{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,5,17]],"date-time":"2026-05-17T04:18:46Z","timestamp":1778991526853,"version":"3.51.4"},"reference-count":17,"publisher":"Pharmaceutical Society of Japan","issue":"3","content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Chem. Pharm. Bull.","CHEMICAL &amp; PHARMACEUTICAL BULLETIN"],"published-print":{"date-parts":[[2019,3,1]]},"DOI":"10.1248\/cpb.c18-00598","type":"journal-article","created":{"date-parts":[[2019,2,28]],"date-time":"2019-02-28T22:31:49Z","timestamp":1551393109000},"page":"224-235","source":"Crossref","is-referenced-by-count":13,"title":["Bis-Heteroaryl Pyrazoles: Identification of Orally Bioavailable Inhibitors of Activin Receptor-Like Kinase-2 (R206H)"],"prefix":"10.1248","volume":"67","author":[{"given":"Katsuhiko","family":"Sekimata","sequence":"first","affiliation":[{"name":"Drug Discovery Chemistry Platform Unit, RIKEN Center for Sustainable Resource Science"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Tomohiro","family":"Sato","sequence":"additional","affiliation":[{"name":"Drug Discovery Computational Chemistry Platform Unit, RIKEN Center for Biosystems Dynamics Research"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Naoki","family":"Sakai","sequence":"additional","affiliation":[{"name":"Drug Discovery Structural Biology Platform Unit, RIKEN Biosystems Dynamics Research"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Hisami","family":"Watanabe","sequence":"additional","affiliation":[{"name":"Drug Discovery Structural Biology Platform Unit, RIKEN Biosystems Dynamics Research"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Chiemi","family":"Mishima-Tsumagari","sequence":"additional","affiliation":[{"name":"Drug Discovery Structural Biology Platform Unit, RIKEN Biosystems Dynamics Research"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Tomonori","family":"Taguri","sequence":"additional","affiliation":[{"name":"Drug Discovery Chemistry Platform Unit, RIKEN Center for Sustainable Resource Science"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Takehisa","family":"Matsumoto","sequence":"additional","affiliation":[{"name":"Drug Discovery Structural Biology Platform Unit, RIKEN Biosystems Dynamics Research"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Yoshifumi","family":"Fujii","sequence":"additional","affiliation":[{"name":"Crystallographic Drug Discovery Platform Unit, RIKEN Systems and Structural Biology Center"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Noriko","family":"Handa","sequence":"additional","affiliation":[{"name":"Crystallographic Drug Discovery Platform Unit, RIKEN Systems and Structural Biology Center"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Teruki","family":"Honma","sequence":"additional","affiliation":[{"name":"Drug Discovery Computational Chemistry Platform Unit, RIKEN Center for Biosystems Dynamics Research"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Akiko","family":"Tanaka","sequence":"additional","affiliation":[{"name":"Drug Discovery Structural Biology Platform Unit, RIKEN Biosystems Dynamics Research"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Mikako","family":"Shirouzu","sequence":"additional","affiliation":[{"name":"Drug Discovery Structural Biology Platform Unit, RIKEN Biosystems Dynamics Research"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Shigeyuki","family":"Yokoyama","sequence":"additional","affiliation":[{"name":"Crystallographic Drug Discovery Platform Unit, RIKEN Systems and Structural Biology Center"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Kohei","family":"Miyazono","sequence":"additional","affiliation":[{"name":"Department of Molecular Pathology, Graduate School of Medicine, The University of Tokyo"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Yoshinobu","family":"Hashizume","sequence":"additional","affiliation":[{"name":"RIKEN Program for Drug Discovery and Medical Technology Platforms"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Hiroo","family":"Koyama","sequence":"additional","affiliation":[{"name":"Drug Discovery Chemistry Platform Unit, RIKEN Center for Sustainable Resource Science"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"163","reference":[{"key":"1","doi-asserted-by":"crossref","unstructured":"1) Shore E. M., Xu M., Feldman G. J., Fenstermacher D. A., Cho T. J., Choi I. H., Connor J. M., Delai P., Glaser D. L., LeMerrer M., Morhart R., Rogers J. G., Smith R., Triffitt J. T., Urtizberea J. A., Zasloff M., Brown M. A., Kaplan F. S., <i>Nat. Genet.<\/i>, <b>38<\/b>, 525\u2013527 (2006).","DOI":"10.1038\/ng1783"},{"key":"2","doi-asserted-by":"crossref","unstructured":"2) Cappato S., Giacopelli F., Ravazzolo R., Bocciardi R., <i>Int. J. Mol. Sci.<\/i>, <b>19<\/b>, 989 (2018).","DOI":"10.3390\/ijms19040989"},{"key":"3","doi-asserted-by":"crossref","unstructured":"3) Buczkowicz P., Hoeman C., Rakopoulos P., Pajovic S., Letourneau L., Dzamba M., Morrison A., Lewis P., Bouffet E., Bartels U., Zuccaro J., Agnihotri S., Ryall S., Barszczyk M., Chornenkyy Y., Bourgey M., Bourque G., Montpetit A., Cordero F., Castelo-Branco P., Mangerel J., Tabori U., Ho K. C., Huang A., Taylor K. R., Mackay A., Bendel A. E., Nazarian J., Fangusaro J. R., Karajannis M. A., Zagzag D., Foreman N. K., Donson A., Hegert J. V., Smith A., Chan J., Lafay-Cousin L., Dunn S., Hukin J., Dunham C., Scheinemann K., Michaud J., Zelcer S., Ramsay D., Cain J., Brennan C., Souweidane M. M., Jones C., Allis C. D., Brudno M., Becher O., Hawkins C., <i>Nat. Genet.<\/i>, <b>46<\/b>, 451\u2013456 (2014).","DOI":"10.1038\/ng.2936"},{"key":"4","doi-asserted-by":"crossref","unstructured":"4) Pacifici M., Shore E. M., <i>Cytokine Growth Factor Rev.<\/i>, <b>27<\/b>, 93\u2013104 (2016).","DOI":"10.1016\/j.cytogfr.2015.12.007"},{"key":"5","doi-asserted-by":"crossref","unstructured":"5) Mohedas A. H., Xing X., Armstrong K. A., Bullock A. N., Cuny G. D., Yu P. B., <i>ACS Chem. Biol.<\/i>, <b>8<\/b>, 1291\u20131302 (2013).","DOI":"10.1021\/cb300655w"},{"key":"6","doi-asserted-by":"crossref","unstructured":"6) Sliwoski G. I., Kothiwale S., Meiler J., Lowe E. W. Jr., <i>Pharmacol. Rev.<\/i>, <b>66<\/b>, 334\u2013395 (2013).","DOI":"10.1124\/pr.112.007336"},{"key":"7","unstructured":"7) Detailed <i>in silico<\/i> and <i>in vitro<\/i> screening studies will be published elsewhere."},{"key":"8","unstructured":"8) Hashizume Y., Sekimata K., Kubota H., Yamamoto H., Koda Y., Koyama H., Taguri T., Sato T., Tanaka A., Miyazono K., Patent WO 2018\/124001 (A1) (2018)."},{"key":"9","doi-asserted-by":"crossref","unstructured":"9) Cho Y. S., Borland M., Brain C., Chen C. H., Cheng H., Chopra R., Chung K., Groarke J., He G., Hou Y., Kim S., Kovats S., Lu Y., O\u2019Reilly M., Shen J., Smith T., Trakshel G., V\u00f6gtle M., Xu M., Xu M., Sung M. J., <i>J. Med. Chem.<\/i>, <b>53<\/b>, 7938\u20137957 (2010).","DOI":"10.1021\/jm100571n"},{"key":"10","doi-asserted-by":"crossref","unstructured":"10) Ralph J. M., Faitg T. H., Silva D. J., Feng Y., Blackledge C. W., Adams J. L., <i>Tetrahedron Lett.<\/i>, <b>50<\/b>, 1377\u20131380 (2009).","DOI":"10.1016\/j.tetlet.2008.12.113"},{"key":"11","doi-asserted-by":"crossref","unstructured":"11) Hocek M., Votruba I., Dvorakova H., <i>Tetrahedron<\/i>, <b>59<\/b>, 607\u2013611 (2003).","DOI":"10.1016\/S0040-4020(02)01586-7"},{"key":"12","doi-asserted-by":"crossref","unstructured":"12) Kabsch W., <i>Acta Crystallogr. D Biol. Crystallogr.<\/i>, <b>66<\/b>, 125\u2013132 (2010).","DOI":"10.1107\/S0907444909047337"},{"key":"13","doi-asserted-by":"crossref","unstructured":"13) Winn M. D., Ballard C. C., Cowtan K. D., Dodson E. J., Emsley P., Evans P. R., Keegan R. M., Krissinel E. B., Leslie A. G. W., McCoy A., McNicholas S. J., Murshudov G. N., Pannu N. S., Potterton E. A., Powell H. R., Read R. J., Vagin A., Wilson K. S., <i>Acta Crystallogr. D Biol. Crystallogr.<\/i>, <b>67<\/b>, 235\u2013242 (2011).","DOI":"10.1107\/S0907444910045749"},{"key":"14","doi-asserted-by":"crossref","unstructured":"14) Vagin A. A., Isupov M. N., <i>Acta Crystallogr. D Biol. Crystallogr.<\/i>, <b>57<\/b>, 1451\u20131456 (2001).","DOI":"10.1107\/S0907444901012409"},{"key":"15","doi-asserted-by":"crossref","unstructured":"15) Adams P. D., Afonine P. V., Bunkoczi G., Chen V. B., Davis I. W., Echols N., Headd J. J., Hung L.-W., Kapral G. J., Grosse-Kunstleve R. W., McCoy A. J., Moriarty N. W., Oeffner R., Read R. J., Richardson D. C., Richardson J. S., Terwilliger T. C., Zwart P. H., <i>Acta Crystallogr. D Biol. Crystallogr.<\/i>, <b>66<\/b>, 213\u2013221 (2010).","DOI":"10.1107\/S0907444909052925"},{"key":"16","doi-asserted-by":"crossref","unstructured":"16) Emsley P., Lohkamp B., Scott W. G., Cowtan K., <i>Acta Crystallogr. D Biol. Crystallogr.<\/i>, <b>66<\/b>, 486\u2013501 (2010).","DOI":"10.1107\/S0907444910007493"},{"key":"17","doi-asserted-by":"crossref","unstructured":"17) Tabata K., Yamaoko K., Kaibara A., Suzuki S., <i>Xenobio. Meta. Dispos.<\/i>, <b>14<\/b>, 286\u2013293 (1999).","DOI":"10.2133\/dmpk.14.286"}],"container-title":["Chemical and Pharmaceutical Bulletin"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/www.jstage.jst.go.jp\/article\/cpb\/67\/3\/67_c18-00598\/_pdf","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2019,11,19]],"date-time":"2019-11-19T18:58:26Z","timestamp":1574189906000},"score":1,"resource":{"primary":{"URL":"https:\/\/www.jstage.jst.go.jp\/article\/cpb\/67\/3\/67_c18-00598\/_article"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2019,3,1]]},"references-count":17,"journal-issue":{"issue":"3","published-print":{"date-parts":[[2019]]}},"URL":"https:\/\/doi.org\/10.1248\/cpb.c18-00598","relation":{},"ISSN":["0009-2363","1347-5223"],"issn-type":[{"value":"0009-2363","type":"print"},{"value":"1347-5223","type":"electronic"}],"subject":[],"published":{"date-parts":[[2019,3,1]]}}}