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Page 1
Discovery of a Parenteral Small Molecule Coagulation Factor XIa Inhibitor Clinical Candidate (BMS-962212).
Pinto DJP, Orwat MJ, Smith LM 2nd, Quan ML, Lam PYS, Rossi KA, Apedo A, Bozarth JM, Wu Y, Zheng JJ, Xin B, Toussaint N, Stetsko P, Gudmundsson O, Maxwell B, Crain EJ, Wong PC, Lou Z, Harper TW, Chacko SA, Myers JE Jr, Sheriff S, Zhang H, Hou X, Mathur A, Seiffert DA, Wexler RR, Luettgen JM, Ewing WR. Pinto DJP, et al. Among authors: stetsko p. J Med Chem. 2017 Dec 14;60(23):9703-9723. doi: 10.1021/acs.jmedchem.7b01171. Epub 2017 Nov 17. J Med Chem. 2017. PMID: 29077405
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: stetsko p. J Med Chem. 2014 Sep 25;57(18):7509-22. doi: 10.1021/jm500026w. Epub 2014 Sep 9. J Med Chem. 2014. PMID: 25165888
Reductions in log P improved protein binding and clearance predictions enabling the prospective design of cannabinoid receptor (CB1) antagonists with desired pharmacokinetic properties.
Ellsworth BA, Sher PM, Wu X, Wu G, Sulsky RB, Gu Z, Murugesan N, Zhu Y, Yu G, Sitkoff DF, Carlson KE, Kang L, Yang Y, Lee N, Baska RA, Keim WJ, Cullen MJ, Azzara AV, Zuvich E, Thomas MA, Rohrbach KW, Devenny JJ, Godonis HE, Harvey SJ, Murphy BJ, Everlof GG, Stetsko PI, Gudmundsson O, Johnghar S, Ranasinghe A, Behnia K, Pelleymounter MA, Ewing WR. Ellsworth BA, et al. Among authors: stetsko pi. J Med Chem. 2013 Dec 12;56(23):9586-600. doi: 10.1021/jm4010835. Epub 2013 Nov 20. J Med Chem. 2013. PMID: 24182233
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: stetsko p. 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
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: stetsko p. 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
Pharmacodynamics-based approach for efficacious human dose projection of BMS-986260, a small molecule transforming growth factor beta receptor 1 inhibitor.
Parrish KE, Swanson J, Cheng L, Luk E, Stetsko P, Smalley J, Shu YZ, Huang J, Pabalan JG, Sun Y, Zvyaga T, Cvijic ME, Burke J, Borzilleri R, Murtaza A, Augustine K, Yang Z. Parrish KE, et al. Among authors: stetsko p. Biopharm Drug Dispos. 2021 Apr;42(4):137-149. doi: 10.1002/bdd.2256. Epub 2021 Jan 8. Biopharm Drug Dispos. 2021. PMID: 33354831
Estimation of the extent of in vivo formation of a mutagenic aromatic amine from a potent thyromimetic compound: correlation of in vitro and in vivo findings.
Behnia K, Cornelius G, Wang J, Shipkova P, Johnghar S, Washburn W, Brigance R, Stetsko P, Henwood A, Wojciechowski JP, Marathe P, Rodrigues AD, Humphreys WG. Behnia K, et al. Among authors: stetsko p. Chem Res Toxicol. 2011 Jun 20;24(6):905-12. doi: 10.1021/tx200087q. Epub 2011 Jun 1. Chem Res Toxicol. 2011. PMID: 21574629
19 results