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Page 1
Screening Hit to Clinical Candidate: Discovery of BMS-963272, a Potent, Selective MGAT2 Inhibitor for the Treatment of Metabolic Disorders.
Turdi H, Chao H, Hangeland JJ, Ahmad S, Meng W, Brigance R, Zhao G, Wang W, Moore F, Ye XY, Mathur A, Hou X, Kempson J, Wu DR, Li YX, Azzara AV, Ma Z, Chu CH, Chen L, Cullen MJ, Rooney S, Harvey S, Kopcho L, Panemangelor R, Abell L, O'Malley K, Keim WJ, Dierks E, Chang S, Foster K, Apedo A, Harden D, Dabros M, Gao Q, Pelleymounter MA, Whaley JM, Robl JA, Cheng D, Lawrence RM, Devasthale P. Turdi H, et al. Among authors: keim wj. J Med Chem. 2021 Oct 14;64(19):14773-14792. doi: 10.1021/acs.jmedchem.1c01356. Epub 2021 Oct 6. J Med Chem. 2021. PMID: 34613725
Synthesis and SAR of potent and selective tetrahydropyrazinoisoquinolinone 5-HT(2C) receptor agonists.
Zhao G, Kwon C, Bisaha SN, Stein PD, Rossi KA, Cao X, Ung T, Wu G, Hung CP, Malmstrom SE, Zhang G, Qu Q, Gan J, Keim WJ, Cullen MJ, Rohrbach KW, Devenny J, Pelleymounter MA, Miller KJ, Robl JA. Zhao G, et al. Among authors: keim wj. Bioorg Med Chem Lett. 2013 Jul 1;23(13):3914-9. doi: 10.1016/j.bmcl.2013.04.061. Epub 2013 Apr 29. Bioorg Med Chem Lett. 2013. PMID: 23683593
Tricyclic dihydroquinazolinones as novel 5-HT2C selective and orally efficacious anti-obesity agents.
Ahmad S, Ngu K, Miller KJ, Wu G, Hung CP, Malmstrom S, Zhang G, O'Tanyi E, Keim WJ, Cullen MJ, Rohrbach KW, Thomas M, Ung T, Qu Q, Gan J, Narayanan R, Pelleymounter MA, Robl JA. Ahmad S, et al. Among authors: keim wj. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1128-33. doi: 10.1016/j.bmcl.2009.12.014. Epub 2009 Dec 6. Bioorg Med Chem Lett. 2010. PMID: 20022752
Acylation of acylglycerols by acyl coenzyme A:diacylglycerol acyltransferase 1 (DGAT1). Functional importance of DGAT1 in the intestinal fat absorption.
Cheng D, Iqbal J, Devenny J, Chu CH, Chen L, Dong J, Seethala R, Keim WJ, Azzara AV, Lawrence RM, Pelleymounter MA, Hussain MM. Cheng D, et al. Among authors: keim wj. J Biol Chem. 2008 Oct 31;283(44):29802-11. doi: 10.1074/jbc.M800494200. Epub 2008 Sep 3. J Biol Chem. 2008. PMID: 18768481 Free PMC article.
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: keim wj. J Med Chem. 2013 Dec 12;56(23):9586-600. doi: 10.1021/jm4010835. Epub 2013 Nov 20. J Med Chem. 2013. PMID: 24182233
Discovery of (R)-9-ethyl-1,3,4,10b-tetrahydro-7-trifluoromethylpyrazino[2,1-a]isoindol- 6(2H)-one, a selective, orally active agonist of the 5-HT(2C) receptor.
Wacker DA, Varnes JG, Malmstrom SE, Cao X, Hung CP, Ung T, Wu G, Zhang G, Zuvich E, Thomas MA, Keim WJ, Cullen MJ, Rohrbach KW, Qu Q, Narayanan R, Rossi K, Janovitz E, Lehman-McKeeman L, Malley MF, Devenny J, Pelleymounter MA, Miller KJ, Robl JA. Wacker DA, et al. Among authors: keim wj. J Med Chem. 2007 Mar 22;50(6):1365-79. doi: 10.1021/jm0612968. Epub 2007 Feb 23. J Med Chem. 2007. PMID: 17315987