{"id":"https://openalex.org/W2020200168","doi":"https://doi.org/10.1021/jm0407613","title":"Synthesis and Biological Evaluation of 3-Heterocyclyl-7,8,9,10-tetrahydro-(7,10-ethano)-1,2,4-triazolo[3,4-a]phthalazines and Analogues as Subtype-Selective Inverse Agonists for the GABAA\u03b15 Benzodiazepine Binding Site","display_name":"Synthesis and Biological Evaluation of 3-Heterocyclyl-7,8,9,10-tetrahydro-(7,10-ethano)-1,2,4-triazolo[3,4-a]phthalazines and Analogues as Subtype-Selective Inverse Agonists for the GABAA\u03b15 Benzodiazepine Binding Site","publication_year":2004,"publication_date":"2004-05-28","ids":{"openalex":"https://openalex.org/W2020200168","doi":"https://doi.org/10.1021/jm0407613","mag":"2020200168","pmid":"https://pubmed.ncbi.nlm.nih.gov/15214791"},"language":"en","primary_location":{"id":"doi:10.1021/jm0407613","doi":"https://doi.org/10.1021/jm0407613","is_oa":false,"landing_page_url":"https://doi.org/10.1021/jm0407613","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/A5112443924","display_name":"Leslie J. Street","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210087189","display_name":"MSD (UK) Limited (United Kingdom)","ror":"https://ror.org/004nn4n27","country_code":"GB","type":"company","lineage":["https://openalex.org/I1285764155","https://openalex.org/I4210087189"]}],"countries":["GB"],"is_corresponding":true,"raw_author_name":"Leslie J. Street","raw_affiliation_strings":["Departments of Medicinal Chemistry, Biochemistry, and Pharmacology, Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Departments of Medicinal Chemistry, Biochemistry, and Pharmacology, Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK","institution_ids":["https://openalex.org/I4210087189"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5069446741","display_name":"Francine Sternfeld","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210087189","display_name":"MSD (UK) Limited (United Kingdom)","ror":"https://ror.org/004nn4n27","country_code":"GB","type":"company","lineage":["https://openalex.org/I1285764155","https://openalex.org/I4210087189"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"Francine Sternfeld","raw_affiliation_strings":["Departments of Medicinal Chemistry, Biochemistry, and Pharmacology, Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Departments of Medicinal Chemistry, Biochemistry, and Pharmacology, Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK","institution_ids":["https://openalex.org/I4210087189"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5005264945","display_name":"Richard A. Jelley","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210087189","display_name":"MSD (UK) Limited (United Kingdom)","ror":"https://ror.org/004nn4n27","country_code":"GB","type":"company","lineage":["https://openalex.org/I1285764155","https://openalex.org/I4210087189"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"Richard A. Jelley","raw_affiliation_strings":["Departments of Medicinal Chemistry, Biochemistry, and Pharmacology, Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Departments of Medicinal Chemistry, Biochemistry, and Pharmacology, Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK","institution_ids":["https://openalex.org/I4210087189"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5110056834","display_name":"Austin J. Reeve","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210087189","display_name":"MSD (UK) Limited (United Kingdom)","ror":"https://ror.org/004nn4n27","country_code":"GB","type":"company","lineage":["https://openalex.org/I1285764155","https://openalex.org/I4210087189"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"Austin J. Reeve","raw_affiliation_strings":["Departments of Medicinal Chemistry, Biochemistry, and Pharmacology, Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Departments of Medicinal Chemistry, Biochemistry, and Pharmacology, Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK","institution_ids":["https://openalex.org/I4210087189"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5080950417","display_name":"Robert W. Carling","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210087189","display_name":"MSD (UK) Limited (United Kingdom)","ror":"https://ror.org/004nn4n27","country_code":"GB","type":"company","lineage":["https://openalex.org/I1285764155","https://openalex.org/I4210087189"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"Robert W. Carling","raw_affiliation_strings":["Departments of Medicinal Chemistry, Biochemistry, and Pharmacology, Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Departments of Medicinal Chemistry, Biochemistry, and Pharmacology, Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK","institution_ids":["https://openalex.org/I4210087189"]}]},{"author_position":"middle","author":{"id":null,"display_name":"Kevin W. Moore","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210087189","display_name":"MSD (UK) Limited (United Kingdom)","ror":"https://ror.org/004nn4n27","country_code":"GB","type":"company","lineage":["https://openalex.org/I1285764155","https://openalex.org/I4210087189"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"Kevin W. Moore","raw_affiliation_strings":["Departments of Medicinal Chemistry, Biochemistry, and Pharmacology, Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Departments of Medicinal Chemistry, Biochemistry, and Pharmacology, Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK","institution_ids":["https://openalex.org/I4210087189"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5055238379","display_name":"Ruth M. McKernan","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210087189","display_name":"MSD (UK) Limited (United Kingdom)","ror":"https://ror.org/004nn4n27","country_code":"GB","type":"company","lineage":["https://openalex.org/I1285764155","https://openalex.org/I4210087189"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"Ruth M. McKernan","raw_affiliation_strings":["Departments of Medicinal Chemistry, Biochemistry, and Pharmacology, Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Departments of Medicinal Chemistry, Biochemistry, and Pharmacology, Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK","institution_ids":["https://openalex.org/I4210087189"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5010570002","display_name":"Bindi Sohal","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210087189","display_name":"MSD (UK) Limited (United Kingdom)","ror":"https://ror.org/004nn4n27","country_code":"GB","type":"company","lineage":["https://openalex.org/I1285764155","https://openalex.org/I4210087189"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"Bindi Sohal","raw_affiliation_strings":["Departments of Medicinal Chemistry, Biochemistry, and Pharmacology, Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Departments of Medicinal Chemistry, Biochemistry, and Pharmacology, Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK","institution_ids":["https://openalex.org/I4210087189"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5005640939","display_name":"Susan M. Cook","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210087189","display_name":"MSD (UK) Limited (United Kingdom)","ror":"https://ror.org/004nn4n27","country_code":"GB","type":"company","lineage":["https://openalex.org/I1285764155","https://openalex.org/I4210087189"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"Susan Cook","raw_affiliation_strings":["Departments of Medicinal Chemistry, Biochemistry, and Pharmacology, Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Departments of Medicinal Chemistry, Biochemistry, and Pharmacology, Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK","institution_ids":["https://openalex.org/I4210087189"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5111596145","display_name":"Andrew J. Pike","orcid":"https://orcid.org/0000-0001-6078-7501","observed_orcids":["https://orcid.org/0000-0001-6078-7501"]},"institutions":[{"id":"https://openalex.org/I4210087189","display_name":"MSD (UK) Limited (United Kingdom)","ror":"https://ror.org/004nn4n27","country_code":"GB","type":"company","lineage":["https://openalex.org/I1285764155","https://openalex.org/I4210087189"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"Andrew Pike","raw_affiliation_strings":["Departments of Medicinal Chemistry, Biochemistry, and Pharmacology, Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Departments of Medicinal Chemistry, Biochemistry, and Pharmacology, Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK","institution_ids":["https://openalex.org/I4210087189"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5071764366","display_name":"Gerard R. Dawson","orcid":"https://orcid.org/0000-0002-8624-7500","observed_orcids":["https://orcid.org/0000-0002-8624-7500"]},"institutions":[{"id":"https://openalex.org/I4210087189","display_name":"MSD (UK) Limited (United Kingdom)","ror":"https://ror.org/004nn4n27","country_code":"GB","type":"company","lineage":["https://openalex.org/I1285764155","https://openalex.org/I4210087189"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"Gerard R. Dawson","raw_affiliation_strings":["Departments of Medicinal Chemistry, Biochemistry, and Pharmacology, Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Departments of Medicinal Chemistry, Biochemistry, and Pharmacology, Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK","institution_ids":["https://openalex.org/I4210087189"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5016509330","display_name":"Frances A. Bromidge","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210087189","display_name":"MSD (UK) Limited (United Kingdom)","ror":"https://ror.org/004nn4n27","country_code":"GB","type":"company","lineage":["https://openalex.org/I1285764155","https://openalex.org/I4210087189"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"Frances A. Bromidge","raw_affiliation_strings":["Departments of Medicinal Chemistry, Biochemistry, and Pharmacology, Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Departments of Medicinal Chemistry, Biochemistry, and Pharmacology, Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK","institution_ids":["https://openalex.org/I4210087189"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5072439028","display_name":"Keith A. Wafford","orcid":"https://orcid.org/0000-0002-8508-4738","observed_orcids":["https://orcid.org/0000-0002-8508-4738","https://orcid.org/0000-0003-4537-4690"]},"institutions":[{"id":"https://openalex.org/I4210087189","display_name":"MSD (UK) Limited (United Kingdom)","ror":"https://ror.org/004nn4n27","country_code":"GB","type":"company","lineage":["https://openalex.org/I1285764155","https://openalex.org/I4210087189"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"Keith A. Wafford","raw_affiliation_strings":["Departments of Medicinal Chemistry, Biochemistry, and Pharmacology, Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Departments of Medicinal Chemistry, Biochemistry, and Pharmacology, Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK","institution_ids":["https://openalex.org/I4210087189"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5011976598","display_name":"Guy R. Seabrook","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210087189","display_name":"MSD (UK) Limited (United Kingdom)","ror":"https://ror.org/004nn4n27","country_code":"GB","type":"company","lineage":["https://openalex.org/I1285764155","https://openalex.org/I4210087189"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"Guy R. Seabrook","raw_affiliation_strings":["Departments of Medicinal Chemistry, Biochemistry, and Pharmacology, Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Departments of Medicinal Chemistry, Biochemistry, and Pharmacology, Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK","institution_ids":["https://openalex.org/I4210087189"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5109227522","display_name":"Sally Anne Thompson","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210087189","display_name":"MSD (UK) Limited (United Kingdom)","ror":"https://ror.org/004nn4n27","country_code":"GB","type":"company","lineage":["https://openalex.org/I1285764155","https://openalex.org/I4210087189"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"Sally A. Thompson","raw_affiliation_strings":["Departments of Medicinal Chemistry, Biochemistry, and Pharmacology, Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Departments of Medicinal Chemistry, Biochemistry, and Pharmacology, Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK","institution_ids":["https://openalex.org/I4210087189"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5104305302","display_name":"George R. Marshall","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210087189","display_name":"MSD (UK) Limited (United Kingdom)","ror":"https://ror.org/004nn4n27","country_code":"GB","type":"company","lineage":["https://openalex.org/I1285764155","https://openalex.org/I4210087189"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"George Marshall","raw_affiliation_strings":["Departments of Medicinal Chemistry, Biochemistry, and Pharmacology, Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Departments of Medicinal Chemistry, Biochemistry, and Pharmacology, Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK","institution_ids":["https://openalex.org/I4210087189"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5012516575","display_name":"Goplan V. Pillai","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210087189","display_name":"MSD (UK) Limited (United Kingdom)","ror":"https://ror.org/004nn4n27","country_code":"GB","type":"company","lineage":["https://openalex.org/I1285764155","https://openalex.org/I4210087189"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"Goplan V. Pillai","raw_affiliation_strings":["Departments of Medicinal Chemistry, Biochemistry, and Pharmacology, Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Departments of Medicinal Chemistry, Biochemistry, and Pharmacology, Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK","institution_ids":["https://openalex.org/I4210087189"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5110255976","display_name":"Jos\u00e9 L. Castro","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210087189","display_name":"MSD (UK) Limited (United Kingdom)","ror":"https://ror.org/004nn4n27","country_code":"GB","type":"company","lineage":["https://openalex.org/I1285764155","https://openalex.org/I4210087189"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"Jos\u00e9 L. Castro","raw_affiliation_strings":["Departments of Medicinal Chemistry, Biochemistry, and Pharmacology, Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Departments of Medicinal Chemistry, Biochemistry, and Pharmacology, Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK","institution_ids":["https://openalex.org/I4210087189"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5027021273","display_name":"John R. Atack","orcid":"https://orcid.org/0000-0002-3410-791X","observed_orcids":["https://orcid.org/0000-0002-3410-791X"]},"institutions":[{"id":"https://openalex.org/I4210087189","display_name":"MSD (UK) Limited (United Kingdom)","ror":"https://ror.org/004nn4n27","country_code":"GB","type":"company","lineage":["https://openalex.org/I1285764155","https://openalex.org/I4210087189"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"John R. Atack","raw_affiliation_strings":["Departments of Medicinal Chemistry, Biochemistry, and Pharmacology, Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Departments of Medicinal Chemistry, Biochemistry, and Pharmacology, Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK","institution_ids":["https://openalex.org/I4210087189"]}]},{"author_position":"last","author":{"id":"https://openalex.org/A5032877342","display_name":"Angus M. MacLeod","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210087189","display_name":"MSD (UK) Limited (United Kingdom)","ror":"https://ror.org/004nn4n27","country_code":"GB","type":"company","lineage":["https://openalex.org/I1285764155","https://openalex.org/I4210087189"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"Angus M. MacLeod","raw_affiliation_strings":["Departments of Medicinal Chemistry, Biochemistry, and Pharmacology, Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Departments of Medicinal Chemistry, Biochemistry, and Pharmacology, Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK","institution_ids":["https://openalex.org/I4210087189"]}]}],"institutions":[],"countries_distinct_count":1,"institutions_distinct_count":1,"corresponding_author_ids":["https://openalex.org/A5112443924"],"corresponding_institution_ids":["https://openalex.org/I4210087189"],"apc_list":{"value":4500,"currency":"USD","value_usd":4500},"apc_paid":null,"fwci":2.3903,"has_fulltext":false,"cited_by_count":74,"citation_normalized_percentile":{"value":0.87952207,"is_in_top_1_percent":false,"is_in_top_10_percent":false},"cited_by_percentile_year":{"min":88,"max":99},"biblio":{"volume":"47","issue":"14","first_page":"3642","last_page":"3657"},"is_retracted":false,"is_paratext":false,"is_xpac":false,"primary_topic":{"id":"https://openalex.org/T10077","display_name":"Neuroscience and Neuropharmacology Research","score":0.8314999938011169,"subfield":{"id":"https://openalex.org/subfields/2804","display_name":"Cellular and Molecular Neuroscience"},"field":{"id":"https://openalex.org/fields/28","display_name":"Neuroscience"},"domain":{"id":"https://openalex.org/domains/1","display_name":"Life Sciences"}},"topics":[{"id":"https://openalex.org/T10077","display_name":"Neuroscience and Neuropharmacology Research","score":0.8314999938011169,"subfield":{"id":"https://openalex.org/subfields/2804","display_name":"Cellular and Molecular Neuroscience"},"field":{"id":"https://openalex.org/fields/28","display_name":"Neuroscience"},"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":0.07180000096559525,"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/T13105","display_name":"Synthesis and pharmacology of benzodiazepine derivatives","score":0.020800000056624413,"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/benzodiazepine-binding-site","display_name":"benzodiazepine binding site","score":0.9070000052452087},{"id":"https://openalex.org/keywords/inverse-agonists","display_name":"inverse agonists","score":0.984000027179718},{"id":"https://openalex.org/keywords/functional-selectivity","display_name":"functional selectivity","score":0.7089999914169312},{"id":"https://openalex.org/keywords/binding-selectivity","display_name":"binding selectivity","score":0.9660000205039978},{"id":"https://openalex.org/keywords/2-pyridyl-substituents","display_name":"2-pyridyl substituents","score":0.6460000276565552},{"id":"https://openalex.org/keywords/oral-bioavailability","display_name":"oral bioavailability","score":0.7139999866485596},{"id":"https://openalex.org/keywords/gabaa-receptor-subtypes","display_name":"GABAA receptor subtypes","score":0.7879999876022339}],"concepts":[{"id":"https://openalex.org/C185592680","wikidata":"https://www.wikidata.org/wiki/Q2329","display_name":"Chemistry","level":0,"score":0.839336097240448},{"id":"https://openalex.org/C2777527159","wikidata":"https://www.wikidata.org/wiki/Q6593919","display_name":"Phthalazine","level":2,"score":0.8003414273262024},{"id":"https://openalex.org/C118792377","wikidata":"https://www.wikidata.org/wiki/Q108584245","display_name":"Selectivity","level":3,"score":0.7811565399169922},{"id":"https://openalex.org/C89951826","wikidata":"https://www.wikidata.org/wiki/Q1671731","display_name":"Inverse agonist","level":4,"score":0.6259176135063171},{"id":"https://openalex.org/C2778938600","wikidata":"https://www.wikidata.org/wiki/Q389934","display_name":"Agonist","level":3,"score":0.552106499671936},{"id":"https://openalex.org/C71240020","wikidata":"https://www.wikidata.org/wiki/Q186011","display_name":"Stereochemistry","level":1,"score":0.4889880418777466},{"id":"https://openalex.org/C114373084","wikidata":"https://www.wikidata.org/wiki/Q273499","display_name":"Chemical synthesis","level":3,"score":0.4354637563228607},{"id":"https://openalex.org/C170493617","wikidata":"https://www.wikidata.org/wiki/Q208467","display_name":"Receptor","level":2,"score":0.28330132365226746},{"id":"https://openalex.org/C155647269","wikidata":"https://www.wikidata.org/wiki/Q243455","display_name":"Medicinal chemistry","level":1,"score":0.14337125420570374},{"id":"https://openalex.org/C55493867","wikidata":"https://www.wikidata.org/wiki/Q7094","display_name":"Biochemistry","level":1,"score":0.1123054027557373},{"id":"https://openalex.org/C202751555","wikidata":"https://www.wikidata.org/wiki/Q221681","display_name":"In vitro","level":2,"score":0.07003802061080933},{"id":"https://openalex.org/C161790260","wikidata":"https://www.wikidata.org/wiki/Q82264","display_name":"Catalysis","level":2,"score":0.0}],"mesh":[{"descriptor_ui":"D000284","descriptor_name":"Administration, Oral","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":"D001665","descriptor_name":"Binding Sites","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D001682","descriptor_name":"Biological Availability","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D002460","descriptor_name":"Cell Line","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D005260","descriptor_name":"Female","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":"D007555","descriptor_name":"Isoxazoles","qualifier_ui":"Q000138","qualifier_name":"chemical synthesis","is_major_topic":true},{"descriptor_ui":"D007555","descriptor_name":"Isoxazoles","qualifier_ui":"Q000494","qualifier_name":"pharmacology","is_major_topic":false},{"descriptor_ui":"D007555","descriptor_name":"Isoxazoles","qualifier_ui":"Q000737","qualifier_name":"chemistry","is_major_topic":false},{"descriptor_ui":"D008297","descriptor_name":"Male","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D009865","descriptor_name":"Oocytes","qualifier_ui":"Q000187","qualifier_name":"drug effects","is_major_topic":false},{"descriptor_ui":"D009865","descriptor_name":"Oocytes","qualifier_ui":"Q000502","qualifier_name":"physiology","is_major_topic":false},{"descriptor_ui":"D010793","descriptor_name":"Phthalazines","qualifier_ui":"Q000138","qualifier_name":"chemical synthesis","is_major_topic":true},{"descriptor_ui":"D010793","descriptor_name":"Phthalazines","qualifier_ui":"Q000493","qualifier_name":"pharmacokinetics","is_major_topic":false},{"descriptor_ui":"D010793","descriptor_name":"Phthalazines","qualifier_ui":"Q000494","qualifier_name":"pharmacology","is_major_topic":false},{"descriptor_ui":"D010793","descriptor_name":"Phthalazines","qualifier_ui":"Q000737","qualifier_name":"chemistry","is_major_topic":false},{"descriptor_ui":"D011869","descriptor_name":"Radioligand Assay","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":"D014230","descriptor_name":"Triazoles","qualifier_ui":"Q000138","qualifier_name":"chemical synthesis","is_major_topic":true},{"descriptor_ui":"D014230","descriptor_name":"Triazoles","qualifier_ui":"Q000493","qualifier_name":"pharmacokinetics","is_major_topic":false},{"descriptor_ui":"D014230","descriptor_name":"Triazoles","qualifier_ui":"Q000494","qualifier_name":"pharmacology","is_major_topic":false},{"descriptor_ui":"D014982","descriptor_name":"Xenopus laevis","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D018408","descriptor_name":"Patch-Clamp Techniques","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D018782","descriptor_name":"Maze Learning","qualifier_ui":"Q000187","qualifier_name":"drug effects","is_major_topic":false},{"descriptor_ui":"D021122","descriptor_name":"Protein Subunits","qualifier_ui":"Q000819","qualifier_name":"agonists","is_major_topic":false},{"descriptor_ui":"D051381","descriptor_name":"Rats","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D058785","descriptor_name":"GABA-A Receptor Agonists","qualifier_ui":null,"qualifier_name":null,"is_major_topic":true}],"locations_count":2,"locations":[{"id":"doi:10.1021/jm0407613","doi":"https://doi.org/10.1021/jm0407613","is_oa":false,"landing_page_url":"https://doi.org/10.1021/jm0407613","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:15214791","doi":null,"is_oa":false,"landing_page_url":"https://pubmed.ncbi.nlm.nih.gov/15214791","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":[{"display_name":"Good health and well-being","id":"https://metadata.un.org/sdg/3","score":0.4000000059604645}],"study_designs":[],"awards":[],"funders":[],"has_content":{"grobid_xml":false,"pdf":false},"content_urls":null,"referenced_works_count":22,"referenced_works":["https://openalex.org/W207568132","https://openalex.org/W828580598","https://openalex.org/W1669533272","https://openalex.org/W1964287283","https://openalex.org/W2001619275","https://openalex.org/W2003542826","https://openalex.org/W2004010919","https://openalex.org/W2020117882","https://openalex.org/W2022378061","https://openalex.org/W2025250480","https://openalex.org/W2046418300","https://openalex.org/W2077378517","https://openalex.org/W2080639248","https://openalex.org/W2081822887","https://openalex.org/W2087519774","https://openalex.org/W2089571336","https://openalex.org/W2091373599","https://openalex.org/W2095684169","https://openalex.org/W2106001183","https://openalex.org/W2110059977","https://openalex.org/W2165223719","https://openalex.org/W2418722848"],"related_works":["https://openalex.org/W1969130118","https://openalex.org/W2952556363","https://openalex.org/W2174613601","https://openalex.org/W2418722848","https://openalex.org/W2057078667","https://openalex.org/W2080639248","https://openalex.org/W2089885271","https://openalex.org/W1971011105","https://openalex.org/W2089571336","https://openalex.org/W2067192948"],"abstract_inverted_index":{"The":[0],"identification":[1],"of":[2,6,25,48,50,63,69],"a":[3,42,90],"novel":[4],"series":[5],"7,8,9,10-tetrahydro-(7,10-ethano)-1,2,4-triazolo[3,4-a]phthalazines":[7],"as":[8,89],"GABA(A)alpha5":[9,82,96],"inverse":[10,92],"agonists,":[11],"which":[12],"have":[13],"both":[14],"binding":[15,23],"and":[16,30,74,107],"functional":[17,56,83,99],"(efficacy)":[18],"selectivity":[19,38,57,100],"for":[20,81],"the":[21,46,51,61,64,67,70,95,102],"benzodiazepine":[22],"site":[24],"alpha5-":[26],"over":[27,101],"alpha1-,":[28],"alpha2-,":[29],"alpha3-containing":[31],"GABA(A)":[32,104],"receptor":[33,105],"subtypes,":[34],"is":[35],"described.":[36],"Binding":[37],"was":[39,58,87],"determined":[40],"to":[41,78],"large":[43],"part":[44],"by":[45],"degree":[47],"planarity":[49],"fused":[52],"ring":[53],"system":[54],"whereas":[55],"dependent":[59],"on":[60],"nature":[62],"heterocycle":[65],"at":[66,94],"3-position":[68],"triazolopyridazine":[71],"ring.":[72],"3-Furan":[73],"5-methylisoxazole":[75],"were":[76],"shown":[77],"be":[79],"optimal":[80],"selectvity.":[84],"3-(5-Methylisoxazol-3-yl)-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazine":[85],"(43)":[86],"identified":[88],"full":[91],"agonist":[93],"subtype":[97],"with":[98],"other":[103],"subtypes":[106],"good":[108],"oral":[109],"bioavailability.":[110]},"counts_by_year":[{"year":2026,"cited_by_count":3},{"year":2025,"cited_by_count":3},{"year":2024,"cited_by_count":1},{"year":2023,"cited_by_count":1},{"year":2022,"cited_by_count":2},{"year":2020,"cited_by_count":1},{"year":2019,"cited_by_count":2},{"year":2018,"cited_by_count":2},{"year":2017,"cited_by_count":1},{"year":2016,"cited_by_count":3},{"year":2015,"cited_by_count":3},{"year":2014,"cited_by_count":9},{"year":2013,"cited_by_count":5},{"year":2012,"cited_by_count":3}],"updated_date":"2026-11-11T12:16:26.678958","created_date":"2016-06-24T00:00:00"}
