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Dihydropyrrolopyrazol-6-one MCHR1 antagonists for the treatment of obesity: Insights on in vivo efficacy from a novel FLIPR assay setup.
Devasthale P, Wang W, Hernandez AS, Moore F, Renduchintala K, Sridhar R, Pelleymounter MA, Longhi D, Huang N, Flynn N, Azzara AV, Rohrbach K, Devenny J, Rooney S, Thomas M, Glick S, Godonis H, Harvey S, Cullen MJ, Zhang H, Caporuscio C, Stetsko P, Grubb M, Huang C, Zhang L, Freeden C, Li YX, Murphy BJ, Robl JA, Washburn WN. Devasthale P, et al. Among authors: zhang l, zhang h. Bioorg Med Chem Lett. 2015 Jul 15;25(14):2793-9. doi: 10.1016/j.bmcl.2015.05.008. Epub 2015 May 15. Bioorg Med Chem Lett. 2015. PMID: 26022839
Identification of a nonbasic melanin hormone receptor 1 antagonist as an antiobesity clinical candidate.
Washburn WN, Manfredi M, Devasthale P, Zhao G, Ahmad S, Hernandez A, Robl JA, Wang W, Mignone J, Wang Z, Ngu K, Pelleymounter MA, Longhi D, Zhao R, Wang B, Huang N, Flynn N, Azzara AV, Barrish JC, Rohrbach K, Devenny JJ, Rooney S, Thomas M, Glick S, Godonis HE, Harvey SJ, Cullen MJ, Zhang H, Caporuscio C, Stetsko P, Grubb M, Maxwell BD, Yang H, Apedo A, Gemzik B, Janovitz EB, Huang C, Zhang L, Freeden C, Murphy BJ. Washburn WN, et al. Among authors: zhang l, zhang h. J Med Chem. 2014 Sep 25;57(18):7509-22. doi: 10.1021/jm500026w. Epub 2014 Sep 9. J Med Chem. 2014. PMID: 25165888
Non-basic azolotriazinone MCHR1 antagonists for the treatment of obesity: An empirical brain-exposures-driven candidate selection for in vivo efficacy studies.
Devasthale P, Wang W, Mignone J, Renduchintala K, Radhakrishnan S, Dhanapal J, Selvaraj J, Kuppusamy R, Pelleymounter MA, Longhi D, Huang N, Flynn N, Azzara AV, Rohrbach K, Devenny J, Rooney S, Thomas M, Glick S, Godonis H, Harvey S, Cullen MJ, Zhang H, Caporuscio C, Stetsko P, Grubb M, Huang C, Zhang L, Freeden C, Murphy BJ, Robl JA, Washburn WN. Devasthale P, et al. Among authors: zhang l, zhang h. Bioorg Med Chem Lett. 2015 Oct 15;25(20):4412-8. doi: 10.1016/j.bmcl.2015.09.018. Epub 2015 Sep 8. Bioorg Med Chem Lett. 2015. PMID: 26386604
Synthesis and Antiobesity Properties of 6-(4-Chlorophenyl)-3-(4-((3,3-difluoro-1-hydroxycyclobutyl)methoxy)-3-methoxyphenyl)thieno[3,2-d]pyrimidin-4(3H)-one (BMS-814580): A Highly Efficacious Melanin Concentrating Hormone Receptor 1 (MCHR1) Inhibitor.
Ahmad S, Washburn WN, Hernandez AS, Bisaha S, Ngu K, Wang W, Pelleymounter MA, Longhi D, Flynn N, Azzara AV, Rohrbach K, Devenny J, Rooney S, Thomas M, Glick S, Godonis H, Harvey S, Zhang H, Gemzik B, Janovitz EB, Huang C, Zhang L, Robl JA, Murphy BJ. Ahmad S, et al. Among authors: zhang l, zhang h. J Med Chem. 2016 Oct 13;59(19):8848-8858. doi: 10.1021/acs.jmedchem.6b00676. Epub 2016 Sep 15. J Med Chem. 2016. PMID: 27564419
Discovery of a phenylpyrazole amide ROCK inhibitor as a tool molecule for in vivo studies.
Hu Z, Wang C, Glunz PW, Li J, Cheadle NL, Chen AY, Chen XQ, Myers JE, Guarino VR, Rose A, Sack JS, Sitkoff D, Taylor DS, Xu S, Yan C, Zhang H, Zhang L, Hennan J, Adam LP, Wexler RR, Quan ML. Hu Z, et al. Among authors: zhang l, zhang h. Bioorg Med Chem Lett. 2020 Nov 1;30(21):127495. doi: 10.1016/j.bmcl.2020.127495. Epub 2020 Aug 13. Bioorg Med Chem Lett. 2020. PMID: 32798651
A novel function of CXCL10 in mediating monocyte production of proinflammatory cytokines.
Zhao Q, Kim T, Pang J, Sun W, Yang X, Wang J, Song Y, Zhang H, Sun H, Rangan V, Deshpande S, Tang H, Cvijic ME, Westhouse R, Olah T, Xie J, Struthers M, Salter-Cid L. Zhao Q, et al. Among authors: zhang h. J Leukoc Biol. 2017 Nov;102(5):1271-1280. doi: 10.1189/jlb.5A0717-302. Epub 2017 Sep 12. J Leukoc Biol. 2017. PMID: 28899907
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