{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,9,11]],"date-time":"2026-09-11T04:11:47Z","timestamp":1789099907993,"version":"build-2803163510"},"reference-count":21,"publisher":"Elsevier BV","license":[{"start":{"date-parts":[[2025,12,1]],"date-time":"2025-12-01T00:00:00Z","timestamp":1764547200000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/tdm\/userlicense\/1.0\/"},{"start":{"date-parts":[[2025,12,1]],"date-time":"2025-12-01T00:00:00Z","timestamp":1764547200000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/legal\/tdmrep-license"},{"start":{"date-parts":[[2025,12,1]],"date-time":"2025-12-01T00:00:00Z","timestamp":1764547200000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-017"},{"start":{"date-parts":[[2025,12,1]],"date-time":"2025-12-01T00:00:00Z","timestamp":1764547200000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-037"},{"start":{"date-parts":[[2025,12,1]],"date-time":"2025-12-01T00:00:00Z","timestamp":1764547200000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-012"},{"start":{"date-parts":[[2025,12,1]],"date-time":"2025-12-01T00:00:00Z","timestamp":1764547200000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-029"},{"start":{"date-parts":[[2025,12,1]],"date-time":"2025-12-01T00:00:00Z","timestamp":1764547200000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-004"}],"funder":[{"DOI":"10.13039\/100017534","name":"Inner Mongolia Medical University","doi-asserted-by":"publisher","award":["ZY20241203"],"award-info":[{"award-number":["ZY20241203"]}],"id":[{"id":"10.13039\/100017534","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/100017963","name":"Department of Education of Inner Mongolia Autonomous Region","doi-asserted-by":"publisher","award":["NJZY21591"],"award-info":[{"award-number":["NJZY21591"]}],"id":[{"id":"10.13039\/100017963","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":["elsevier.com","sciencedirect.com"],"crossmark-restriction":true},"short-container-title":["Bioorganic & Medicinal Chemistry Letters"],"published-print":{"date-parts":[[2025,12]]},"DOI":"10.1016\/j.bmcl.2025.130391","type":"journal-article","created":{"date-parts":[[2025,8,29]],"date-time":"2025-08-29T15:49:15Z","timestamp":1756482555000},"page":"130391","update-policy":"https:\/\/doi.org\/10.1016\/elsevier_cm_policy","source":"Crossref","is-referenced-by-count":3,"special_numbering":"C","title":["Discovery of A20 with 4-(2-methoxyphenyl)-1H-pyrazole scaffold as a potent and selective ROCK2 inhibitor"],"prefix":"10.1016","volume":"129","author":[{"given":"Junzheng","family":"Wang","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Bin","family":"Peng","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Guodong","family":"Liang","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yan","family":"Zhao","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Xin","family":"Gao","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yuting","family":"Zhao","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Lu","family":"Ga","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ruijuan","family":"Li","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yuheng","family":"Ma","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"78","reference":[{"key":"10.1016\/j.bmcl.2025.130391_bb0005","doi-asserted-by":"crossref","first-page":"2383","DOI":"10.1016\/j.bmcl.2016.03.113","article-title":"A review on ROCK-II inhibitors: from molecular modelling to synthesis","volume":"26","author":"Shah","year":"2016","journal-title":"Bioorg Med Chem Lett"},{"key":"10.1016\/j.bmcl.2025.130391_bb0010","doi-asserted-by":"crossref","DOI":"10.1016\/j.phrs.2020.105093","article-title":"Should we keep rocking? Portraits from targeting rho kinases in cancer","volume":"160","author":"de Sousa","year":"2020","journal-title":"Pharmacol Res"},{"key":"10.1016\/j.bmcl.2025.130391_bb0015","doi-asserted-by":"crossref","first-page":"446","DOI":"10.1038\/nrm1128","article-title":"Rocks: multifunctional kinases in cell behaviour","volume":"4","author":"Riento","year":"2003","journal-title":"Nat Rev Mol Cell Biol"},{"key":"10.1016\/j.bmcl.2025.130391_bb0020","doi-asserted-by":"crossref","first-page":"6611","DOI":"10.1016\/j.febslet.2005.10.055","article-title":"Phosphorylation of Thr695 and Thr850 on the myosin phosphatase target subunit: inhibitory effects and occurrence in A7r5 cells","volume":"579","author":"Mur\u00e1nyi","year":"2005","journal-title":"FEBS Lett"},{"key":"10.1016\/j.bmcl.2025.130391_bb0025","doi-asserted-by":"crossref","first-page":"555","DOI":"10.1007\/s00109-007-0165-6","article-title":"LIM kinases: function, regulation and association with human disease","volume":"85","author":"Scott","year":"2007","journal-title":"J Mol Med (Berlin)"},{"key":"10.1016\/j.bmcl.2025.130391_bb0030","doi-asserted-by":"crossref","first-page":"536","DOI":"10.1091\/mbc.e07-08-0818","article-title":"Adducin promotes micrometer-scale organization of beta2-spectrin in lateral membranes of bronchial epithelial cells","volume":"19","author":"Abdi","year":"2008","journal-title":"Mol Biol Cell"},{"key":"10.1016\/j.bmcl.2025.130391_bb0035","doi-asserted-by":"crossref","first-page":"381","DOI":"10.1248\/bpb.b16-01011","article-title":"Pathophysiological roles of Ezrin\/radixin\/Moesin proteins","volume":"40","author":"Kawaguchi","year":"2017","journal-title":"Biol Pharm Bull"},{"key":"10.1016\/j.bmcl.2025.130391_bb0040","doi-asserted-by":"crossref","first-page":"250","DOI":"10.1016\/j.trecan.2022.12.001","article-title":"Preclinical to clinical utility of ROCK inhibitors in cancer","volume":"9","author":"Barcelo","year":"2023","journal-title":"Trends Cancer"},{"key":"10.1016\/j.bmcl.2025.130391_bb0045","doi-asserted-by":"crossref","DOI":"10.3389\/fnins.2024.1481983","article-title":"Role of rho-associated kinases and their inhibitor fasudil in neurodegenerative diseases","volume":"18","author":"Ye","year":"2024","journal-title":"Front Neurosci"},{"key":"10.1016\/j.bmcl.2025.130391_bb0050","doi-asserted-by":"crossref","DOI":"10.3389\/fimmu.2022.858069","article-title":"ROCK inhibition with Y-27632 reduces joint inflammation and damage in serum-induced arthritis model and decreases in vitro osteoclastogenesis in patients with early arthritis","volume":"13","author":"Rodr\u00edguez-Trillo","year":"2022","journal-title":"Front Immunol"},{"key":"10.1016\/j.bmcl.2025.130391_bb0055","doi-asserted-by":"crossref","first-page":"4812","DOI":"10.1016\/j.bmcl.2014.09.002","article-title":"Novel ROCK inhibitors for the treatment of pulmonary arterial hypertension","volume":"24","author":"Shaw","year":"2014","journal-title":"Bioorg Med Chem Lett"},{"key":"10.1016\/j.bmcl.2025.130391_bb0060","doi-asserted-by":"crossref","DOI":"10.1016\/j.bmcl.2021.128138","article-title":"Discovery of 3,4-dihydrobenzo[f][1,4]oxazepin-5(2H)-one derivatives as a new class of ROCK inhibitors for the treatment of glaucoma","volume":"45","author":"Sun","year":"2021","journal-title":"Bioorg Med Chem Lett"},{"key":"10.1016\/j.bmcl.2025.130391_bb0065","doi-asserted-by":"crossref","first-page":"189","DOI":"10.1016\/0014-5793(96)00811-3","article-title":"ROCK-I and ROCK-II, two isoforms of rho-associated coiled-coil forming protein serine\/threonine kinase in mice","volume":"392","author":"Nakagawa","year":"1996","journal-title":"FEBS Lett"},{"key":"10.1016\/j.bmcl.2025.130391_bb0070","doi-asserted-by":"crossref","first-page":"900","DOI":"10.1038\/embor.2012.127","article-title":"Rho-associated kinases in tumorigenesis: re-considering ROCK inhibition for cancer therapy","volume":"13","author":"Rath","year":"2012","journal-title":"EMBO Rep"},{"key":"10.1016\/j.bmcl.2025.130391_bb0075","doi-asserted-by":"crossref","first-page":"295","DOI":"10.1517\/13543776.2014.863279","article-title":"Rho kinase inhibitors: a patent review (2012\u20132013)","volume":"24","author":"Feng","year":"2014","journal-title":"Expert Opin Ther Pat"},{"key":"10.1016\/j.bmcl.2025.130391_bb0080","doi-asserted-by":"crossref","first-page":"1677","DOI":"10.1007\/s40265-021-01593-z","article-title":"Belumosudil: first approval","volume":"81","author":"Blair","year":"2021","journal-title":"Drugs"},{"key":"10.1016\/j.bmcl.2025.130391_bb0085","unstructured":"Clifford D.J., Peter B., Gary P., et al. Preparation of heterocyclylamino-substituted triazoles, especially indazolylaminotriazoles, as modulators of Rho-associated protein kinase: WO2019145729 A1 [P]. 2019-08-01."},{"key":"10.1016\/j.bmcl.2025.130391_bb0090","unstructured":"Hongjun W., Zewang F., Nana T., et al. Solid form of rho-associated protein kinase inhibitor or solvate thereof, preparation method and use thereof: WO2023041026 A1 [P]. 2023-03-23."},{"key":"10.1016\/j.bmcl.2025.130391_bb0095","unstructured":"Joerg R., Matthew D.A., Kenneth M.R., et al. Kinase inhibitors for treatment of disease: WO2019014322 A1 [P]. 2019-01-17."},{"key":"10.1016\/j.bmcl.2025.130391_bb0100","doi-asserted-by":"crossref","first-page":"11074","DOI":"10.1021\/acs.jmedchem.8b01098","article-title":"Identification of selective dual ROCK1 and ROCK2 inhibitors using structure-based drug design","volume":"61","author":"Hobson","year":"2018","journal-title":"J Med Chem"},{"key":"10.1016\/j.bmcl.2025.130391_bb0105","doi-asserted-by":"crossref","first-page":"595","DOI":"10.1002\/cbic.201300723","article-title":"3-substituted indazoles as configurationally locked 4EGI-1 mimetics and inhibitors of the eIF4E\/eIF4G interaction","volume":"15","author":"Yefidoff-Freedman","year":"2014","journal-title":"Chembiochem"}],"container-title":["Bioorganic & Medicinal Chemistry Letters"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0960894X25003002?httpAccept=text\/xml","content-type":"text\/xml","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0960894X25003002?httpAccept=text\/plain","content-type":"text\/plain","content-version":"vor","intended-application":"text-mining"}],"deposited":{"date-parts":[[2026,7,27]],"date-time":"2026-07-27T16:17:11Z","timestamp":1785169031000},"score":1,"resource":{"primary":{"URL":"https:\/\/linkinghub.elsevier.com\/retrieve\/pii\/S0960894X25003002"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2025,12]]},"references-count":21,"alternative-id":["S0960894X25003002"],"URL":"https:\/\/doi.org\/10.1016\/j.bmcl.2025.130391","relation":{},"ISSN":["0960-894X"],"issn-type":[{"value":"0960-894X","type":"print"}],"subject":[],"published":{"date-parts":[[2025,12]]},"assertion":[{"value":"Elsevier","name":"publisher","label":"This article is maintained by"},{"value":"Discovery of A20 with 4-(2-methoxyphenyl)-1H-pyrazole scaffold as a potent and selective ROCK2 inhibitor","name":"articletitle","label":"Article Title"},{"value":"Bioorganic & Medicinal Chemistry Letters","name":"journaltitle","label":"Journal Title"},{"value":"https:\/\/doi.org\/10.1016\/j.bmcl.2025.130391","name":"articlelink","label":"CrossRef DOI link to publisher maintained version"},{"value":"article","name":"content_type","label":"Content Type"},{"value":"\u00a9 2025 Elsevier Ltd. All rights are reserved, including those for text and data mining, AI training, and similar technologies.","name":"copyright","label":"Copyright"}],"article-number":"130391"}}