidata":"https://www.wikidata.org/wiki/Q128406","display_name":"Pharmacology","level":1,"score":0.2623000144958496},{"id":"https://openalex.org/C21951064","wikidata":"https://www.wikidata.org/wiki/Q899212","display_name":"Combinatorial chemistry","level":1,"score":0.26170000433921814},{"id":"https://openalex.org/C40000846","wikidata":"https://www.wikidata.org/wiki/Q915868","display_name":"Spliceosome","level":5,"score":0.2524999976158142}],"mesh":[],"locations_count":3,"locations":[{"id":"doi:10.1111/bph.70344","doi":"https://doi.org/10.1111/bph.70344","is_oa":true,"landing_page_url":"https://doi.org/10.1111/bph.70344","pdf_url":null,"source":{"id":"https://openalex.org/S55107261","display_name":"British Journal of Pharmacology","issn_l":"0007-1188","issn":["0007-1188","1476-5381"],"is_oa":false,"is_in_doaj":false,"is_core":true,"listed_in":["anvur-scientific","cwts-core","dongbi-b","doyens","jufo-3","ki-jl-2","medline","norway-2","poland-140","russia-white-list-1","vabb-shw"],"host_organization":"https://openalex.org/P4310320595","host_organization_name":"Wiley","host_organization_lineage":["https://openalex.org/P4310320595"],"host_organization_lineage_names":["Wiley"],"type":"journal"},"license":"cc-by","license_id":"https://openalex.org/licenses/cc-by","version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"British Journal of Pharmacology","raw_type":"journal-article"},{"id":"pmid:41736234","doi":null,"is_oa":false,"landing_page_url":"https://pubmed.ncbi.nlm.nih.gov/41736234","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":"British journal of pharmacology","raw_type":"Journal Article"},{"id":"pmh:oai:spiral.imperial.ac.uk:10044/1/126886","doi":null,"is_oa":true,"landing_page_url":"https://hdl.handle.net/10044/1/126886","pdf_url":null,"source":{"id":"https://openalex.org/S4306401396","display_name":"Spiral (Imperial College London)","issn_l":null,"issn":null,"is_oa":false,"is_in_doaj":false,"is_core":false,"listed_in":[],"host_organization":"https://openalex.org/I47508984","host_organization_name":"Imperial College London","host_organization_lineage":["https://openalex.org/I47508984"],"host_organization_lineage_names":[],"type":"repository"},"license":"cc-by","license_id":"https://openalex.org/licenses/cc-by","version":"submittedVersion","is_accepted":false,"is_published":false,"raw_source_name":null,"raw_type":"Journal Article"}],"best_oa_location":{"id":"doi:10.1111/bph.70344","doi":"https://doi.org/10.1111/bph.70344","is_oa":true,"landing_page_url":"https://doi.org/10.1111/bph.70344","pdf_url":null,"source":{"id":"https://openalex.org/S55107261","display_name":"British Journal of Pharmacology","issn_l":"0007-1188","issn":["0007-1188","1476-5381"],"is_oa":false,"is_in_doaj":false,"is_core":true,"listed_in":["anvur-scientific","cwts-core","dongbi-b","doyens","jufo-3","ki-jl-2","medline","norway-2","poland-140","russia-white-list-1","vabb-shw"],"host_organization":"https://openalex.org/P4310320595","host_organization_name":"Wiley","host_organization_lineage":["https://openalex.org/P4310320595"],"host_organization_lineage_names":["Wiley"],"type":"journal"},"license":"cc-by","license_id":"https://openalex.org/licenses/cc-by","version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"British Journal of Pharmacology","raw_type":"journal-article"},"sustainable_development_goals":[{"display_name":"Good health and well-being","id":"https://metadata.un.org/sdg/3","score":0.5683000087738037}],"sustainable_development_goals_aurora":[{"display_name":"Industry, innovation and infrastructure","id":"https://metadata.un.org/sdg/9","score":0.644711971282959}],"study_designs":[],"awards":[{"id":"https://openalex.org/G8685505878","display_name":"EPSRC Centre for Doctoral Training in Chemical Biology - Innovation for the Life Sciences","funder_award_id":"EP/S023518/1","funder_id":"https://openalex.org/F4320334627","funder_display_name":"Engineering and Physical Sciences Research Council"}],"funders":[{"id":"https://openalex.org/F4320334627","display_name":"Engineering and Physical Sciences Research Council","ror":"https://ror.org/0439y7842"}],"has_content":{"pdf":false,"grobid_xml":false},"content_urls":null,"referenced_works_count":0,"referenced_works":[],"related_works":[],"abstract_inverted_index":{"Abstract":[0],"Covalent":[1],"drug":[2,54,125],"discovery":[3,60],"is":[4],"currently":[5],"experiencing":[6],"a":[7,135],"boom":[8],"in":[9,99],"industrial":[10],"and":[11,30,70,80,87,105],"academic":[12],"interest.":[13],"To":[14],"date,":[15],"at":[16],"least":[17],"75":[18],"covalent":[19,45,116,124,136],"drugs":[20],"have":[21,83],"received":[22],"regulatory":[23,95],"approval,":[24],"targeting":[25,46,63,74],"both":[26],"traditional":[27],"target":[28],"classes":[29],"more":[31],"challenging":[32],"proteins":[33],"for":[34,49],"which":[35,130],"other":[36],"approaches":[37],"failed.":[38],"In":[39],"many":[40],"cases,":[41],"unique":[42],"aspects":[43],"of":[44,52,61,109,134],"are":[47],"essential":[48],"the":[50,53,59,100,110,115,132],"efficacy":[51],"molecule.":[55],"Famous":[56],"successes":[57],"include":[58],"therapies":[62],"KRAS":[64,75],"G12C":[65],",":[66,77],"EGFR":[67],"L858R,":[68],"T790M":[69],"BTK,":[71],"whilst":[72],"molecules":[73,129],"G12D":[76],"WRN":[78],"helicase":[79],"p53":[81],"Y220C":[82],"recently":[84],"been":[85],"disclosed":[86],"will":[88],"represent":[89],"significant":[90],"achievements":[91],"if":[92],"they":[93],"receive":[94],"approval.":[96],"Increased":[97],"interest":[98],"field":[101],"has":[102],"catalysed":[103],"innovation":[104],"advanced":[106],"theoretical":[107],"understanding":[108],"distinct":[111],"considerations":[112],"resulting":[113],"from":[114],"interaction.":[117],"Here,":[118],"we":[119],"review":[120],"progress":[121],"against":[122],"key":[123],"targets,":[126],"emphasising":[127],"notable":[128],"exemplify":[131],"advantages":[133],"approach.":[137]},"counts_by_year":[{"year":2026,"cited_by_count":3}],"updated_date":"2026-10-09T09:14:12.587421","created_date":"2026-02-03T00:00:00"}
