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Items: 31

1.

Discovery of a First-in-Class Receptor Interacting Protein 2 (RIP2) Kinase Specific Clinical Candidate, 2-((4-(Benzo[d]thiazol-5-ylamino)-6-(tert-butylsulfonyl)quinazolin-7-yl)oxy)ethyl Dihydrogen Phosphate, for the Treatment of Inflammatory Diseases.

Haile PA, Casillas LN, Votta BJ, Wang GZ, Charnley AK, Dong X, Bury MJ, Romano JJ, Mehlmann JF, King BW, Erhard KF, Hanning CR, Lipshutz DB, Desai BM, Capriotti CA, Schaeffer MC, Berger SB, Mahajan MK, Reilly MA, Nagilla R, Rivera EJ, Sun HH, Kenna JK, Beal AM, Ouellette MT, Kelly M, Stemp G, Convery MA, Vossenkämper A, MacDonald TT, Gough PJ, Bertin J, Marquis RW.

J Med Chem. 2019 Jul 25;62(14):6482-6494. doi: 10.1021/acs.jmedchem.9b00575. Epub 2019 Jul 2.

PMID:
31265286
2.

Identification of a RIP1 Kinase Inhibitor Clinical Candidate (GSK3145095) for the Treatment of Pancreatic Cancer.

Harris PA, Marinis JM, Lich JD, Berger SB, Chirala A, Cox JA, Eidam PM, Finger JN, Gough PJ, Jeong JU, Kang J, Kasparcova V, Leister LK, Mahajan MK, Miller G, Nagilla R, Ouellette MT, Reilly MA, Rendina AR, Rivera EJ, Sun HH, Thorpe JH, Totoritis RD, Wang W, Wu D, Zhang D, Bertin J, Marquis RW.

ACS Med Chem Lett. 2019 May 9;10(6):857-862. doi: 10.1021/acsmedchemlett.9b00108. eCollection 2019 Jun 13.

3.

Discovery and Lead-Optimization of 4,5-Dihydropyrazoles as Mono-Kinase Selective, Orally Bioavailable and Efficacious Inhibitors of Receptor Interacting Protein 1 (RIP1) Kinase.

Harris PA, Faucher N, George N, Eidam PM, King BW, White GV, Anderson NA, Bandyopadhyay D, Beal AM, Beneton V, Berger SB, Campobasso N, Campos S, Capriotti CA, Cox JA, Daugan A, Donche F, Fouchet MH, Finger JN, Geddes B, Gough PJ, Grondin P, Hoffman BL, Hoffman SJ, Hutchinson SE, Jeong JU, Jigorel E, Lamoureux P, Leister LK, Lich JD, Mahajan MK, Meslamani J, Mosley JE, Nagilla R, Nassau PM, Ng SL, Ouellette MT, Pasikanti KK, Potvain F, Reilly MA, Rivera EJ, Sautet S, Schaeffer MC, Sehon CA, Sun H, Thorpe JH, Totoritis RD, Ward P, Wellaway N, Wisnoski DD, Woolven JM, Bertin J, Marquis RW.

J Med Chem. 2019 May 23;62(10):5096-5110. doi: 10.1021/acs.jmedchem.9b00318. Epub 2019 May 2.

PMID:
31013427
4.

Identification of Quinoline-Based RIP2 Kinase Inhibitors with an Improved Therapeutic Index to the hERG Ion Channel.

Haile PA, Casillas LN, Bury MJ, Mehlmann JF, Singhaus R Jr, Charnley AK, Hughes TV, DeMartino MP, Wang GZ, Romano JJ, Dong X, Plotnikov NV, Lakdawala AS, Convery MA, Votta BJ, Lipshutz DB, Desai BM, Swift B, Capriotti CA, Berger SB, Mahajan MK, Reilly MA, Rivera EJ, Sun HH, Nagilla R, LePage C, Ouellette MT, Totoritis RD, Donovan BT, Brown BS, Chaudhary KW, Gough PJ, Bertin J, Marquis RW.

ACS Med Chem Lett. 2018 Sep 26;9(10):1039-1044. doi: 10.1021/acsmedchemlett.8b00344. eCollection 2018 Oct 11.

5.

Identification of an antibody-based immunoassay for measuring direct target binding of RIPK1 inhibitors in cells and tissues.

Finger JN, Brusq JM, Campobasso N, Cook MN, Deutsch J, Haag H, Harris PA, Jenkins EL, Joglekar D, Lich JD, Maguire S, Nagilla R, Rivera EJ, Sun H, Votta BJ, Bertin J, Gough PJ.

Pharmacol Res Perspect. 2017 Dec;5(6). doi: 10.1002/prp2.377.

6.

Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases.

Harris PA, Berger SB, Jeong JU, Nagilla R, Bandyopadhyay D, Campobasso N, Capriotti CA, Cox JA, Dare L, Dong X, Eidam PM, Finger JN, Hoffman SJ, Kang J, Kasparcova V, King BW, Lehr R, Lan Y, Leister LK, Lich JD, MacDonald TT, Miller NA, Ouellette MT, Pao CS, Rahman A, Reilly MA, Rendina AR, Rivera EJ, Schaeffer MC, Sehon CA, Singhaus RR, Sun HH, Swift BA, Totoritis RD, Vossenkämper A, Ward P, Wisnoski DD, Zhang D, Marquis RW, Gough PJ, Bertin J.

J Med Chem. 2017 Feb 23;60(4):1247-1261. doi: 10.1021/acs.jmedchem.6b01751. Epub 2017 Feb 10.

PMID:
28151659
7.

The Identification and Pharmacological Characterization of 6-(tert-Butylsulfonyl)-N-(5-fluoro-1H-indazol-3-yl)quinolin-4-amine (GSK583), a Highly Potent and Selective Inhibitor of RIP2 Kinase.

Haile PA, Votta BJ, Marquis RW, Bury MJ, Mehlmann JF, Singhaus R Jr, Charnley AK, Lakdawala AS, Convery MA, Lipshutz DB, Desai BM, Swift B, Capriotti CA, Berger SB, Mahajan MK, Reilly MA, Rivera EJ, Sun HH, Nagilla R, Beal AM, Finger JN, Cook MN, King BW, Ouellette MT, Totoritis RD, Pierdomenico M, Negroni A, Stronati L, Cucchiara S, Ziółkowski B, Vossenkämper A, MacDonald TT, Gough PJ, Bertin J, Casillas LN.

J Med Chem. 2016 May 26;59(10):4867-80. doi: 10.1021/acs.jmedchem.6b00211. Epub 2016 May 4.

PMID:
27109867
8.

DNA-Encoded Library Screening Identifies Benzo[b][1,4]oxazepin-4-ones as Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitors.

Harris PA, King BW, Bandyopadhyay D, Berger SB, Campobasso N, Capriotti CA, Cox JA, Dare L, Dong X, Finger JN, Grady LC, Hoffman SJ, Jeong JU, Kang J, Kasparcova V, Lakdawala AS, Lehr R, McNulty DE, Nagilla R, Ouellette MT, Pao CS, Rendina AR, Schaeffer MC, Summerfield JD, Swift BA, Totoritis RD, Ward P, Zhang A, Zhang D, Marquis RW, Bertin J, Gough PJ.

J Med Chem. 2016 Mar 10;59(5):2163-78. doi: 10.1021/acs.jmedchem.5b01898. Epub 2016 Feb 23.

PMID:
26854747
9.

Characterization of GSK'963: a structurally distinct, potent and selective inhibitor of RIP1 kinase.

Berger SB, Harris P, Nagilla R, Kasparcova V, Hoffman S, Swift B, Dare L, Schaeffer M, Capriotti C, Ouellette M, King BW, Wisnoski D, Cox J, Reilly M, Marquis RW, Bertin J, Gough PJ.

Cell Death Discov. 2015 Jul 27;1:15009. doi: 10.1038/cddiscovery.2015.9. eCollection 2015.

10.

Discovery of Small Molecule RIP1 Kinase Inhibitors for the Treatment of Pathologies Associated with Necroptosis.

Harris PA, Bandyopadhyay D, Berger SB, Campobasso N, Capriotti CA, Cox JA, Dare L, Finger JN, Hoffman SJ, Kahler KM, Lehr R, Lich JD, Nagilla R, Nolte RT, Ouellette MT, Pao CS, Schaeffer MC, Smallwood A, Sun HH, Swift BA, Totoritis RD, Ward P, Marquis RW, Bertin J, Gough PJ.

ACS Med Chem Lett. 2013 Nov 4;4(12):1238-43. doi: 10.1021/ml400382p. eCollection 2013 Dec 12.

11.
12.

Effect of dodecylmaltoside (DDM) on uptake of BCS III compounds, tiludronate and cromolyn, in Caco-2 cells and rat intestine model.

Deshmukh DD, Nagilla R, Ravis WR, Betageri GV.

Drug Deliv. 2010 Apr;17(3):145-51. doi: 10.3109/10717541003604882.

PMID:
20136582
13.

Improving the developability profile of pyrrolidine progesterone receptor partial agonists.

Kallander LS, Washburn DG, Hoang TH, Frazee JS, Stoy P, Johnson L, Lu Q, Hammond M, Barton LS, Patterson JR, Azzarano LM, Nagilla R, Madauss KP, Williams SP, Stewart EL, Duraiswami C, Grygielko ET, Xu X, Laping NJ, Bray JD, Thompson SK.

Bioorg Med Chem Lett. 2010 Jan 1;20(1):371-4. doi: 10.1016/j.bmcl.2009.10.092. Epub 2009 Oct 25.

PMID:
19926282
14.

Discovery of orally active, pyrrolidinone-based progesterone receptor partial agonists.

Washburn DG, Hoang TH, Frazee JS, Johnson L, Hammond M, Manns S, Madauss KP, Williams SP, Duraiswami C, Tran TB, Stewart EL, Grygielko ET, Glace LE, Trizna W, Nagilla R, Bray JD, Thompson SK.

Bioorg Med Chem Lett. 2009 Aug 15;19(16):4664-8. doi: 10.1016/j.bmcl.2009.06.081. Epub 2009 Jun 25.

PMID:
19616429
15.

Design and synthesis of orally bioavailable serum and glucocorticoid-regulated kinase 1 (SGK1) inhibitors.

Hammond M, Washburn DG, Hoang HT, Manns S, Frazee JS, Nakamura H, Patterson JR, Trizna W, Wu C, Azzarano LM, Nagilla R, Nord M, Trejo R, Head MS, Zhao B, Smallwood AM, Hightower K, Laping NJ, Schnackenberg CG, Thompson SK.

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4441-5. doi: 10.1016/j.bmcl.2009.05.051. Epub 2009 May 18.

PMID:
19497745
16.

Discovery of novel aminothiadiazole amides as selective EP(3) receptor antagonists.

Hilfiker MA, Wang N, Hou X, Du Z, Pullen MA, Nord M, Nagilla R, Fries HE, Wu CW, Sulpizio AC, Jaworski JP, Morrow D, Edwards RM, Jin J.

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4292-5. doi: 10.1016/j.bmcl.2009.05.074. Epub 2009 May 27.

PMID:
19487124
17.

Synthesis and SAR of amino acid-derived heterocyclic progesterone receptor full and partial agonists.

Hammond M, Patterson JR, Manns S, Hoang TH, Washburn DG, Trizna W, Glace L, Grygielko ET, Nagilla R, Nord M, Fries HE, Minick DJ, Laping NJ, Bray JD, Thompson SK.

Bioorg Med Chem Lett. 2009 May 15;19(10):2637-41. doi: 10.1016/j.bmcl.2009.03.146. Epub 2009 Apr 5.

PMID:
19376703
18.

Enantiomeric disposition of ketorolac in goats following administration of a single intravenous and oral dose.

Nagilla R, Deshmukh DD, Copedge KJ, Miller S, Martin B, Bell EC, Duran SH, Ravis WR.

J Vet Pharmacol Ther. 2009 Feb;32(1):49-55. doi: 10.1111/j.1365-2885.2008.00999.x.

PMID:
19161455
19.

AMTB, a TRPM8 channel blocker: evidence in rats for activity in overactive bladder and painful bladder syndrome.

Lashinger ES, Steiginga MS, Hieble JP, Leon LA, Gardner SD, Nagilla R, Davenport EA, Hoffman BE, Laping NJ, Su X.

Am J Physiol Renal Physiol. 2008 Sep;295(3):F803-10. doi: 10.1152/ajprenal.90269.2008. Epub 2008 Jun 18.

20.

Potent and selective small-molecule human urotensin-II antagonists with improved pharmacokinetic profiles.

McAtee JJ, Dodson JW, Dowdell SE, Erhard K, Girard GR, Goodman KB, Hilfiker MA, Jin J, Sehon CA, Sha D, Shi D, Wang F, Wang GZ, Wang N, Wang Y, Viet AQ, Yuan CC, Zhang D, Aiyar NV, Behm DJ, Carballo LH, Evans CA, Fries HE, Nagilla R, Roethke TJ, Xu X, Douglas SA, Neeb MJ.

Bioorg Med Chem Lett. 2008 Jul 1;18(13):3716-9. doi: 10.1016/j.bmcl.2008.05.058. Epub 2008 May 20.

PMID:
18524591
21.

Development of potent and selective small-molecule human Urotensin-II antagonists.

McAtee JJ, Dodson JW, Dowdell SE, Girard GR, Goodman KB, Hilfiker MA, Sehon CA, Sha D, Wang GZ, Wang N, Viet AQ, Zhang D, Aiyar NV, Behm DJ, Carballo LH, Evans CA, Fries HE, Nagilla R, Roethke TJ, Xu X, Yuan CC, Douglas SA, Neeb MJ.

Bioorg Med Chem Lett. 2008 Jun 15;18(12):3500-3. doi: 10.1016/j.bmcl.2008.05.027. Epub 2008 May 10.

PMID:
18502123
22.

Stereoselective pharmacokinetics of ketorolac in calves after a single intravenous and oral dose.

Nagilla R, Deshmukh DD, Duran SH, Ravis WR.

J Vet Pharmacol Ther. 2007 Oct;30(5):437-42.

PMID:
17803736
23.

Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.

Evans CA, Jolivette LJ, Nagilla R, Ward KW.

Drug Metab Dispos. 2006 Jul;34(7):1255-65. Epub 2006 Apr 18.

PMID:
16621936
24.

Investigation of the utility of published in vitro intrinsic clearance data for prediction of in vivo clearance.

Nagilla R, Frank KA, Jolivette LJ, Ward KW.

J Pharmacol Toxicol Methods. 2006 Mar-Apr;53(2):106-16. Epub 2005 Sep 26. Review.

PMID:
16188462
25.

Comparative evaluation of oral systemic exposure of 56 xenobiotics in rat, dog, monkey and human.

Ward KW, Nagilla R, Jolivette LJ.

Xenobiotica. 2005 Feb;35(2):191-210.

PMID:
16019946
26.

A comprehensive analysis of the role of correction factors in the allometric predictivity of clearance from rat, dog, and monkey to humans.

Nagilla R, Ward KW.

J Pharm Sci. 2004 Oct;93(10):2522-34. Erratum in: J Pharm Sci. 2005 Jan;94(1):231-2.

PMID:
15349961
27.

Pharmacokinetics of flunixin meglumine in llamas following a single intravenous dose.

Navarre CB, Ravis WR, Nagilla R, Deshmukh D, Simpkins A, Duran SH, Pugh DG.

J Vet Pharmacol Ther. 2001 Oct;24(5):361-4. No abstract available.

PMID:
11696088
28.

Pharmacokinetics of phenylbutazone in llamas following single intravenous and oral doses.

Navarre CB, Ravis WR, Nagilla R, Simpkins A, Duran SH, Pugh DG.

J Vet Pharmacol Ther. 2001 Jun;24(3):227-31. No abstract available.

PMID:
11442803
29.

Stereoselective pharmacokinetics of ketoprofen in llamas following intravenous administration.

Navarre CB, Ravis WR, Campbell J, Nagilla R, Duran SH, Pugh DG.

J Vet Pharmacol Ther. 2001 Jun;24(3):223-6. No abstract available.

PMID:
11442802
30.

Effect of once weekly treatment with 3,4-methylenedioxymethamphetamine on schedule-controlled behavior in rats.

Nagilla R, Newland MC, Snyder J, Bronson ME.

Eur J Pharmacol. 1998 Sep 25;358(1):1-8.

PMID:
9809862
31.

Nasal route for direct delivery of solutes to the central nervous system: fact or fiction?

Mathison S, Nagilla R, Kompella UB.

J Drug Target. 1998;5(6):415-41. Review.

PMID:
9783675

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