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Items: 35

1.

Discovery of a JAK1/3 Inhibitor and Use of a Prodrug To Demonstrate Efficacy in a Model of Rheumatoid Arthritis.

Spergel SH, Mertzman ME, Kempson J, Guo J, Stachura S, Haque L, Lippy JS, Zhang RF, Galella M, Pitt S, Shen G, Fura A, Gillooly K, McIntyre KW, Tang V, Tokarski J, Sack JS, Khan J, Carter PH, Barrish JC, Nadler SG, Salter-Cid LM, Schieven GL, Wrobleski ST, Pitts WJ.

ACS Med Chem Lett. 2019 Feb 13;10(3):306-311. doi: 10.1021/acsmedchemlett.8b00508. eCollection 2019 Mar 14.

PMID:
30891131
2.

Discovery of 4-Azaindole Inhibitors of TGFβRI as Immuno-oncology Agents.

Zhang Y, Zhao Y, Tebben AJ, Sheriff S, Ruzanov M, Fereshteh MP, Fan Y, Lippy J, Swanson J, Ho CP, Wautlet BS, Rose A, Parrish K, Yang Z, Donnell AF, Zhang L, Fink BE, Vite GD, Augustine-Rauch K, Fargnoli J, Borzilleri RM.

ACS Med Chem Lett. 2018 Oct 17;9(11):1117-1122. doi: 10.1021/acsmedchemlett.8b00357. eCollection 2018 Nov 8.

PMID:
30429955
3.

Conversion of carbazole carboxamide based reversible inhibitors of Bruton's tyrosine kinase (BTK) into potent, selective irreversible inhibitors in the carbazole, tetrahydrocarbazole, and a new 2,3-dimethylindole series.

Liu Q, Batt DG, Chaudhry C, Lippy JS, Pattoli MA, Surti N, Xu S, Carter PH, Burke JR, Tino JA.

Bioorg Med Chem Lett. 2018 Oct 1;28(18):3080-3084. doi: 10.1016/j.bmcl.2018.07.041. Epub 2018 Jul 30.

PMID:
30097367
4.

Miniaturized High-Throughput Multiparameter Flow Cytometry Assays Measuring In Vitro Human Dendritic Cell Maturation and T-Cell Activation in Mixed Lymphocyte Reactions.

Fan Y, Naglich JG, Koenitzer JD, Ribeiro H, Lippy J, Blum J, Li X, Milburn C, Barnhart B, Zhang L, Fereshteh MP.

SLAS Discov. 2018 Aug;23(7):742-750. doi: 10.1177/2472555218775409. Epub 2018 Jun 6.

PMID:
29873570
5.

Heterobicyclic inhibitors of transforming growth factor beta receptor I (TGFβRI).

Harikrishnan LS, Warrier J, Tebben AJ, Tonukunuru G, Madduri SR, Baligar V, Mannoori R, Seshadri B, Rahaman H, Arunachalam PN, Dikundwar AG, Fink BE, Fargnoli J, Fereshteh M, Fan Y, Lippy J, Ho CP, Wautlet B, Sheriff S, Ruzanov M, Borzilleri RM.

Bioorg Med Chem. 2018 Mar 1;26(5):1026-1034. doi: 10.1016/j.bmc.2018.01.014. Epub 2018 Jan 31.

PMID:
29422332
6.

Leveraging the IncuCyte Technology for Higher-Throughput and Automated Chemotaxis Assays for Target Validation and Compound Characterization.

Chen J, Ribeiro B, Li H, Myer L, Chase P, Surti N, Lippy J, Zhang L, Cvijic ME.

SLAS Discov. 2018 Feb;23(2):122-131. doi: 10.1177/2472555217733437. Epub 2017 Sep 28.

PMID:
28957636
7.

Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinase δ (PI3Kδ) Inhibitor for the Treatment of Immunological Disorders.

Liu Q, Shi Q, Marcoux D, Batt DG, Cornelius L, Qin LY, Ruan Z, Neels J, Beaudoin-Bertrand M, Srivastava AS, Li L, Cherney RJ, Gong H, Watterson SH, Weigelt C, Gillooly KM, McIntyre KW, Xie JH, Obermeier MT, Fura A, Sleczka B, Stefanski K, Fancher RM, Padmanabhan S, Rp T, Kundu I, Rajareddy K, Smith R, Hennan JK, Xing D, Fan J, Levesque PC, Ruan Q, Pitt S, Zhang R, Pedicord D, Pan J, Yarde M, Lu H, Lippy J, Goldstine C, Skala S, Rampulla RA, Mathur A, Gupta A, Arunachalam PN, Sack JS, Muckelbauer JK, Cvijic ME, Salter-Cid LM, Bhide RS, Poss MA, Hynes J, Carter PH, Macor JE, Ruepp S, Schieven GL, Tino JA.

J Med Chem. 2017 Jun 22;60(12):5193-5208. doi: 10.1021/acs.jmedchem.7b00618. Epub 2017 Jun 5.

PMID:
28541707
8.

Discovery of potent and efficacious pyrrolopyridazines as dual JAK1/3 inhibitors.

Hynes J Jr, Wu H, Kempson J, Duan JJ, Lu Z, Jiang B, Stachura S, Tokarski JS, Sack JS, Khan JA, Lippy JS, Zhang RF, Pitt S, Shen G, Gillooly K, McIntyre K, Carter PH, Barrish JC, Nadler SG, Salter-Cid LM, Fura A, Schieven GL, Pitts WJ, Wrobleski ST.

Bioorg Med Chem Lett. 2017 Jul 15;27(14):3101-3106. doi: 10.1016/j.bmcl.2017.05.043. Epub 2017 May 15.

PMID:
28539220
9.

Inhibition of AAK1 Kinase as a Novel Therapeutic Approach to Treat Neuropathic Pain.

Kostich W, Hamman BD, Li YW, Naidu S, Dandapani K, Feng J, Easton A, Bourin C, Baker K, Allen J, Savelieva K, Louis JV, Dokania M, Elavazhagan S, Vattikundala P, Sharma V, Das ML, Shankar G, Kumar A, Holenarsipur VK, Gulianello M, Molski T, Brown JM, Lewis M, Huang Y, Lu Y, Pieschl R, O'Malley K, Lippy J, Nouraldeen A, Lanthorn TH, Ye G, Wilson A, Balakrishnan A, Denton R, Grace JE, Lentz KA, Santone KS, Bi Y, Main A, Swaffield J, Carson K, Mandlekar S, Vikramadithyan RK, Nara SJ, Dzierba C, Bronson J, Macor JE, Zaczek R, Westphal R, Kiss L, Bristow L, Conway CM, Zambrowicz B, Albright CF.

J Pharmacol Exp Ther. 2016 Sep;358(3):371-86. doi: 10.1124/jpet.116.235333. Epub 2016 Jul 13.

10.

Development of a Human Whole Blood Screening Platform to Monitor JAK/STAT Signaling Using High-Throughput Flow Cytometry.

Fereshteh MP, Li X, Li S, Fan Y, Zhang R, Farr GA, Kolodin G, Lippy J, Naglich JG, Schieven G, Schweizer L, Zhang L.

J Biomol Screen. 2016 Sep;21(8):866-74. doi: 10.1177/1087057116645095. Epub 2016 May 3.

PMID:
27142718
11.

Discovery of Isonicotinamides as Highly Selective, Brain Penetrable, and Orally Active Glycogen Synthase Kinase-3 Inhibitors.

Luo G, Chen L, Burton CR, Xiao H, Sivaprakasam P, Krause CM, Cao Y, Liu N, Lippy J, Clarke WJ, Snow K, Raybon J, Arora V, Pokross M, Kish K, Lewis HA, Langley DR, Macor JE, Dubowchik GM.

J Med Chem. 2016 Feb 11;59(3):1041-51. doi: 10.1021/acs.jmedchem.5b01550. Epub 2016 Jan 22.

PMID:
26751161
12.

Design and synthesis of carbazole carboxamides as promising inhibitors of Bruton's tyrosine kinase (BTK) and Janus kinase 2 (JAK2).

Liu Q, Batt DG, Lippy JS, Surti N, Tebben AJ, Muckelbauer JK, Chen L, An Y, Chang C, Pokross M, Yang Z, Wang H, Burke JR, Carter PH, Tino JA.

Bioorg Med Chem Lett. 2015 Oct 1;25(19):4265-9. doi: 10.1016/j.bmcl.2015.07.102. Epub 2015 Aug 6.

PMID:
26320619
13.

Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms.

Wan H, Schroeder GM, Hart AC, Inghrim J, Grebinski J, Tokarski JS, Lorenzi MV, You D, Mcdevitt T, Penhallow B, Vuppugalla R, Zhang Y, Gu X, Iyer R, Lombardo LJ, Trainor GL, Ruepp S, Lippy J, Blat Y, Sack JS, Khan JA, Stefanski K, Sleczka B, Mathur A, Sun JH, Wong MK, Wu DR, Li P, Gupta A, Arunachalam PN, Pragalathan B, Narayanan S, K C N, Kuppusamy P, Purandare AV.

ACS Med Chem Lett. 2015 Jul 12;6(8):850-5. doi: 10.1021/acsmedchemlett.5b00226. eCollection 2015 Aug 13.

14.

Structure-Based Design of Selective Janus Kinase 2 Imidazo[4,5-d]pyrrolo[2,3-b]pyridine Inhibitors.

Hart AC, Schroeder GM, Wan H, Grebinski J, Inghrim J, Kempson J, Guo J, Pitts WJ, Tokarski JS, Sack JS, Khan JA, Lippy J, Lorenzi MV, You D, McDevitt T, Vuppugalla R, Zhang Y, Lombardo LJ, Trainor GL, Purandare AV.

ACS Med Chem Lett. 2015 Jul 10;6(8):845-9. doi: 10.1021/acsmedchemlett.5b00225. eCollection 2015 Aug 13.

15.

9H-Carbazole-1-carboxamides as potent and selective JAK2 inhibitors.

Zimmermann K, Sang X, Mastalerz HA, Johnson WL, Zhang G, Liu Q, Batt D, Lombardo LJ, Vyas D, Trainor GL, Tokarski JS, Lorenzi MV, You D, Gottardis MM, Lippy J, Khan J, Sack JS, Purandare AV.

Bioorg Med Chem Lett. 2015 Jul 15;25(14):2809-12. doi: 10.1016/j.bmcl.2015.04.101. Epub 2015 May 11.

PMID:
25987372
16.

Discovery of new acylaminopyridines as GSK-3 inhibitors by a structure guided in-depth exploration of chemical space around a pyrrolopyridinone core.

Sivaprakasam P, Han X, Civiello RL, Jacutin-Porte S, Kish K, Pokross M, Lewis HA, Ahmed N, Szapiel N, Newitt JA, Baldwin ET, Xiao H, Krause CM, Park H, Nophsker M, Lippy JS, Burton CR, Langley DR, Macor JE, Dubowchik GM.

Bioorg Med Chem Lett. 2015 May 1;25(9):1856-63. doi: 10.1016/j.bmcl.2015.03.046. Epub 2015 Mar 24.

PMID:
25845281
17.

Synthesis and biological evaluation of novel pyrrolidine acid analogs as potent dual PPARα/γ agonists.

Zhang H, Ding CZ, Lai Z, Chen SS, Devasthale P, Herpin T, Morton G, Qu F, Ryono D, Smirk R, Wang W, Wu S, Ye XX, Li YX, Apedo A, Farrelly D, Wang T, Gu L, Morgan N, Flynn N, Chu C, Kunselman L, Lippy J, Locke K, O'Malley K, Harrity T, Cap M, Zhang L, Hosagrahara V, Kadiyala P, Xu C, Doweyko AM, Zahler R, Hariharan N, Cheng PT.

Bioorg Med Chem Lett. 2015 Mar 15;25(6):1196-205. doi: 10.1016/j.bmcl.2015.01.066. Epub 2015 Feb 4.

PMID:
25686852
18.

Discovery of pyrrolo[1,2-b]pyridazine-3-carboxamides as Janus kinase (JAK) inhibitors.

Duan JJ, Lu Z, Jiang B, Yang BV, Doweyko LM, Nirschl DS, Haque LE, Lin S, Brown G, Hynes J Jr, Tokarski JS, Sack JS, Khan J, Lippy JS, Zhang RF, Pitt S, Shen G, Pitts WJ, Carter PH, Barrish JC, Nadler SG, Salter-Cid LM, McKinnon M, Fura A, Schieven GL, Wrobleski ST.

Bioorg Med Chem Lett. 2014 Dec 15;24(24):5721-5726. doi: 10.1016/j.bmcl.2014.10.061. Epub 2014 Oct 24.

PMID:
25453808
19.

Identification of a phenylacylsulfonamide series of dual Bcl-2/Bcl-xL antagonists.

Perez HL, Banfi P, Bertrand J, Cai ZW, Grebinski JW, Kim K, Lippy J, Modugno M, Naglich J, Schmidt RJ, Tebben A, Vianello P, Wei DD, Zhang L, Galvani A, Lombardo LJ, Borzilleri RM.

Bioorg Med Chem Lett. 2012 Jun 15;22(12):3946-50. doi: 10.1016/j.bmcl.2012.04.103. Epub 2012 May 2.

PMID:
22608961
20.

Pyrazole and pyrimidine phenylacylsulfonamides as dual Bcl-2/Bcl-xL antagonists.

Schroeder GM, Wei D, Banfi P, Cai ZW, Lippy J, Menichincheri M, Modugno M, Naglich J, Penhallow B, Perez HL, Sack J, Schmidt RJ, Tebben A, Yan C, Zhang L, Galvani A, Lombardo LJ, Borzilleri RM.

Bioorg Med Chem Lett. 2012 Jun 15;22(12):3951-6. doi: 10.1016/j.bmcl.2012.04.106. Epub 2012 Apr 30.

PMID:
22608393
21.

Case study: technology initiative led to advanced lead optimization screening processes at Bristol-Myers Squibb, 2004-2009.

Zhang L, Cvijic ME, Lippy J, Myslik J, Brenner SL, Binnie A, Houston JG.

Drug Discov Today. 2012 Jul;17(13-14):733-40. doi: 10.1016/j.drudis.2012.02.012. Epub 2012 Mar 7. Review.

PMID:
22425710
22.

Pyrrolo[1,2-f]triazines as JAK2 inhibitors: achieving potency and selectivity for JAK2 over JAK3.

Harikrishnan LS, Kamau MG, Wan H, Inghrim JA, Zimmermann K, Sang X, Mastalerz HA, Johnson WL, Zhang G, Lombardo LJ, Poss MA, Trainor GL, Tokarski JS, Lorenzi MV, You D, Gottardis MM, Baldwin KF, Lippy J, Nirschl DS, Qiu R, Miller AV, Khan J, Sack JS, Purandare AV.

Bioorg Med Chem Lett. 2011 Mar 1;21(5):1425-8. doi: 10.1016/j.bmcl.2011.01.022. Epub 2011 Jan 11.

PMID:
21282055
23.

Trends in kinase selectivity: insights for target class-focused library screening.

Posy SL, Hermsmeier MA, Vaccaro W, Ott KH, Todderud G, Lippy JS, Trainor GL, Loughney DA, Johnson SR.

J Med Chem. 2011 Jan 13;54(1):54-66. doi: 10.1021/jm101195a. Epub 2010 Dec 3.

PMID:
21128601
24.

Synthesis and structure-activity relationships of 2-aryl-4-oxazolylmethoxy benzylglycines and 2-aryl-4-thiazolylmethoxy benzylglycines as novel, potent PPARalpha selective activators- PPARalpha and PPARgamma selectivity modulation.

Ye XY, Chen S, Zhang H, Locke KT, O'Malley K, Zhang L, Srivastava R, Miao B, Meyers D, Monshizadegan H, Search D, Grimm D, Zhang R, Lippy J, Twamley C, Muckelbauer JK, Chang C, An Y, Hosagrahara V, Zhang L, Yang TJ, Mukherjee R, Cheng PT, Tino JA.

Bioorg Med Chem Lett. 2010 May 1;20(9):2933-7. doi: 10.1016/j.bmcl.2010.03.019. Epub 2010 Mar 7.

PMID:
20356736
25.

An electrophoretic mobility shift assay for the identification and kinetic analysis of acetyl transferase inhibitors.

Fanslau C, Pedicord D, Nagulapalli S, Gray H, Pang S, Jayaraman L, Lippy J, Blat Y.

Anal Biochem. 2010 Jul 1;402(1):65-8. doi: 10.1016/j.ab.2010.03.025. Epub 2010 Mar 23.

PMID:
20338149
26.

Discovery of N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a selective and orally efficacious inhibitor of the Met kinase superfamily.

Schroeder GM, An Y, Cai ZW, Chen XT, Clark C, Cornelius LA, Dai J, Gullo-Brown J, Gupta A, Henley B, Hunt JT, Jeyaseelan R, Kamath A, Kim K, Lippy J, Lombardo LJ, Manne V, Oppenheimer S, Sack JS, Schmidt RJ, Shen G, Stefanski K, Tokarski JS, Trainor GL, Wautlet BS, Wei D, Williams DK, Zhang Y, Zhang Y, Fargnoli J, Borzilleri RM.

J Med Chem. 2009 Mar 12;52(5):1251-4. doi: 10.1021/jm801586s.

PMID:
19260711
27.

Design, synthesis and structure-activity relationships of azole acids as novel, potent dual PPAR alpha/gamma agonists.

Zhang H, Ryono DE, Devasthale P, Wang W, O'Malley K, Farrelly D, Gu L, Harrity T, Cap M, Chu C, Locke K, Zhang L, Lippy J, Kunselman L, Morgan N, Flynn N, Moore L, Hosagrahara V, Zhang L, Kadiyala P, Xu C, Doweyko AM, Bell A, Chang C, Muckelbauer J, Zahler R, Hariharan N, Cheng PT.

Bioorg Med Chem Lett. 2009 Mar 1;19(5):1451-6. doi: 10.1016/j.bmcl.2009.01.030. Epub 2009 Jan 15.

PMID:
19201606
28.

Discovery of pyrrolopyridine-pyridone based inhibitors of Met kinase: synthesis, X-ray crystallographic analysis, and biological activities.

Kim KS, Zhang L, Schmidt R, Cai ZW, Wei D, Williams DK, Lombardo LJ, Trainor GL, Xie D, Zhang Y, An Y, Sack JS, Tokarski JS, Darienzo C, Kamath A, Marathe P, Zhang Y, Lippy J, Jeyaseelan R Sr, Wautlet B, Henley B, Gullo-Brown J, Manne V, Hunt JT, Fargnoli J, Borzilleri RM.

J Med Chem. 2008 Sep 11;51(17):5330-41. doi: 10.1021/jm800476q. Epub 2008 Aug 9.

PMID:
18690676
29.

Design, synthesis, and structure-activity relationships of piperidine and dehydropiperidine carboxylic acids as novel, potent dual PPARalpha/gamma agonists.

Ye XY, Li YX, Farrelly D, Flynn N, Gu L, Locke KT, Lippy J, O'Malley K, Twamley C, Zhang L, Ryono DE, Zahler R, Hariharan N, Cheng PT.

Bioorg Med Chem Lett. 2008 Jun 15;18(12):3545-50. doi: 10.1016/j.bmcl.2008.05.014. Epub 2008 May 6.

PMID:
18511276
30.

Discovery of azetidinone acids as conformationally-constrained dual PPARalpha/gamma agonists.

Wang W, Devasthale P, Farrelly D, Gu L, Harrity T, Cap M, Chu C, Kunselman L, Morgan N, Ponticiello R, Zebo R, Zhang L, Locke K, Lippy J, O'Malley K, Hosagrahara V, Zhang L, Kadiyala P, Chang C, Muckelbauer J, Doweyko AM, Zahler R, Ryono D, Hariharan N, Cheng PT.

Bioorg Med Chem Lett. 2008 Mar 15;18(6):1939-44. doi: 10.1016/j.bmcl.2008.01.126. Epub 2008 Feb 7.

PMID:
18291645
31.

Identification of 2-amino-5-(thioaryl)thiazoles as inhibitors of nerve growth factor receptor TrkA.

Kim SH, Tokarski JS, Leavitt KJ, Fink BE, Salvati ME, Moquin R, Obermeier MT, Trainor GL, Vite GG, Stadnick LK, Lippy JS, You D, Lorenzi MV, Chen P.

Bioorg Med Chem Lett. 2008 Jan 15;18(2):634-9. Epub 2007 Nov 28.

PMID:
18055203
32.

A rapid, homogeneous, fluorescence polarization binding assay for peroxisome proliferator-activated receptors alpha and gamma using a fluorescein-tagged dual PPARalpha/gamma activator.

Seethala R, Golla R, Ma Z, Zhang H, O'Malley K, Lippy J, Cheng L, Mookhtiar K, Farrelly D, Zhang L, Hariharan N, Cheng PT.

Anal Biochem. 2007 Apr 15;363(2):263-74. Epub 2007 Jan 28.

PMID:
17335769
33.

A scintillation proximity assay for rna detection.

Liu J, Feldman PA, Lippy JS, Bobkova E, Kurilla MG, Chung TD.

Anal Biochem. 2001 Feb 15;289(2):239-45.

PMID:
11161317
34.

Selective inhibition of bacterial dihydroorotate dehydrogenases by thiadiazolidinediones.

Marcinkeviciene J, Rogers MJ, Kopcho L, Jiang W, Wang K, Murphy DJ, Lippy J, Link S, Chung TD, Hobbs F, Haque T, Trainor GL, Slee A, Stern AM, Copeland RA.

Biochem Pharmacol. 2000 Aug 1;60(3):339-42.

PMID:
10856428
35.

Quantitative, high-throughput cell-based assays for inhibitors of trkA receptor.

Angeles TS, Lippy JS, Yang SX.

Anal Biochem. 2000 Feb 15;278(2):93-8.

PMID:
10660449

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